US2002115657A1PendingUtilityA1
Substituted hetero-polycyclic compounds as PPARalpha and PPARgamma
Priority: Oct 21, 1998Filed: Feb 8, 2002Published: Aug 22, 2002
Est. expiryOct 21, 2018(expired)· nominal 20-yr term from priority
C07D 273/06C07D 471/04C07D 209/86C07D 279/34C07D 223/22C07D 209/88
51
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Claims
Abstract
The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
Claims
exact text as granted — not AI-modified1 . A compound of formula (Ia)
wherein R 1 , R 2 , R 3 , and R 4 independently of each other represent hydrogen, halogen, perhalomethyl, hydroxy, nitro, cyano, formyl, or C 1-12 -alkyl, C 4-12 -alkenynyl, C 2-12 -alkenyl, C 2-12 -alkynyl, C 1-12 -alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyC 1-12 -alkyl, amino, acylamino, C 1-12 -alkylamino, arylamino, aralkylamino, aminoC 1-12 -alkyl, C 1-12 -alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, C 1-12 -alkoxyC 1-12 -alkyl, aryloxyC 1-12 -alkyl, aralkoxyC 1-12 -alkyl, C 1-12 -alkylthio, thioC 1-12 -alkyl, C 1-12 -alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR 11 , or —SO 2 R 2 , wherein R 11 and R 12 independently of each other are selected from hydroxy, halogen, perhalomethyl, C 1-6 -alkoxy or amino optionally substituted with one or more C 1-6 -alkyl, perhalomethyl or aryl; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano;
or R 1 and R 2 , R 2 and R 3 and/or R 3 and R 4 may form a cyclic ring containing from 5 to 7 carbon atoms optionally substituted with one or more C 1-6 -alkyl;
ring A fused to the ring containing X and N represents a 5-6 membered cyclic ring, optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro, cyano, formyl, or C 1-12 -alkyl, C 4-12 -alkenynyl, C 2-12 -alkenyl, C 2-12 -alkynyl, C 1-12 -alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyC 1-12 -alkyl, amino, acylamino, C 1-12 -alkylamino, arylamino, aralkylamino, aminoC 1-12 -alkyl, C 1-12 -alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, C 1-12 -alkoxyC 1-12 -alkyl, aryloxyC 1-12 -alkyl, aralkoxyC 1-12 -alkyl, C 1-12 -alkylthio, thioC 1-12 -alkyl, C 1-12 -alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR 11 , or —SO 2 R 12 , wherein R 11 and R 12 independently of each other are selected from hydroxy, halogen, perhalomethyl, C 1-6 -alkoxy or amino optionally substituted with one or more C 1-6 -alkyl, perhalomethyl or aryl; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano; X is a valence bond, —(CHR 9 )—, —(CHR 9 )—CH 2 —, —CH═CH—, —O—(CHR 9 )—, —S—(CHR 9 )—, —(NR 9 )—CH 2 —, —(CHR 9 )—CH═CH—, —(CHR 9 )—CH 2 —CH 2 , —(C═O)—, —O—CH 2 —O—, —(NR 9 )—S(O 2 )—, —CH═(CR 9 )—, —(CO)—(CHR 9 )—, —CH 2 —(SO)—, —(SO)—, —(SO 2 )—, —CH 2 —(SO 2 )—, —CH 2 —O—CH 2 —, wherein R 9 is hydrogen, halogen, hydroxy, nitro, cyano, formyl, C 1-12 -alkyl, C 1-12 -alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyalkyl, amino, acylamino, C 1-12 -alkylamino, arylamino, aralkylamino, aminoC 1-12 -alkyl, C 1-12 -alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, C 1-12 -alkoxyC 1-12 -alkyl, aryloxyC 1-12 -alkyl, aralkoxyC 1-12 -alkyl, C 1-12 -alkylthio, thioC 1-12 -alkyl, C 1-12 -alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR 13 , or —SO 2 R 14 , wherein R 13 and R 14 independently of each other are selected from hydroxy, halogen, C 1-6 -alkoxy, amino optionally substituted with one or more C 1-6 -alkyl, perhalomethyl or aryl;
Ar represents arylene, heteroarylene, or a divalent heterocyclic group optionally substituted with one or more C 1-6 -alkyl or aryl;
R 5 represents hydrogen, hydroxy, halogen, C 1-12 -alkoxy, C 1-12 -alkyl, C 4-12 -alkenynyl, C 2-12 -alkenyl, C 2-12 -alkynyl or aralkyl; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano; or R 5 forms a bond together with R 6 ,
R 6 represents hydrogen, hydroxy, halogen, C 1-12 -alkoxy, C 1-12 -alkyl, C 4-12 -alkenynyl, C 2-12 -alkenyl, C 2-12 -alkynyl, acyl or aralkyl; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano; or R 6 forms a bond together with R 5 ,
R 7 represents hydrogen, C 1-12 -alkyl, C 4-12 -alkenynyl, C 2 -, 2 -alkenyl, C 2-12 -alkynyl, aryl C 1-12 -alkoxyC 1-12 -alkyl, C 1-12 -alkoxycarbonyl, aryloxycarbonyl, C 112 -alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl or heteroaralkyl groups; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano;
R 8 represents hydrogen, C 1-12 -alkyl, C 4-12 -alkenynyl, C 2-12 -alkenyl, C 2-12 -alkynyl, aryl, aralkyl heterocyclyl, heteroaryl or heteroaralkyl groups; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano;
Y represents oxygen, sulphur or NR 10 , where R 10 represents hydrogen, C 1-12 -alkyl, aryl, hydroxyC 1-12 -alkyl or aralkyl groups or when Y is NR 10 , R 8 and R 10 may form a 5 or 6 membered nitrogen containing ring, optionally substituted with one or more C 1-6 -alkyl;
n is an integer ranging from 1 to 4 and m is an integer ranging from 0 to 1;
or a pharmaceutically acceptable salt thereof.
