Pyrrolopyrimidine and pyrrolopyridine derivatives substituted with cyclic amino group
Abstract
An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. [Solution] A pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.
Claims
exact text as granted — not AI-modified1 . A pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by the following formula [I]:
(wherein the cyclic amino group is represented by the following formula [II]:
in which the cyclic amino group is a 3- to 8-membered saturated cyclic amine or a 3- to 8-membered saturated cyclic amine bridged with C 1-5 alkylene or C 1-4 alkylene-O—C 1-4 alkylene between any different two carbon atoms of the cyclic amine, which cyclic amine is substituted with a group represented by —(CR 1 R 2 ) m —(CHR 3 ) n —X, R 4 and R 5 independently on the same or different carbon atoms of the cyclic amine;
X is cyano, hydroxy or —OR 9 ;
Y is N or CR 10 ;
R 1 is hydrogen, hydroxy, C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl or hydroxy-C 1-5 alkyl;
R 2 is hydrogen or C 1-5 alkyl;
R 3 is hydrogen, cyano, C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl or hydroxy-C 1-5 alkyl;
m is an integer selected from 0, 1, 2, 3, 4 and 5;
n is 0 or 1;
with the proviso that when X is hydroxy or OR 9 , and n is 0, then m is an integer selected from 1, 2, 3, 4 and 5;
R 4 is hydrogen, hydroxy, hydroxy-C 1-5 alkyl, cyano, cyano-C 1-5 alkyl or C 1-5 alkyl;
R 5 is hydrogen or C 1-5 alkyl;
R 6 is hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, hydroxy, C 1-5 alkoxy, C 3-8 cycloalkyloxy or —N(R 11 )R 12 ;
R 7 and R 8 are the same or different, and independently are hydrogen, halogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, hydroxy, C 1-5 alkoxy, C 3-8 cycloalkyloxy, —N(R 11a )R 12a , —CO 2 R 13 , cyano, nitro, C 1-5 alkylthio, trifluoromethyl or trifluoromethoxy; or R 7 and R 8 are taken together to form —CH 2 —CH 2 —CH 2 —CH 2 — or —CH═CH—CH═CH—;
R 9 is C 1-24 acyl, C 1-10 alkoxycarbonyl, aryl-C 1-5 alkyloxycarbonyl, —CO—O—CHR 14 —O—CO—R 15 , —P(═O)(OR 14a )OR 15a , —CO—(CH 2 ) p —(CHR 16 ) q —NR 17 R 18 , arylcarbonyl or heteroarylcarbonyl, wherein each said acyl, aryl and heteroaryl is unsubstituted or substituted with C 1-5 alkoxy, and C 1-24 acyl optionally includes one to six double bonds;
R 10 is hydrogen, C 1-5 alkyl, halogen, cyano or —CO 2 R 19 ;
Ar is aryl or heteroaryl which aryl or heteroaryl is unsubstituted or substituted with 1 or more substituents, which are the same or different, selected from the group consisting of halogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 2-5 alkenyl, C 2-5 alkynyl, C 1-5 alkoxy, C 1-5 alkylthio, C 1-5 alkylsulfinyl, C 1-5 alkylsulfonyl, cyano, nitro, hydroxy, —CO 2 R 19a , C(═O)R 19a , CONR 11b R 12b , —OC(═O)R 19a , —NR 11b CO 2 R 19b , —S(O) r NR 11b R 12b , hydroxy-C 2-5 alkylamino-C 2-5 alkoxy, trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoromethoxy, methylenedioxy, ethylenedioxy and —N(R 20 )R 21 ; with the proviso that when X is hydroxy, Y is N, and the cyclic amino group is 5-membered ring, then Ar is aryl or heteroaryl which aryl or heteroaryl is substituted with at least one of substituents which are selected from halogen and trifluoromethyl;
R 11 and R 12 are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-5 alkyl;
R 11a and R 12a are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-5 alkyl;
R 11b and R 12b are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-5 alkyl;
R 13 is hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl, C 3-8 cycloalkyloxy-C 1-5 alkyl or phenyl;
R 14 and R 15 are the same or different, and independently are hydrogen, C 1-5 alkyl or aryl-C 1-5 alkyl;
R 14a and R 15a are the same or different, and independently are hydrogen, C 1-5 alkyl or aryl-C 1-5 alkyl;
R 16 is hydrogen, C 1-5 alkyl, aryl, heteroaryl, aryl-C 1-5 alkyl, heteroaryl-C 1-5 alkyl, hydroxy-C 1-5 alkyl, hydroxycarbonyl-C 1-5 alkyl, hydroxyphenyl-C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl, amino-C 1-5 alkyl, guanidino-C 1-5 alkyl, mercapto-C 1-5 alkyl, C 1-5 alkylthio-C 1-5 alkyl or aminocarbonyl-C 1-5 alkyl;
R 17 and R 18 are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, C 1-10 acyl, C 1-10 alkoxycarbonyl or aryl-C 1-5 alkyloxycarbonyl;
or R 16 and R 17 are taken together to form —CH 2 —, —CH 2 CH 2 —, —CH 2 CH 2 CH 2 — or —CH 2 CH 2 CH 2 CH 2 —;
p is an integer selected from 0, 1, 2, 3, 4 and 5;
q is 0 or 1;
R 19 is hydrogen or C 1-5 alkyl;
R 19a is hydrogen or C 1-5 alkyl;
r is 1 or 2;
R 20 and R 21 are the same or different, and independently are hydrogen or C 1-5 alkyl), individual isomers thereof, racemic or non-racemic mixtures of isomers thereof or N-oxide thereof, or pharmaceutically acceptable salts and hydrates thereof.
