Claims
- 1. A compound of formula (Ia)
33wherein R1, R2, R3, and R4 independently of each other represent hydrogen, halogen, perhalomethyl, hydroxy, nitro, cyano, formyl, or C1-12alkyl, C4-12-alkenynyl, C2-12-alkenyl, C2-12-alkynyl, C1-12alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyC1-12alkyl, amino, acylamino, C1-12alkyl-amino, arylamino, aralkylamino, aminoC1-12alkyl, C1-12alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, C1-12alkoxyC1-12alkyl, aryloxyC1-12alkyl, aralkoxyC1-12alkyl, C1-12alkylthio, thioC1-12alkyl, C1-12alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR11, or —SO2R12, wherein R11 and R12 independently of each other are selected from hydroxy, halogen, perhalomethyl, C1-6alkoxy or amino optionally substituted with one or more C1-6alkyl, perhalomethyl or aryl; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano; or R1 and R2, R2 and R3 and/or R3 and R4 may form a cyclic ring containing from 5 to 7 carbon atoms optionally substituted with one or more C1-6alkyl; ring A represents a 5-6 membered cyclic ring, optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro, cyano, formyl, or C1-12alkyl, C4-12-alkenynyl, C2-12-alkenyl, C2-12-alkynyl, C1-12alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyC1-12alkyl, amino, acylamino, C1-12alkyl-amino, arylamino, aralkylamino, aminoC1-12alkyl, C1-12alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, C1-12alkoxyC1-12alkyl, aryloxyC1-12alkyl, aralkoxyC1-12alkyl, C1-12alkylthio, thioC1-12alkyl, C1-12alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR11, or —SO2R12, wherein R11 and R12 independently of each other are selected from hydroxy, halogen, perhalomethyl, C1-12alkoxy or amino optionally substituted with one or more C1-6alkyl, perhalomethyl or aryl; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano; X is a valence bond, —(CHR9)—, —(CHR9)—CH2—, —CH═CH—, —O—, —O—(CHR9)—, —S—(CHR9)—, —(NR9)—CH2—, —(CHR9)—CH═CH—, —(CHR9)—CH2—CH2—, —(C═O)—, —O—CH2—O—, —(NR9)—, —(NR9)—S(O2)—, —CH═(CR9)—, —(CO)—(CHR9)—, —CH2—(SO)—, —S—, —(SO)—, —(SO2)—, —CH2—(SO2)—, —CH2—O—CH2—, wherein R9 is hydrogen, halogen, hydroxy, nitro, cyano, formyl, C1-12alkyl, C1-12alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyalkyl, amino, acylamino, C1-12alkyl-amino, arylamino, aralkylamino, aminoC1-12alkyl, C1-12alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, C1-12alkoxyC1-12alkyl, aryloxyC1-12alkyl, aralkoxyC1-12alkyl, C1-12alkylthio, thioC1-12alkyl, C1-12alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR13, or —SO2R14, wherein R13 and R14 independently of each other are selected from hydroxy, halogen, C1-6alkoxy, amino optionally substituted with one or more C1-6alkyl, perhalomethyl or aryl; T is >N—, >CH—, >C<, —CH2—N<; Z is —CH2—, ═CH—, >N—, —O—, —S—, >CO, >SO, >SO2, >NR15, wherein R15 is hydrogen, halogen, hydroxy, nitro, cyano, formyl, C1-12alkyl, C1-12alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyalkyl, amino, acylamino, C1-12alkyl-amino, arylamino, aralkylamino, aminoC1-12alkyl, C1-12alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, C1-12alkoxyC1-12alkyl, aryloxyC1-12alkyl, aralkoxyC1-12alkyl, C1-12alkylthio, thioC1-12alkyl, C1-12alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR16, or —SO2R17, wherein R16 and R17 independently of each other are selected from hydroxy, halogen, C1-6alkoxy, amino optionally substituted with one or more C1-6alkyl, perhalomethyl or aryl; Q is —O—, —S—, >NR18, wherein R18 is