2 . A compound according to claim 1 wherein R 1 , R 2 , R 3 , and R 4 independently of each other represent hydrogen, halogen, perhalomethyl, hydroxy, cyano, or C 1-7 -alkyl, C 4-7 -alkenynyl, C 2-7 -alkenyl, C 2-7 -alkynyl, C 2-7 -alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyC 1-7 -alkyl, amino, acylamino, C 1-7 -alkylamino, arylamino, aralkylamino, aminoC 1-7 -alkyl, C 1-7 -alkoxyC 1-7 -alkyl, aryloxyC 1-7 -alkyl, aralkoxyC 1-7 -alkyl, C 1-7 -alkylthio, thioC 1-7 -alkyl, C 1-7 -alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR 11 , or —SO 2 R 12 , wherein R 11 and R 12 independently of each other are selected from hydroxy, perhalomethyl or amino optionally substituted with one or more C 1-6 -alkyl, perhalomethyl or aryl; optionally substituted with one or more halogen, perhalomethyl, hydroxy or cyano;
or R 1 and R 2 , R 2 and R 3 and/or R 3 and R 4 may form a cyclic ring containing from 5 to 7 carbon atoms optionally substituted with one or more C 1-6 -alkyl.
3 . A compound according to anyone of the preceding claims wherein R 1 , R 2 , R 3 , and R 4 independently of each other represent hydrogen, halogen, perhalomethyl, hydroxy, cyano, or C 1-7 -alkyl, C 4-7 -alkenynyl, C 2-7 -alkenyl, C 2-7 -alkynyl, C 1-7 -alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, amino, acylamino, C 1-7 -alkylamino, arylamino, aralkylamino, aminoC 1-7 -alkyl, C 1-7 -alkoxyC 1-7 -alkyl, aryloxyC 1-7 -alkyl, aralkoxyC 1-7 -alkyl, C 1-7 -alkylthio, thioC 1-7 -alkyl; optionally substituted with one or more halogen or hydroxy.
4 . A compound according to anyone of the preceding claims wherein R 1 , R 2 , R 3 , and R 4 independently of each other represent hydrogen, halogen, perhalomethyl, hydroxy or C 1-7 -alkyl, C 2-7 -alkenyl, C 2-7 -alkynyl, C 1-7 -alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heteroaryl, heteroaryloxy, heteroaralkoxy, acyl, arylamino, aryloxyC 1-7 -alkyl.
5 . A compound according to anyone of the preceding claims wherein R 1 , R 2 , R 3 , and R 4 independently of each other represent hydrogen, halogen, perhalomethyl, hydroxy , C 1-7 -alkyl, C 2-7 alkenyl, C 2-7 -alkynyl, C 1-7 -alkoxy or aryl.
6 . A compound according to anyone of the preceding claims wherein R 1 , R 2 , R 3 and R 4 independently of each other represent hydrogen, halogen or phenyl.
7 . A compound according to anyone of the preceding claims wherein ring A fused to the ring containing X and N represents a 5-6 membered cyclic ring, optionally substituted with one or more hydrogen, halogen, perhalomethyl, hydroxy, cyano, or C 1-7 -alkyl, C 4-7 -alkenynyl, C 2-7 -alkenyl, C 2-7 -alkynyl, C 1-7 -alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyC 1-7 -alkyl, amino, acylamino, C 1-7 alkylamino, arylamino, aralkylamino, aminoC 1-7 -alkyl, C 1-7 -alkoxyC 1-7 -alkyl, aryloxyC 1-7 -alkyl, aralkoxyC 1-7 -alkyl, C 1-7 -alkylthio, thioC 1-7 -alkyl, C 1-7 -alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR 11 , or —SO 2 R 2 , wherein R 11 and R 12 independently of each other are selected from hydroxy, perhalomethyl or amino optionally substituted with one or more C 1-6 -alkyl, perhalomethyl or aryl; optionally substituted with one or more halogen, perhalomethyl, hydroxy or cyano.
8 . A compound according to anyone of the preceding claims wherein ring A fused to the ring containing X and N represents a 5-6 membered cyclic ring, optionally substituted with one or more hydrogen, halogen, perhalomethyl, hydroxy, cyano, or C 1-7 -alkyl, C 7 -alkenynyl, C 2-7 -alkenyl, C 2-7 -alkynyl, C 1-7 -alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, amino, acylamino, C 1-7 -alkylamino, arylamino, aralkylamino, aminoC 1-7 -alkyl, C 1-7 -alkoxyC 1-7 -alkyl, aryloxyC 1-7 -alkyl, aralkoxyC 1-7 -alkyl, C 1-7 -alkylthio, thioC 1-7 -alkyl; optionally substituted with one or more halogen or hydroxy.
