Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade

Abstract

The invention relates to polycyclic aryl and heteroaryl substituted 4-pyrone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

1 . A compound of the Formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of: 
 (i) phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 32 , (b) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 36 , (c) a ring carbon or nitrogen in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 32 , is optionally substituted by R 33 , (d) a ring carbon or nitrogen in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 36 , is optionally substituted by R 35 , and (e) a ring carbon or nitrogen, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 33  and R 35 , respectively, is optionally substituted by R 34 ;  
 (ii) hydrido, trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 35 , and R 36 ; and  
 (iii) C3-C12 cycloalkyl or C4-C9 saturated heterocyclyl, wherein (a) each ring carbon may be optionally substituted with R 33 , (b) a ring carbon, other than the ring carbon at the point of attachment of B to A, may be optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, (c) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (d) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (e) a ring carbon or nitrogen atom, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (f) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , (g) a ring carbon or nitrogen, if present, in a first gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 10 , is optionally substituted by R 11 , (h) a ring carbon or nitrogen, if present, in a second gamma position relative to the carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 12 , is optionally substituted by R 33 , and (i) a ring carbon or nitrogen, if present, in a delta position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 11  and R 33 , respectively, is optionally substituted by R 34 ;  
 
 R 9 , R 10 , R 11 , R 12 , R 13 , R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkylenedioxy, haloalkylthio, alkanoyloxy, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy, heterocyclyloxy, heterocyclylalkoxy, alkoxyalkyl, haloalkoxylalkyl, hydroxy, amino, alkoxyamino, nitro, alkylamino, N-alkyl-N-arylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylthio, alkylthioalkyl, alkylsulfinyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, alkylsulfonylalkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkylsulfonamido, amidosulfonyl, alkanoyl, haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyhaloalkyl, hydroxyalkyl, aminoalkyl, haloalkoxyalkyl, carboxyalkyl, carboalkoxy, carboxy, carboxamido, carboxamidoalkyl, and cyano; and R 32 , R 33 , R 34 , R 35 , and R 36  are independently optionally Q b ;  
 A is selected from the group consisting of a bond, (W 7 ) rr -(CH(R 15 )) pa , and (CH(R 15 )) pa -(W 7 ) rr  wherein rr is 0 or 1, pa is an integer selected from 0 through 6, and W 7  is selected from the group consisting of O, S, C(O), (R 7 )NC(O), (R 7 )NC(S), and N(R 7 ) with the proviso that no more than one of the group consisting of rr and pa is 0 at the same time;  
 R 7  is selected from the group consisting of hydrido, hydroxy, and alkyl;  
 R 15  is selected from the group consisting of hydrido, hydroxy, halo, alkyl, and haloalkyl;  
 Ψ is NH or NOH;  
 X 0  is selected from the group consisting of hydrido, alkyl, alkenyl, cyano, halo, haloalkyl, haloalkoxy, haloalkylthio, amino, aminoalkyl, alkylamino, amidino, hydroxy, hydroxyamino, alkoxy, hydroxyalkyl, alkoxyamino, thiol, and alkylthio;  
 R 2  is Z 0 -Q;  
 Z 0  is selected from the group consisting of: 
 (i) a bond, (CR 41 R 42 ) q  wherein q is an integer selected from 1 through 3, and (CH(R 41 )) g —W 0 —(CH(R 42 )) p  wherein g and p are integers independently selected from through 3 and W 0  is selected from the group consisting of O, S, C(O), S(O), N(R 41 ), and ON(R 41 ); and  
 (ii) (CH(R 41 )) e —W 22 —(CH(R 42 )) h  wherein e and h are independently 0 or 1 and W 22  is selected from the group consisting of CR 41 ═CR 42 , 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl, 2,3-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, and 3,4-tetrahydrofuranyl, wherein Z 0  is directly bonded to the 4-pyrone ring and W 22  is optionally substituted with one or more substituents selected from the group consisting of R 9 , R 10 , R 11 , R 12 , and R 13 ;  
 
 R 41  and R 42  are independently selected from the group consisting of amidino, hydroxyamino, hydrido, hydroxy, amino, and alkyl;  
 Q is selected from the group consisting of: 
 (i) phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon or nitrogen in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon or nitrogen in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon or nitrogen, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ; and  
 (ii) hydrido with the proviso that Z 0  is selected from other than a bond;  
 
 K is selected from the group consisting of: 
 (i) CR 4a R 4b ; and  
 (ii) (CH(R 14 )) j -T wherein j is 0 or 1 and T is a bond or N(R 7 ) with the proviso that (CH(R 14 )) j  is bonded to the phenyl ring;  
 
 R 4a  and R 4b  are independently selected from the group consisting of halo, hydrido, hydroxyalkyl, alkyl, alkoxyalkyl, alkylthioalkyl, and haloalkyl;  
 E 0  is selected from the group consisting of: 
 (i) E 1 , with the proviso that K is CR 4a R 4b , wherein E 1  is selected from the group consisting of a covalent single bond, C(O)N(H), (H)NC(O), C(S)N(H), (H)NC(S), S(O) 2 N(H), N(H)S(O) 2 , S(O) 2 N(H)C(O), and C(O)N(H)S(O) 2 ; and  
 (ii) E 2 , with the proviso that K is (CH(R 14 )) j -T, wherein E 2  is selected from the group consisting of C(O)N(H), (H)NC(O), C(S)N(H), (H)NC(S), S(O) 2 N(H), N(H)S(O) 2 , S(O) 2 N(H)C(O), and C(O)N(H)S(O) 2 ;  
 
 R 14  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;  
 Y 0  is selected from the group consisting of: 
 (i) the formula  
                     
 wherein J 5 , J 6 , D 5 , D 6  and the ring carbon atoms to which they are attached define a phenyl or 5- or 6-membered heteroaryl ring, T, wherein one of J 5  and J 6  is absent when T is a 5-membered heteroaryl ring, J 5  is optionally substituted by R 17  when J 5  is a carbon atom, J 6  is optionally substituted by R 18  when J 6  is a carbon atom, D 5  is optionally substituted by R 16  when D 5  is a carbon atom and D 6  is optionally substituted by R 19  when D 6  is a carbon atom;  
 (ii) Y AT  wherein Y AT  is Q b -Q s ;  
 (iii) Q b -Q ss , wherein Q ss  is (CH(R 14 )) e —W 2 —(CH(R 15 )) h , wherein e and h are independently 1 or 2 and W 2  is CR 4a ═CR 4b , with the proviso that (CH(R 14 )) e  is bonded to E 0 ; and  
 (iv) Q b -Q ssss  or Q b -Q ssssr  wherein Q ssss  is (CH(R 38 )) r —W 5 , Q ssssr  is (CH(R 38 )) r —W 6 , r is 1 or 2, W 5  and W 6  are independently selected from the group consisting of 1,4-indenyl, 1,5-indenyl, 1,6-indenyl, 1,7-indenyl, 2,7-indenyl, 2,6-indenyl, 2,5-indenyl, 2,4-indenyl, 3,4-indenyl, 3,5-indenyl, 3,6-indenyl, 3,7-indenyl, 2,4-benzofuranyl, 2,5-benzofuranyl, 2,6-benzofuranyl, 2,7-benzofuranyl, 3,4-benzofuranyl, 3,5-benzofuranyl, 3,6-benzofuranyl, 3,7-benzofuranyl, 2,4-benzothiophenyl, 2,5-benzothiophenyl, 2,6-benzothiophenyl, 2,7-benzothiophenyl, 3,4-benzothiophenyl, 3,5-benzothiophenyl, 3,6-benzothiophenyl, 3,7-benzothiophenyl, 2,7-imidazo(1,2-a)pyridinyl, 3,4-imidazo(1,2-a)pyridinyl, 3,5-imidazo(1,2-a)pyridinyl, 3,6-imidazo(1,2-a)pyridinyl, 3,7-imidazo(1,2-a)pyridinyl, 2,4-indolyl, 2,5-indolyl, 2,6-indolyl, 2,7-indolyl, 3,4-indolyl, 3,5-indolyl, 3,6-indolyl, 3,7-indolyl, 1,4-isoindolyl, 1,5-isoindolyl, 1,6-isoindolyl, 2,4-isoindolyl, 2,5-isoindolyl, 2,6-isoindolyl, 2,7-isoindolyl, 1,3-isoindolyl, 3,4-indazolyl, 3,5-indazolyl, 3,6-indazolyl, 3,7-indazolyl, 2,4-benzoxazolyl, 2,5-benzoxazolyl, 2,6-benzoxazolyl, 2,7-benzoxazolyl, 3,4-benzisoxazolyl, 3,5-benzisoxazolyl, 3,6-benzisoxazolyl, 3,7-benzisoxazolyl, 1,4-naphthyl, 1,5-naphthyl, 1,6-naphthyl, 1,7-naphthyl, 1,8-naphthyl, 2,4-naphthyl, 2,5-naphthyl, 2,6-naphthyl, 2,7-naphthyl, 2,8-naphthyl, 2,4-quinolinyl, 2,5-quinolinyl, 2,6-quinolinyl, 2,7-quinolinyl, 2,8-quinolinyl, 3,4-quinolinyl, 3,5-quinolinyl, 3,6-quinolinyl, 3,7-quinolinyl, 3,8-quinolinyl, 4,5-quinolinyl, 4,6-quinolinyl, 4,7-quinolinyl, 4,8-quinolinyl, 1,4-isoquinolinyl, 1,5-isoquinolinyl, 1,6-isoquinolinyl, 1,7-isoquinolinyl, 1,8-isoquinolinyl, 3,4-isoquinolinyl, 3,5-isoquinolinyl, 3,6-isoquinolinyl, 3,7-isoquinolinyl, 3,8-isoquinolinyl, 4,5-isoquinolinyl, 4,6-isoquinolinyl, 4,7-isoquinolinyl, 4,8-isoquinolinyl, 3,4-cinnolinyl, 3,5-cinnolinyl, 3,6-cinnolinyl, 3,7-cinnolinyl, 3,8-cinnolinyl, 4,5-cinnolinyl, 4,6-cinnolinyl, 4,7-cinnolinyl, and 4,8-cinnolinyl, and each carbon and hyrido containing nitrogen member of the ring of the W 5  and of the ring of the W 6 , other than the points of attachment of W 5  and W 6 , is optionally substituted with one or more of the group consisting of R 9 , R 10 , R 11 , and R 12 , with the proviso that Q b  is bonded to lowest number substituent position of each W 5 , with the further proviso that Q b  is bonded to highest number substituent position of each W 6 , and with the additional proviso that (CH(R 38 )) r  is bonded to E 0 ;  
 
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, nitro, alkoxyamino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, alkenyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, haloalkoxyalkyl, carboalkoxy, and cyano;  
 Q b  is selected from the group consisting of NR 20 R 21 , aminoalkyl, hydrido, N(R 26 )C(NR 25 )N(R 23 )(R 24 ), and C(NR 25 )NR 23 R 24 , with the proviso that no more than one of R 20  and R 21  is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time, with the further proviso that no more than one of R 23  and R 24  is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time;  
 R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, alkyl, hydroxy, aminoalkyl, amino, dialkylamino, alkylamino, and hydroxyalkyl;  
 Q s  is selected from the group consisting of a bond, (CR 37 R 38 ) b  wherein b is an integer selected from 1 through 4, and (CH(R 14 )) c —W 1 —(CH(R 15 )) d  wherein c and d are integers independently selected from 1 through 3 and W 1  is selected from the group consisting of C(O)N(R 14 ), (R 14 )NC(O), S(O), S(O) 2 , S(O) 2 N(R 14 ), N(R 14 )S(O) 2 , and N(R 14 ), with the proviso that R 14  is selected from other than halo when directly bonded to N, and with the additional proviso that (CR 37 R 38 ) b  and (CH(R 14 )) c  are bonded to E 0 ;  
 R 37  and R 38  are independently selected from the group consisting of hydrido, alkyl, and haloalkyl; and  
 R 38  is optionally aroyl or heteroaroyl, wherein R 38  is optionally substituted with one or more substituents selected from the group consisting of R 16 , R 17 , R 18 , and R 19 .  
 
