1-Aryl-3-quinoline- and 1-aryl-3-isoquinoline-carboxamides, a process for their preparation and their use as medicaments
申请人:HOECHST-ROUSSEL
PHARMACEUTICALS INCORPORATED
公开号:EP0317991A2
公开(公告)日:1989-05-31
This invention relates to 1-aryl-3-quinolinecarboxamides and 1-aryl-3-isoquinolinecarboxamides of the formula I
wherein WXYZR is the bivalent radical N-CH=C-C=O, N-CH₂-CH-C=O, N-CH₂-C=C-OH, C=N-CH-C=O, or C=N-C=C-OH; R¹ and R² are independently halogen, loweralkyl or loweralkoxy; R³ is substituted or unsubstituted phenyl, pyridyl, pyrimidyl, pyrazinyl, triazinyl, thiazolyl, thiadiazolyl, isoxazolyl, oxadiazolyl, quinolyl, isoquinolyl, or benzothiazolyl; and m and n are integers independently having values of zero or 1; the optical antipodes and pharmaceutically acceptable acid addition salts thereof, and to a process for their preparation. The 1-aryl-3-quinolinecarboxamides and 1-aryl-3-isoquinolinecarboxamides of the present invention are useful as antiinflammatory and analgetic agents.
本发明涉及式 I 的 1-芳基-3-喹啉甲酰胺和 1-芳基-3-异喹啉甲酰胺。
其中 WXYZR 是二价基 N-CH=C-C=O、N-CH₂-CH-C=O、N-CH₂-C=C-OH、C=N-CH-C=O 或 C=N-C=C-OH;R¹ 和 R² 独立地是卤素、低级烷基或低级烷氧基;R³ 是取代或未取代的苯基、吡啶基、嘧啶基、吡嗪基、三嗪基、噻唑基、噻二唑基、异噁唑基、噁二唑基、喹啉基、异喹啉基或苯并噻唑基;m和n分别为数值为0或1的整数;它们的光学对位物和药学上可接受的酸加成盐,以及它们的制备方法。本发明的 1-芳基-3-喹啉甲酰胺和 1-芳基-3-异喹啉甲酰胺可用作抗炎和镇痛剂。