2 . The pyrrolopyrimidine or pyrrolopyridine derivative substituted with the cyclic amino group according to claim 1 , which is a compound represented by the following formula [III]:
(wherein the cyclic amino group is represented by the following formula [IV]:
in which the cyclic amino group is a 3- to 8-membered saturated cyclic amine or a 3- to 8-membered saturated cyclic amine bridged with C 1-5 alkylene or C 1-4 alkylene-O—C 1-4 alkylene between any different two carbon atoms of the cyclic amine, which cyclic amine is substituted with a group represented by —(CR 1 R 2 ) m —(CHR 3 ) n —CN, R 4 and R 5 independently on the same or different carbon atoms of the cyclic amine;
Y is N or CR 10 ;
R 1 is hydrogen, hydroxy, C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl or hydroxy-C 1-5 alkyl;
R 2 is hydrogen or C 1-5 alkyl;
R 3 is hydrogen, cyano, C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl or hydroxy-C 1-5 alkyl;
m is an integer selected from 0, 1, 2, 3, 4 and 5;
n is 0 or 1;
R 4 is hydrogen, hydroxy, hydroxy-C 1-5 alkyl, cyano, cyano-C 1-5 alkyl or C 1-5 alkyl;
R 5 is hydrogen or C 1-5 alkyl;
R 6 is hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, hydroxy, C 1-5 alkoxy, C 3-8 cycloalkyloxy or —N(R 11 )R 12 ;
R 7 and R 8 are the same or different, and independently are hydrogen, halogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, hydroxy, C 1-5 alkoxy, C 3-8 cycloalkyloxy, —N(R 11a )R 12a , —CO 2 R 13 , cyano, nitro, C 1-5 alkylthio, trifluoromethyl or trifluoromethoxy; or R 7 and R 8 are taken together to form —CH 2 —CH 2 —CH 2 —CH 2 — or —CH═CH—CH═CH—;
R 10 is hydrogen, C 1-5 alkyl, halogen, cyano or —CO 2 R 19 ;
Ar is aryl or heteroaryl which aryl or heteroaryl is unsubstituted or substituted with 1 or more substituents, which are the same or different, selected from the group consisting of halogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 2-5 alkenyl, C 2-5 alkynyl, C 1-5 alkoxy, C 1-5 alkylthio, C 1-5 alkylsulfinyl C 1-5 alkylsulfonyl, cyano, nitro, hydroxy, —CO 2 R 19a , —C(═O)R 19a , —CONR 11b R 12b , —OC(═O)R 19a , —NR 11b CO 2 R 19a , S(O) r NR 11b R 12b , hydroxy-C 2-5 alkylamino-C 2-5 alkoxy, trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoromethoxy, methylenedioxy, ethylenedioxy and —N(R 20 )R 21 ;
R 11 and R 12 are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-5 alkyl;
R 11 and R 12 are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-5 alkyl;
R 11b and R 12b are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-15 alkyl;
R 13 is hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl, C 3-8 cycloalkyloxy-C 1-5 alkyl or phenyl;
R 19 is hydrogen or C 1-5 alkyl;
R 19a is hydrogen or C 1-5 alkyl;
r is 1 or 2;
R 20 and R 21 are the same or different, and independently are hydrogen or C 1-5 alkyl), individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
3 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 2 represented by formula [III], wherein Y is N; the cyclic amino group, m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and Ar are as defined in claim 2; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
4 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 2 represented by formula [III], wherein Y is N; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; the cyclic amino group, m, R 6 , R 7 , R 8 and Ar are as defined in claim 2; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
5 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 2 represented by formula [III], wherein Y is N; the cyclic amino group is a 4- to 7-membered saturated cyclic amine; m is an integer selected from 0, 1, 2 and 3; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or C 1-5 alkyl; Ar is phenyl or pyridyl which phenyl or pyridyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of halogen, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and —N(R 20 )R 21 (wherein R 20 and R 21 are the same or different, and independently are hydrogen or C 1-3 alkyl); individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
6 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 2 represented by formula [III], wherein Y is N; the cyclic amino group is a 6-membered saturated cyclic amine; m is 0 or 1; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or methyl; Ar is phenyl which phenyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of chloro, bromo, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and dimethylamino; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
7 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 2 represented by formula [III], wherein Y is CR 10 ; the cyclic amino group, m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 R 8 , R 10 and Ar are as defined in claim 2; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
8 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 2 represented by formula [III], wherein Y is CR 10 ; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 10 is hydrogen or halogen; the cyclic amino group, m, R 6 , R 7 , R 8 and Ar are as defined in claim 2; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
9 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 2 represented by formula [III], wherein Y is CR 10 ; the cyclic amino group is a 4- to 7-membered saturated cyclic amine; m is an integer selected from 0, 1, 2 and 3; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or C 1-5 alkyl; R 10 is hydrogen or halogen; Ar is phenyl or pyridyl which phenyl or pyridyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of halogen, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and —N(R 20 )R 21 (wherein R 20 and R 21 are the same or different, and independently are hydrogen or C 1-3 alkyl); individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
10 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 2 represented by formula [III], wherein Y is CR 10 ; the cyclic amino group is a 6-membered saturated cyclic amine; m is 0 or 1; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or methyl; R 10 is hydrogen; Ar is phenyl which phenyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of chloro, bromo, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and dimethylamino; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
11 . The pyrrolopyrimidine or pyrrolopyridine derivative substituted with the cyclic amino group according to claim 1 , which is a compound represented by the following formula [V]:
(wherein the cyclic amino group is represented by the following formula [VI]:
in which the cyclic amino group is a 3- to 8-membered saturated cyclic amine or a 3- to 8-membered saturated cyclic amine bridged with C 1-5 alkylene or C 1-4 alkylene-O—C 1-4 alkylene between any different two carbon atoms of the cyclic amine, which cyclic amine is substituted with a group represented by —(CR 1 R 2 ) m —(CHR 3 ) n —OH, R 4 and R 5 independently on the same or different carbon atoms of the cyclic amine;