     
     
         2 . Compound of  claim 1  of the formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of: 
 (i) phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 32 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 36 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 32 , is optionally substituted by R 33 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 36 , is optionally substituted by R 35 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 33  and R 35 , respectively, is optionally substituted by R 34 ;  
 (ii) hydrido, trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 35 , and R 36 ; and  
 (iii) C3-C12 cycloalkyl or a C4-C9 saturated heterocyclyl, wherein (a) each ring carbon may be optionally substituted with R 33 , (b) a ring carbon, other than the ring carbon at the point of attachment of B to A, may be optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, (c) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (d) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (e) a ring carbon or nitrogen atom, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (f) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , (g) a ring carbon or nitrogen, if present, in a first gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 10 , is optionally substituted by R 11 , (h) a ring carbon or nitrogen, if present, in a second gamma position relative to the carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 12 , is optionally substituted by R 33 , and (i) a ring carbon or nitrogen, if present, in a delta position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 11  and R 33 , respectively, is optionally substituted by R 34 ;  
 
 R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkylenedioxy, haloalkylthio, alkanoyloxy, alkoxy, hydroxy, amino, alkoxyamino, haloalkanoyl, nitro, alkylamino, alkylthio, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkylsulfonamido, amidosulfonyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;  
 R 9 , R 10 , R 11 , R 12 , and R 13  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, alkoxyamino, alkanoyl, haloalkanoyl, amidino, guanidino, alkylenedioxy, haloalkylthio, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy, heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkylamino, N-alkyl-N-arylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylthio, alkylsulfinyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfamido, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, amidosulfonyl, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, and cyano;  
 A is bond or (CH(R 5 )) pa -(W 7 ), wherein rr is 0 or 1, pa is an integer selected from 0 through 3, and W 7  is selected from the group consisting of O, S, C(O), (R 7 )NC(O), (R 7 )NC(S), and N(R 7 ), with the proviso that W 7  is bonded to the N(H) on the 4-pyrone ring;  
 R 7  is selected from the group consisting of hydrido, hydroxy and alkyl;  
 R 15  is selected from the group consisting of hydrido, hydroxy, halo, alkyl, and haloalkyl;  
 X 0  is selected from the group consisting of hydrido, alkyl, cyano, halo, haloalkyl, haloalkoxy, amino, aminoalkyl, alkylamino, amidino, hydroxy, hydroxyamino, alkoxy, hydroxyalkyl, alkoxyamino, thiol, and alkylthio;  
 R 2  is Z 0 -Q;  
 Z 0  is selected from the group consisting of: 
 (i) a bond, (CR 41 R 42 ) q  wherein q is 1 or 2, and (CH(R 41 )) g —W 0 —(CH(R 42 )) p  wherein g and p are integers independently selected from 0 through 3 and W 0  is selected from the group consisting of O, S, C(O), S(O), N(R 41 ), and ON(R 41 ); and  
 (ii) (CH(R 41 )) e —W 22 —(CH(R 42 )) h  wherein e and h are independently 0 or 1 and W 22  is selected from the group consisting of CR 41 ═CR 42 , 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl, 2,3-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, and 3,4-tetrahydrofuranyl, wherein Z 0  is directly bonded to the 4-pyrone ring and W 22  is optionally substituted with one or more substituents selected from the group consisting of R 9 , R 10 , R 11 , R 12 , and R 13 ;  
 
 R 41  and R 42  are independently selected from the group consisting of hydrido, hydroxy, alkyl, and amino;  
 Q is selected from the group consisting of: 
 (i) phenyl or a heteroaryl of 5 or 6 ring members, wherein wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ; and  
 (ii) hydrido with the proviso that Z 0  is other than a bond;  
 
 K is selected from the group consisting of: 
 (i) CR 4a R 4b ; and  
 
 (ii) (CH(R 14 )) j -T wherein j is 0 or 1 and T is a bond or N(R 7 ) with the proviso that (CH(R 14 )) j  is bonded to the phenyl ring;  
 R 4a  and R 4b  are independently selected from the group consisting of hydrido, hydroxyalkyl, alkyl, alkoxyalkyl, alkylthioalkyl, and haloalkyl;  
 E 0  is selected from the group consisting of: 
 (i) E 1 , with the proviso that K is CR 4a R 4b , wherein E 1  is selected from the group consisting of a covalent single bond, C(O)N(H), (H)NC(O), S(O) 2 N(H), and N(H)S(O) 2 ; and  
 (ii) E 2 , with the proviso that K is (CH(R 14 )) j -T, wherein E 2  is selected from the group consisting of C(O)N(H), (H)NC(O), C(S)N(H), (H)NC(S), S(O) 2 N(H), N(H)S(O) 2 , S(O) 2 N(H)C(O), and C(O)N(H)S(O) 2 ;  
 
 R 14  is hydrido or halo;  
 Y 0  is selected from the group consisting of: 
 (i) the formula  
                     
 wherein J 5 , J 6 , D 5 , D 6  and the ring carbon atoms to which they are attached define a phenyl or 5- or 6-membered heteroaryl ring, T, wherein one of J 5  and J 6  is absent when T is a 5-membered heteroaryl ring, J 5  is optionally substituted by R 17  when J 5  is a carbon atom, J 6  is optionally substituted by R 18  when J 6  is a carbon atom, D 5  is optionally substituted by R 16  when D 5  is a carbon atom and D 6  is optionally substituted by R 19  when D 6  is a carbon atom; and  
 (ii) Y AT  wherein Y AT  is Q b -Q s ; and  
 (iii) Q b -Q ss  wherein Q ss  is (CH(R 14 )) e —W 2 —(CH(R 15 )) h , wherein e and h are independently 1 or 2 and W 2  is CR 4a ═CR 4b  with the proviso that (CH(R 14 )) e  is bonded to E 0 ;  
 
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
 Q b  is selected from the group consisting of NR 20 R 21 , hydrido, N(R 26 )C(NR 25 )N(R 23 )(R 24 ), and C(NR 25 )NR 23 R 24 , with the proviso that no more than one of R 20  and R 21  is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time, with the further proviso that no more than one of R 23  and R 24  is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino at the same time;  
 R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, alkyl, hydroxy, amino, alkylamino and dialkylamino;  
 Q s  is selected from the group consisting of a bond, (CR 37 R 38 ) b  wherein b is an integer selected from 1 through 4, and (CH(R 14 )) c —W 1 —(CH(R 15 )) d  wherein c and d are integers independently selected from 1 through 3 and W 1  is selected from the group consisting of C(O)N(R 14 ), (R 14 )NC(O), S(O), S(O) 2 , S(O) 2 N(R 14 ), N(R 14 )S(O) 2 , and N(R 14 ), with the proviso that R 14  is selected from other than halo when directly bonded to N, and with the additional proviso that (CR 37 R 38 ) b  and (CR 37 R 38 ) b , and (CH(R 14 )) c  are bonded to E 0 ;  
 R 37  and R 38  are independently selected from the group consisting of hydrido, alkyl, and haloalkyl; and  
 R 38  is optionally aroyl or heteroaroyl, wherein R 38  is optionally substituted with one or more substituents selected from the group consisting of R 16 , R 17 , R 18 , and R 19 .  
 
     
     
         3 . Compound of  claim 2  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 35 , and R 36 ;    R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;    A is (CH(R 15 )) pa —W 7  wherein pa is an integer selected from 0 through 3 and W 7  is selected from the group consisting of O, S, and N(R 7 ) wherein R 7  is hydrido or alkyl;    R 15  is selected from the group consisting of hydrido, hydroxy, halo, alkyl, and haloalkyl;    X 0  is selected from the group consisting of hydrido, amino, alkyl, cyano, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;    R 2  is Z 0 -Q;    Z 0  is a bond or (CR 41 R 42 ) q  wherein q is 1 or 2;    R 41  and R 42  are independently selected from the group consisting of hydrido, hydroxy, and amino;    Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 10 , R 11 , R 12 , and R 13  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, alkoxyamino, alkanoyl, haloalkanoyl, amidino, guanidino, alkylenedioxy, haloalkylthio, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy, heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkylamino, N-alkyl-N-arylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylthio, alkylsulfinyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfamido, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, amidosulfonyl, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, and cyano;    K is CHR 4a  wherein R 4a  is selected from the group consisting of hydrido, hydroxyalkyl, alkyl, alkoxyalkyl, alkylthioalkyl, and haloalkyl;    E 0  is selected from the group consisting of a bond, C(O)N(H), (H)NC(O), (R 7 )NS(O) 2 , and S(O) 2 N(R 7 );    Y 0  is selected from the group consisting of: 
 (i) the formula  
                     
 wherein J 5 , J 6 , D 5 , D 6  and the ring carbon atoms to which they are attached define a phenyl or 5- or 6-membered heteroaryl ring, T, wherein one of J 5  and J 6  is absent when T is a 5-membered heteroaryl ring, J 5  is optionally substituted by R 17  when J 5  is a carbon atom, J 6  is optionally substituted by R 18  when J 6  is a carbon atom, D 5  is optionally substituted by R 16  when D 5  is a carbon atom and D 6  is optionally substituted by R 19  when D 6  is a carbon atom; and  
 (ii) Q b -Q ss  wherein Q ss  is (CH(R 14 )) e —W 2 —(CH(R 15 )) h , wherein e and h are integers independently selected from 1 through 2 and W 2  is CR 4a ═CH with the proviso that (CH(R 14 )) e  is bonded to E 0 ;  
   R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkoxyamino, lower alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;    Q b  is selected from the group consisting of NR 20 R 21 , hydrido, N(R 26 )C(NR 25 )N(R 23 )(R 24 ), and C(NR 25 )NR 23 R 24 , with the proviso that no more than one of R 20  and R 21  is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino and with the further proviso that no more than one of R 23  and R 24  is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino;    R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, alkyl, hydroxy, amino, alkylamino and dialkylamino;    Q s  is selected from the group consisting of a bond, (CR 37 R 38 ) b  wherein b is an integer selected from 1 through 3, and (CH(R 14 )) c —W 1 —(CH(R 15 )) d  wherein c and d are independently 1 or 2 and W 1  is selected from the group consisting of C(O)N(R 14 ), (R 14 )NC(O), S(O), S(O) 2 , S(O) 2 N(R 14 ), N(R 14 )S(O) 2 , and N(R 14 ), with the proviso that R 14  is selected from other than halo when directly bonded to N and with the further proviso that (CR 37 R 38 ) b , and (CH(R 14 )) c  are bonded to E 0 ;    R 14  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;    R 37  is selected from the group consisting of hydrido, alkyl, and haloalkyl; and    R 38  is selected from the group consisting of hydrido, alkyl, haloalkyl, aroyl and heteroaroyl.    
     
     
         4 . Compound of  claim 3  of the Formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, trialkylsilyl, C2-C4 alkyl, C3-C5 alkylenyl, C3-C4 alkenyl, C3-C4 alkynyl, and C2-C4 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 3 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , and R 34 ;  
 R 32 , R 33 , and R 34  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, and cyano;  
 A is (CH(R 15 )) pa —N(R 7 ) wherein pa is an integer selected from 0 through 2 and R 7  is hydrido or alkyl;  
 R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;  
 X 0  is selected from the group consisting of hydrido, amino, alkyl, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;  
 R 2  is Z 0 -Q;  
 Z 0  is a bond or CH 2 ;  
 Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;  
 R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboxy, carboxamido, and cyano;  
 R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy, heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkoxyamino, alkylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylsulfonamido, amidosulfonyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, halo, haloalkyl, and cyano;  
 Y 0  is the formula  
                     
 wherein J 5 , J 6 , D 5 , D 6  and the ring carbon atoms to which they are attached define a phenyl or 5- or 6-membered heteroaryl ring, T, wherein one of J 5  and J 6  is absent when T is a 5-membered heteroaryl ring, J 5  is optionally substituted by R 17  when J 5  is a carbon atom, J 6  is optionally substituted by R 18  when J 6  is a carbon atom, D 5  is optionally substituted by R 16  when D 5  is a carbon atom and D 6  is optionally substituted by R 19  when D 6  is a carbon atom;  
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
 Q b  is selected from the group consisting of NR 20 R 21 , hydrido, C(N 25 )NR 23 R 24 , and N(R 26 )C(NR 25 )N(R 23 )(R 24 ), with the proviso that no more than one of R 20  and R 21  is hydroxy at the same time and with the further proviso that no more than one of R 23  and R 24  is hydroxy at the same time;  
 R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, alkyl, and hydroxy; and  
 Q s  is selected from the group consisting of a bond, CH 2 , and CH 2 CH 2 .  
 
     
     
         5 . Compound of  claim 4  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, —CH 2 CH 2 CH 2 —, —CH 2 CH 2 CH 2 CH 2 —, butyl, 2-butenyl, 3-butenyl, 2-butynyl, sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 2,2,2-trifluoroethyl, 3,3,3-trifluoropropyl, and 2,2-difluoropropyl, wherein each member of group B is optionally substituted at any carbon up to and including 3 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , and R 34 ;    R 32 , R 33 , and R 34  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;    A is selected from the group consisting of a bond, NH, and N(CH 3 );    X 0  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methylthio, ethylthio, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is a bond or CH 2 ;    Q is selected from the group consisting of phenyl and 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl, N-isopropylamidocarbonyl, N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy, cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy, cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy, 3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino, 5-bromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl, 4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino, 4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy, 4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl, 5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy, 2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy, 3,5-difluorophenoxy, 3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy, 2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy, 3,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy, 3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy, 3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy, 4-fluorobenzyloxy, 2-fluoro-3-trifluoromethylbenzyloxy, 3-fluoro-5-trifluoromethylbenzyloxy, 4-fluoro-2-trifluoromethylbenzyloxy, 4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy, 2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy, 4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino, 1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino, phenylsulfonyl, 3-trifluoromethoxybenzyloxy, 4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy, 4-trifluoromethoxyphenoxy, 3-trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy, 2,4-bis-trifluoromethylbenzyloxy, 3-trifluoromethylbenzyl, 3,5-bis-trifluoromethylbenzyloxy, 4-trifluoromethylphenoxy, 3-trifluoromethylphenoxy, 3-trifluoromethylthiobenzyloxy, 4-trifluoromethylthiobenzyloxy, 2,3,4-trifluorophenoxy, 2,3,5-trifluorophenoxy, 3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and 3-trifluoromethylthiophenoxy;    Y 0  is selected from the group consisting of:                          R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino,    N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, and cyano;    R 16  or R 19  is optionally selected from the group consisting of NR 2 —OR 21 , N(R 26 )C(NR 25 )N(R 23 )(R 24 ), and C(NR 25 )NR 23 R 24 , with the proviso that R 16 , R 19 , and Q b  are not simultaneously hydrido;    Q b  is selected from the group consisting of NR 20 R 21 , hydrido, C(NR 25 )NR 23 R 24 , and N(R 26 )C(NR 25 )N(R 23 )(R 24 ), with the proviso that no more than one of R 20 , R 21 , R 23 , and R 24  can be hydroxy, when any two of the group consisting of R 20 , R 21 , R 23 , and R 24  are bonded to the same atom and with the further proviso that said Q b  group is bonded directly to a carbon atom;    R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, methyl, ethyl, propyl, butyl, isopropyl, and hydroxy;    Q s  is selected from the group consisting of a bond, CH 2 , and CH 2 CH 2 .    
     
