Claims
- 1. A compound selected from Formula I: ##STR167## wherein; Y is a bond;
- A-B is ##STR168## R.sub.1 is H, halogen (chlorine, fluorine, bromine, iodine), OH, --S-lower alkyl (C.sub.1 -C.sub.3), --SH, --SO lower alkyl (C.sub.1 -C.sub.3), --SO.sub.2 lower alkyl (C.sub.1 -C.sub.3), --CO lower alkyl (C.sub.1 -C.sub.3), --CF.sub.3, lower alkyl (C.sub.1 -C.sub.3), --O lower alkyl (C.sub.1 -C.sub.3), --NO.sub.2, --NH.sub.2, --NHCO lower alkyl (C.sub.1 -C.sub.3), --N--�lower alkyl (C.sub.1 -C.sub.3)!.sub.2, SO.sub.2 NH.sub.2, --SO.sub.2 NH lower alkyl (C.sub.1 -C.sub.3), or --SO.sub.2 N �lower alkyl (C.sub.1 -C.sub.3)!.sub.2 ;
- R.sub.2 is H, Cl, Br, I, F, --OH, lower alkyl (C.sub.1 -C.sub.3), --O lower alkyl (C.sub.1 -C.sub.3); or
- R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy;
- R.sub.3 is the moiety ##STR169## wherein Ar is a moiety selected from the group ##STR170## and X is selected from O, S, --NCH.sub.3, or --N--COCH.sub.3 ; R.sub.4 is selected from H, lower alkyl (C.sub.1 -C.sub.3), --CO--lower alkyl (C.sub.1 -C.sub.3), SO.sub.2 lower alkyl (C.sub.1 -C.sub.3), or the moieties of the formulae: ##STR171## R.sub.5 is H, --CH.sub.3, --C.sub.2 H.sub.5, Cl, Br, F, --O--CH.sub.3, or --O--C.sub.2 H.sub.5 ;
- R.sub.6 is selected from:
- (a) moieties of the formula: ##STR172## wherein cycloalkyl is defined as C.sub.3 -C.sub.6 cycloalkyl, cyclohexenyl or cyclopentenyl;
- R.sub.2 is as hereinbefore defined;
- n is 0-2;
- R.sub.7 is H, --CH.sub.3, --CH.sub.2 H.sub.5, Cl, Br, F, --OCH.sub.3, --OC.sub.2 H.sub.5, or --CF.sub.3 ;
- R.sub.a is hydrogen, CH.sub.3, C.sub.2 H.sub.5, moieties of the formulae: ##STR173## --(CH.sub.2).sub.2 --O--lower alkyl (C.sub.1 -C.sub.3) or --CH.sub.2 CH.sub.2 OH;
- q is one or two;
- R.sub.b is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 ;
- Ar' is selected from the group: ##STR174## wherein R.sub.4, R.sub.5 are as hereinbefore defined;
- R.sub.8 and R.sub.9 are independently hydrogen, lower alkyl (C.sub.1 -C.sub.3), O-lower alkyl (C.sub.1 -C.sub.3), S-lower alkyl (C.sub.1 -C.sub.3), --CF.sub.3, --CN, --OH, --SCF.sub.3, --OCF.sub.3, halogen, NO.sub.2, amino, or --NH-lower alkyl (C.sub.1 -C.sub.3);
- R.sub.10 is selected from halogen, hydrogen, or lower alkyl (C.sub.1 -C.sub.3);
- W' is selected from O, S, NH, N-lower alkyl (C.sub.1 -C.sub.3), --NCO-lower alkyl (C.sub.1 -C.sub.3), or NSO.sub.2 -lower alkyl (C.sub.1 -C.sub.3); or
- (b) a moiety of the formula: ##STR175## where R.sub.2 is as hereinbefore defined;