Y is N or CR 10 ;
R 1 is hydrogen, hydroxy, C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl or hydroxy-C 1-5 alkyl;
R 2 is hydrogen or C 1-5 alkyl;
R 3 is hydrogen, cyano, C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl or hydroxy-C 1-5 alkyl;
m is an integer selected from 0, 1, 2, 3, 4 and 5;
n is 0 or 1;
with the proviso that when n is 0, m is an integer selected from 1, 2, 3, 4 and 5;
R 4 is hydrogen, hydroxy, hydroxy-C 1-5 alkyl, cyano, cyano-C 1-5 alkyl or C 1-5 alkyl;
R 5 is hydrogen or C 1-5 alkyl;
R 6 is hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, hydroxy, C 1-5 alkoxy, C 3-8 cycloalkyloxy or —N(R 11 )R 12 ;
R 7 and R 8 are the same or different, and independently are hydrogen, halogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, hydroxy, C 1-5 alkoxy, C 3-8 cycloalkyloxy, —N(R 11a )R 12a , —CO 2 R 13 , cyano, nitro, C 1-5 alkylthio, trifluoromethyl or trifluoromethoxy; or R 7 and R 8 are taken together to form —CH 2 —CH 2 —CH 2 —CH 2 — or —CH═CH—CH═CH—;
R 10 is hydrogen, C 1-5 alkyl, halogen, cyano or —CO 2 R 19 ;
Ar is aryl or heteroaryl which aryl or heteroaryl is unsubstituted or substituted with 1 or more substituents, which are the same or different, selected from the group consisting of halogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 2-5 alkenyl, C 2-5 alkynyl, C 1-5 alkoxy, C 1-5 alkylthio, C 1-5 alkylsulfinyl, C 1-5 alkylsulfonyl, cyano, nitro, hydroxy, —CO 2 R 19a , C(═O)R 19a , CONR 11b R 12b —OC(═O)R 19a , —NR 11b CO 2 R 19a , —S(O) r NR 11b R 12b , hydroxy-C 2-5 alkylamino-C 2-5 alkoxy, trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoromethoxy, methylenedioxy, ethylenedioxy and —N(R 20 )R 21 ; with the proviso that when Y is N, and the cyclic amino group is 5-membered ring, then Ar is aryl or heteroaryl which aryl or heteroaryl is substituted with at least one of substituents which are selected from halogen and trifluoromethyl;
R 11 and R 12 are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-5 alkyl;
R 11a and R 12a are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-5 alkyl;
R 11b and R 12b are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-5 alkyl;
R 13 is hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl, C 3-8 cycloalkyloxy-C 1-5 alkyl or phenyl;
R 19 is hydrogen or C 1-5 alkyl;
R 19a is hydrogen or C 1-5 alkyl;
r is 1 or 2;
R 20 and R 21 are the same or different, and independently are hydrogen or C 1-5 alkyl), individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
12 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is N; the cyclic amino group, m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and Ar are as defined in claim 11; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
13 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is N; m is an integer selected from 1, 2, 3, 4 and 5; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; the cyclic amino group, R 6 , R 7 , R 8 and Ar are as defined in claim 11; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
14 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is N; the cyclic amino group is a 4- to 7-membered saturated cyclic amine; m is an integer selected from 1, 2 and 3; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or C 1-5 alkyl; Ar is phenyl or pyridyl which phenyl or pyridyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of halogen, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and —N(R 20 R 21 (wherein R 20 and R 21 are the same or different, and independently are hydrogen or C 1-3 alkyl); with the proviso that when the cyclic amino group is 5-membered ring, Ar is phenyl or pyridyl which phenyl or pyridyl is substituted with at least one of substituents which are selected from halogen and trifluoromethyl; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
15 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is N; the cyclic amino group is a 6-membered saturated cyclic amine; m is an integer selected from 1, 2 and 3; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or methyl; Ar is phenyl which phenyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of chloro, bromo, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and dimethylamino; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
16 . The pyrrolopyrimidine derivatives substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is N; m is 1; n is 0; R 1 is C 1-5 alkyl or hydroxy-C 1-5 alkyl; R 2 , R 4 and R 5 are hydrogen; the cyclic amino group, R 6 , R 7 , R 8 and Ar are as defined in claim 11; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
17 . The pyrrolopyrimidine derivatives substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is N; m is 1; n is 0; the cyclic amino group is a 4- to 7-membered saturated cyclic amine; R 1 is C 1-5 alkyl or hydroxy-C 1-5 alkyl; R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or C 1-5 alkyl; Ar is phenyl or pyridyl which phenyl or pyridyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of halogen, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and —N(R 20 )R 21 (wherein R 20 and R 21 are the same or different, and independently are hydrogen or C 1-3 alkyl); individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
18 . The pyrrolopyrimidine derivatives substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is N; m is 1; n is 0; the cyclic amino group is a 6-membered saturated cyclic amine; R 1 is C 1-5 alkyl or hydroxy-C 1-5 alkyl; R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and RB are the same or different, and independently are hydrogen or methyl; Ar is phenyl which phenyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of chloro, bromo, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and dimethylamino; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
19 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is N; m is an integer selected from 1, 2, 3, 4 and 5; n is 0; R 1 , R 2 and R 5 are hydrogen; R 4 is cyano; the cyclic amino group, R 6 , R 7 , R 8 and Ar are as defined in claim 11 , wherein a group represented by —(CR 1 R 2 ) m —(CHR 3 ) n —OH and R 4 are substituted on the same carbon atom of the cyclic amine; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
20 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is N; the cyclic amino group is a 4- to 7-membered saturated cyclic amine; m is an integer selected from 1, 2 and 3; n is 0; R 1 , R 2 and R 5 are hydrogen; R 4 is cyano; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or C 1-5 alkyl; Ar is phenyl or pyridyl which phenyl or pyridyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of halogen, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and —N(R 20 )R 21 (wherein R 20 and R 21 are the same or different, and independently are hydrogen or C 1-3 alkyl), wherein a group represented by —(CR 1 R 2 ) m —(CHR 3 ) n —OH and R 4 are substituted on the same carbon atom of the cyclic amine; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