     
         6 . Compound of  claim 4 , or a pharmaceutically acceptable salt thereof, wherein; 
 A is selected from the group consisting of CH 2 N(CH 3 ), CH 2 N(CH 2 CH 3 ), CH 2 CH 2 N(CH 3 ), and CH 2 CH 2 N(CH 2 CH 3 );    X O  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methylthio, ethylthio, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is a bond or CH 2 ;    Q is selected from the group consisting of phenyl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl, wherein a carbon adjacent to the carbon at the point of attachment of said phenyl or heteroaryl ring to Z 0  is optionally substituted by R 9 , the other carbon adjacent to the carbon at the point of attachment is optionally substituted by R 13 , a carbon adjacent to R 9  and two atoms from the carbon at the point of attachment is optionally substituted by R 10 , a carbon adjacent to R 13  and two atoms from the carbon at the point of attachment is optionally substituted by R 12 , and any carbon adjacent to both R 10  and R 12  is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl, N-isopropylamidocarbonyl, N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy, cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy, cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy, 3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino, 5-bromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl, 4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino, 4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy, 4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl, 5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy, 2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy, 3,5-difluorophenoxy, 3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy, 2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy, 3,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy, 3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy, 3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy, 4-fluorobenzyloxy, 2-fluoro-3-trifluoromethylbenzyloxy, 3-fluoro-5-trifluoromethylbenzyloxy, 4-fluoro-2-trifluoromethylbenzyloxy, 4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy, 2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy, 4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino, 1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino, phenylsulfonyl, 3-trifluoromethoxybenzyloxy, 4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy, 4-trifluoromethoxyphenoxy, 3-trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy, 2,4-bis-trifluoromethylbenzyloxy, 3-trifluoromethylbenzyl, 3,5-bis-trifluoromethylbenzyloxy, 4-trifluoromethylphenoxy, 3-trifluoromethylphenoxy, 3-trifluoromethylthiobenzyloxy, 4-trifluoromethylthiobenzyloxy, 2,3,4-trifluorophenoxy, 2,3,5-trifluorophenoxy, 3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and 3-trifluoromethylthiophenoxy;    Y 0  is selected from the group consisting of:                          R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, aminomethyl,    1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, and cyano;    Q b  is selected from the group consisting of NR 20 R 21 , C(NR 25 )NR 23 R 24 , and N(R 26 )C(NR 25 )N(R 23 )(R 24 ), with the proviso that no more than one of R 20 , R 21 , R 23 , and R 24  can be hydroxy, when any two of the group consisting of R 20 , R 21 , R 23 , and R 24  are bonded to the same atom, and with the further proviso that said Q b  group is bonded directly to a carbon atom;    R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, methyl, ethyl, propyl, butyl, isopropyl, and hydroxy; and    Q s  is selected from the group consisting of a bond, CH 2 , and CH 2 CH 2 .    
     
     
         7 . Compound of  claim 6  or a pharmaceutically acceptable salt thereof, wherein; 
 A is selected from the group consisting of CH 2 N(CH 3 ), CH 2 N(CH 2 CH 3 ), CH 2 CH 2 N(CH 3 ), and CH 2 CH 2 N(CH 2 CH 3 );    X o  is selected from the group consisting of hydrido, hydroxy, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is a bond or CH 2 ;    Q is selected from the group consisting of 3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-benzylphenyl, 3-amino-5-(2-phenylethyl)phenyl, 3-amino-5-benzylaminophenyl, 3-amino-5-(2-phenylethylamino)phenyl, 3-amino-5-benzyloxyphenyl, 3-amino-5-(2-phenylethoxy)phenyl, 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, 3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl, 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl, 3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl, 3-amino-5-N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl, 3-amino-5-(N-benzylamidosulfonyl)phenyl, 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, 3-amino-5-(N-ethylamidocarbonyl)phenyl, 3-amino-5-(N-isopropylamidocarbonyl)phenyl, 3-amino-5-(N-propylamidocarbonyl)phenyl, 3-amino-5-(N-isobutylamidocarbonyl)phenyl, 3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl, 3-amino-5-(N-cyclobutylamidocarbonyl)phenyl, 3-amino-5-(N-cyclopentylamidocarbonyl)phenyl, 3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl, 3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5-hydroxyphenyl, 3-amino-5-carboxyphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl;    Y 0  is selected from the group consisting of:                          R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;    R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;    Q b  is C(NR 25 )NR 23 R 24 ;    R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido and methyl; and    Q s  is CH 2 .    
     
     
         8 . A compound as recited in  claim 7  or a pharmaceutically acceptable salt thereof where said compound is selected from the group consisting of: 
 2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-aminophenyl]-5-[N,N-dimethylhydrazino]-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-aminophenyl]-5-[N-ethyl-N-methylhydrazino]-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-aminophenyl]-5-[N,N-dimethylhydrazino]-6-chloro-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-aminophenyl]-5-[N-ethyl-N-methylhydrazino]-6-chloro-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3,5-diaminophenyl]-5-[N,N-dimethylhydrazino]-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3,5-diaminophenyl]-5-[N-ethyl-N-methylhydrazino]-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3,5-diaminophenyl]-5-[N,N-dimethylhydrazino]-6-chloro-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3,5-diaminophenyl]-5-[N-ethyl-N-methylhydrazino]-6-chloro-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-carboxyphenyl]-5-[N,N-dimethylhydrazino]-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-carboxyphenyl]-5-[N-ethyl-N-methylhydrazino]-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-carboxyphenyl]-5-[N,N-dimethylhydrazino]-6-chloro-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-carboxyphenyl]-5-[N-ethyl-N-methylhydrazino]-6-chloro-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-(N-benzylamidocarbonyl)phenyl]-5-[N,N-dimethylhydrazino]-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-(N-benzylamidocarbonyl)phenyl]-5-[N-ethyl-N-methylhydrazino]-4-pyronyl]]acetamide;    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2-[3-amino-5-(N-benzylamidocarbonyl)phenyl]-5-[N,N-dimethylhydrazino]-6-chloro-4-pyronyl]]acetamide; and    2-[3-[N-[[4-aminoiminomethylphenyl]methyl]-2[3-amino-5-(N-benzylamidocarbonyl)phenyl]-5-[N-ethyl-N-methylhydrazino]-6-chloro-4-pyronyl]]acetamide.    
     
     
         9 . Compound of  claim 2  of the formula:  
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof, wherein; 
 B is phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 32 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 36 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 32 , is optionally substituted by R 33 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 36 , is optionally substituted by R 35 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 33  and R 35 , respectively, is optionally substituted by R 34 ;  
 
         R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;  
         A is a bond or (CH(R 15 )) pa -(W 7 ) rr  wherein rr is 0 or 1, pa is an integer selected from 0 through 3, and W 7  is (R 7 )NC(O) or N(R 7 );  
         R 7  is selected from the group consisting of hydrido, hydroxy and alkyl;  
         R 5  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;  
         X 0  is selected from the group consisting of hydrido, amino, alkyl, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;  
         R 2  is Z 0 -Q;  
         Z 0  is selected from the group consisting of a bond, CH 2 , CH 2 CH 2 , W 0 —(CH(R 42 )) p  wherein p is 0 or 1 and W 0  is selected from the group consisting of O, S, and N(R 41 );  
         R 41  and R 42  are independently hydrido or alkyl;  
         Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;  
         R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboxy, carboxamido, and cyano;  
         R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy, heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkoxyamino, alkylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylsulfonamido, amidosulfonyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, halo, haloalkyl, and cyano;  
         Y 0  is the formula  
         
           
             
             
                 
                 
             
           
         
         wherein J 5 , J 6 , D 5 , D 6  and the ring carbon atoms to which they are attached define a phenyl or 5- or 6-membered heteroaryl ring, T, wherein one of J 5  and J 6  is absent when T is a 5-membered heteroaryl ring, J 5  is optionally substituted by R 17  when J 5  is a carbon atom, J 6  is optionally substituted by R 18  when J 6  is a carbon atom, D 5  is optionally substituted by R 16  when D 5  is a carbon atom and D 6  is optionally substituted by R 19  when D 6  is a carbon atom;  
         R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
         Q b  is selected from the group consisting of NR 20 R 21 , hydrido, and C(NR 25 )NR 23 R 24 , with the proviso that no more than one of R 20  and R 21  is hydroxy and with the further proviso that no more than one of R 23  and R 24  is hydroxy;  
         R 20 , R 21 , R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido, alkyl, and hydroxy; and  
         Q s  is selected from the group consisting of a bond, CH 2 , and CH 2 CH 2 .  
       
     
     
         10 . Compound of  claim 9  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of phenyl and 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 32 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 36 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 32 , is optionally substituted by R 33 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 36 , is optionally substituted by R 35 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 33  and R 35 , respectively, is optionally substituted by R 34 ;    R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano, and Q b ;    A is selected from the group consisting of a bond, NH, N(CH 3 ), N(OH), CH 2 , CH 3 CH, CF 3 CH, NHC(O), N(CH 3 )C(O), C(O)NH, C(O)N(CH 3 ), CH 2 CH 2 , CH 2 CH 2 CH 2 , CH 3 CHCH 2 , and CF 3 CHCH 2 ;    X 0  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methylthio, ethylthio, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a bond, CH 2 , CH 2 CH 2 , O, S, NH, N(CH 3 ), OCH 2 , SCH 2 , N(H)CH 2 , and N(CH 3 )CH 2 ;    Q is selected from the group consisting of phenyl and 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl, N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl, N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl, N-cyclohexylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy, cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy, cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy, 3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino, 5-bromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl, 4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino, 4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy, 4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl, 5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy, 2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy, 3,5-difluorophenoxy, 3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy, 2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy, 5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy, 3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy, 3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy, 4-fluorobenzyloxy, 2-fluoro-3-trifluoromethylbenzyloxy, 3-fluoro-5-trifluoromethylbenzyloxy, 4-fluoro-2-trifluoromethylbenzyloxy, 4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy, 2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy, 4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino, 1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino, phenylsulfonyl, 3-trifluoromethoxybenzyloxy, 4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy, 4-trifluoromethoxyphenoxy, 3-trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy, 2,4-bis-trifluoromethylbenzyloxy, 3-trifluoromethylbenzyl, 3,5-bis-trifluoromethylbenzyloxy, 4-trifluoromethylphenoxy, 3-trifluoromethylphenoxy, 3-trifluoromethylthiobenzyloxy, 4-trifluoromethylthiobenzyloxy, 2,3,4-trifluorophenoxy, 2,3,5-trifluorophenoxy, 3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and 3-trifluoromethylthiophenoxy;    Y 0  is selected from the group consisting of:                          R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, and cyano;    Q b  is C(NR 25 )NR 23 R 24  or hydrido, with the proviso that no more than one of R 23  and R 24  is hydroxy at the same time;    R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido, methyl, ethyl, and hydroxy; and    Q s  is selected from the group consisting of a bond, CH 2  and CH 2 CH 2 .    
     
     
         11 . Compound of  claim 10  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of 2-aminophenyl, 3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl, 3-carboxyphenyl, 3-carboxy-5-hydroxyphenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 3,4-difluorophenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3-methoxyaminophenyl, 3-methoxyphenyl, 4-methoxyphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoromethylphenyl, 2-imidazoyl, 2-pyridyl, 3-pyridyl, 5-chloro-3-trifluoromethyl-2-pyridyl, 4-pyridyl, 2-thienyl, 3-thienyl, and 3-trifluoromethyl-2-pyridyl;    A is selected from the group consisting of CH 2 , CH 3 CH, CF 3 CH, NHC(O), CH 2 CH 2 , and CH 2 CH 2 CH 2 ;    X 0  is selected from the group consisting of hydrido, hydroxy, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a bond, CH 2 , O, S, NH, N(CH 3 ), OCH 2 , and SCH 2 ;    Q is selected from the group consisting of    3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-benzylphenyl, 3-amino-5-(2-phenylethyl)phenyl, 3-amino-5-benzylaminophenyl, 3-amino-5-(2-phenylethylamino)phenyl, 3-amino-5-benzyloxyphenyl, 3-amino-5-(2-phenylethoxy)phenyl, 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, 3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-benzylamidosulfonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,    3-amino-5-(N-ethylamidocarbonyl)phenyl,    3-amino-5-(N-isopropylamidocarbonyl)phenyl,    3-amino-5-(N-propylamidocarbonyl)phenyl,    3-amino-5-(N-isobutylamidocarbonyl)phenyl,    3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,    3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,    3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,    3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,    3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,    3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl, 3-amino-5-(4-trifluoromethylbenzylamino)phenyl,    3-amino-5-(4-trifluoromethylbenzyloxy)phenyl, 3-carboxyphenyl,    3-carboxy-5-hydroxyphenyl, 3-amino-5-carboxyphenyl, 3-chlorophenyl,    2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl,    2-fluorophenyl, 3-fluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl,    3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl,    3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl,    3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl,    2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,    3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl; 
 Y 0  is selected from the group consisting of:  
                     
 R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;  
 R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;  
 Q b  is C(NR 25 )NR 23 R 24  or hydrido;  
 R 23 , R 24 , and R 25  are independently hydrido or methyl; and  
 Q b  is CH 2 .  
   
     
     
         12 . Compound of  claim 9 , or a pharmaceutically acceptable salt thereof, wherein; 
 B is phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 32 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 36 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 32 , is optionally substituted by R 33 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 36 , is optionally substituted by R 35 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 33  and R 35 , respectively, is optionally substituted by R 34 ;    R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;    A is a bond or (CH(R 5 )) pa -(W 7 ) rr  wherein rr is 0 or 1, pa is an integer selected from 0 through 3, and W 7  is N(R 7 );    R 7  is hydrido or alkyl;    R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;    X 0  is selected from the group consisting of hydrido, alkyl, halo, haloalkyl, aminoalkyl, and hydroxyalkyl;    R 2  is Z 0 -Q;    Z 0  is a bond;    Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, hydroxy, amino, alkylamino, alkylsulfonamido, amidosulfonyl, hydroxyalkyl, aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxamido, carboxyalkyl, and cyano;    Y 0  is the formula                          wherein J 5 , J 6 , D 5 , D 6  and the ring carbon atoms to which they are attached define a phenyl or 5- or 6-membered heteroaryl ring, T, wherein one of J 5  and J 6  is absent when T is a 5-membered heteroaryl ring, J 5  is optionally substituted by R 17  when J 5  is a carbon atom, J 6  is optionally substituted by R 18  when J 6  is a carbon atom, D 5  is optionally substituted by R 16  when D 5  is a carbon atom and D 6  is optionally substituted by R 19  when D 6  is a carbon atom;    R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;    Q b  is selected from the group consisting of NR 20 R 21 , hydrido, and C(NR 25 )NR 23 R 24 ;    R 20 , R 21 , R 23 , R 24 , and R 25  are independently hydrido or alkyl; and    Q s  is CH 2 .    
     