hydrogen, halogen, hydroxy, nitro, cyano, formyl, C1-12alkyl, C1-12alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryi, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyalkyl, amino, acylamino, C1-12alkyl-amino, arylamino, aralkylamino, aminoC1-12alkyl, C1-12alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, C1-12alkoxyC1-12alkyl, aryloxyC1-12alkyl, aralkoxyC1-12alkyl, C1-12alkylthio, thioC1-12alkyl, C1-12alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR19, or —SO2R20, wherein R19 and R20 independently of each other are selected from hydroxy, halogen, C1-6alkoxy, amino optionally substituted with one or more C1-6alkyl, perhalomethyl or aryl; U is —O—, —S—, >SO2, >NR21, wherein R21 is hydrogen or C1-6alkyl; T==(Z)p represents a single bond or a double bond; Ar represents arylene, heteroarylene, or a divalent heterocyclic group optionally substituted with one or more C1-6alkyl or aryl; R5 represents hydrogen, hydroxy, halogen, C1-12alkoxy, C1-12alkyl, C4-12-alkenynyl, C2-12-alkenyl, C2-12-alkynyl or aralkyl; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano; or R5 forms a bond together with R6; R6 represents hydrogen, hydroxy, halogen, C1-12alkoxy, C1-12alkyl, C4-12-alkenynyl, C2-12-alkenyl, C2-12-alkynyl, acyl or aralkyl; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano; or R8 forms a bond together with R5; R7 represents hydrogen, C1-12alkyl, C4-12-alkenynyl, C2-12-alkenyl, C2-12-alkynyl, aryl, aralkyl, C1-12alkoxyC1-12alkyl, C1-12alkoxycarbonyl, aryloxycarbonyl, C1-12alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl or heteroaralkyl groups; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano; R8 represents hydrogen, C1-12alkyl, C4-12-alkenynyl, C2-12-alkenyl, C2-12-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 NR10, where R10 represents hydrogen, C1-12alkyl, aryl, hydroxyC1-12alkyl or aralkyl groups or when Y is NR10, R8 and R10 may form a 5 or 6 membered nitrogen containing ring, optionally substituted with one or more C1-6alkyl; n is an integer ranging from 1 to 4; p is an integer ranging from 0 to 1; or a pharmaceutically acceptable salt thereof.
- 2. A compound of claim 1 wherein R1, R2, R3, and R4 independently of each other represent hydrogen, halogen, perhalomethyl, hydroxy, cyano, or C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl, C1-7alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyC1-7alkyl, amino, acylamino, C1-7alkyl-amino, arylamino, aralkylamino, aminoC1-7alkyl, C1-7alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, C1-7alkoxyC1-7alkyl, aryloxyC1-7alkyl, aralkoxyC1-7alkyl, C1-7alkylthio, thioC1-7alkyl, C1-7alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR11, or —SO2R12, wherein R11 and R12 independently of each other are selected from hydroxy, perhalomethyl, C1-6alkoxy or amino optionally substituted with one or more C1-6alkyl, perhalomethyl or aryl; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano;
or R1 and R2, R2 and R3 and/or R3 and R4 may form a cyclic ring containing from 5 to 7 carbon atoms optionally substituted with one or more C1-6alkyl.
- 3. A compound of claim 1 wherein R1, R2, R3, and R4 independently of each other represent hydrogen, halogen, perhalomethyl, hydroxy, cyano, or C1-7alkyl, C4-7-alkenynyl, C27-alkenyl, C2-7-alkynyl, C1-7alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, hydroxyC1-7alkyl, amino, acylamino, C1-7alkyl-amino, arylamino, aralkylamino, aminoC1-7alkyl, C1-7alkoxyC1-7alkyl, aryloxyC1-7alkyl, aralkoxyC1-7alkyl, C1-7alkylthio, thioC1-7alkyl, C1-7alkoxycarbonylamino, aryloxycarbonylamino or aralkoxycarbonylamino.