9 . A compound according to anyone of the preceding claims wherein ring A fused to the ring containing X and N represents a 5-6 membered cyclic ring, optionally substituted with one or more hydrogen, halogen, perhalomethyl, hydroxy or C 1-7 -alkyl, C 2-7 -alkenyl, C 2-7 -alkynyl, C 1-7 -alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heteroaryl, heteroaryloxy, heteroaralkoxy, acyl, arylamino, aryloxyC 1-7 -alkyl.
10 . A compound according to anyone of the preceding claims wherein ring A fused to the ring containing X and N represents a 5-6 membered cyclic ring, optionally substituted with one or more-hydrogen, halogen, perhalomethyl, hydroxy or C 1-7 -alkyl, C 2-7 -alkenyl, C 2-7 -alkynyl, C 1-7 -alkoxy or aryl.
11 . A compound according to anyone of the preceding claims wherein ring A fused to the ring containing X and N represents a 5-6 membered cyclic ring, optionally substituted with one or more hydrogen, halogen or phenyl.
12 . A compound according to anyone of the preceding claims wherein X is a valence bond, —(CHR 9 )—, —(CHR 9 )—CH 2 —, —CH═CH—, —O—(CHR 9 )—, —S—(CHR 9 )—, —(NR 9 )—CH 2 —, —(CHR 9 )—CH═CH—, —(CHR 9 )—CH 2 —CH 2 —, —(C═O)—, —O—CH 2 —O—, —(NR 9 )—S(O 2 )—, —CH═(CR 9 )—, —(CO)—(CHR 9 )—, —CH 2 —(SO)—, —(SO)—, —(SO 2 )—, —CH 2 —(SO 2 )—, —CH 2 —O—CH 2 —, wherein R is hydrogen, halogen, hydroxy, cyano, C 1-7 -alkyl, C 1-7 -alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyalkyl, amino, acylamino, C 1-7 -alkylamino, arylamino, aralkylamino, aminoC 1-7 -alkyl, C 1-7 -alkoxyC 1-7 -alkyl, aryloxyC 1-7 -alkyl, aralkoxyC 1-7 alkyl, C 1-7 -alkylthio or thioC 1-7 -alkyl.
13 . A compound according to anyone of the preceding claims wherein X is a valence bond, —(CHR 9 )—, —(CHR 9 )—CH 2 —, —CH═CH—, —O—(CHR 9 )—, —S—(CHR 9 )—, —(NR 9 )—CH 2 —, —(CHR 9 )—CH═CH—, —(CHR 9 )—CH 2 —CH 2 —, —(C═O)—, —O—CH 2 —O—, —(NR 9 )—S(O 2 )—, —CH═(CR 9 )—, —(CO)—(CHR 9 )—, —CH 2 —(SO)—, —(SO)—, —(SO 2 )—, —CH 2 —(SO 2 )—, —CH 2 —O—CH 2 —, wherein R 9 is hydrogen, halogen, hydroxy, C 1-7 -alkyl, C 1-7 -alkoxy or aryl.
14 . A compound according to anyone of the preceding claims wherein X is a valence bond, —(CHR 9 )—, —(CHR 9 )—CH 2 —, —CH═CH—, —O—(CHR 9 )—, —S—(CHR 9 )—, —(NR 9 )—CH 2 —, —(CHR 9 )—CH═CH—, —(CHR 9 )—CH 2 —CH 2 —, —(C═O)—, —O—CH 2 —, —(NR 9 )—S(O 2 )—, —CH═(CR 9 )—, —(CO)—(CHR 9 )—, —CH 2 —(SO)—, —(SO)—, —(SO 2 )—, —CH 2 —(SO 2 )—, —CH 2 —O—CH 2 —, wherein R 9 is hydrogen, halogen, hydroxy, C 1-4 -alkyl or C 1-4 -alkoxy.
15 . A compound according to anyone of the preceding claims wherein X is a valence bond, —(CHR 9 )—, —(CHR 9 )—CH 2 —, —CH═CH—, —(CHR 9 )—, —(CHR 9 )—CH═CH—, —(CHR 9 )—CH 2 —CH 2 —, —(C═O)—, —O—CH 2 —, —CH═(CR 9 )—, —(CO)—(CHR 9 )—, —CH 2 —(SO)—, (SO)—, —(SO 2 )—, —CH 2 —(SO 2 )—, —CH 2 —O—CH 2 —, wherein R 9 is hydrogen.
16 . A compound according to anyone of the preceding claims wherein Ar represents arylene, heteroarylene, or a divalent heterocyclic group optionally substituted with one or more C 1-6 -alkyl or aryl;
R 5 represents hydrogen, hydroxy, halogen, C 1-7 -alkoxy, C 1-7 -alkyl, C 4-7 -alkenynyl, C 2-7 -alkenyl, C 2-7 -alkynyl; or R 5 forms a bond together with R 6 , R 6 represents hydrogen, hydroxy, halogen, C 1-7 alkoxy, C 1-7 -alkyl, C 4-7 -alkenynyl, C 2-7 -alkenyl, C 2-7 -alkynyl; or R 6 forms a bond together with R 5 , R 7 represents hydrogen, C 1-7 -alkyl, C 4-7 -alkenynyl, C 2-7 -alkenyl, C 2-7 -alkynyl, aryl, aralkyl, C 1-7 -alkoxyC 1-7 alkyl, C 1-7 alkoxycarbonyl, aryloxycarbonyl, C 1-7 alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl or heteroaralkyl groups; R 8 represents hydrogen, C 1-7 -alkyl, C 1-7 -alkenynyl, C 2-7 -alkenyl, C 2-7 -alkynyl, aryl, aralkyl, heterocyclyl, heteroaryl or heteroaralkyl. Y represents oxygen, sulphur or NR 10 , where R 10 represents hydrogen, C 1-7 -alkyl, hydroxyC 1-7 -alkyl; n is an integer ranging from 2 to 3 and m is an integer ranging from 0 to 1.