     
         13 . Compound of  claim 12  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of phenyl and 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, and 5-isoxazolyl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 32 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 36 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 32 , is optionally substituted by R 33 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 36 , is optionally substituted by R 35 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 33  and R 35 , respectively, is optionally substituted by R 34 ;    R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, dimethylamino, methoxyamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, carboxy, cyano, and Q b ;    A is selected from the group consisting of a bond, NH, N(CH 3 ), CH 2 , CH 3 CH, and CH 2 CH 2 ;    X o  is selected from the group consisting of hydrido, aminomethyl, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 2-hydroxyethyl, chloro, and fluoro;    R 2  is selected from the group consisting of phenyl and 2-thienyl, 2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl, and 3-pyridyl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, carboxy, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl, N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl, N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl, N-cyclohexylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino, dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro, chloro, bromo, and cyano;    Y 0  is selected from the group consisting of:                          R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, hydroxymethyl, carboxy, and cyano;    Q b  is NR 20 R 21  or C(NR 25 )NR 23 R 24 ;    R 20 , R 21 , R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido, methyl, and ethyl; and    Q s  is CH 2 .    
     
     
         14 . Compound of  claim 13  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of 2-aminophenyl, 3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl, 3-carboxyphenyl, 3-carboxy-5-hydroxyphenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 3,4-difluorophenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3-methoxyaminophenyl, 3-methoxyphenyl, 4-methoxyphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoromethylphenyl, 2-imidazoyl, 2-pyridyl, 3-pyridyl, 5-chloro-3-trifluoromethyl-2-pyridyl, 4-pyridyl, 2-thienyl, 3-thienyl, and 3-trifluoromethyl-2-pyridyl;    A is CH 2  or CH 2 CH 2 ;    X o  is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 2-hydroxyethyl, chloro, and fluoro;    R 2  is selected from the group consisting of    3-amidocarbonyl-5-aminophenyl, 3-amidocarbonyl-5-aminophenyl,    3-amino-5-(N-benzylamidocarbonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-benzylamidosulfonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,    3-amino-5-(N-ethylamidocarbonyl)phenyl,    3-amino-5-(N-isopropylamidocarbonyl)phenyl,    3-amino-5-(N-propylamidocarbonyl)phenyl,    3-amino-5-(N-isobutylamidocarbonyl)phenyl,    3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,    3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,    3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,    3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,    3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,    3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,    3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl,    3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl,    3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl; 
 Y 0  is selected from the group consisting of:  
                     
 R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;  
 R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;  
 Q b  is C(NR 25 )NR 23 R 24 ;  
 R 23 , R 24 , and R 25  are independently hydrido or methyl; and  
 Q s  is CH 2 .  
   
     
     
         15 . Compound of  claim 14  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of 3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 2-fluorophenyl, 4-methylphenyl, phenyl, 2-imidazoyl, 3-pyridyl, 4-pyridyl, and 3-trifluoromethyl-2-pyridyl;    A is CH 2  or CH 2 CH 2 ;    X o  is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, chloro, and fluoro;    R 2  is selected from the group consisting of    3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-benzylamidosulfonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,    3-amino-5-(N-ethylamidocarbonyl)phenyl,    3-amino-5-(N-isopropylamidocarbonyl)phenyl,    3-amino-5-(N-propylamidocarbonyl)phenyl,    3-amino-5-(N-isobutylamidocarbonyl)phenyl,    3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,    3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,    3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,    3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 3-aminophenyl,    3-carboxy-5-aminophenyl, 3-chlorophenyl, 3,5-diaminophenyl,    3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl,    3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl,    3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl; and 
 Y 0  is selected from the group consisting of 5-amidino-2-thienylmethyl, 4-amidinobenzyl, 2-fluoro-4-amidinobenzyl, and 3-fluoro-4-amdinobenzyl.  
   
     
     
         16 . Compound of  claim 9 , or a pharmaceutically acceptable salt thereof, wherein: 
 R 2  is 3-aminophenyl, B is phenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is hydrido;    R 2  is 3-aminophenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is methyl;    R 2  is 3-aminophenyl, B is phenyl, A is CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is methyl;    R 2  is 3-aminophenyl, B is 2-imidazoyl, A is CH 2 CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is methyl;    R 2  is 3-amidocarbonyl-5-aminophenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is methyl;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is methyl;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is methyl;    R 2  is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is methyl;    R 2  is 3,5-diaminophenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is methyl;    R 2  is 3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is methyl;    R 2  is 3-amidocarbonyl-5-aminophenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is hydrido;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is hydrido;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is hydrido;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is hydrido;    R 2  is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X 0  is hydrido;    R 2  is 3,5-diaminophenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X o  is hydrido; or    R 2  is 3-amino-5-carboxyphenyl, B is 3-chlorophenyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X o  is hydrido.    
     
     
         17 . Compound of  claim 2  of the Formula:  
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof, wherein;  
         B is selected from the group consisting of hydrido, C2-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 35 , and R 36 ;  
         R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;  
         A is a bond or (CH(R 15 )) pa -(W 7 ) rr  wherein rr is 0 or 1, pa is an integer selected from 0 through 3, and W 7  is (R 7 )NC(O) or N(R 7 );  
         R 7  is selected from the group consisting of hydrido, hydroxy and alkyl;  
         R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;  
         X 0  is selected from the group consisting of hydrido, amino, alkyl, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;  
         R 2  is Z 0 -Q;  
         Z 0  is selected from the group consisting of a bond, CH 2 , CH 2 CH 2 , W 0 —(CH(R 42 )) p  wherein p is 0 or 1 and W 0  is selected from the group consisting of O, S, and N(R 41 );  
         R 41  and R 42  are independently hydrido or alkyl;  
         Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;  
         R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboxy, carboxamido, and cyano;  
         R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy, heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkoxyamino, alkylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylsulfonamido, amidosulfonyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, halo, haloalkyl, and cyano;  
         Y 0  is the formula  
         
           
             
             
                 
                 
             
           
         
         wherein J 5 , J 6 , D 5 , D 6  and the ring carbon atoms to which they are attached define a phenyl or 5- or 6-membered heteroaryl ring, T, wherein one of J 5  and J 6  is absent when T is a 5-membered heteroaryl ring, J 5  is optionally substituted by R 17  when J 5  is a carbon atom, J 6  is optionally substituted by R 18  when J 6  is a carbon atom, D 5  is optionally substituted by R 16  when D 5  is a carbon atom and D 6  is optionally substituted by R 19  when D 6  is a carbon atom;  
         R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
         Q b  is selected from the group consisting of NR 20 R 21 , hydrido, C(NR 25 )NR 23 R 24 , and N(R 26 )C(NR 25 )N(R 23 )(R 24 ), with the proviso that no more than one of R 20  and R 21  is hydroxy and with the further proviso that no more than one of R 23  and R 24  is hydroxy;  
         R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, alkyl, and hydroxy; and  
         Q s  is selected from the group consisting of a bond, CH 2 , and CH 2 CH 2 .  
       
     
     
         18 . Compound of  claim 17  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, ethyl, 2-propynyl, 2-propenyl, propyl, isopropyl, butyl, 2-butenyl, 3-butenyl, 2-butynyl, sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl, 1-methyl-2-butenyl, 1-methyl-3-butenyl, 1-methyl-2-butynyl, 3-pentyl, 1-ethyl-2-propenyl, 2-methylbutyl, 2-methyl-2-butenyl, 2-methyl-3-butenyl, 2-methyl-3-butynyl, 3-methylbutyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl, 1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-4-pentenyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl, 1-ethyl-3-butenyl, 1-propyl-2-propenyl, 1-ethyl-2-butynyl, 1-heptyl, 2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 6-heptenyl, 2-heptynyl, 3-heptynyl, 4-heptynyl, 5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl, 1-methyl-3-hexenyl, 1-methyl-4-hexenyl, 1-methyl-5-hexenyl, 1-methyl-2-hexynyl, 1-methyl-3-hexynyl, 1-methyl-4-hexynyl, 3-heptyl, 1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl, 1-ethyl-4-pentenyl, 1-butyl-2-propenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, 2,2,2-trifluoroethyl, 2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl, 4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl, and 3,3,3-trifluoropropyl, wherein each member of group B is optionally substituted at any carbon up to and including 5 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 35 , and R 36 ;    R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano, and Q b ;    A is selected from the group consisting of bond, NH, N(CH 3 ), N(OH), CH 2 , CH 3 CH, CF 3 CH, NHC(O), N(CH 3 )C(O), C(O)NH, C(O)N(CH 3 ), CH 2 CH 2 , CH 2 CH 2 CH 2 , CH 3 CHCH 2 , and CF 3 CHCH 2 ;    X 0  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methylthio, ethylthio, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a bond, CH 2 , CH 2 CH 2 , O, S, NH, N(CH 3 ), OCH 2 , SCH 2 , N(H)CH 2 , and N(CH 3 )CH 2 ;    Q is selected from the group consisting of phenyl and 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl, N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl, N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl, N-cyclohexylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy, cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy, cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy, 3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino, 5-bromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl, 4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino, 4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy, 4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl, 5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy, 2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy, 3,5-difluorophenoxy, 3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy, 2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy, 3,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy, 3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy, 3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy, 4-fluorobenzyloxy, 2-fluoro-3-trifluoromethylbenzyloxy, 3-fluoro-5-trifluoromethylbenzyloxy, 4-fluoro-2-trifluoromethylbenzyloxy, 4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy, 2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy, 4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy,    4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino, 1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino, phenylsulfonyl, 3-trifluoromethoxybenzyloxy, 4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy, 4-trifluoromethoxyphenoxy, 3-trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy, 2,4-bis-trifluoromethylbenzyloxy, 3-trifluoromethylbenzyl, 3,5-bis-trifluoromethylbenzyloxy, 4-trifluoromethylphenoxy, 3-trifluoromethylphenoxy, 3-trifluoromethylthiobenzyloxy, 4-trifluoromethylthiobenzyloxy, 2,3,4-trifluorophenoxy, 2,3,5-trifluorophenoxy, 3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and 3-trifluoromethylthiophenoxy;    Y 0  is selected from the group consisting of:                          R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, and cyano;    Q b  is selected from the group consisting of NR 20 R 21 , hydrido, C(NR 25 )NR 23 R 24 , and N(R 26 )C(NR 25 )N(R 23 )(R 24 ), with the proviso that no more than one of R 20  and R 21  is hydroxy and with the further proviso that no more than one of R 23  and R 24  is hydroxy;    R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, methyl, ethyl, propyl, butyl, isopropyl, and hydroxy; and    Q s  is selected from the group consisting of a bond, CH 2 , and CH 2 CH 2 .    
     
     
         19 . Compound of  claim 18  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl, (S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4-methyl-2-pentyl, 3-hydroxypropyl, 1-methoxy-2-propyl, 2-methoxyethyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl, 2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl;    A is selected from the group consisting of a bond, CH 2 , NHC(O), CH 2 CH 2 , CH 2 CH 2 CH 2 , and CH 3 CHCH 2 ;    X o  is selected from the group consisting of hydrido, hydroxy, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a bond, CH 2 , O, S, NH, N(CH 3 ), OCH 2 , and SCH 2 ;    Q is selected from the group consisting of    3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-benzylphenyl, 3-amino-5-(2-phenylethyl)phenyl,    3-amino-5-benzylaminophenyl, 3-amino-5-(2-phenylethylamino)phenyl,    3-amino-5-benzyloxyphenyl, 3-amino-5-(2-phenylethoxy)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-benzylamidosulfonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,    3-amino-5-(N-ethylamidocarbonyl)phenyl,    3-amino-5-(N-isopropylamidocarbonyl)phenyl,    3-amino-5-(N-propylamidocarbonyl)phenyl,    3-amino-5-(N-isobutylamidocarbonyl)phenyl,    3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,    3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,    3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,    3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,    3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,    3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,    3-aminophenyl, 3-amino-5-(4-trifluoromethylbenzylamino)phenyl,    3-amino-5-(4-trifluoromethylbenzyloxy)phenyl, 3-carboxyphenyl,    3-carboxy-5-hydroxyphenyl, 3-amino-5-carboxyphenyl, 3-chlorophenyl,    2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl,    2-fluorophenyl, 3-fluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl,    3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl,    3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl,    3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl,    2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,    3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl; 
 Y 0  is selected from the group consisting of:  
                     
 R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;  
 R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;  
 Q b  is C(NR 25 )NR 23 R 24  or hydrido;  
 R 23 , R 24 , and R 25  are independently hydrido or methyl; and  
 Q s  is CH 2 .  
   
     
     
         20 . Compound of  claim 17 , or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, C2-C8 alkyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 35 , and R 36 ;    R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;    A is a bond or (CH(R 15 )) pa -(W 7 ) rr  wherein rr is 0 or 1, pa is an integer selected from 0 through 3, and W 7  is N(R 7 );    R 7  is hydrido or alkyl;    R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;    X 0  is selected from the group consisting of hydrido, alkyl, halo, haloalkyl, aminoalkyl, and hydroxyalkyl;    R 2  is Z 0 -Q;    Z 0  is a bond;    Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, hydroxy, amino, alkylamino, alkylsulfonamido, amidosulfonyl, hydroxyalkyl, aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxamido, carboxyalkyl, and cyano;    Y 0  is the formula                          wherein J 5 , J 6 , D 5 , D 6  and the ring carbon atoms to which they are attached define a phenyl or 5- or 6-membered heteroaryl ring, T, wherein one of J 5  and J 6  is absent when T is a 5-membered heteroaryl ring, J 5  is optionally substituted by R 17  when J 5  is a carbon atom, J 6  is optionally substituted by R 18  when J 6  is a carbon atom, D 5  is optionally substituted by R 16  when D 5  is a carbon atom and D 6  is optionally substituted by R 19  when D 6  is a carbon atom;    R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;    Q b  is selected from the group consisting of NR 20 R 21 , hydrido, N(R 26 )C(NR 25 )N(R 23 )(R 24 ), and C(NR 25 )NR 23 R 24 ;    R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently hydrido or alkyl; and    Q s  is CH 2 .    
     