- 4. A compound of claim 1 wherein R1, R2, R3, and R4 independently of each other represent hydrogen, halogen, perhalomethyl, hydroxy, cyano, or C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl, C1-7alkoxy, aryl, aryloxy, aralkyl, aralkoxy, acyl, hydroxyC1-7alkyl, amino, C1-7alkyl-amino, arylamino, aralkylamino, C1-7alkoxyC1-7alkyl, aryloxyC1-7alkyl, aralkoxyC1-7alky or C1-7alkylthio.
- 5. A compound of claim 1 wherein R1, R2, R3, and R4 independently of each other represent hydrogen, halogen, perhalomethyl, or C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl, aryl, aralkyl, hydroxyC1-7alkyl, C1-7alkoxyC1-7alkyl, aryloxyC1-7alkyl or aralkoxyC1-7alkyl.
- 6. A compound of claim 1 wherein R1, R2, R3, and R4 independently of each other represent hydrogen, halogen or C1-7alkyl.
- 7. A compound of claim 1 wherein R1, R2, R3, and R4 represent hydrogen.
- 8. A compound of claim 1 wherein ring A represents a 5-6 membered cyclic ring, optionally substituted with one or more halogen, perhalomethyl, hydroxy, cyano, or C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl, C1-7alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyC1-7alkyl, amino, acylamino, C1-7alkyl-amino, arylamino, aralkylamino, aminoC1-7alkyl, C1-7alkoxyC1-7alkyl, aryloxyC1-7alkyl, aralkoxyC1-7alkyl, C1-7alkylthio, thioC1-7alkyl, C1-7alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR11, or —SO2R12, wherein R11 and R12 independently of each other are selected from hydroxy, perhalomethyl, C1-6alkoxy or amino optionally substituted with one or more C1-6alkyl, perhalomethyl or aryl; optionally substituted with one or more halogen, perhafomethyl, hydroxy or cyano.
- 9. A compound of claim 1 wherein ring A represents a 5-6 membered cyclic ring, optionally substituted with one or more halogen, perhalomethyl, hydroxy, cyano, or C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl, C1-7alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, hydroxyC1-7alkyl, amino, acylamino, C1-7alkyl-amino, arylamino, aralkylamino, aminoC1-7alkyl, C1-7alkoxyC1-7alkyl, aryloxyC1-7alkyl, aralkoxyC1-7alkyl, C1-7alkylthio, thioC1-7alkyl, C1-7alkoxycarbonylamino, aryloxycarbonylamino or aralkoxycarbonylamino.
- 10. A compound of claim 1 wherein ring A represents a 5-6 membered cyclic ring, optionally substituted with one or more halogen, perhalomethyl, hydroxy, cyano, or C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl, C1-7alkoxy, aryl, aryloxy, aralkyl, aralkoxy, acyl, hydroxyC1-7alkyl, amino, C1-7alkyl-amino, arylamino, aralkylamino, C1-7alkoxyC1-7alkyl, aryloxyC1-7alkyl, aralkoxyC1-7alkyl or C1-7alkylthio.
- 11. A compound of claim 1 wherein ring A represents a 5-6 membered cyclic ring, optionally substituted with one or more halogen, perhalomethyl or C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl, C1-7alkoxy, aryl, aralkyl, hydroxyC1-7alkyl, C1-7alkoxyC1-7alkyl, aryloxyC1-7alkyl or aralkoxyC1-7alkyl.
- 12. A compound of claim 1 wherein ring A represents a 6 membered cyclic ring, optionally substituted with one or rriore chlorine or methyl groups.
- 13. A compound of claim 1 wherein ring A represent a phenyl ring.
- 14. A compound of claim 1 wherein X is a valence bond, —(CHR9)—, —(CHR9)—CH2—, —CH═CH—, —O—, —O—(CHR9)—, —S—(CHR9)—, —(NR9)—CH2—, —(CHR9)—CH═CH—, —(CHR9)—CH2—CH2—, —(C═O)—, —O—CH2—O—, —(NR9)—S(O2)—, —(NR9)—, —CH═(CR9)—, —(CO)—(CHR9)—, —CH2—(SO)—, —S—, —(SO)—, —(SO2)—, —CH2—(SO2)— or —CH2—O—CH2—, wherein R9 is hydrogen, halogen, hydroxy, C1-7alkyl, C1-7alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, hydroxyalkyl, amino, acylamino, C1-7alkyl-amino, arylamino, aralkylamino, aminoC1-7alkyl, C1-7alkoxyC1-12alkyl, aryloxyC1-7alkyl, aralkoxyC1-7alkyl, C1-12alkylthio, thioC1-7alkyl, C1-7alkoxycarbonylamino, aryloxycarbonylamino or aralkoxycarbonylamino.