- (c) a moiety of the formula: ##STR176## wherein J is R.sub.a, lower alkyl (C.sub.1 -C.sub.8) branched or unbranched, lower alkenyl (C.sub.2 -C.sub.8) branched or unbranched, --O-lower alkyl (C.sub.1 -C.sub.8) branched or unbranched, --O-lower alkenyl (C.sub.2 -C.sub.8) branched or unbranched, tetrahydrofuran, tetrahydrothiophene, or --CH.sub.2 -K wherein K is halogen, --OH, tetrahydrofuran, tetrahydrothiophene or the heterocyclic ring moiety: ##STR177## wherein D, E, F and G are selected from carbon or nitrogen and wherein the carbon atoms may be optionally substituted with halogen, (C.sub.1 -C.sub.3)lower alkyl, hydroxy, --CO-lower alkyl (C.sub.1 -C.sub.3), CHO, (C.sub.1 -C.sub.3)lower alkoxy, or --CO.sub.2 -lower alkyl (C.sub.1 -C.sub.3), and R.sub.a and R.sub.b are as hereinbefore defined;
- (d) a moiety selected from those of the formulae: ##STR178## wherein R.sub.c is selected from halogen, (C.sub.1 -C.sub.3) lower alkyl, --O-lower alkyl (C.sub.1 -C.sub.3) or OH;
- R.sub.b is as hereinbefore defined;
- q is 1 or 2;
- wherein Ar' is selected from the group: ##STR179## R.sub.7 is hydrogen, --CH.sub.3, --C.sub.2 H.sub.5, Cl, Br, F, --OCH.sub.3, --OC.sub.2 H.sub.5, or --CF.sub.3 ;
- R.sub.8 and R.sub.9 are independently hydrogen, lower alkyl (C.sub.1 -C.sub.3), O-lower alkyl (C.sub.1 -C.sub.3), S-lower alkyl (C.sub.1 -C.sub.3), --CF.sub.3, --CN, --OH, --SCF.sub.3, --OCF.sub.3, halogen, NO.sub.2, amino, or --NH-lower alkyl (C.sub.1 -C.sub.3);
- R.sub.10 is selected from the group of halogen, hydrogen, or lower alkyl (C.sub.1 -C.sub.3);
- W' is selected from O, S, NH, N-lower alkyl (C.sub.1 -C.sub.3), --NCO-lower alkyl (C.sub.1 -C.sub.3), or NSO.sub.2 -lower alkyl (C.sub.1 -C.sub.3);
- the moiety ##STR180## represents a fused thiazole ring or fused substituted thiazole ring optionally substituted by one or two substituents selected from (C.sub.1 -C.sub.3) lower alkyl, halogen, formyl, (C.sub.1 -C.sub.3) lower alkoxy or a moiety of the formula: ##STR181## q is one or two; or a pharmaceutically acceptable salt, ester or prodrug thereof.
- 2. A compound according to claim 1 wherein R.sub.3 is the moiety ##STR182## wherein Ar is a moiety selected from the group ##STR183## R.sub.6 is selected from the group ##STR184## or --CH.sub.2 COAr'; wherein
- n is 0-2;
- Ar' is ##STR185## W' is O or S; A-B, R.sub.a, R.sub.b, R.sub.1, R.sub.2, R.sub.4, R.sub.5, R7, R.sub.8, R.sub.9, and cycloalkyl are as defined in claim 1;
- or a pharmaceutically acceptable salt, ester or prodrug thereof.