21 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is N; the cyclic amino group is a 6-membered saturated cyclic amine; m is an integer selected from 1, 2 and 3; n is 0; R 1 , R 2 and R 5 are hydrogen; R 4 is cyano; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or methyl; Ar is phenyl which phenyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of chloro, bromo, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and dimethylamino, wherein a group represented by —(CR 1 R 2 ) m , —(CHR 3 ) n —OH and R 4 are substituted on the same carbon atom of the cyclic amine; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
22 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is CR 10 ; the cyclic amino group, m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 10 and Ar are as defined in claim 11; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
23 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is CR 10 ; m is an integer selected from 1, 2, 3, 4 and 5; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 10 is hydrogen or halogen; the cyclic amino group, R 6 , R 7 , R 9 and Ar are as defined in claim 11; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof or pharmaceutically acceptable salts and hydrates thereof.
24 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is CR 10 ; the cyclic amino group is a 4- to 7-membered saturated cyclic amine; m is an integer selected from 1, 2 and 3; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or C 1-5 alkyl; R 10 is hydrogen or halogen; Ar is phenyl or pyridyl which phenyl or pyridyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of halogen, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and —N(R 20 )R 21 (wherein R 20 and R 21 are the same or different, and independently are hydrogen or C 1-3 alkyl); individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
25 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is CR 10 ; the cyclic amino group is a 6-membered saturated cyclic amine; m is an integer selected from 1, 2 and 3;
n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or methyl; R 10 is hydrogen; Ar is phenyl which phenyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of chloro, bromo, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and dimethylamino; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
26 . The pyrrolopyridine derivatives substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is CR 10 ; m is 1; n is 0; R 1 is C 1-5 alkyl or hydroxy-C 1-5 alkyl; R 2 , R 4 and R 5 are hydrogen; R 10 is hydrogen or halogen; the cyclic amino group, R 6 , R 7 , R 8 and Ar are as defined in claim 11; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
27 . The pyrrolopyridine derivatives substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is CR 10 ; m is 1; n is 0; the cyclic amino group is a 4- to 7-membered saturated cyclic amine; R 1 is C 1-5 alkyl or hydroxy-C 1-5 alkyl; R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or C 1-5 alkyl; R 10 is hydrogen or halogen; Ar is phenyl or pyridyl which phenyl or pyridyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of halogen, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and —N(R 20 )R 21 (wherein R 20 and R 21 are the same or different, and independently are hydrogen or C 1-3 alkyl); individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
28 . The pyrrolopyridine derivatives substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is CR 10 ; m is 1; n is 0; the cyclic amino group is a 6-membered saturated cyclic amine; R 1 is C 1-5 alkyl or hydroxy-C 1-5 alkyl; R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or methyl; R 10 is hydrogen; Ar is phenyl which phenyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of chloro, bromo, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and dimethylamino; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
29 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is CR 10 ; m is an integer selected from 1, 2, 3, 4 and 5; n is 0; R 1 , R 2 and R 5 are hydrogen; R 4 is cyano; R 10 is hydrogen or halogen; the cyclic amino group, R 6 , R 7 , R 8 and Ar are as defined in claim 11 , wherein a group represented by —(CR 1 R 2 ) m —(CHR 3 ) n —OH and R 4 are substituted on the same carbon atom of the cyclic amine; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
30 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is CR 10 ; the cyclic amino group is a 4- to 7-membered saturated cyclic amine; m is an integer selected from 1, 2 and 3; n is 0; R 1 , R 2 and R 5 are hydrogen; R 4 is cyano; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or C 1-5 alkyl; R 10 is hydrogen or halogen; Ar is phenyl or pyridyl which phenyl or pyridyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of halogen, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and —N(R 20 )R 21 (wherein R 20 and R 21 are the same or different, and independently are hydrogen or C 1-3 alkyl), wherein a group represented by (CR 1 R 2 ) m —(CHR 3 ) n —OH and R 4 are substituted on the same carbon atom of the cyclic amine; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
31 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 11 represented by formula [V], wherein Y is CR 10 ; the cyclic amino group is a 6-membered saturated cyclic amine; m is an integer selected from 1, 2 and 3; n is 0; R 1 , R 2 and R 5 are hydrogen; R 4 is cyano; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or methyl; R 10 is hydrogen; Ar is phenyl which phenyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of chloro, bromo, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and dimethylamino, wherein a group represented by —(CR 1 R 2 ) m —(CHR 3 ) n —OH and R 4 are substituted on the same carbon atom of the cyclic amine; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
32 . The pyrrolopyrimidine or pyrrolopyridine derivative substituted with the cyclic amino group according to claim 1 , which is a compound represented by the following formula [VII]:
(wherein the cyclic amino group is represented by the following formula [VIII]:
in which the cyclic amino group is a 3- to 8-membered saturated cyclic amine or a 3- to 8-membered saturated cyclic amine bridged with C 1-5 alkylene or C 1-4 alkylene-O—C 1-4 alkylene between any different two carbon atoms of the cyclic amine, which cyclic amine is substituted with a group represented by —(CR 1 R 2 ) m —(CHR 3 ) n —OR 9 , R 4 and R 5 independently on the same or different carbon atoms of the cyclic amine;
Y is N or CR 10 ;
R 1 is hydrogen, hydroxy, C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl or hydroxy-C 1-5 alkyl;
R 2 is hydrogen or C 1-5 alkyl;
R 3 is hydrogen, cyano, C 105 alkyl, C 1-5 alkoxy-C 1-5 alkyl or hydroxy-C 1-5 alkyl;
