申请人:PFIZER INC.
公开号:EP0393936A1
公开(公告)日:1990-10-24
This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.
本发明涉及新型 3-取代-2-氧化吲哚衍生物,它们是前列腺素 H2 合酶、5-脂氧合酶和白细胞介素-1 生物合成的抑制剂。本发明的化合物本身可用作前列腺素 H2 合酶和白细胞介素-1 生物合成的抑制剂,也可用作治疗慢性炎症性疾病的镇痛、抗炎和抗关节炎药物。本发明还涉及包含所述 3-取代-2-氧化吲哚衍生物的药物组合物;涉及抑制前列腺素 H2 合酶和白细胞介素-1 生物合成的方法;涉及用所述化合物治疗哺乳动物的慢性炎症疾病。此外,本发明还涉及某些可用作制备本发明 3-取代-2-吲哚衍生物中间体的新型羧酸,以及制备 3-取代-2-吲哚衍生物的工艺。