17 . A compound according to anyone of the preceding claims wherein Ar represents arylene or heteroarylene;
R 5 represents hydrogen, hydroxy, halogen; or R 5 forms a bond together with R 6 , R 6 represents hydrogen, hydroxy, halogen; or R 6 forms a bond together with R 5 , R 7 represents hydrogen, C 1-7 -alkyl, C 2-7 -alkenyl, C 2-7 -alkynyl, aryl, aralkyl, C 1-7 -alkoxyC 1-7 -alkyl, C 1-7 -alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl or heteroaralkyl groups; R 8 represents hydrogen, C 1-7 -alkyl, C 2-7 -alkenyl, C 2-7 -alkynyl; Y represents oxygen or sulphur, n is an integer ranging from 2 to 3 and m is 1.
18 . A compound according to anyone of the preceding claims wherein Ar represents arylene or heteroarylene;
R 5 represents hydrogen; R 5 represents hydrogen; R 7 represents hydrogen, C 1-7 -alkyl, C 2-7 -alkenyl, C 2-7 -alkynyl, aryl, aralkyl, C,- 7 -alkoxyC 1-7 -alkyl; R 8 represents hydrogen, C 1-7 -alkyl, C 2-7 -alkenyl, C 2-7 -alkynyl; Y represents oxygen; n is an integer ranging from 2 to 3 and m is 1.
19 . A compound according to anyone of the preceding claims wherein Ar represents arylene
R 5 represents hydrogen; R 6 represents hydrogen; R 7 represents hydrogen, C 1-4 -alkyl, C 2-4 -alkenyl, C 2-7 -alkynyl, R 8 represents hydrogen, C 1-4 -alkyl, Y represents oxygen; n is an integer ranging from 2 to 3 and m is 1.
20 . A compound according to anyone of the preceding claims wherein Ar represents phenylene,
R 5 represents hydrogen; R 6 represents hydrogen; R 7 represents hydrogen, C 1-4 -alkyl, R 8 represents hydrogen Y represents oxygen; n is an integer ranging from 2 to 3 and m is 1.
21 . A compound according to anyone of the preceding claims wherein A is benzo optionally substituted with one or more halogen or phenyl.
22 . A compound according to anyone of the preceding claims wherein A is pyrido.
23 . A compound according to anyone of the preceding claims wherein Ar is arylene.
24 . A compound according to anyone of the preceding claims wherein X is —(CHR 9 )—CH 2 —, wherein R 9 is H.
25 . A compound according to anyone of the preceding claims wherein X is —CH═CH—.
26 . A compound according to anyone of the preceding claims wherein X is —(SO)—.
27 . A compound according to anyone of the preceding claims wherein X is —O—CH 2 —O—.
28 . A compound according to anyone of the preceding claims wherein X is a valence bond.
29 . A compound according to anyone of the preceding claims X is —O—CH 2 —.
30 . A compound according to anyone of the preceding claims wherein X is —(CHR 9 )—CH 2 —CH 2 , wherein R 9 is H.
31 . A compound according to anyone of the preceding claims wherein X is —(CO)—(CHR 9 )—, wherein R 9 is H.
32 . A compound according to anyone of the preceding claims wherein X is —CH═(CR 9 )—, wherein R 9 is C 1-12 -alkoxy, preferably methoxy.
33 . A compound according to anyone of the preceding claims wherein X is —(NR 9 )—S(O 2 )—, wherein R 9 is C 1-12 -alkyl, preferably methyl.
34 . A compound according to anyone of the preceding claims wherein X is —(C═O)—.
35 . A compound according to anyone of the preceding claims wherein R 1 , R 2 , R 3 and R 4 are H.
36 . A compound according to anyone of the preceding claims wherein n is 2.
37 . A compound according to anyone of the preceding claims wherein n is 3.
38 . A compound according to anyone of the preceding claims wherein m is 1.
39 . A compound according to anyone of the preceding claims wherein R 5 is H.
40 . A compound according to anyone of the preceding claims wherein R 6 is H.
41 . A compound according to anyone of the preceding claims wherein R 7 is ethyl.
42 . A compound according to anyone of the preceding claims wherein R 8 is H.
43 . A compound according to anyone of the preceding claims wherein R 8 is ethyl.
44 . A compound according to anyone of the preceding claims wherein Y is oxygen.