m is an integer selected from 0, 1, 2, 3, 4 and 5;
n is 0 or 1;
with the proviso that when n is 0, m is an integer selected from 1, 2, 3, 4 and 5;
R 4 is hydrogen, hydroxy, hydroxy-C 1-5 alkyl, cyano, cyano-C 1-5 alkyl or C 1-5 alkyl;
R 5 is hydrogen or C 1-5 alkyl;
R 6 is hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, hydroxy, C 1-5 alkoxy, C 3-8 cycloalkyloxy or —N(R 11 )R 12 ;
R 7 and R 8 are the same or different, and independently are hydrogen, halogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, hydroxy, C 1-5 alkoxy, C 3-8 cycloalkyloxy —N(R 11a )R 12a , —CO 2 R 13 , cyano, nitro, C 1-5 alkylthio, trifluoromethyl or trifluoromethoxy; or R 7 and R 8 are taken together to form —CH 2 —CH 2 —CH 2 —CH 2 — or —CH═CH—CH═CH—;
R 9 is C 1-24 acyl, C 1-10 alkoxycarbonyl, aryl-C 1-5 alkyloxycarbonyl, —CO—O—CHR 14 —O—CO—R 15 , P(═O)(OR 14a )OR 15a , —CO—(CH 2 ) p —(CHR 16 ) q —NR 17 R 18 , arylcarbonyl or heteroarylcarbonyl, wherein each said acyl, aryl and heteroaryl is unsubstituted or substituted with C 1-5 alkoxy, and C 1-24 acyl optionally includes one to six double bonds;
R 10 is hydrogen, C 1-5 alkyl, halogen, cyano or —CO 2 R 19 ;
Ar is aryl or heteroaryl which aryl or heteroaryl is unsubstituted or substituted with 1 or more substituents, which are the same or different, selected from the group consisting of halogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 2-5 alkenyl, C 2-5 alkynyl, C 1-5 alkoxy, C 1-5 alkylthio, C 1-5 alkylsulfinyl, C 1-5 alkylsulfonyl, cyano, nitro, hydroxy, —CO 2 R 19a , —C(═O)R 19a , —CONR 11b R 12b , —OC(═O)R 19a , —NR 11b CO 2 R 19a , —S(O) r NR 11b R 12b , hydroxy-C 2-5 alkylamino-C 2-5 alkoxy, trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoromethoxy, methylenedioxy, ethylenedioxy and —N(R 20 )R 21 ;
R 11 and R 12 are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-5 alkyl;
R 11a and R 12a are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-5 alkyl;
R 11b and R 12b are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkyl-C 1-5 alkyl;
R 13 is hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl, C 3-8 cycloalkyloxy-C 1-5 alkyl or phenyl;
R 14 and R 15 are the same or different, and independently are hydrogen, C 1-5 alkyl or aryl-C 1-5 alkyl;
R 14a and R 15a are the same or different, and independently are hydrogen, C 1-5 alkyl or aryl-C 1-5 alkyl;
R 16 is hydrogen, C 1-5 alkyl, aryl, heteroaryl, aryl-C 1-5 alkyl, heteroaryl-C 1-5 alkyl, hydroxy-C 1-5 alkyl, hydroxycarbonyl-C 1-5 alkyl, hydroxyphenyl-C 1-5 alkyl, C 1-5 alkoxy-C 1-5 alkyl, amino-C 1-5 alkyl, guanidino-C 1-5 alkyl, mercapto-C 1-5 alkyl, C 1-5 alkylthio-C 1-5 alkyl or aminocarbonyl-C 1-5 alkyl;
R 17 and R 18 are the same or different, and independently are hydrogen, C 1-5 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-5 alkyl, C 1-10 acyl, C 1-10 alkoxycarbonyl and aryl-C 1-5 alkyloxycarbonyl,
or R 16 and R 17 are taken together to form —CH 2 —, —CH 2 CH 2 —, —CH 2 CH 2 CH 2 — or —CH 2 CH 2 CH 2 CH 2 —;
p is an integer selected from 0, 1, 2, 3, 4 and 5;
q is 0 or 1;
R 19 is hydrogen or C 1-5 alkyl;
R 19a is hydrogen or C 1-5 alkyl;
r is 1 or 2;
R 20 and R 21 are the same or different, and independently are hydrogen or C 1-5 alkyl), individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
33 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 32 represented by the formula [VII], wherein Y is N; the cyclic amino group, m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and Ar are as defined in claim 32; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
34 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 32 represented by formula [VII], wherein Y is N; m is an integer selected from 1, 2, 3, 4 and 5; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; the cyclic amino group, R 6 , R 7 , R 8 , R 9 and Ar are as defined in claim 32; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
35 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 32 represented by the formula [VII], wherein the cyclic amino group is a 4- to 7-membered saturated cyclic amine; m is an integer selected from 1, 2, 3, 4 and 5; n is 0; Y is N; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or C 1-5 alkyl; Ar is phenyl or pyridyl which phenyl or pyridyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of halogen, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and —N(R 20 )R 21 (wherein R 20 and R 21 are the same or different, and independently are hydrogen or C 1-3 alkyl); R 9 is as defined in claim 32; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
36 . The pyrrolopyrimidine derivative substituted with the cyclic amino group according to claim 32 represented by the formula [VII], wherein the cyclic amino group is a 6-membered saturated cyclic amine; m is an integer selected from 1, 2 and 3; n is 0;
Y is N; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or methyl; Ar is phenyl which phenyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of chloro, bromo, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and dimethylamino; R 9 is as defined in claim 32; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
37 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 32 represented by formula [VII], wherein Y is CR 10 ; the cyclic amino group, m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 and Ar are as defined in claim 32; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
38 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 32 represented by formula [VII], wherein Y is CR 10 ; m is an integer selected from 1, 2, 3, 4 and 5; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; the cyclic amino group, R 6 , R 7 , R 8 , R 9 , R 10 and Ar are as defined in claim 32; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
39 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 32 represented by formula [VII], wherein Y is CR 10 ; the cyclic amino group is a 4- to 7-membered saturated cyclic amine; m is an integer selected from 1, 2 and 3; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 8 are the same or different, and independently are hydrogen or C 1-5 alkyl; R 10 is hydrogen or halogen; Ar is phenyl or pyridyl which phenyl or pyridyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of halogen, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and —N(R 20 )R 21 (wherein R 20 and R 21 are the same or different, and independently are hydrogen or C 1-3 alkyl); R 9 is as defined in claim 32; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