- 3. A compound of the formula: ##STR186## wherein; Y is a bond;
- A-B is ##STR187## R.sub.1 is H, halogen (Cl, F, Br, I), OH, --S-lower alkyl (C.sub.1 -C.sub.3), --SH, --SO lower alkyl (C.sub.1 -C.sub.3), --SO.sub.2 lower alkyl (C.sub.1 -C.sub.3), --CO lower alkyl (C.sub.1 -C.sub.3), --CF.sub.3, lower alkyl (C.sub.1 -C.sub.3), --O lower alkyl (C.sub.1 -C.sub.3), --NO.sub.2, --NH.sub.2, --NHCO lower alkyl (C.sub.1 -C.sub.3), --N--� lower alkyl (C.sub.1 -C.sub.3)!.sub.2, SO.sub.2 NH.sub.2, --SO.sub.2 NH lower alkyl (C.sub.1 -C.sub.3), or --SO.sub.2 N �lower alkyl (C.sub.1 -C.sub.3)!.sub.2 ;
- R.sub.2 is selected from H, Cl, Br, I, F, --OH, lower alkyl (C.sub.1 -C.sub.3), or --O lower alkyl (C.sub.1 -C.sub.3); or
- R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy;
- R.sub.3 is the moiety ##STR188## wherein Ar is a moiety selected from the group ##STR189## R.sub.5 is H, --CH.sub.3, -C.sub.2 H.sub.5, Cl, Br, F, --O--CH.sub.3, or --O--C.sub.2 H.sub.5 ;
- R.sub.6 is selected from: ##STR190## wherein cycloalkyl is defined as C.sub.3 -C.sub.6 cycloalkyl, cyclohexenyl or cyclopentenyl;
- n is 0-2;
- and wherein Ar' is selected from the moieties: ##STR191## wherein R.sub.a and R.sub.b are independently selected from H, --CH.sub.3, or --C.sub.2 H.sub.5 ;
- R.sub.7 is H, --CH.sub.3, --C.sub.2 H.sub.5, Cl, Br, F, --O--CH.sub.3, --O--C.sub.2 H.sub.5 or --CF.sub.3 ;
- R.sub.8 and R.sub.9 are independently selected from hydrogen, lower alkyl (C.sub.1 -C.sub.3), O-lower alkyl (C.sub.1 -C.sub.3), S-lower alkyl (C.sub.1 -C.sub.3), --CF.sub.3, --CN, --OH, --SCF.sub.3, --OCF.sub.3, halogen, NO.sub.2, amino, or --NH-lower alkyl (C.sub.1 -C.sub.3);
- W' is selected from O, S, NH, N-lower alkyl (C.sub.1 -C.sub.3), --NCO-lower alkyl (C.sub.1 -C.sub.3), or NSO.sub.2 -lower alkyl (C.sub.1 -C.sub.3);
- the moiety ##STR192## represents a fused thiazole ring or fused substituted thiazole ring optionally substituted by one or two substituents selected from (C.sub.1 -C.sub.3) lower alkyl, halogen, formyl, (C.sub.1 -C.sub.3) lower alkoxy or a moiety of the formula: ##STR193## q is one or two; or a pharmaceutically acceptable salt, ester or prodrug thereof.
- 4. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!phenyl!-5-fluoro-2-methylbenzamide.
- 5. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!phenyl!-2,4-dichlorobenzamide.
- 6. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2,3-dichlorobenzamide.
- 7. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-methyl-4-chlorobenzamide.
- 8. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-methoxybenzamide.
- 9. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-methoxy-4-chlorobenzamide.
- 10. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-(trifluoromethoxy)-benzamide.
- 11. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-(trifluoromethyl)-benzamide.
- 12. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2,6-dichlorobenzamide.
- 13. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2,3-dimethylbenzamide.
- 14. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2,5-dimethylbenzamide.
- 15. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-3-(trifluoromethyl)-benzamide.
- 16. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-(methylthio)benzamide.
- 17. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-methyl-3-thiophene-carboxamide.
- 18. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-3-methyl-2-thiophene-carboxamide.
- 19. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-3-methyl-2-furane-carboxamide.
- 20. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-methylbenzeneacetamide.
- 21. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-3-fluoro-2-methylbenzamide.
- 22. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-5- fluoro-2-methylbenzamide.
- 23. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-4-fluoro-2-methylbenzamide.
- 24. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-fluoro-4-(trifluoromethyl)benzamide.
- 25. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-3-fluoro-5-(trifluoromethyl)benzamide.
- 26. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-chloro-4-fluorobenzamide.
- 27. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-chloro-5-fluorobenzamide.
- 28. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-4-fluoro-2-(trifluoromethyl)benzamide.
- 29. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-fluorophenyl!-2-chloro-4-fluorobenzamide.
- 30. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-fluorophenyl!-3-fluoro-2-methylbenzamide.
- 31. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-fluorophenyl!-5-fluoro-2-methylbenzamide.
- 32. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-fluorophenyl!-2-chloro-4-fluorobenzamide.
- 33. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-3-fluoro-2-methylbenzamide.
- 34. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2-methylbenzamide.
- 35. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-5-fluoro-2-methylbenzamide.
- 36. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2-chloro-5-fluorobenzamide.
