-
公开(公告)号:EP0208518B1
公开(公告)日:1991-09-11
申请号:EP86305188.4
申请日:1986-07-04
IPC分类号: C07D237/04 , C07D401/12 , C07C279/18 , C07C279/28 , C07C311/60 , A61K31/50
CPC分类号: C07D401/12 , C07C279/28 , C07D237/04
-
公开(公告)号:EP0208518A2
公开(公告)日:1987-01-14
申请号:EP86305188.4
申请日:1986-07-04
IPC分类号: C07D237/04 , C07D401/12 , C07C279/18 , C07C279/28 , C07C311/60 , A61K31/50
CPC分类号: C07D401/12 , C07C279/28 , C07D237/04
摘要: Compounds of the formula (I) :
or a pharmaceutically acceptable salt are described wherein R' is hydrogen or methyl, R 2 is C 1-4 alkyl, substituted by one or two groups selected from hydroxy, C 1-4 alkoxy, carbamoyl, C 1-4 alkoxycarbonyl and trifluoromethyl, provided that the carbon atom adjacent to the nitrogen atom is not substituted by hydroxy and that no carbon atom is disubstituted by hydroxy, or -A-R 4 where A is C 1-4 alkylene - (straight or branched) and R' is optionally substituted aryl or heteroaryl, R 3 is cyano, -COR 5 or - SO 2 R 6 where R 5 is C 1-4 alkoxy or optionally substituted phenyl and R 6 is NHR 7 , C 1-4 alkyl or optionally substituted aryl; and R 7 is hydrogen or C 1-4 alkyl, R 2 can also be C 3-6 cycloalkyl, allyl or propargyl when R 3 is cyano, and R 2 can also be hydrogen or C,. 4 alkyl when R 3 is -COR 5 or -SO 2 R 6 .
These compounds have inotropic, vasodilator, broncho-dilating and platelet aggregation inhibiting properties. Pharmaceutical compositions are described as are methods of use. Intermediates and processes for the preparation of the compounds of the formula (I) are described.摘要翻译: 其中R 1是氢或甲基,R 2是被一个或两个选自羟基,C 1 -C 6的基团取代的C 1-4烷基,式(I)的化合物:...
...或其药学上可接受的盐 -4-烷氧基,氨基甲酰基,C 1-4烷氧基羰基和三氟甲基,条件是与氮原子相邻的碳原子不被羟基取代,也没有碳原子被羟基取代,或-AR 4,其中A是C 1-4亚烷基(直链 或支链),R 4是任选取代的芳基或杂芳基,R 3是氰基,-COR 5或-SO 2 R 6,其中R 5是C 1-4烷氧基或任选取代的苯基, 6>是NHR 7,C 1-4烷基或任选取代的芳基; 且R 7为氢或C 1-4烷基时,当R 3为氰基时,R 2也可为C 3-6环烷基,烯丙基或炔丙基,当R 3为R 1时,R 2也可为氢或C 1-4烷基, 3>是-COR 5或-SO 2 R 6。 这些化合物具有变力,血管扩张剂,支气管扩张和血小板聚集抑制性质。 药物组合物被描述为使用的方法。 描述了制备式(I)化合物的中间体和方法。
-