40 . The pyrrolopyridine derivative substituted with the cyclic amino group according to claim 32 represented by formula [VII], wherein Y is CR 10 ; the cyclic amino group is a 6-membered saturated cyclic amine; m is an integer selected from 1, 2 and 3; n is 0; R 1 , R 2 , R 4 and R 5 are hydrogen; R 6 is methyl; R 7 and R 9 are the same or different, and independently are hydrogen or methyl; R 10 is hydrogen; Ar is phenyl which phenyl is substituted with two or three substituents, which are the same or different, selected from the group consisting of chloro, bromo, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkylthio, trifluoromethyl, trifluoromethoxy and dimethylamino; R 9 is as defined in claim 32; individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
41 . Compounds represented by formula [I] according to claim 1 , which compounds are selected from the group consisting of
2-{1-[7-(2,6-dibromo-4-trifluoromethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-2-yl}-ethanol, 2-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-2-yl}-ethanol, 2-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-2-yl}-ethanol, 2-{1-[7-(4-bromo-2,6-diethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-2-yl}-ethanol, 2-{1-[2,5-dimethyl-7-(2,4,6-tribromo-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-2-yl}-ethanol, 3-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-2-yl}-pro pan-1-ol, 3-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-2-yl}-propan-1-ol, {1-[7-(2,4-dibromo-6-methoxy-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-methanol, {1-[7-(2,4-dibromo-6-methylsulfanyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-methanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-methanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-methanol, {1-[2,5-dimethyl-7-(2,4,6-tribromo-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-methanol, 2-{1-[7-(2,6-dibromo-4-trifluoromethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-ethanol, 2-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-y}}-ethanol, 2-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-ethanol, 2-{1-[2,5-dimethyl-7-(2,4,6-tribromo-phenyl)-7H-pyrrolo-2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-ethanol, {1-[2,5,6-trimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[2,5-dimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(2,6-dibromo-4-trifluoromethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[2-methyl-9-(2,4,6-trimethyl-phenyl)-9H-1,3,9-triaza-fluoren-4-yl]-piperidin-4-yl}-methanol, {1-[7-(4-bromo-2,6-diethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(4-bromo-2,6-diethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[2,5,6-trimethyl-7-(2,4,6-tribromo-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[2,5-dimethyl-7-(2,4,6-tribromo-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(4-bromo-2,6-dichloro-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(4-bromo-2,6-dichloro-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(2,6-dibromo-4-isopropyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(2,6-dibromo-4-isopropyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(4-chloro-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(4-chloro-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, 2-{1-[7-(2,6-dibromo-4-trifluoromethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[2,5,6-trimethyl-7-(2,4,6-tribromo-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[2,5-dimethyl-7-(2,4,6-tribromo-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-ethanol, 3-{1-[2,5,6-trimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[2,5-dimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[7-(2,6-dibromo-4-trifluoromethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[2,5-dimethyl-7-(2,4,6-tribromo-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[7-(4-bromo-2,6-dichloro-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[7-(4-bromo-2,6-dichloro-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-propan-1-ol, {1-[7-(2,6-dibromo-4-trifluoromethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-3-methyl-piperidin-3-yl}-methanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-3-methyl-piperidin-3-yl}-methanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-3-methyl-piperidin-3-yl}-methanol, 1-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-ethane-1,2-diol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-pyrrolidin-2-yl}-methanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-pyrrolidin-2-yl}-methanol, 2-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-pyrrolidin-3-yl}-ethanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-azepan-4-yl}-methanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-azepan-4-yl}-methanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-2-yl}-acetonitrile, 1-[2,5,6-trimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-3-carbonitrile, 1-[2,5-dimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-3-carbonitrile, 1-[7-(2,4-dibromo-6-methylsulfanyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-3-carbonitrile, 1-[7-(2,6-dibromo-4-trifluoromethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-3-carbonitrile, 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-3-carbonitrile, 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-3-carbonitrile, 1-[7-(4-isopropyl-2-methylsulfanyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-3-carbonitrile, 1-[7-(4-isopropyl-2-methylsulfanyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-3-carbonitrile, 1-[7-(2-bromo-4-trifluoromethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-3-carbonitrile, 1-[7-(4-bromo-2,6-diethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-3-carbonitrile, 1-[7-(4-bromo-2,6-diethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-3-carbonitrile, {1-[7-(2,6-dibromo-4-trifluoromethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-acetonitrile, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-acetonitrile, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-acetonitrile, 3-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-propionitrile, 3-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-3-yl}-propionitrile, 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-4-carbonitrile, 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-4-carbonitrile, {1-[2,5,6-trimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(2,6-dibromo-4-trifluoromethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(4-bromo-2,6-diethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(4-bromo-2,6-diethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[2,5,6-trimethyl-7-(2,4,6-tribromo-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[2,5-dimethyl-7-(2,4,6-tribromo-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(4-bromo-2,6-dichloro-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(4-bromo-2,6-dichloro-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(2,6-dibromo-4-isopropyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(2,6-dibromo-4-isopropyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(4-methoxy-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(4-methoxy-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(4-chloro-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(4-chloro-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, 