45 . The compound according to claim 1 which is
3-{4-[2-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-2-ethoxy-propionic acid,
3-{4-[2-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-2-methoxy-propionic acid,
3-{4-[2-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-2-propoxy-propionic acid,
3-{4-[2-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-2-benzyloxy-propionic acid,
3-{4-[2-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-propoxy]-phenyl}-2-ethoxy-propionic acid,
3-{4-[2-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-propoxy]-phenyl}-2-methoxy-propionic acid,
3-{4-[2-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-propyl]-phenyl}-2-ethoxy-propionic acid,
3-{4-[2-(1,11-Dihydro-dibenzo[b,f]azepin-5-yl)-propyl]-phenyl}-2-methoxy-propionic acid,
3-{4-[2-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-methoxy]-phenyl}-2-ethoxy-propionic acid,
2-Ethoxy-3-(4-[2-(5,11 -dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-ethoxy]-phenyl)-propionic acid,
2-Methoxy-3-(4-[2-(5,11 -dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-ethoxy]-phenyl)-propionic acid,
2-Propoxy-3-(4-[2-(5,11-dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-ethoxy]-phenyl)-propionic acid,
2-Benzyloxy-3-(4-[2-(5,11-dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-ethoxy]-phenyl)-propionic acid,
2-Ethoxy-3-(4-[3-(5,11-dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-propoxy]-phenyl)-propionic acid,
2-Methoxy-3-(4-[3-(5,11-dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-propoxy]-phenyl)-propionic acid,
2-Benzyloxy-3-(4-[3-(5,11-dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-propoxy]phenyl)-propionic acid,
2-Ethoxy-3-(4-[3-(5,11-dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-propyl]-phenyl)-acid,
2-Methoxy-3-(4-[3-(5,11-dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-propyl]-phenyl)-propionic acid,
2-Benzyloxy-3-(4-[3-(5,11-dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-propyl]-phenyl)-propionic acid,
2-Ethoxy-3-(4-[1-(5,11-dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-methoxy]phenyl)-propionic acid,
3-{4-[2-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-ethoxy]-phenyl}-2-ethoxy-propionic acid,
3-{4-[2-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-ethoxy]-phenyl}-2-propoxy-propionic acid,
3-{4-[2-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-ethoxy]-phenyl}-2-methoxy-propionic acid,
3-{4-[2-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-ethoxy]-phenyl}-2-benzyloxy-propionic acid,
3-{4-[1-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-methoxy]-phenyl}-2-ethoxy-propionic acid,
3-{4-[3-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-propoxy]-phenyl}-2-ethoxy-propionic acid,
3-{4-[3-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-propoxy]-phenyl}-2-methoxy-propionic acid,
3-{4-[3-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-propoxy]-phenyl}-2-benzyloxy-propionic acid,
3-{4-[3-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-propyl]-phenyl}2-ethoxy-propionic acid,
3-{4-[3-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-propyl]-phenyl}-2-methoxy-propionic acid,
3-{4-[3-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-propyl]-phenyl}-2-benzyloxy-propionic acid,
2-Ethoxy-3-{4-[2-(10-oxo-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Methoxy-3-{4-[2-(10-oxo-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Propoxy-3-{4-[2-(10-oxo-10,11 -dihydro-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[2-(10-oxo-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[1 -(10-oxo-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-methoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[3-(10-oxo-10,11 -dihydro-dibenzo[b,f]azepin-5-yl)-propoxy]-phenyl}-propionic acid,
2-Methoxy-3-{4-[3-(10-oxo-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-propoxy]-phenyl}-propionic acid,
2-Propoxy-3-{4-[3-(10-oxo-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-propoxy]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[3-(10-oxo-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-propoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[3-(10-oxo-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-propyl]-phenyl}-propionic acid,
2-Methoxy-3-{4-[3-(10-oxo-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-propyl]-phenyl}-propion acid,
2-Propoxy-3-{4-[3-(10-oxo-10,11 -dihydro-dibenzo[b,f]azepin-5-yl)-propyl]-phenyl}-propion acid,
2-Benzyloxy-3-{4-[3-(10-oxo-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-propyl]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[2-(10-methoxy-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Methoxy-3-{4-[2-(10-methoxy-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Propoxy-3-{4-[2-(10-methoxy-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[1-(10-methoxy-dibenzo[b,f]azepin-5-yl)-methoxy]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[2-(10-methoxy-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[3-(10-methoxy-dibenzo[b,f]azepin-5-yl)-propoxy]-phenyl}-propionic acid,