     
         21 . Compound of  claim 20  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butenyl, 2-butynyl, sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl, 3-pentyl, 2-methylbutyl, 2-methyl-2-butenyl, 3-methylbutyl, 3-methyl-2-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl, 1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl, 1-heptyl, 2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 2-heptynyl, 3-heptynyl, 4-heptynyl, 5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl, 1-methyl-3-hexenyl, 1-methyl-4-hexenyl, 1-methyl-2-hexynyl, 1-methyl-3-hexynyl, 1-methyl-4-hexynyl, 3-heptyl, 1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, 2,2,2-trifluoroethyl, 2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl, 4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl, and 3,3,3-trifluoropropyl, wherein each member of group B is optionally substituted at any carbon up to and including 5 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 35 , and R 36 ;    R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, dimethylamino, methoxyamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, carboxy, cyano, and Q b ;    A is selected from the group consisting of: 
 (i) a bond, NH, N(CH 3 ), CH 2 , CH 3 CH, and CH 2 CH 2 ; and  
 (ii) CH 2 N(CH 3 ), CH 2 N(CH 2 CH 3 ), CH 2 CH 2 N(CH 3 ), and CH 2 CH 2 N(CH 2 CH 3 ) with the proviso that B is hydrido;  
   X o  is selected from the group consisting of hydrido, aminomethyl, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 2-hydroxyethyl, chloro, and fluoro;    R 2  is selected from the group consisting of phenyl and 2-thienyl, 2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl, and 3-pyridyl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 11 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, carboxy, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl, N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl, N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl, N-cyclohexylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino, dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro, chloro, bromo, and cyano;    Y 0  is selected from the group consisting of:                          R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, hydroxymethyl, carboxy, and cyano;    Q b  is selected from the group consisting of NR 20 R 21 , C(NR 25 )NR 23 R 24 , and N(R 26 )C(NR 25 )N(R 23 )(R 24 );    R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, methyl, and ethyl; and    Q s  is CH 2 .    
     
     
         22 . Compound of  claim 21  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl, (S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4-methyl-2-pentyl, 3-hydroxypropyl, 1-methoxy-2-propyl, 2-methoxyethyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl, 2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl;    A is selected from the group consisting of a bond, CH 2 , CH 3 CH, and CH 2 CH 2 ;    X 0  is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 2-hydroxyethyl, chloro, and fluoro;    R 2  is selected from the group consisting of    3-amidocarbonyl-5-aminophenyl, 3-amidocarbonyl-5-aminophenyl,    3-amino-5-(N-benzylamidocarbonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,    3-amino-5-N-(1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-benzylamidosulfonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,    3-amino-5-(N-ethylamidocarbonyl)phenyl,    3-amino-5-(N-isopropylamidocarbonyl)phenyl,    3-amino-5-(N-propylamidocarbonyl)phenyl,    3-amino-5-(N-isobutylamidocarbonyl)phenyl,    3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,    3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,    3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,    3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,    3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,    3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,    3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl,    3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl,    3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl,    2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl,    3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl,    3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl,    2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl; 
 Y 0  is selected from the group consisting of:  
                     
 R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;  
 R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;  
 Q b  is C(R 25 )NR 23 R 24 ;  
 R 23 , R 24 , and R 25  are independently hydrido or methyl; and  
 Q s  is CH 2 .  
   
     
     
         23 . Compound of  claim 22  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl, (S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4-methyl-2-pentyl, 3-hydroxypropyl, 1-methoxy-2-propyl, 2-methoxyethyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl, 2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl;    A is selected from the group consisting of a bond, CH 2 , CH 3 CH, and CH 2 CH 2 ;    X o  is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, chloro, and fluoro;    R 2  is selected from the group consisting of    3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-benzylamidosulfonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,    3-amino-5-(N-ethylamidocarbonyl)phenyl,    3-amino-5-(N-isopropylamidocarbonyl)phenyl,    3-amino-5-(N-propylamidocarbonyl)phenyl,    3-amino-5-(N-isobutylamidocarbonyl)phenyl,    3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,    3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,    3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,    3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 3-aminophenyl,    3-carboxy-5-aminophenyl, 3-chlorophenyl, 3,5-diaminophenyl,    3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl,    3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl,    3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl; and 
 Y 0  is selected from the group consisting of 5-amidino-2-thienylmethyl, 4-amidinobenzyl, 2-fluoro-4-amidinobenzyl, and 3-fluoro-4-amidinobenzyl.  
   
     
     
         24 . Compound of  claim 17 , or a pharmaceutically acceptable salt thereof, wherein: 
 R 2  is 3-aminophenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is (S)-2-butyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 5-amino-2-fluorophenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is is methyl;    R 2  is 2-methyl-3-aminophenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is ethyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is ethyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 2-propenyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is isopropyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 2-butyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is (R)-2-butyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 2-propynyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 3-pentyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is hydrido, A is CH 2 , Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is ethyl, A is CH 2 , Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 2-methypropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 2-propyl, A is CH 3 CH, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is propyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 6-amidocarbonylhexyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is tert-butyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is tert-butyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 3-hydroxypropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 2-methylpropyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is butyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 1-methoxy-2-propyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 2-methoxyethyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 2-propyl, A is a bond, Y 0  is 5-amidino-2-thienylmethyl, and X O  is methyl;    R 2  is 5-amino-2-methylthiophenyl, B is 2-propyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-carboxyphenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-carbomethoxyphenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is ethyl;    R 2  is 3-amino-5-carboxamidophenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzyl-N-methylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-phenyl-2-propyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2,4-dichlorobenzyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(4-bromobenzyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(3-trifluoromethylbenzyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-isobutylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-cyclobutylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-cyclopentylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-cycloheptylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-pyridylmethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(3-pyridylmethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-(4-methoxyphenyl)ethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(3-phenylpropyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2,2-diphenylethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-naphthylmethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(1,2,3,4-tetrahydronaphth-2-ylmethyl)amidocarbonyl)phenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 2-propyl, A is a bond, Y 0  is 4-amidino-3-fluorobenzyl, and X O  is hydrido;    R 2  is 3-carboxyphenyl, B is 2-propyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is 2-propyl, A is a bond, Y 0  is 4-amidino-3-fluorobenzyl, and X O  is methyl;    R 2  is 3,5-diaminophenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3,5-diaminophenyl, B is (S)-2-butyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzylbenzyl, and X O  is methyl;    R 2  is 3,5-diaminophenyl, B is ethyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3,5-diaminophenyl, B is ethyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-amino-5-carboxyphenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-carboxyphenyl, B is (S)-2-butyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-carboxyphenyl, B is isopropyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzylbenzyl, and X O  is methyl;    R 2  is 3-amino-5-carboxyphenyl, B is ethyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-carboxyphenyl, B is ethyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is 2,2,2-trifluoroethyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is (S)-2-butyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, A is a bond, Y° is 4-amidino-2-fluorobenzylbenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is ethyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl; or    R 2  is 3,5-diaminophenyl, B is isopropyl, A is a bond, Y 0  is 4-amidinobenzylbenzyl, and R 1  is hydrido.    
     
     
         25 . Compound of  claim 2  of the Formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is a C3-C7 cycloalkyl or a C4-C6 saturated heterocyclyl, wherein (a) each ring carbon may be optionally substituted with R 33 , (b) a ring carbon, other than the ring carbon at the point of attachment of B to A, may be optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, (c) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (d) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (e) a ring carbon or nitrogen atom, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (f) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , (g) a ring carbon or nitrogen, if present, in a first gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 10 , is optionally substituted by R 11 , (h) a ring carbon or nitrogen, if present, in a second gamma position relative to the carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 12 , is optionally substituted by R 33 , and (i) a ring carbon or nitrogen, if present, in a delta position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 11  and R 33 , respectively, is optionally substituted by R 34 ;  
 R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkylsulfonamido, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, alkoxy, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboxy, carboxamido, and cyano;  
 R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy, heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkoxyamino, alkylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylsulfonamido, amidosulfonyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, halo, haloalkyl, and cyano;  
 R 33  and R 34  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, carboalkoxy, carboxy, carboxamido, and cyano; and R 33  is optionally Q b ;  
 A is a bond or (CH(R 15 )) pa -(W 7 ) rr  wherein rr is 0 or 1, pa is an integer selected from 0 through 3, and W 7  is (R 7 )NC(O) or N(R 7 );  
 R 7  is selected from the group consisting of hydrido, hydroxy and alkyl;  
 R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;  
 X 0  is selected from the group consisting of hydrido, amino, alkyl, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;  
 R 2  is Z 0 -Q;  
 Z 0  is selected from the group consisting of a bond, CH 2 , CH 2 CH 2 , W 0 —(CH(R 42 )) p  wherein p is 0 or 1 and W 0  is selected from the group consisting of O, S, and N(R 41 );  
 R 41  and R 42  are independently hydrido or alkyl;  
 Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;  
 Y 0  is the formula  
                     
 wherein J 5 , J 6 , D 5 , D 6  and the ring carbon atoms to which they are attached define a phenyl or 5- or 6-membered heteroaryl ring, T, wherein one of J 5  and J 6  is absent when T is a 5-membered heteroaryl ring, J 5  is optionally substituted by R 17  when J 5  is a carbon atom, J 6  is optionally substituted by R 18  when J 6  is a carbon atom, D 5  is optionally substituted by R 16  when D 5  is a carbon atom and D 6  is optionally substituted by R 19  when D 6  is a carbon atom;  
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
 Q b  is selected from the group consisting of NR 20 R 21 , hydrido, and C(NR 25 )NR 23 R 24 , with the proviso that no more than one of R 20  and R 21  is hydroxy and with the further proviso that no more than one of R 23  and R 24  is hydroxy;  
 R 20 , R 21 , R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido, alkyl, and hydroxy; and  
 Q s  is selected from the group consisting of a bond, CH 2 , and CH 2 CH 2 .  
 
     
     
         26 . Compound of  claim 25  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of cyclopropyl, cyclobutyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, thiaetan-3-yl, cyclopentyl, cyclohexyl, norbornyl, 7-oxabicyclo[2.2.1]heptan-2-yl, bicyclo[3.1.0]hexan-6-yl, cycloheptyl, 2-morpholinyl, 3-morpholinyl, 4-morpholinyl, 1-piperazinyl, 2-piperazinyl, 1-piperidinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl, 2-dioxanyl, 4H-2-pyranyl, 4H-3-pyranyl, 4H-4-pyranyl, 4H-pyran-4-one-2-yl, 4H-pyran-4-one-3-yl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl, 2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl, 2-tetrahydrothienyl, and 3-tetrahydrothienyl, wherein (a) each ring carbon may be optionally substituted with R 33 , (b) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (c) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (d) a ring carbon or nitrogen atom, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , and (e) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, carboxymethyl, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methanesulfonamido, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl, N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl, N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl, N-cyclohexylamidocarbonyl, fluoro, chloro, bromo, cyano, cyclobutoxy, cyclohexoxy, cyclohexylmethoxy, 4-trifluoromethycyclohexylmethoxy, cyclopentoxy, benzyl, benzyloxy, 4-bromo-3-fluorophenoxy, 3-bromobenzyloxy, 4-bromobenzyloxy, 4-bromobenzylamino, 5-bromopyrid-2-ylmethylamino, 4-butoxyphenamino, 3-chlorobenzyl, 4-chlorophenoxy, 4-chloro-3-ethylphenoxy, 4-chloro-3-ethylbenzylamino, 4-chloro-3-ethylphenylamino, 3-chlorobenzyloxy, 4-chlorobenzyloxy, 4-chlorobenzylsulfonyl, 4-chlorophenylamino, 4-chlorophenylsulfonyl, 5-chloropyrid-3-yloxy, 2-cyanopyrid-3-yloxy, 2,3-difluorobenzyloxy, 2,4-difluorobenzyloxy, 3,4-difluorobenzyloxy, 2,5-difluorobenzyloxy, 3,5-difluorophenoxy, 3,5-difluorobenzyloxy, 4-difluoromethoxybenzyloxy, 2,3-difluorophenoxy, 2,4-difluorophenoxy, 2,5-difluorophenoxy, 3,5-dimethylphenoxy, 3,4-dimethylphenoxy, 3,4-dimethylbenzyloxy, 3,5-dimethylbenzyloxy, 4-ethoxyphenoxy, 4-ethylbenzyloxy, 3-ethylphenoxy, 4-ethylaminophenoxy, 3-ethyl-5-methylphenoxy, 4-fluorobenzyloxy, 2-fluoro-3-trifluoromethylbenzyloxy, 3-fluoro-5-trifluoromethylbenzyloxy, 4-fluoro-2-trifluoromethylbenzyloxy, 4-fluoro-3-trifluoromethylbenzyloxy, 2-fluorophenoxy, 4-fluorophenoxy, 2-fluoro-3-trifluoromethylphenoxy, 2-fluorobenzyloxy, 4-fluorophenylamino, 2-fluoro-4-trifluoromethylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, 4-isopropylbenzyloxy, 3-isopropylphenoxy, 4-isopropylphenoxy, 4-isopropyl-3-methylphenoxy, phenylamino, 1-phenylethoxy, 2-phenylethoxy, 2-phenylethyl, 2-phenylethylamino, phenylsulfonyl, 3-trifluoromethoxybenzyloxy, 4-trifluoromethoxybenzyloxy, 3-trifluoromethoxyphenoxy, 4-trifluoromethoxyphenoxy, 3-trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy, 2,4-bis-trifluoromethylbenzyloxy, 3-trifluoromethylbenzyl, 3,5-bis-trifluoromethylbenzyloxy, 4-trifluoromethylphenoxy, 3-trifluoromethylphenoxy, 3-trifluoromethylthiobenzyloxy, 4-trifluoromethylthiobenzyloxy, 2,3,4-trifluorophenoxy, 2,3,5-trifluorophenoxy, 3-pentafluoroethylphenoxy, 3-(1,1,2,2-tetrafluoroethoxy)phenoxy, and 3-trifluoromethylthiophenoxy;    R 33  is selected from the group consisting of hydrido, amidino, guanidino, carboxy, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, methoxyamino, ethoxyamino, acetamido, trifluoroacetamido, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, 2,2,2-trifluoro-1-hydroxyethyl, methoxycarbonyl, ethoxycarbonyl, amidocarbonyl, N-methylamidocarbonyl, N,N-dimethylamidocarbonyl, cyano, and Q b ;    A is selected from the group consisting of a bond, NH, N(CH 3 ), N(OH), CH 2 , CH 3 CH, CF 3 CH, NHC(O), N(CH 3 )C(O), C(O)NH, C(O)N(CH 3 ), CH 2 CH 2 , CH 2 CH 2 CH 2 , CH 3 CHCH 2 , and CF 3 CHCH 2 ;    X o  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methylthio, ethylthio, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a bond, CH 2 , CH 2 CH 2 , O, S, NH, N(CH 3 ), OCH 2 , SCH 2 , N(H)CH 2 , and N(CH 3 )CH 2 ;    Q is selected from the group consisting of phenyl and 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, 5-isoxazolyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 5-pyrimidinyl, 3-pyridazinyl, 4-pyridazinyl, and 1,3,5-triazin-2-yl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    Y 0  is selected from the group consisting of:                          R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, isopropyl, propyl, carboxy, amidino, guanidino, methoxy, ethoxy, isopropoxy, propoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, N-ethylamino, methylthio, ethylthio, isopropylthio, trifluoromethylthio, methylsulfinyl, ethylsulfinyl, methylsulfonyl, ethylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, 2,2,3,3,3-pentafluoropropyl, trifluoromethoxy, 1,1,2,2-tetrafluoroethoxy, fluoro, chloro, bromo, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, and cyano;    Q b  is C(NR 25 )NR 23 R 24  or hydrido, with the proviso that no more than one of R 23  and R 24  is hydroxy;    R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido, methyl, ethyl, and hydroxy; and    Q s  is selected from the group consisting of a bond, CH 2  and CH 2 CH 2 .    
     