- 37. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2,3-dimethylbenzamide.
- 38. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2,5-dimethylbenzamide.
- 39. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2,4-dichlorobenzamide.
- 40. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2-methoxy-4-chlorobenzamide.
- 41. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2-(trifluoromethoxy)-benzamide.
- 42. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2-(methylthio)benzamide.
- 43. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-2-methylbenzamide.
- 44. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-2,4-dichlorobenzamide.
- 45. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-2-chloro-4-fluorobenzamide.
- 46. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-3-fluoro-2-methylbenzamide.
- 47. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-5-fluoro-2-methylbenzamide.
- 48. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-2,3-dimethylbenzamide.
- 49. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-2-methylbenzeneacetamide.
- 50. The compound according to claim 1, N-�4-�(4,5-dihydro-2-methyl-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-2-chlorobenzeneacetamide.
- 51. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-methylbenzeneacetamide.
- 52. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-3-fluoro-2-methylbenzamide.
- 53. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-5-fluoro-2-methylbenzamide.
- 54. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-4-fluoro-2-methylbenzamide.
- 55. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-3-fluoro-5-(trifluoromethyl)benzamide.
- 56. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-chloro-4-fluorobenzamide.
- 57. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-chlorophenyl!-2-chloro-5-fluorobenzamide.
- 58. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-fluorophenyl!-3-fluoro-2-methylbenzamide.
- 59. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-fluorophenyl!-5-fluoro-2-methylbenzamide.
- 60. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-fluorophenyl!-2-chloro-4-fluorobenzamide.
- 61. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-3-fluoro-2-methylbenzamide.
- 62. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-5-fluoro-2-methylbenzamide.
- 63. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2-chloro-5-fluorobenzamide.
- 64. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2,3-dimethylbenzamide.
- 65. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2,5-dimethylbenzamide.
- 66. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2,4-dichlorobenzamide.
- 67. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2-methoxy-4-chlorobenzamide.
- 68. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methylphenyl!-2-(trifluoromethoxy)benzamide.
- 69. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-2,4-dichlorobenzamide.
- 70. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-2-chloro-4-fluorobenzamide.
- 71. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-3 -fluoro-2-methylbenzamide.
- 72. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-5-fluoro-2-methylbenzamide.
- 73. The compound according to claim 1, N-�4-�(4,5-dihydro-6H-thiazolo�5,4-d!�1!benzazepin-6-yl)carbonyl!-3-methoxyphenyl!-2-methylbenzeneacetamide.
- 74. A pharmaceutical composition useful for treating disease in a mammal characterized by excess renal reabsorption of water, the pharmaceutical composition comprising an effective amount of a compound of claim 1, or a pharmaceutically acceptable salt, ester or prodrug form thereof, and a suitable pharmaceutical carrier.
- 75. The pharmaceutical composition of claim 74 wherein the disease in a mammal characterized by excess renal reabsorption of water is congestive heart failure, nephrotic syndrome, hyponatremia, coronary vasospasm, cardiac ischemia, renal vasospasm, liver cirrhosis, brain edema, cerebral ischemia, or cerebral hemorrhage-stroke.
- 76. A method for treating disease in a mammal characterized by excess renal reabsorption of water, the method comprising administering to a mammal in need thereof an effective amount of a compound of claim 1, or a pharmaceutically acceptable salt, ester or prodrug form thereof, and a suitable pharmaceutical carrier.
- 77. The method of claim 76 wherein the disease in a mammal characterized by excess renal reabsorption of water is congestive heart failure, nephrotic syndrome, hyponatremia, coronary vasospasm, cardiac ischemia, renal vasospasm, liver cirrhosis, brain edema, cerebral ischemia, or cerebral hemorrhage-stroke.
Parent Case Info
This case is a continuation-in-part of U.S. Ser. No. 254,823, now U.S. Pat. No. 5,512,563 filed Jun. 13, 1994 which, in turn, is a continuation-in-part of Ser. No. 100,003, filed Jul. 29, 1993, now abandoned.
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Continuation in Parts (2)
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Number |
Date |
Country |
Parent |
254823 |
Jun 1994 |
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Parent |
100003 |
Jul 1993 |
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