N,3-disubstituted 2-oxindole-1-carboxamides as analgesic and antiinflammatory agents
申请人:PFIZER INC.
公开号:EP0164860A1
公开(公告)日:1985-12-18
Certain 2-oxindole-lcarboxamide compounds having an acyl substituent at the 3-position, and also further substituted on the carboxamide nitrogen by an alkyl, cycloalkyl, phenyl or substituted phenyl group, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and antiinflammatory agents in mammalian subjects. These 2-oxindole-lcarboxamide compounds are of particular value for ameliorating pain in human patients recovering from surgery or trauma, and alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and ostoarthritis, in human subjects.
Certain 2-oxind ole-1-carboxamide compounds unsubstituted at C-3, but having a substituent on the carboxamide nitrogen, are useful as intermediates to the analgesic and antiinflammatory agents of the invention.
某些 2-氧吲哚-甲酰胺化合物在 3 位上具有酰基取代基,在羧酰胺氮上还进一步被烷基、环烷基、苯基或取代苯基取代,是环氧化酶(CO)和脂氧合酶(LO)的抑制剂,可用作哺乳动物的镇痛剂和抗炎剂。这些 2-氧化吲哚-甲酰胺化合物对于改善手术或创伤后恢复期人类患者的疼痛,以及减轻人类慢性疾病(如类风湿性关节炎和骨关节炎)的症状具有特殊价值。
某些在 C-3 处未被取代但在羧酰胺氮上具有取代基的 2-氧代吲哚-1-甲酰胺化合物可作为本发明镇痛剂和抗炎剂的中间体。