- 15. A compound of claim 1 wherein X is a valence bond, —(CHR9)—, —(CHR9)—CH2—, —CH═CH—, —O—, —O—(CHR9)—, —S—(CHR9)—, —(NR9)—CH2—, —(CHR9)—CH═CH—, —(CHR9)—CH2—CH2—, —(C═O)—, —O—CH2—O—, —(NR9)—S(O2)—, —(NR9)—, —CH═(CR9)—, —(CO)—(CHR9)—, —CH2—(SO)—, —S—, —(SO)—, —(SO2)—, —CH2—(SO2)— or —CH2—O—CH2—, wherein R9 is hydrogen, halogen, hydroxy, C1-7alkyl, aryl, aralkyl, C1-7alkoxyC1-12alkyl, aryloxyC1l7alkyl or aralkoxyC1-7alkyl.
- 16. A compound of claim 1 wherein X is a valence bond, —(CHR9)—, —(CHR9)—CH2—, —CH═CH—, —O—, —O—(CHR9)—, —S—(CHR9)—, —(NR9)—CH2—, —(CHR9)—CH═CH—, —(CHR9)—CH2—CH2—, —(C═O)—, —O—CH2—O—, —(NR9)—S(O2)—, —(NR9)—, —CH═(CR9)—, —(CO)—(CHR9)—, —CH2—(SO)—, —S—, —(SO)—, —(SO2)—, —CH2—(SO2)— or —CH2—O—CH2—, wherein R9 is hydrogen.
- 17. A compound of claim 1 wherein X is a valence bond, —(CHR9)—, —(CHR9)—CH2—, —CH═CH—, —O—, —O—(CHR9)—, —S—(CHR9)—, —(NR9)—CH2—, —O—CH2—O—, —(NR9)—, —S—, —(SO)— or —CH2—O—CH2—, wherein R9 is hydrogen.
- 18. A compound of claim 1 wherein X is a valence bond, —(CHR9)—, —(CHR9)—CH2—, —CH═CH—, —O—, —O—(CHR9)—, —S—(CHR9)—, —(NR9)—CH2—, —C—CH2—O—, —(NR9)—, —S— or —CH2—O—CH2—, wherein R9 is hydrogen.
- 19. A compound of claim 1 wherein X is a valence bond, —(CHR9)—, —(CHR9)—CH2—, —CH═CH—, —O—, —O—(CHR9)—, —S—(CHR9)—, —O—CH2—O— or —S—, wherein R9 is hydrogen.
- 20. A compound of claim 1 wherein X is —S—.
- 21. A compound of claim 1 wherein T is >C<.
- 22. A compound of claim 1 wherein Z is —CH2—, ═CH—, >N—, —O—, —S—, >CO, >SO, >SO2.
- 23. A compound of claim 1 wherein Z is >N—.
- 24. A compound of claim 1 wherein Q is —O—, —S—, >NR18, wherein R18 is hydrogen or C1-7alkyl.
- 25. A compound of claim 1 wherein Q is >NR18, wherein R18 is hydrogen.
- 26. A compound of claim 1 wherein U is —O—.
- 27. A compound of claim 1 wherein T==(Z)p represents a double bond.
- 28. A compound of claim 1 wherein Ar represents arylene optionally substituted with one or more C1-6alkyl or aryl.
- 29. A compound of claim 1 wherein Ar is phenyl.
- 30. A compound of claim 1 wherein R5 represents hydrogen, hydroxy, halogen, C1-7alkoxy, C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl or aralkyl, or R5 forms a bond together with R6.
- 31. A compound of claim 1 wherein R5 represents hydrogen or R5 forms a bond together with R6.
