发明授权
US4658037A Intermediates for 1,3-disubstituted 2-oxindoles as analgesic and
antiinflammatory agents
失效
1,3-二取代的2-羟基吲哚的中间体作为止痛剂和抗炎剂
- 专利标题: Intermediates for 1,3-disubstituted 2-oxindoles as analgesic and antiinflammatory agents
- 专利标题(中): 1,3-二取代的2-羟基吲哚的中间体作为止痛剂和抗炎剂
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申请号: US814719申请日: 1985-12-30
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公开(公告)号: US4658037A公开(公告)日: 1987-04-14
- 发明人: Saul B. Kadin
- 申请人: Saul B. Kadin
- 申请人地址: NY New York
- 专利权人: Pfizer Inc.
- 当前专利权人: Pfizer Inc.
- 当前专利权人地址: NY New York
- 主分类号: C07D495/04
- IPC分类号: C07D495/04 ; A61K20060101 ; A61K31/00 ; A61K31/33 ; A61K31/395 ; A61K31/40 ; A61K31/403 ; A61K31/404 ; A61K31/405 ; A61K33/00 ; A61P25/04 ; A61P29/00 ; A61P43/00 ; C07C20060101 ; C07D20060101 ; C07D209/00 ; C07D209/02 ; C07D209/32 ; C07D209/34 ; C07D209/38 ; C07D307/00 ; C07D333/00 ; C07D405/06 ; C07D405/12 ; C07D407/06 ; C07D409/06 ; C07D409/12 ; C07D491/048 ; C07D491/056
摘要:
Certain 2-oxindole-1-carboxamide compounds having an acyl substituent at the 3-position, and also on the carboxamide nitrogen atom, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic agents and anti-inflammatory agents in mammalian subjects. Certain 2-oxindole compounds unsubstituted at the 1-position but having an acyl substituent at C-3 of the formula ##STR1## and the base salts thereof, wherein X is hydrogen, 5-fluoro, 5-chloro or 5-trifluoromethyl; Y is hydrogen, 6-fluoro, 6-chloro or 6-trifluoromethyl; and R.sup.1 is benzyl, furyl, thienyl or thienylmethyl; provided that when X and Y are both hydrogen, R.sup.1 is not benzyl are useful as intermediates to the aforementioned analgesic and anti-inflammatory agents.
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