8-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-8-aza-bicyclo[3.2.1]octane-3-carbonitrile, 8-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-8-aza-bicyclo[3.2.1]octane-3-carbonitrile, 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-pyrrolidine-3-carbonitrile, 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-pyrrolidine-3-carbonitrile, 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-azepane-4-carbonitrile, 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-azepane-4-carbonitrile, 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-3-hydroxymethyl-piperidine-3-carbonitrile, {1-[7-(4-isopropyl-2-methylsulfanyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(2-bromo-4-isopropyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(2,4-dibromo-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(2,6-dibromo-4-chloro-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, 2-{1-[7-(2,6-dibromo-4-chloro-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-ethanol, 1-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-propane-1,3-diol, {1-[7-(2,6-dibromo-4-chloro-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-pyrrolidin-3-yl}-acetonitrile, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-pyrrolidin-3-yl}-acetonitrile, {1-[2,5-dimethyl-7-(2,4,6-trichloro-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, {1-[7-(2,6-dichloro-4-trifluoromethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-methanol, 3-{1-[7-(4-chloro-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-propan-1-ol, 1-[7-(4-chloro-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidine-4-carbonitrile, {1-[7-(2,6-Dichloro-4-trifluoromethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-acetonitrile, 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-azetidine-3-carbonitrile, 1-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-ethanol, 1-{1-[7-(4-isopropyl-2-methylsulfanyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-ethanol, 1-{1-[7-(4-chloro-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-ethanol, 1-{1-[7-(4-chloro-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-ethanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-3-methyl-piperidin-4-yl}-methanol, {1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-3-methyl-piperidin-4-yl}-methanol, {8-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-8-aza-bicyclo[3.2.1]oct-3-yl}-methanol, {8-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-8-aza-bicyclo[3.2.1]oct-3-yl}-methanol, {8-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-8-aza-bicyclo[3.2.1]oct-3-yl}-acetonitrile, {8-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-8-aza-bicyclo[3.2.1]oct-3-yl}-acetonitrile, 2-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-malononitrile, 2-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-yl}-malononitrile, 2-{1-[1-(2,4-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-3-yl}-ethanol, 2-{1-[1-(4-bromo-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-3-yl}-ethanol, {1-[1-(2,4-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(4-bromo-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, 2-{1-[1-(2,4-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(4-bromo-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 3-{1-[1-(2,4-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[1-(4-bromo-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 1-[1-(2,4-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-3-carbonitrile, 1-[1-(4-bromo-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-3-carbonitrile, {1-[1-(2,4-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-3-yl}-acetonitrile, 1-[1-(2,4-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(4-bromo-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, {1-[1-(2,4-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, 2-{1-[1-(4-bromo-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-3-yl}-ethanol, {1-[1-(4-bromo-2,6-dimethyl-phenyl)-2,3,6-trimethyl-H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(4-chloro-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(4-chloro-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, 2-{1-[1-(4-bromo-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(4-chloro-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(4-chloro-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 3-{1-[1-(4-bromo-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[1-(4-chloro-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[1-(4-chloro-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 1-[1-(4-bromo-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-3-carbonitrile, 1-[1-(4-bromo-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(4-chloro-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(4-chloro-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, {1-[1-(4-bromo-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(4-bromo-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(4-chloro-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(2,6-dibromo-4-isopropyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(2,6-dibromo-4-isopropyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[2,3,6-trimethyl-1-(2,4,6-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[3,6-dimethyl-1-(2,4,6-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(4-bromo-2,6-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(4-bromo-2,6-dichloro-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[2,3,6-trimethyl-1-(2,4,6-trichloro-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[3,6-dimethyl-1-(2,4,6-trichloro-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(2,6-dibromo-4-chloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(2,6-dibromo-4-chloro-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(4-methoxy-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(4-methoxy-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(2-bromo-4-isopropyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(4-isopropyl-2-methylsulfanyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(2,4-dibromo-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[1-(2-bromo-4-trifluoromethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[2,3,6-trimethyl-1-(2,4,5-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, {1-[3,6-dimethyl-1-(2,4,5-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-methanol, 