     
         27 . Compound of  claim 26  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, 1-pyrrolidinyl, 1-piperidinyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, 7-oxabicyclo[2.2.1]heptan-2-yl, bicyclo[3.1.0]hexan-6-yl, 2-morpholinyl, 3-morpholinyl, 4-morpholinyl, 1-piperazinyl, 2-piperazinyl, 1-piperidinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl, 2-dioxanyl, 4H-2-pyranyl, 4H-3-pyranyl, 4H-4-pyranyl, 4H-pyran-4-one-2-yl, 4H-pyran-4-one-3-yl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl, 2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl, 2-tetrahydrothienyl, and 3-tetrahydrothienyl;    A is selected from the group consisting of a bond, CH 2 , NHC(O), CH 2 CH 2 , and CH 2 CH 2 CH 2 ;    X 0  is selected from the group consisting of hydrido, hydroxy, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, fluoro, chloro, and bromo;    R 2  is Z 0 -Q;    Z 0  is selected from the group consisting of a bond, CH 2 , O, S, NH, N(CH 3 ), OCH 2 , and SCH 2 ;    Q is selected from the group consisting of    3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-benzylphenyl, 3-amino-5-(2-phenylethyl)phenyl,    3-amino-5-benzylaminophenyl, 3-amino-5-(2-phenylethylamino)phenyl, 3-amino-5-benzyloxyphenyl, 3-amino-5-(2-phenylethoxy)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,    3-amino-5-N-(1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-benzylamidosulfonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,    3-amino-5-(N-ethylamidocarbonyl)phenyl,    3-amino-5-(N-isopropylamidocarbonyl)phenyl,    3-amino-5-(N-propylamidocarbonyl)phenyl,    3-amino-5-(N-isobutylamidocarbonyl)phenyl,    3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,    3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,    3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,    3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,    3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,    3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,    3-aminophenyl, 3-amino-5-(4-trifluoromethylbenzylamino)phenyl,    3-amino-5-(4-trifluoromethylbenzyloxy)phenyl, 3-carboxyphenyl,    3-carboxy-5-hydroxyphenyl, 3-amino-5-carboxyphenyl, 3-chlorophenyl,    2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl,    2-fluorophenyl, 3-fluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl,    3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl,    3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl,    3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl,    2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,    3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl; 
 Y 0  is selected from the group consisting of:  
                     
 R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;  
 R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;  
 Q b  is C(NR 25 )NR 23 R 24  or hydrido;  
 R 23 , R 24 , and R 25  are independently hydrido or methyl; and  
 Q s  is CH 2 .  
   
     
     
         28 . Compound of  claim 25 , or a pharmaceutically acceptable salt thereof, wherein; 
 B is a C3-C7 cycloalkyl or a C4-C6 saturated heterocyclyl, wherein (a) each ring carbon is optionally substituted with R 33 , (b) a ring carbon, other than the ring carbon at the point of attachment, is optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, (c) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (d) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (e) a ring carbon or nitrogen, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (f) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , (g) a ring carbon or nitrogen, if present, in a first gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 10 , is optionally substituted by R 11 , and (h) a ring carbon or nitrogen, if present, in a second gamma position relative to the carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 12 , is optionally substituted by R 33 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, hydroxy, amino, amidino, guanidino, alkylamino, alkylthio, alkoxy, alkylsulfinyl, alkylsulfonyl, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboxy, carboxamido, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkyl, alkoxy, alkoxyamino, hydroxy, amino, alkylamino, alkylsulfonamido, amidosulfonyl, hydroxyalkyl, aminoalkyl, halo, haloalkyl, carboalkoxy, carboxy, carboxamido, carboxyalkyl, and cyano;    R 33  and R 34  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, amidosulfonyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, carboalkoxy, carboxy, carboxamido, and cyano, and R 33  is optionally Q b ;    A is a bond or (CH(R 15 )) pa -(W 7 ) rr  wherein rr is 0 or 1, pa is an integer selected from 0 through 3, and W 7  is N(R 7 );    R 7  is hydrido or alkyl;    R 15  is selected from the group consisting of hydrido, halo, alkyl, and haloalkyl;    X 0  is selected from the group consisting of hydrido, alkyl, halo, haloalkyl, aminoalkyl, and hydroxyalkyl;    R 2  is Z 0 -Q;    Z 0  is a bond;    Q is phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    Y 0  is the formula                          wherein J 5 , J 6 , D 5 , D 6  and the ring carbon atoms to which they are attached define a phenyl or 5- or 6-membered heteroaryl ring, T, wherein one of J 5  and J 6  is absent when T is a 5-membered heteroaryl ring, J 5  is optionally substituted by R 17  when J 5  is a carbon atom, J 6  is optionally substituted by R 18  when J 6  is a carbon atom, D 5  is optionally substituted by R 16  when D 5  is a carbon atom and D 6  is optionally substituted by R 19  when D 6  is a carbon atom;    R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;    Q b  is selected from the group consisting of NR 20 R 21 , hydrido, and C(NR 25 )NR 23 R 24 ;    R 20 , R 21 , R 23 , R 24 , and R 25  are independently hydrido or alkyl; and    Q s  is CH 2 .    
     
     
         29 . Compound of  claim 28  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, bicyclo[3.1.0]hexan-6-yl, 2-morpholinyl, 3-morpholinyl, 4-morpholinyl, 1-piperazinyl, 2-piperazinyl, 1-piperidinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl, 2-dioxanyl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl, 2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl, 2-tetrahydrothienyl, and 3-tetrahydrothienyl, wherein (a) each ring carbon may be optionally substituted with R 33 , (b) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (c) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (d) a ring carbon or nitrogen atom, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , and (e) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 ;    R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, carboxy, and cyano;    R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl, N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl, N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl, N-cyclohexylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino, dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro, chloro, bromo, and cyano;    R 33  is selected from the group consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, carboxy, amino, N-methylamino, dimethylamino, methoxyamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, cyano, and Q b ;    A is selected from the group consisting of a bond, NH, N(CH 3 ), CH 2 , CH 3 CH, CH 2 CH 2 , and CH 2 CH 2 CH 2 ;    X o  is selected from the group consisting of hydrido, aminomethyl, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 2-hydroxyethyl, chloro, and fluoro;    R 2  is selected from the group consisting of phenyl and 2-thienyl, 2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl, and 3-pyridyl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 11 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;    Y 0  is selected from the group consisting of:                          R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, hydroxymethyl, carboxy, and cyano;    Q b  is NR 20 R 21  or C(NR 25 )NR 23 R 24 ;    R 20 , R 21 , R 23 , R 24 , and R 25  are independently selected from the group consisting of hydrido, methyl, and ethyl; and    Q s  is CH 2 .    
     
     
         30 . Compound of  claim 29  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, 1-pyrrolidinyl and 1-piperidinyl;    A is selected from the group consisting of a bond, CH 2 , CH 2 CH 2  and CH 2 CH 2 CH 2 ;    X o  is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 2-hydroxyethyl, chloro, and fluoro;    R 2  is selected from the group consisting of    3-amidocarbonyl-5-aminophenyl, 3-amidocarbonyl-5-aminophenyl,    3-amino-5-(N-benzylamidocarbonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-benzylamidosulfonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,    3-amino-5-(N-ethylamidocarbonyl)phenyl,    3-amino-5-(N-isopropylamidocarbonyl)phenyl,    3-amino-5-(N-propylamidocarbonyl)phenyl,    3-amino-5-(N-isobutylamidocarbonyl)phenyl,    3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,    3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,    3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,    3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 5-amino-2-fluorophenyl,    3-amino-5-hydroxymethylphenyl, 5-amino-3-methoxycarbonylphenyl,    3-amidinophenyl, 3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl,    3-aminophenyl, 3-carboxyphenyl, 3-carboxy-5-aminophenyl,    3-carboxy-5-hydroxyphenyl, 3-carboxymethyl-5-aminophenyl,    3-carboxymethyl-5-hydroxyphenyl, 3-carboxymethylphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl, 3,5-diaminophenyl, 3-dimethylaminophenyl,    2-fluorophenyl, 3-fluorophenyl, 2,5-difluorophenyl, 2-hydroxyphenyl,    3-hydroxyphenyl, 3-methanesulfonylaminophenyl, 2-methoxyphenyl,    3-methoxyphenyl, 3-methoxyaminophenyl, 3-methoxycarbonylphenyl,    2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl,    3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl; 
 Y 0  is selected from the group consisting of:  
                     
 R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;  
 R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;  
 Q b  is C(NR 25 )NR 23 R 24 ;  
 R 23 , R 24 , and R 25  are independently hydrido or methyl; and  
 Q s  is CH 2 .  
   
     
     
         31 . Compound of  claim 30  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, and 1-piperidinyl;    A is selected from the group consisting of a bond, CH 2 , CH 2 CH 2  and CH 2 CH 2 CH 2 ;    X o  is selected from the group consisting of hydrido, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, chloro, and fluoro;    R 2  is selected from the group consisting of    3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-benzylamidosulfonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,    3-amino-5-(N-ethylamidocarbonyl)phenyl,    3-amino-5-(N-isopropylamidocarbonyl)phenyl,    3-amino-5-(N-propylamidocarbonyl)phenyl,    3-amino-5-(N-isobutylamidocarbonyl)phenyl,    3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,    3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,    3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,    3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 3-aminophenyl,    3-carboxy-5-aminophenyl, 3-chlorophenyl, 3,5-diaminophenyl,    3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl,    3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl,    3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl; and 
 Y 0  is selected from the group consisting of 5-amidino-2-thienylmethyl, 4-amidinobenzyl, 2-fluoro-4-amidinobenzyl, and 3-fluoro-4-amdinobenzyl.  
   
     
     
         32 . Compound of  claim 25 , or a pharmaceutically acceptable salt thereof, wherein: 
 R 2  is 3-aminophenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X 0  is methyl;    R 2  is 3-aminophenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is is methyl;    R 2  is 3-aminophenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-3-fluorobenzyl, and X 0  is methyl;    R 2  is 3-aminophenyl, B is cyclopentyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 5-amino-2-thienyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is cyclopropyl, A is CH 2 , Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 2-(2R)-bicyclo[2.2.1]-heptyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is cyclopentyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is cyclohexyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is oxalan-2-yl, A is CH 2 , Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 1-piperidinyl, A is CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-aminophenyl, B is 1-pyrrolidinyl, A is CH 2 CH 2 CH 2 , Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3-amino-5-carboxyphenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 2-amino-6-carboxy-4-pyridyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3-amino-5-carbomethoxyphenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-carboxyphenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3,5-diaminophenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3,5-diaminophenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3,5-diaminophenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-3-fluorobenzyl, and X O  is methyl;    R 2  is 3,5-diaminophenyl, B is cyclopentyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-carboxy-5-aminophenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-carboxy-5-aminophenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-3-fluorobenzyl, and X O  is methyl;    R 2  is 3-carboxy-5-aminophenyl, B is cyclopentyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and R 1  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-3-fluorobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclopentyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-3-fluorobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl, B is cyclopentyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclopropyl, A is a bond, Y 0  is 4-amidino-2-fluorobenzyl, and X O  is methyl;    R 2  is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is hydrido;    R 2  is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclobutyl, A is a bond, Y 0  is 4-amidino-3-fluorobenzyl, and X O  is methyl; or    R 2  is 3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)-phenyl, B is cyclopentyl, A is a bond, Y 0  is 4-amidinobenzyl, and X O  is methyl.    
     