2-Methoxy-3-{4-[3-(10-methoxy-dibenzo[b,f]azepin-5-yl)-propoxy]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[3-(10-methoxy-dibenzo[b,f]azepin-5-yl)-propoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[3-(10-methoxydibenzo[b,f]azepin-5-yl)-propyl]-phenyl}-propionic acid,
2-Methoxy-3-{4-[3-(10-methoxy-dibenzo[b,f]azepin-5-yl)-propyl]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[3-(10-methoxy-dibenzo[b,f]azepin-5-yl)-propyl]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[2-(11 -methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a, d]cyclohepten-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Methoxy-3-{4-[2-(11-methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a,d]cyclohepten-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Propoxy-3-{4-[2-(11-methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a,d]cyclohepten-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[2-(11-methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a,d]cyclohepten-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[1-(11-methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a,d]cyclohepten-5-yl)-methoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[3-(11-methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a,d]cyclohepten-5-yl)-propoxy]-phenyl}-propionic acid,
2-Propoxy-3-{4-[3-(11-methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a,d]cyclohepten-5-yl)-propoxy]-phenyl}-propionic acid,
2-Methoxy-3-{4-[3-(11-methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a,d]cyclohepten-5-yl)-propoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[3-(11-methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a,d]cyclohepten-5-yl)-propyl]-phenyl}-propionic acid,
2-Propoxy-3-{4-[3-(11-methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a,d]cyclohepten-5-yl)-propyl]-phenyl}propionic acid,
2-Methoxy-3-{4-[3-(11-methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a,d]cyclohepten-5-yl)-propyl]-phenyl}propionic acid,
2-Ethoxy-3-{4-[2-(9-oxo-9H-acridin-10-yl)-ethoxy]-phenyl}-propionic acid,
2-Methoxy-3-{4-[2-(9-oxo-9H-acridin-10-yl)-ethoxy]-phenyl}-propionic acid,
2-Propoxy-3-{4-[2-(9-oxo-9H-acridin-10-yl)-ethoxy]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[2-(9-oxo-9H-acridin-10-yl)-ethoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[1-(9-oxo-9H-acridin-10-yl)-methoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[3-(9-oxo-9H-acridin-10-yl)-propoxy]-phenyl}-propionic acid,
2-Propoxy-3-{4-[3-(9-oxo-9H-acridin-10-yl)-propoxy]-phenyl}-propionic acid,
2-Methoxy-3-{4-[3-(9-oxo-9H-acridin-10-yl)-propoxy]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[3-(9-oxo-9H-acridin-10-yl)-propoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[3-(9-oxo-9H-acridin-10-yl)-propyl]-phenyl}-propionic acid,
2-Propoxy-3-{4-[3-(9-oxo-9H-acridin-10-yl)-propyl]-phenyl}-propionic acid,
2-Methoxy-3-{4-[3-(9-oxo-9H-acridin-10-yl)-propyl]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[3-(9-oxo-9H-acridin-10-yl)-propyl]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[2-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-ethoxy]-phenyl}-propionic acid,
2-Methoxy-3-{4-[2-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-ethoxy]-phenyl}-propionic acid,
2-Propoxy-3-{4-[2-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-ethoxy]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[2-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-ethoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[3-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-propoxy]-phenyl}-propionic acid,
2-Propoxy-3-{4-[3-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-propoxy]-phenyl}-propionic acid
2-Methoxy-3-{4-[3-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-propoxy]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[3-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-propoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[3-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-propyl]-phenyl}-propionic acid,
2-Propoxy-3-{4-[3-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-propyl]-phenyl}-propionic acid,
2-Methoxy-3-{4-[3-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-propyl]-phenyl}-propionic acid,
2-Benzyloxy-3-{4-[3-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-propyl]-phenyl}-propionic acid,
2-Ethoxy-3-{4-(1-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-methoxy]-phenyl}-propionic acid,
3-(4-(2-(2-Chloro-5-oxo-phenothiazin-10-yl)-ethoxy)-phenyl)-2-ethoxy-propionic acid,
3-(4-(2-(2-Chloro-5-oxo-phenothiazin-10-yl)-ethoxy)-phenyl)-2-propoxy-propionic acid,
3-(4-(2-(2-Chloro-5-oxo-phenothiazin-10-yl)-ethoxy)-phenyl)-2-methoxy-propionic acid,
3-(4-(2-(2-Chloro-5-oxo-phenothiazin-10-yl)-ethoxy)-phenyl)-2-benzyloxy-propionic acid,
3-(4-(1-(2-Chloro-5-oxo-phenothiazin-10-yl)-methoxy)-phenyl)-2-ethoxy-propionic acid,
3-(4-(3-(2-Chloro-5-oxo-phenothiazin-10-yl)-propoxy)-phenyl)-2-ethoxy-propionic acid,
3-(4-(3-(2-Chloro-5-oxo-phenothiazin-10-yl)-propoxy)-phenyl)-2-propoxy-propionic acid,
3-(4-(3-(2-Chloro-5-oxo-phenothiazin-10-yl)-propoxy)-phenyl)-2-methoxy-propionic acid,