2-{1-[1-(2,6-dibromo-4-isopropyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(2,6-dibromo-4-isopropyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[2,3,6-trimethyl-1-(2,4,6-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[3,6-dimethyl-1-(2,4,6-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(4-bromo-2,6-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(4-bromo-2,6-dichloro-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[2,3,6-trimethyl-1-(2,4,6-trichloro-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[3,6-dimethyl-(2,4,6-trichloro-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(2,6-dibromo-4-chloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(2,6-dibromo-4-chloro-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(4-methoxy-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(4-methoxy-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(2-bromo-4-isopropyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(4-isopropyl-2-methylsulfanyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[1-(2,4-dibromo-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[2,3,6-trimethyl-1-(2,4,5-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[3,6-dimethyl-1-(2,4,5-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 2-{1-[5-bromo-1-(4-chloro-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethanol, 3-{1-[1-(2,6-dibromo-4-isopropyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[1-(2,6-dibromo-4-isopropyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[2,3,6-trimethyl-1-(2,4,6-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[3,6-dimethyl-1-(2,4,6-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[1-(4-bromo-2,6-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[1-(4-bromo-2,6-dichloro-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[2,3,6-trimethyl-1-(2,4,6-trichloro-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[3,6-dimethyl-1-(2,4,6-trichloro-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[1-(2,6-dibromo-4-chloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[1-(2,6-dibromo-4-chloro-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[1-(4-methoxy-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-pro pan-1-ol, 3-{1-[1-(4-methoxy-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[1-(4-isopropyl-2-methylsulfanyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[2,3,6-trimethyl-1-(2,4,5-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 3-{1-[3,6-dimethyl-1-(2,4,5-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propan-1-ol, 1-{1-[1-(4-bromo-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethane-1,2-diol, 1-{1-[1-(4-bromo-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-ethane-1,2-diol, 1-{1-[1-(4-bromo-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propane-1,3-diol, 1-{1-[1-(4-bromo-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-propane-1,3-diol, 1-[1-(2,6-dibromo-4-isopropyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(2,6-dibromo-4-isopropyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[2,3,6-trimethyl-1-(2,4,6-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[3,6-dimethyl-1-(2,4,6-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(4-bromo-2,6-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(4-bromo-2,6-dichloro-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[2,3,6-trimethyl-1-(2,4,6-trichloro-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[3,6-dimethyl-1-(2,4,6-trichloro-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(2,6-dibromo-4-chloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(2,6-dibromo-4-chloro-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(4-methoxy-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(4-methoxy-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(2-bromo-4-isopropyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(4-isopropyl-2-methylsulfanyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(2,4-dibromo-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[1-(2-bromo-4-trifluoromethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[2,3,6-trimethyl-1-(2,4,5-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, 1-[3,6-dimethyl-1-(2,4,5-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidine-4-carbonitrile, {1-[1-(4-chloro-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(2,6-dibromo-4-isopropyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(2,6-dibromo-4-isopropyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[2,3,6-trimethyl-1-(2,4,6-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[3,6-dimethyl-1-(2,4,6-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(4-bromo-2,6-dichloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(4-bromo-2,6-dichloro-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[2,3,6-trimethyl-1-(2,4,6-trichloro-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[3,6-dimethyl-1-(2,4,6-trichloro-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(2,6-dibromo-4-chloro-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(2,6-dibromo-4-chloro-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(4-methoxy-2,6-dimethyl-phenyl)-2,3,6-trimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(4-methoxy-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(2-bromo-4-isopropyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(4-isopropyl-2-methylsulfanyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(2,4-dibromo-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[1-(2-bromo-4-trifluoromethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, {1-[3,6-dimethyl-1-(2,4,5-tribromo-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-yl}-acetonitrile, carbonic acid 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-ylmethyl ester ethyl ester, pyridine-2-carboxylic acid 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-ylmethyl ester, methoxy-acetic acid 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-ylmethyl ester, methoxy-acetic acid 1-[1-(4-bromo-2,6-dimethyl-phenyl)-3,6-dimethyl-1H-pyrrolo[2,3-b]pyridin-4-yl]-piperidin-4-ylmethyl ester, carbonic acid benzyl ester 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-ylmethyl ester, decanoic acid 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-ylmethyl ester, 3-diethylamino-propionic acid 1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-ylmethyl ester and phosphoric acid mono-{1-[7-(4-bromo-2,6-dimethyl-phenyl)-2,5-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-piperidin-4-ylmethyl} ester, individual isomers thereof or racemic or non-racemic mixtures of isomers thereof, or pharmaceutically acceptable salts and hydrates thereof.
42 . An antagonist for CRF receptors, comprising a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group, a pharmaceutically acceptable salt thereof or its hydrate according to any one of claims 1 to 41 , as an active ingredient.
43 . Use of a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group, a pharmaceutically acceptable salt thereof or its hydrate according to any one of claim 1 to 41 , for the manufacture of an antagonist for CRF receptors.Join the waitlist — get patent alerts
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