- 32. A compound of claim 1 wherein R5 represents hydrogen, hydroxy, halogen, C1-7alkoxy, C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl or aralkyl, or R5 forms a bond together with R6.
- 33. A compound of claim 1 wherein R5 represents hydrogen or R5 forms a bond together with R6.
- 34. A compound of claim 1 wherein R7 represents hydrogen, C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl, aryl, aralkyl, C1-7alkoxyC1-7alkyl, C1-7alkoxycarbonyl, aryloxycarbonyl, C1-7alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl or heteroaralkyl.
- 35. A compound of claim 1 wherein R7 represents hydrogen, C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl or C2-7-alkynyl.
- 36. A compound of claim 1 wherein R7 is C1-12alkyl.
- 37. A compound of claim 1 wherein R8 represents hydrogen, C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl, aryl, aralkyl, heterocyclyl, heteroaryl or heteroaralkyl groups; optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano.
- 38. A compound of claim 1 wherein R8 represents hydrogen, C1-7alkyl, C4-7-alkenynyl, C2-7-alkenyl, C2-7-alkynyl, aryl or aralkyl.
- 39. A compound of claim 1 wherein R8 is hydrogen or C1-12alkyl.
- 40. A compound of claim 1 wherein Y represents oxygen, sulphur or NR10, where R10 represents hydrogen, C1-7alkyl, aryl, hydroxyC1-7alkyl or aralkyl groups.
- 41. A compound of claim 1 wherein Y is oxygen.
- 42. A compound of claim 1 wherein n is an integer ranging from 2 to 3.
- 43. A compound of claim 1 wherein p is 1.
- 44. A compound of claim 1 wherein A is benzo.
- 45. A compound of claim 1 wherein X is —O—.
- 46. A compound of claim 1 wherein X is —S—.
- 47. A compound of claim 1 wherein Z is —S— and p is 1.
- 48. A compound of claim 1 wherein Z is —CH2— and p is 1.
- 49. A compound of claim 1 wherein X is —CH— and p is 1.
- 50. A compound of claim 1 wherein T==(Z)p represents a single bond or a double bond.
- 51. A compound of claim 1 wherein T is >CH—.
- 52. A compound of claim 1 wherein T is >C<.
- 53. A compound of claim 1 wherein Q is —O—.
- 54. A compound of claim 1 wherein Q is —S—.
- 55. A compound of claim 1 wherein Q is >NR18, wherein R18 is H.
- 56. A compound of claim 1 wherein n is 2.
- 57. A compound of claim 1 wherein U is —O—.
- 58. A compound of claim 1 wherein Ar is phenylene.
- 59. A compound of claim 1 wherein R5 is H.
- 60. A compound of claim 1 wherein R6 is H.
- 61. A compound of claim 1 wherein R7 is ethyl.
- 62. A compound of claim 1 wherein R8 is H.
- 63. A compound of claim 1 wherein p is 0.
- 64. A compound of claim 1 A is a five membered ring containing S.
- 65. A compound of claim 1 wherein X is —(CHR9)—CH2—, wherein R9 is H.
- 66. A compound of claim 1 wherein X is —O—(CHR9)—, wherein R9 is H.
- 67. A compound of claim 1 wherein X is —S—(CHR9)—, wherein R9 is H.
- 68. A compound of claim 1 wherein X is —O—CH2—O—.