3-(4-(3-(2-Chloro-5-oxo-phenothiazin-10-yl)-propoxy)-phenyl)-2-benzyloxy-propionic acid,
3-(4-(3-(2-Chloro-5-oxo-phenothiazin-10-yl)-propyl)-phenyl)-2-ethoxy-propionic acid,
3-(4-(3-(2-Chloro-5-oxo-phenothiazin-10-yl)-propyl)-phenyl)-2-propoxy-propionic acid,
3-(4-(3-(2-Chloro-5-oxo-phenothiazin-10-yl)-propyl)-phenyl)-2-methoxy-propionic acid,
3-(4-(3-(2-Chloro-5-oxo-phenothiazin-10-yl)-propyl)-phenyl)-2-benzyloxy-propionic acid,
(S)-3-(4-(2-(Betacarbolin-9-yl)-ethoxy)-phenyl)-2-ethoxy-propionic acid,
(S)-3-(4-(2-(Betacarbolin-9-yl)-ethoxy)-phenyl)-2-methoxy-propionic acid,
(S)-3-(4-(2-(Betacarbolin-9-yl)-ethoxy)-phenyl)-2-propoxy-propionic acid,
(S)-3-(4-(2-(Betacarbolin-9-yl)-ethoxyl)-phenyl)-2-benzyloxy-propionic acid,
(S)-3-(4-(1-(Betacarbolin-9-yl)-methoxy)-phenyl)-2-ethoxy-propionic acid,
(S)-3-(4-(3-(Betacarbolin-9-yl)-propoxy)-phenyl)-2-ethoxy-propionic acid,
(S)-3-(4-(3-(Betacarbolin-9-yl)-propoxy)-phenyl)-2-methoxy-propionic acid,
(S)-3-(4-(3-(Betacarbolin-9-yl)-propoxy)-phenyl)-2-propoxy-propionic acid,
(S)-3-(4-(3-(Betacarbolin-9-yl)-propoxy)-phenyl)-2-benzyloxy-propionic acid,
(S)-3-(4(3-(Betacarbolin-9-yl)-propyl)-phenyl)-2-ethoxy-propionic acid,
(S)-3-(4-(3-(Betacarbolin-9-yl)-propyl)-phenyl)-2-methoxy-propionic acid,
(S)-3-(4-(3-(Betacarbolin-9-yl)-propyl)-phenyl)-2-propoxy-propionic acid,
(S)-3-(4-(3-(Betacarbolin-9-yl)-propyl)-phenyl)-2-benzyloxy-propionic acid,
3-(4-(2-(Betacarbolin-9-yl)-ethoxy)-phenyl)-2-ethoxy-propionic acid,
3-(4-(2-(Dibenzo[b,d]azepin-5-yl)-ethoxy)-phenyl)-2-ethoxy-propionic acid,
3-(4-(2-(Dibenzo[b,f]azepin-5-yl)-ethoxy)-phenyl)-2-methoxy-propionic acid,
3-(4-(2-(Dibenzo[b,f]azepin-5-yl)-ethoxy)-phenyl)-2-propoxy-propionic acid,
3-(4-(2-(Dibenzo[b,f]azepin-5-yl)-ethoxy)-phenyl)-2-benzyloxy-propionic acid,
3-(4-(1-(Dibenzo[b,f]azepin-5-yl)-methoxy)-phenyl)-2-ethoxy-propionic acid,
3-(4-(3-(Dibenzo[b,f]azepin-5-yl)-propoxy)-phenyl)-2-ethoxy-propionic acid,
3-(4-(3-(Dibenzo[b,f]azepin-5-yl)-propoxy)-phenyl)-2-propoxy-propionic acid,
3-(4-(3-(Dibenzo[b,f]azepin-5-yl)-propoxy)-phenyl)-2-benzyloxy-propionic acid,
3-(4-(3-(Dibenzo[b,f]azepin-5-yl)-propyl)-phenyl)-2-ethoxy-propionic acid,
3-(4-(3-(Dibenzo[b,f]azepin-5-yl)-propyl)-phenyl)-2-propoxy-propionic acid,
3-(4-(3-(Dibenzo[b,f]azepin-5-yl)-propyl)-phenyl)-2-benzyloxy-propionic acid,
3-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-propoxy)-phenyl-2-ethoxy-propionic acid,
3-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-propoxy)-phenyl-2-methoxy-propionic acid,
3-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-propoxy)-phenyl-2-propoxy-propionic acid,
3-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-propoxy)-phenyl-2-benzyloxy-propionic acid,
3-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-propyl)-phenyl-2-ethoxy-propionic acid,
3-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-propyl)-phenyl-2-methoxy-propionic acid,
3-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-propyl)-phenyl-2-propoxy-propionic acid,
3-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-propyl)-phenyl-2-benzyloxy-propionic acid,
2-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-ethoxy)-phenyl-2-ethoxy-propionic acid,
2-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-ethoxy)-phenyl-2-propoxy-propionic acid,
1-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-methoxy)-phenyl-2-ethoxy-propionic acid,
2-(4-Dibenzo[d,g]dioxazocin-12-yl)-1-ethoxy)-phenyl-2-benzyloxy-propionic acid,
(S) 3-(4-(2-(3-Phenyl-carbazol-9-yl)-ethoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(2-(3-Phenyl-carbazol-9-yl)-ethoxy)-phenyl)-2-methoxy-propionic acid,
(S) 3-(4-(2-(3-Phenyl-carbazol-9-yl)-ethoxy)-phenyl)-2-propoxy-propionic acid,
(S) 3-(4-(2-(3-Phenyl-carbazol-9-yl)-ethoxy)-phenyl)-2-benzyloxy-propionic acid,
(S) 3-(4-(1-(3-Phenyl-carbazol-9-yl)-methoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(3-(3-Phenyl-carbazol-9-yl)-propyl)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(3-(3-Phenyl-carbazol-9-yl)-propoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(2-(3-Benzyl-carbazol-9-yl)-ethoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(2-(3-(-Pyridyl)-carbazol-9-yl)-methoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(2-(3-(3-Furanyl)l-carbazol-9-yl)-ethoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(2-(3-(2-thionyl)-carbazol-9-yl)-ethoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(2-(3-Bromo-carbazol-9-yl)-ethoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(2-(3-Bromo-carbazol-9-yl)-ethoxy)-phenyl)-2-methoxy-propionic acid,
(S) 3-(4-(2-(3-Bromo-carbazol-9-yl)-ethoxy)-phenyl)-2-benzyloxy-propionic acid,
(S) 3-(4-(1-(3-Bromo-carbazol-9-yl)-methoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(3-(3-Bromo-carbazol-9-yl)-propyl)-phenyl)-2-ethoxy-propionic acid
(S) 3-(4-(2-(3,6 Dibromo-carbazol-9-yl)-ethoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(2-(3,6 Dibromo-carbazol-9-yl)-ethoxy)-phenyl)-2-methoxy-propionic acid,
(S) 3-(4-(2-(3,6 Dibromo-carbazol-9-yl)-ethoxy)-phenyl)-2-propoxy-propionic acid,
(S) 3-(4-(2-(3,6 Dibromo-carbazol-9-yl)-ethoxy)-phenyl)-2-benzyloxy-propionic acid,