     
         33 . Compound of  claim 2  of the Formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of:  
 (i) phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 32 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 36 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 32 , is optionally substituted by R 33 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 36 , is optionally substituted by R 35 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 33  and R 35 , respectively, is optionally substituted by R 34 ; 
 (ii) hydrido, trialkylsilyl, C2-C8 alkyl, C3-C8 alkylenyl, C3-C8 alkenyl, C3-C8 alkynyl, and C2-C8 haloalkyl, wherein each member of group B is optionally substituted at any carbon up to and including 6 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 35 , and R 36 ; and  
 (iii) C3-C12 cycloalkyl or a C4-C9 saturated heterocyclyl, wherein (a) each ring carbon may be optionally substituted with R 33 , (b) a ring carbon, other than the ring carbon at the point of attachment of B to A, may be optionally substituted with oxo provided that no more than one ring carbon is substituted by oxo at the same time, (c) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (d) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (e) a ring carbon or nitrogen atom, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (f) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , (g) a ring carbon or nitrogen, if present, in a first gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 10 , is optionally substituted by R 11 , (h) a ring carbon or nitrogen, if present, in a second gamma position relative to the carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 12 , is optionally substituted by R 33 , and (i) a ring carbon or nitrogen, if present, in a delta position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 11  and R 33 , respectively, is optionally substituted by R 34 ;  
 
 R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, amidino, guanidino, alkylenedioxy, haloalkylthio, alkanoyloxy, alkoxy, hydroxy, amino, alkoxyamino, haloalkanoyl, nitro, alkylamino, alkylthio, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, alkylsulfonamido, amidosulfonyl, alkyl, alkenyl, halo, haloalkyl, haloalkenyl, haloalkoxy, hydroxyalkyl, alkylamino, carboalkoxy, carboxy, carboxamido, cyano, and Q b ;  
 R 9 , R 10 , R 11 , R 12 , and R 13  are independently selected from the group consisting of hydrido, acetamido, haloacetamido, alkoxyamino, alkanoyl, haloalkanoyl, amidino, guanidino, alkylenedioxy, haloalkylthio, alkoxy, cycloalkoxy, cycloalkylalkoxy, aralkoxy, aryloxy, heteroaryloxy, heteroaralkoxy, heterocyclyloxy, heterocyclylalkoxy, hydroxy, amino, alkylamino, N-alkyl-N-arylamino, arylamino, aralkylamino, heteroarylamino, heteroaralkylamino, heterocyclylamino, heterocyclylalkylamino, alkylthio, alkylsulfinyl, arylsulfinyl, aralkylsulfinyl, cycloalkylsulfinyl, heteroarylsulfinyl, alkylsulfamido, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, cycloalkylsulfonyl, heteroarylsulfonyl, amidosulfonyl, alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heterocyclyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, hydroxyhaloalkyl, aminoalkyl, carboalkoxy, carboxy, carboxyalkyl, carboxamido, and cyano;  
 A is a bond or (CH(R 15 )) pa -(W 7 ) rr  wherein rr is 0 or 1, pa is an integer selected from 0 through 3, and W 7  is selected from the group consisting of O, S, C(O), (R 7 )NC(O), (R 7 )NC(S), and N(R 7 );  
 R 7  is selected from the group consisting of hydrido, hydroxy and alkyl;  
 R 15  is selected from the group consisting of hydrido, hydroxy, halo, alkyl, and haloalkyl;  
 X 0  is selected from the group consisting of hydrido, amino, alkyl, cyano, halo, haloalkyl, haloalkoxy, aminoalkyl, hydroxy, alkoxy, hydroxyalkyl, and alkylthio;  
 R 2  is Z 0 -Q;  
 Z 0  is selected from the group consisting of: 
 (i) a bond, (CR 41 R 42 ) q  wherein q is 1 or 2, and (CH(R 41 )) g —W 0 —(CH(R 42 )) p  wherein g and p are integers independently selected from 0 through 3 and W 0  is selected from the group consisting of O, S, C(O), S(O), N(R 41 ), and ON(R 41 ); and  
 (ii) (CH(R 41 )) e —W 22 —(CH(42)) h  wherein e and h are independently 0 or 1 and W 22  is selected from the group consisting of CR 41 ═CR 42 , 1,2-cyclopropyl, 1,2-cyclobutyl, 1,2-cyclohexyl, 1,3-cyclohexyl, 1,2-cyclopentyl, 1,3-cyclopentyl, 2,3-morpholinyl, 2,4-morpholinyl, 2,6-morpholinyl, 3,4-morpholinyl, 3,5-morpholinyl, 1,2-piperazinyl, 1,3-piperazinyl, 2,3-piperazinyl, 2,6-piperazinyl, 1,2-piperidinyl, 1,3-piperidinyl, 2,3-piperidinyl, 2,4-piperidinyl, 2,6-piperidinyl, 3,4-piperidinyl, 1,2-pyrrolidinyl, 1,3-pyrrolidinyl, 2,3-pyrrolidinyl, 2,4-pyrrolidinyl, 2,5-pyrrolidinyl, 3,4-pyrrolidinyl, 2,3-tetrahydrofuranyl, 2,4-tetrahydrofuranyl, 2,5-tetrahydrofuranyl, and 3,4-tetrahydrofuranyl, wherein Z 0  is directly bonded to the 4-pyrone ring and W 22  is optionally substituted with one or more substituents selected from the group consisting of R 9 , R 10 , R 11 , R 12 , and R 13 ;  
 
 R 41  and R 42  are independently selected from the group consisting of hydrido, hydroxy, alkyl, and amino;  
 Q is selected from the group consisting of: 
 (i) phenyl or a heteroaryl of 5 or 6 ring members, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R; and  
 (ii) hydrido with the proviso that Z 0  is selected from other than a bond;  
 
 K is CHR 4a  wherein R 4a  is selected from the group consisting of hydrido, hydroxyalkyl, alkyl, alkoxyalkyl, alkylthioalkyl, and haloalkyl;  
 E 0  is selected from the group consisting of a bond, C(O)N(H), (H)NC(O), (R 7 )NS(O) 2 , and S(O) 2 N(R 7 );  
 Y AT  is Q b -Q s ;  
 Q s  is (CR 37 R 38 ) b  wherein b is an integer selected from 1 through 4, R 37  is selected from the group consisting of hydrido, alkyl, and haloalkyl, and R 38  is selected from the group consisting of hydrido, alkyl, haloalkyl, aroyl, and heteroaroyl with the proviso that there is at least one aroyl or heteroaroyl substituent, with the further proviso that no more than one aroyl or heteroaroyl is bonded to (CR 37 R 38 ) b  at the same time, with the still further proviso that said aroyl and said heteroaroyl are optionally substituted with one or more substituents selected from the group consisting of R 16 , R 17 , R 18 , and R 19 , with another further proviso that said aroyl and said heteroaroyl are bonded to the CR 37 R 38  that is directly bonded to E 0 , with still another further proviso that no more than one alkyl or one haloalkyl is bonded to a CR 37 R 38 , and with the additional proviso that said alkyl and haloalkyl are bonded to a carbon other than the one bonding said aroyl or said heteroaroyl;  
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, amidino, guanidino, carboxy, haloalkylthio, alkoxy, hydroxy, amino, alkoxyamino, alkylamino, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoyl, haloalkanoyl, alkyl, halo, haloalkyl, haloalkoxy, hydroxyalkyl, aminoalkyl, and cyano;  
 Q b  is selected from the group consisting of NR 20 R 21 , hydrido, N(R 26 )C(NR 25 )N(R 23 )(R 24 ), and C(NR 25 )NR 23 R 24 , with the proviso that no more than one of R 20  and R 21  is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino and with the further proviso that no more than one of R 23  and R 24  is selected from the group consisting of hydroxy, amino, alkylamino, and dialkylamino and;  
 R 20 , R 21 , R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, alkyl, hydroxy, amino, alkylamino and dialkylamino.  
 
     
     
         34 . Compound of  claim 33  of the Formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of: 
 (i) phenyl and 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyrrolyl, 3-pyrrolyl, 2-imidazolyl, 4-imidazolyl, 3-pyrazolyl, 4-pyrazolyl, 2-thiazolyl, 3-isoxazolyl, and 5-isoxazolyl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 32 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 36 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 32 , is optionally substituted by R 33 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 36 , is optionally substituted by R 35 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 33  and R 35 , respectively, is optionally substituted by R 34 ;  
 (ii) hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butenyl, 2-butynyl, sec-butyl, tert-butyl, isobutyl, 2-methylpropenyl, 1-pentyl, 2-pentenyl, 3-pentenyl, 2-pentynyl, 3-pentynyl, 2-pentyl, 3-pentyl, 2-methylbutyl, 2-methyl-2-butenyl, 3-methylbutyl, 3-methyl-2-butenyl, 1-hexyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 2-hexyl, 1-methyl-2-pentenyl, 1-methyl-3-pentenyl, 1-methyl-2-pentynyl, 1-methyl-3-pentynyl, 3-hexyl, 1-ethyl-2-butenyl, 1-heptyl, 2-heptenyl, 3-heptenyl, 4-heptenyl, 5-heptenyl, 2-heptynyl, 3-heptynyl, 4-heptynyl, 5-heptynyl, 2-heptyl, 1-methyl-2-hexenyl, 1-methyl-3-hexenyl, 1-methyl-4-hexenyl, 1-methyl-2-hexynyl, 1-methyl-3-hexynyl, 1-methyl-4-hexynyl, 3-heptyl, 1-ethyl-2-pentenyl, 1-ethyl-3-pentenyl, 1-ethyl-2-pentynyl, 1-ethyl-3-pentynyl, 2,2,2-trifluoroethyl, 2,2-difluoropropyl, 4-trifluoromethyl-5,5,5-trifluoropentyl, 4-trifluoromethylpentyl, 5,5,6,6,6-pentafluorohexyl, and 3,3,3-trifluoropropyl, wherein each member of group B is optionally substituted at any carbon up to and including 5 atoms from the point of attachment of B to A with one or more of the group consisting of R 32 , R 33 , R 34 , R 33 , and R 36 ; and  
 (iii) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, bicyclo[3.1.0]hexan-6-yl, 2-morpholinyl, 3-morpholinyl, 4-morpholinyl, 1-piperazinyl, 2-piperazinyl, 1-piperidinyl, 2-piperidinyl, 3-piperidinyl, 4-piperidinyl, 1-pyrrolidinyl, 2-pyrrolidinyl, 3-pyrrolidinyl, 2-dioxanyl, 2-tetrahydrofuranyl, 3-tetrahydrofuranyl, 2-tetrahydropyranyl, 3-tetrahydropyranyl, 4-tetrahydropyranyl, 2-tetrahydrothienyl, and 3-tetrahydrothienyl, wherein (a) each ring carbon may be optionally substituted with R 33 , (b) a ring carbon or nitrogen in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (c) a ring carbon or nitrogen in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (d) a ring carbon or nitrogen atom, if present, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , and (e) a ring carbon or nitrogen, if present, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 ;  
 
 R 32 , R 33 , R 34 , R 35 , and R 36  are independently selected from the group consisting of hydrido, amidino, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, dimethylamino, methoxyamino, methylthio, ethylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, hydroxymethyl, amidocarbonyl, carboxy, cyano, and Q b ;  
 R 9 , R 11 , and R 13  are independently selected from the group consisting of hydrido, methyl, ethyl, methoxy, ethoxy, hydroxy, amino, N-methylamino, N,N-dimethylamino, methylthio, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, fluoro, chloro, bromo, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, hydroxymethyl, 1-hydroxyethyl, amidocarbonyl, N-methylamidocarbonyl, carboxy, and cyano;  
 R 10  and R 12  are independently selected from the group consisting of hydrido, amidino, amidocarbonyl, N-methylamidocarbonyl, N-benzylamidocarbonyl, N-(2-chlorobenzyl)amidocarbonyl, N-(3-fluorobenzyl)amidocarbonyl, N-(2-trifluoromethylbenzyl)amidocarbonyl, N-(1-phenylethyl)amidocarbonyl, N-(1-methyl-1-phenylethyl)amidocarbonyl, N-benzylamidosulfonyl, N-(2-chlorobenzyl)amidosulfonyl, N-ethylamidocarbonyl, N-isopropylamidocarbonyl, N-propylamidocarbonyl, N-isobutylamidocarbonyl, N-(2-butyl)amidocarbonyl, N-cyclobutylamidocarbonyl, N-cyclopentylamidocarbonyl, N-cyclohexylamidocarbonyl, guanidino, methyl, ethyl, methoxy, ethoxy, hydroxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, carboxy, carboxymethyl, amino, acetamido, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoroacetamido, aminomethyl, N-methylamino, dimethylamino, methoxyamino, amidosulfonyl, N-methylamidosulfonyl, N,N-dimethylamidosulfonyl, methanesulfonamido, methoxycarbonyl, fluoro, chloro, bromo, and cyano;  
 A is selected from the group consisting of a bond, NH, N(CH 3 ), CH 2 , CH 3 CH, CH 2 CH 2 , and CH 2 CH 2 CH 2 ;  
 X o  is selected from the group consisting of hydrido, hydroxy, amino, aminomethyl, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, methoxy, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, methylthio, ethylthio, trifluoromethoxy,1,1,2,2-tetrafluoroethoxy, fluoro, chloro, and bromo;  
 R 2  is selected from the group consisting of phenyl and 2-thienyl, 2-furyl, 2-pyrrolyl, 2-imidazolyl, 2-thiazolyl, 3-isoxazolyl, 2-pyridyl, and 3-pyridyl heteroaryl rings, wherein (a) a ring carbon in a first alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 9 , (b) a ring carbon in a second alpha position relative to the ring carbon at the point of attachment is optionally substituted by R 13 , (c) a ring carbon, in a first beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 9 , is optionally substituted by R 10 , (d) a ring carbon, in a second beta position relative to the ring carbon at the point of attachment and in an alpha position relative to the ring atom optionally substituted by R 13 , is optionally substituted by R 12 , and (e) a ring carbon, if present, in the gamma position relative to the ring carbon at the point of attachment and in an alpha position relative to each of the ring atoms optionally substituted by R 10  and R 12 , respectively, is optionally substituted by R 11 ;  
 Y AT  is Q b -Q s ;  
 Q s  is selected from the group consisting of: C[R 37 (benzoyl)(CR 37 R 38 ) b ], C[R 37 (2-pyridylcarbonyl)(CR 37 R 38 ) b ], C[R 37 (3-pyridylcarbonyl)(CR 37 R 38 ) b ], C[R 37 (4-pyridylcarbonyl)(CR 37 R 38 ) b ], C[R 37 (2-thienylcarbonyl)(CR 37 R 38 ) b ], C[R 37 (3-thienylcarbonyl)(CR 37 R 38 ) b ], C[R 37 (2-thiazolylcarbonyl)(CR 37 R 38 ) b ], C[R 37 (4-thiazolylcarbonyl)(CR 37 R 38 ) b ], and C[R 37 (5-thiazolylcarbonyl)((CR 37 R 38 ) b ], wherein b is an integer selected from 1 through 3, R 37  and R 38  are independently selected from the group consisting of hydrido, alkyl, and haloalkyl, with the proviso that said benzoyl and the heteroaroyls are optionally substituted with one or more substituents selected from the group consisting of R 16 , R 17 , R 18 , and R 19  with the proviso that R 17  and R 18  are optionally substituted at a carbon selected from other than the meta and para carbons relative to the carbonyl of the benzoyl or heteroaroyl, with the further proviso that said benzoyl or said heteroaroyl are bonded to the carbon directly bonded to amide nitrogen of the 1-(amidocarbonymethylene) group, and with the still further proviso that is no more than one alkyl or one haloalkyl is bonded to a CR 37 R 38 ;  
 R 16 , R 17 , R 18 , and R 19  are independently selected from the group consisting of hydrido, methyl, ethyl, amidino, guanidino, methoxy, hydroxy, amino, aminomethyl, 1-aminoethyl, 2-aminoethyl, N-methylamino, dimethylamino, methylthio, ethylthio, trifluoromethylthio, methylsulfinyl, methylsulfonyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, trifluoromethoxy, fluoro, chloro, hydroxymethyl, carboxy, and cyano;  
 Q b  is C(NR 25 )NR 23 R 24  or N(R 26 )C(NR 25 )N(R 23 )(R 24 ); and  
 R 23 , R 24 , R 25 , and R 26  are independently selected from the group consisting of hydrido, methyl, and ethyl.  
 