- 69. A compound of claim 1 which is:
2-Ethoxy-3-{4-[2-(11H-5-oxa-10-thia-dibenzo[a,d]cyclohepten-11-yloxy)-ethoxy]-phenyl}-propionic acid, 3-(4-[2-(Dibenzo[b,f]-1,4-thiazepin-11-ylamino)-ethoxy]-phenyl)-2-ethoxy-propionic acid ethyl ester, 3-{4-[2-(Dibenzo[b,f][1,4]thiazepin-11-ylamino)-ethoxy]-phenyl}-2-ethoxy-propionic acid, 3-{4-[2-(10,11-Dihydro-dibenzo[b,f]thiepin-10-ylsulfanyl)-ethoxy]-phenyl}-2-ethoxy-propionic acid, 3-(4-[2-[5H-Dibenzo[a,d]cyclohepten-5-yloxy)-ethoxy]-phenyl)-2-ethoxy-propionic acid ethyl ester, 3-(4-[2-(6,11-Dihydrodibenzo[b,e]thiepin-11-yloxy)-ethoxy]-phenyl)-2-ethoxy-propionic acid ethyl ester, 3-(4-[2-(6,11-Dihydrodibenzo[b,e]thiepin-11-yloxy)-ethoxy]-phenyl)-2-ethoxy-propionic acid, 3-(4-[2-(6,11-Dihydrodibenzo[b,e]oxepin-11-yloxy)-ethoxy]-phenyl)-2-ethoxy-propionic acid ethyl ester, 3-(4-[2-(2,10-Dichloro-12H-5,7-dioxa-dibenzo[a,d]cycloocten-12-yloxy)-ethoxy]-phenyl)-2-ethoxy-propionic acid ethyl ester, 3-(4-[2-(2,10-Dichloro-12H-5,7-dioxa-dibenzo[a,d]cycloocten-12-yloxy)-ethoxy]-phenyl)-2-ethoxy-propionic acid, 2-Ethoxy-3-(4-[2-(2-methyl-9,1 0-dihydro-4H-1-oxa-3-aza-benzo[f]azulen-4-yloxy)-ethoxy]-phenyl)-propionic acid ethyl ester, 3-(4-[2-(10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5-yloxy)-ethoxy]-phenyl)-2-ethoxy-propanoic acid ethyl ester, 3-(4-[2-(10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5-yloxy)-ethoxy]-phenyl)-2-ethoxy-propanoic acid, 3-(4-[2-([10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl]-methyl-amino)-ethoxy]-phenyl)-2-ethoxypropanoic acid ethyl ester, or 3-(4-[2-([10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl]-methyl-amino)-ethoxy]-phenyl)-2-ethoxypropanoic acid; or a pharmaceutically acceptable salt thereof.
- 70. A compound of claim 1 which is:
2-Ethoxy-3-{4-[2-(11H-5-oxa-10-thia-dibenzo[a,d]cyclohepten-11-yloxy)-ethoxy]-phenyl}-propionic acid, 3-{4-[2-(Dibenzo[b,f[1,4]thiazepin-11-ylamino)-ethoxy]-phenyl}-2-ethoxy-propionic acid, or 3-{4-[2-(10,11-Dihydro-dibenzo[b,f]thiepin-10-ylsulfanyl)-ethoxy]-phenyl}-2-ethoxy-propionic acid; or a pharmaceutically acceptable salt thereof.
- 71. A pharmaceutical composition comprising, as an active ingredient, an effective amount of a compound of claim 1 together with a pharmaceutically acceptable carrier or diluent.
- 72. The composition of claim 71 in unit dosage form, comprising from about 0.05 to about 100 mg of the compound.
- 73. The pharmaceutical composition of claim 71 wherein the route of administration is oral, nasal, transdermal, pulmonal, or parenteral.
- 74. A method of treating or preventing conditions mediated by nuclear receptors, the method comprising administering to a subject in need thereof an effective amount of a compound of claim 1.
- 75. The method of claim 74 wherein the nuclear receptors are the Peroxisome Proliferator-Activated Receptors (PPAR).
- 76. A method of treating or preventing diabetes or obesity, the method comprising administering to a subject in need thereof an effective amount of a compound of claim 1.
- 77. The method of claim 74, wherein the effective amount of the compound is in the range of from about 0.05 to about 100 mg per day.
Priority Claims (1)
Number |
Date |
Country |
Kind |
PA 1998 01357 |
Nov 1998 |
DK |
|
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims priority under 35 U.S.C. 119 of U.S. provisional application No. 60/106,658 filed Nov. 2, 1998 and Danish application no. PA 1998 01357 filed Oct. 21, 1998, the contents of which are fully incorporated herein by reference.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60106658 |
Nov 1998 |
US |
Divisions (1)
|
Number |
Date |
Country |
Parent |
09420380 |
Oct 1999 |
US |
Child |
09808495 |
Mar 2001 |
US |