6-Phenyl-pyridazinyl compounds
    2.
    发明公开
    6-Phenyl-pyridazinyl compounds 失效
    6-苯基 - 哒嗪Verbindungen。

    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

    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。