3-(1H-Indazol-3-yl)-4-pyridinamines, a process and intermediates for their preparation and their use as medicaments
申请人:HOECHST-ROUSSEL
PHARMACEUTICALS INCORPORATED
公开号:EP0475352A1
公开(公告)日:1992-03-18
This Invention relates to 4-(1H-indazol-3-yl)-4-pyridinamines of the formula I
where R₁ is hydrogen, loweralkyl, arylalkyl or acyl; R₂ is hydrogen, loweralkyl or arylalkyl; R₃ is hydrogen, loweralkyl or aryl and X is hydrogen, halogen, nitro or amino, or the pharmaceutically acceptable addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesics and as topical antiinflammatory agents for the treatment of various dermatoses.
The invention relates further to intermediates of the formula II
where R₁, R₂ and R₃ have the above meaning, which have also analgesic activity, as well as to processes for the preparation of compounds of both formulae.
本发明涉及式 I 的 4-(1H-吲唑-3-基)-4-吡啶胺
其中,R₁为氢、低级烷基、芳烷基或酰基;R₂为氢、低级烷基或芳烷基;R₃为氢、低级烷基或芳基,X为氢、卤素、硝基或氨基,或其药学上可接受的加成盐,以及(如适用)其几何异构体、光学异构体和外消旋混合物。本发明的化合物可用作镇痛剂和局部消炎剂,用于治疗各种皮肤病。
本发明还涉及式 II 的中间体
其中 R₁、R₂ 和 R₃ 具有上述含义,它们也具有镇痛活性,本发明还涉及制备这两种式化合物的工艺。