     
     
         35 . Compound of  claim 34  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of: 
 (i) 2-aminophenyl, 3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl, 3-carboxyphenyl, 3-carboxy-5-hydroxyphenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 3,4-difluorophenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3-methoxyaminophenyl, 3-methoxyphenyl, 4-methoxyphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoromethylphenyl, 2-imidazoyl, 2-pyridyl, 3-pyridyl, 5-chloro-3-trifluoromethyl-2-pyridyl, 4-pyridyl, 2-thienyl, 3-thienyl, and 3-trifluoromethyl-2-pyridyl;  
 (ii) hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl, (S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4-methyl-2-pentyl, 3-hydroxypropyl, 1-methoxy-2-propyl, 2-methoxyethyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl, 2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl; and  
 (iii) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, 1-pyrrolidinyl and 1-piperidinyl;  
   A is selected from the group consisting of a bond, CH 2 , CH 3 CH, CH 2 CH 2 , and CH 2 CH 2 CH 2 ;    X 0  is selected from the group consisting of hydrido, hydroxy, 1-aminoethyl, methyl, ethyl, trifluoromethyl, pentafluoroethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 1-hydroxyethyl, 2-hydroxyethyl, fluoro, chloro, and bromo;    R 2  is selected from the group consisting of    3-amidocarbonyl-5-aminophenyl, 3-amidocarbonyl-5-aminophenyl,    3-amino-5-(N-benzylamidocarbonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-benzylamidosulfonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,    3-amino-5-(N-ethylamidocarbonyl)phenyl,    3-amino-5-(N-isopropylamidocarbonyl)phenyl,    3-amino-5-(N-propylamidocarbonyl)phenyl,    3-amino-5-(N-isobutylamidocarbonyl)phenyl,    3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,    3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,    3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,    3-amino-5-(N-cyclohexylamidocarbonyl)phenyl,    5-amino-2-fluorophenyl, 3-amino-5-hydroxymethylphenyl,    5-amino-3-methoxycarbonylphenyl, 3-amidinophenyl,    3-amino-2-methylphenyl, 5-amino-2-methylthiophenyl, 3-aminophenyl,    3-carboxyphenyl, 3-carboxy-5-aminophenyl, 3-carboxy-5-hydroxyphenyl,    3-carboxymethyl-5-aminophenyl, 3-carboxymethyl-5-hydroxyphenyl,    3-carboxymethylphenyl, 3-chlorophenyl, 2-chlorophenyl, 3-cyanophenyl,    ,5-diaminophenyl, 3-dimethylaminophenyl, 2-fluorophenyl, 3-fluorophenyl,    2,5-difluorophenyl, 2-hydroxyphenyl, 3-hydroxyphenyl,    3-methanesulfonylaminophenyl, 2-methoxyphenyl, 3-methoxyphenyl,    3-methoxyaminophenyl, 3-methoxycarbonylphenyl, 2-methylaminophenyl, 3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, phenyl, 3-trifluoroacetamidophenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 5-amino-2-thienyl, 5-amino-3-thienyl, 3-bromo-2-thienyl, 3-pyridyl, 4-pyridyl, 2-thienyl, and 3-thienyl; 
 Y AT  is Q b -Q s ;  
 Q s  is selected from the group consisting of: [CH(benzoyl)](CH 2 ) b , [CH(2-pyridylcarbonyl)](CH 2 ) b , [CH(3-pyridylcarbonyl)](CH 2 ) b , [CH(4-pyridylcarbonyl)](CH 2 ) b , [CH(2-thienylcarbonyl)](CH 2 ) b , [CH(3-thienylcarbonyl)](CH 2 ) b , [CH(2-thiazolylcarbonyl)](CH 2 ) b , [CH(4-thiazolylcarbonyl)](CH 2 ) b , and [CH(5-thiazolylcarbonyl)](CH 2 ) b , wherein b is an integer selected from 1 through 3, with the proviso that said benzoyl and said heteroaroyls are optionally substituted with one or more substituents selected from the group consisting of R 16 , R 17 , R 18 , and R 19  with the proviso that R 17  and R 18  are optionally substituted at a carbon selected from other than the meta and para carbons relative to the carbonyl of the benzoyl or the heteroaroyl, and that said benzoyl or said heteroaroyl are bonded to the carbon directly bonded to amide nitrogen of the 1-(amidocarbonymethylene) group;  
 R 16  and R 19  are independently selected from the group consisting of hydrido, amidino, amino, aminomethyl, methoxy, methylamino, hydroxy, hydroxymethyl, fluoro, chloro, and cyano;  
 R 17  and R 18  are independently selected from the group consisting of hydrido, fluoro, chloro, hydroxy, hydroxymethyl, amino, carboxy, and cyano;  
 Q b  is N(R 26 )C(NR 25 )N(R 23 )(R 24 ); and  
 R 23 , R 24 , R 25 , and R 26  are independently hydrido or methyl.  
   
     
     
         36 . Compound of  claim 35  or a pharmaceutically acceptable salt thereof, wherein; 
 B is selected from the group consisting of: 
 (i) 3-aminophenyl, 3-amidinophenyl, 4-amidinophenyl, 3-chlorophenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 2-fluorophenyl, 4-methylphenyl, phenyl, 2-imidazoyl, 3-pyridyl, 4-pyridyl, and 3-trifluoromethyl-2-pyridyl;  
 (ii) hydrido, ethyl, 2-propenyl, 2-propynyl, propyl, isopropyl, butyl, 2-butyl, (R)-2-butyl, (S)-2-butyl, tert-butyl, isobutyl, 1-pentyl, 3-pentyl, 2-methylbutyl, 2,2,2-trifluoroethyl, 6-amidocarbonylhexyl, 4-methyl-2-pentyl, 3-hydroxypropyl, 1-methoxy-2-propyl, 2-methoxyethyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 2-dimethylaminopropyl, 2-cyanoethyl, 6-hydroxyhexyl, 2-hydroxyethyl, 2-amidinoethyl, 2-guanidinoethyl, 3-guanidinopropyl, 4-guanidinobutyl, 3-hydroxypropyl, 4-hydroxybutyl, 6-cyanohexyl, 2-dimethylaminoethyl, 3-methylbutyl, 2-methylbutyl, (S)-2-methylbutyl, 3-aminopropyl, 2-hexyl, and 4-aminobutyl; and  
 (iii) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, oxalan-2-yl, 2-(2R)-bicyclo[2.2.1]-heptyl, oxetan-3-yl, azetidin-1-yl, azetidin-2-yl, azetidin-3-yl, and 1-piperidinyl;  
   A is selected from the group consisting of a bond, CH 2 , CH 2 CH 2  and CH 2 CH 2 CH 2 ;    X o  is selected from the group consisting of hydrido, aminomethyl, methyl, ethyl, trifluoromethyl, 2,2,2-trifluoroethyl, hydroxymethyl, 2-hydroxyethyl, chloro, and fluoro;    R 2  is selected from the group consisting of    3-amidocarbonyl-5-aminophenyl, 3-amino-5-(N-benzylamidocarbonyl)phenyl, 3-amino-5-(N-(2-chlorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(3-fluorobenzyl)amidocarbonyl)phenyl,    3-amino-5-(N-(2-trifluoromethylbenzyl)amidocarbonyl)phenyl,    3-amino-5-N-(1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-N-(1-methyl-1-phenylethyl)amidocarbonyl)phenyl,    3-amino-5-(N-benzylamidosulfonyl)phenyl,    3-amino-5-(N-(2-chlorobenzyl)amidosulfonyl)phenyl,    3-amino-5-(N-ethylamidocarbonyl)phenyl,    3-amino-5-(N-isopropylamidocarbonyl)phenyl,    3-amino-5-(N-propylamidocarbonyl)phenyl,    3-amino-5-(N-isobutylamidocarbonyl)phenyl,    3-amino-5-(N-(2-butyl)amidocarbonyl)phenyl,    3-amino-5-(N-cyclobutylamidocarbonyl)phenyl,    3-amino-5-(N-cyclopentylamidocarbonyl)phenyl,    3-amino-5-(N-cyclohexylamidocarbonyl)phenyl, 3-aminophenyl,    3-carboxy-5-aminophenyl, 3-chlorophenyl, 3,5-diaminophenyl,    3-dimethylaminophenyl, 3-hydroxyphenyl, 3-methanesulfonylaminophenyl,    3-methylaminophenyl, 2-methylphenyl, 3-methylphenyl, phenyl,    3-trifluoroacetamidophenyl, 3-bromo-2-thienyl, 2-thienyl, and 3-thienyl; and 
 Y AT  is selected from the group consisting of 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, 5-guanidino-1-oxo-1-(4-thiazolyl)-2-pentyl, 5-guanidino-1-oxo-1-(5-thiazolyl)-2-pentyl, 5-guanidino-1-oxo-1-(4-amino-2-thiazolyl)-2-pentyl, and 5-guanidino-1-oxo-1-phenyl-2-pentyl.  
   
     
     
         37 . A compound as recited in  claim 33 , or a pharmaceutically acceptable salt thereof, wherein: 
 R 2  is 3-aminophenyl, B is phenyl, A is CH 2 CH 2 , Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3,5-diaminophenyl, B is phenyl, A is CH 2 CH 2 , Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-carboxy-5-aminophenyl, B is phenyl, A is CH 2 CH 2 , Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is phenyl, A is CH 2 CH 2 , Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3,5-diaminophenyl, B is isopropyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-carboxy-5-aminophenyl, B is isopropyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3,5-diaminophenyl, B is cyclobutyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-aminophenyl, B is phenyl, A is CH 2 CH 2 , Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3,5-diaminophenyl, B is phenyl, A is CH 2 CH 2 , Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-carboxy-5-aminophenyl, B is phenyl, A is CH 2 CH 2 , Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is phenyl, A is CH 2 CH 2 , Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3,5-diaminophenyl, B is isopropyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-carboxy-5-aminophenyl, B is isopropyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is isopropyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3,5-diaminophenyl, B is cyclobutyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido;    R 2  is 3-carboxy-5-aminophenyl, B is cyclobutyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido; or    R 2  is 3-amino-5-(N-benzylamidocarbonyl)phenyl, B is cyclobutyl, A is single bond, Y AT  is 5-guanidino-1-oxo-1-(2-thiazolyl)-2-pentyl, and X O  is hydrido.    
     
     
         38 . A composition for inhibiting thrombotic conditions in blood comprising a compound of  claim 1  and a pharmaceutically acceptable carrier.  
     
     
         39 . A method for inhibiting thrombotic conditions in blood comprising adding to blood a therapeutically effective amount of a composition of  claim 38 .  
     
     
         40 . A method for inhibiting formation of blood platelet aggregates in blood comprising adding to blood a therapeutically effective amount of a composition of  claim 38 .  
     
     
         41 . A method for inhibiting thrombus formation in blood comprising adding to blood a therapeutically effective amount of a composition of  claim 38 .  
     
     
         42 . A method for treating or preventing venuous thromboembolism and pulmonary embolism in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of  claim 38 .  
     
     
         43 . A method for treating or preventing deep vein thrombosis in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of  claim 38 .  
     
     
         44 . A method for treating or preventing cardiogenic thromboembolism in a mammal comprising administering to the mammal a therapeutically effective amount of a composition of  claim 38 .  
     
     
         45 . A method for treating or preventing thromboembolic stroke in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of  claim 38 .  
     
     
         46 . A method for treating or preventing thrombosis associated with cancer and cancer chemotherapy in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of  claim 38 .  
     
     
         47 . A method for treating or preventing unstable angina in humans and other mammals comprising administering to the mammal a therapeutically effective amount of a composition of  claim 38 .  
     
     
         48 . A method for inhibiting thrombus formation in blood comprising adding to blood a therapeutically effective amount of a compound of  claim 1  with a therapeutically effective amount of fibrinogen receptor antagonist.