(S) 3-(4-(2-(3,6 Dichloro-carbazol-9-yl)-ethoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(2-(3,6 Dichloro-carbazol-9-yl)-ethoxy)-phenyl)-2-methoxy-propionic acid,
(S) 3-(4-(2-(3,6 Dichloro-carbazol-9-yl)-ethoxy)-phenyl)-2-propoxy-propionic acid,
(S) 3-(4-(2-(3,6 Dichloro-carbazol-9-yl)-ethoxy)-phenyl)-2-benzyloxy-propionic acid,
(S) 3-(4-(2-(3,6 Dibromo-carbazol-9-yl)-methoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(3-(3,6 Dibromo-carbazol-9-yl)-propoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(3-(3,6 Dibromo-carbazol-9-yl)-propyl)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(2-Carbazol-9-yl-ethoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(2-Carbazol-9-yl-ethoxy)-phenyl)-2-methoxy-propionic acid,
(S) 3-(4-(2-Carbazol-9-yl-ethoxy)-phenyl)-2-propoxy-propionic acid,
(S) 3-(4-(2-Carbazol-9-yl-ethoxy)-phenyl)-2-benzyloxy-propionic acid,
(S) 3-(4-(1-Carbazol-9-yl-methoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(3-Carbazol-9-yl-propoxy)-phenyl)-2-ethoxy-propionic acid,
(S) 3-(4-(3-Carbazol-9-yl-propyl)-phenyl)-2-ethoxy-propionic acid;
or a pharmaceutically acceptable salt thereof.
46 . The compound according to claim 1 which is
3-{4-[2-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-2-ethoxy-propionic acid,
2-Ethoxy-3-{4-[2-(5,11-dihydro-5H-dibenzo[b,e][1,4]oxazepin-5-yl)-ethoxy]-phenyl}-acid,
3-{4-[2-(6,7-Dihydro-5H-dibenzo[b,g]azocin-12-yl)-ethoxy]-phenyl}-2-ethoxy-propionic acid,
2-Ethoxy-3-{4-[2-(10-oxo-10,11-dihydro-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[2-(10-methoxy-dibenzo[b,f]azepin-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[2-(11-methyl-10,10-dioxo-10,11-dihydro-10/ 6 -thia-5,11-diaza-dibenzo[a,d]cyclohepten-5-yl)-ethoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[2-(9-oxo-9H-acridin-10-yl)-ethoxy]-phenyl}-propionic acid,
2-Ethoxy-3-{4-[2-(5-oxo-5H-5/ 4 -phenothiazin-10-yl)-ethoxy]-phenyl}-propionic acid; or a
pharmaceutically acceptable salt thereof.
47 . A pharmaceutical composition comprising, as an active ingredient, a compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier or diluent.
48 . A composition according to claim 47 in unit dosage form, comprising from about 0.05 to about 100 mg, preferably from about 0.1 to about 50 mg of the compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof.
49 . A pharmaceutical composition useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR), the composition comprising, as an active ingredient, a compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier or diluent.
50 . A pharmaceutical composition useful in the treatment and/or prevention of diabetes and/or obesity, the composition comprising, as an active ingredient, a compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier or diluent.
51 . A pharmaceutical composition for diabetes and/or obesity, the composition comprising, as an active ingredient, a compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof together with a pharmaceutically acceptable carrier or diluent.
52 . A pharmaceutical composition according to anyone of the claims 47 - 51 for oral, nasal, transdermal, pulmonal, or parenteral administration.
53 . A method for the treatment of ailments, the method comprising administering to a subject in need thereof an effective amount of a compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof, or of a composition according to anyone of the preceding composition claims.
54 . A method for the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR), the method comprising administering to a subject in need thereof an effective amount of a compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof, or of a composition according to anyone of the preceding claims 47 - 52 .
55 . A method for the treatment and/or prevention of diabetes and/or obesity, the method comprising administering to a subject in need thereof an effective amount of a compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof, or of a composition according to anyone of the preceding claims 47 - 52 .
56 . The method according to claims 53 - 55 , wherein the effective amount of the compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt or ester thereof is in the range of from about 0.05 to about 100 mg per day, preferably from about 0.1 to about 50 mg per day.
57 . Use of a compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof for the preparation of a medicament.
58 . Use of a compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof for the preparation of a medicament useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
59 . Use of a compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof for the preparation of a medicament for treatment and/or prevention of diabetes and/or obesity.
60 . Use of a compound according to anyone of the preceding compound claims or a pharmaceutically acceptable salt thereof for the preparation of a medicament for treatment and/or prevention of diabetes and obesity.Join the waitlist — get patent alerts
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