N-(substd. phenyl) 3-amino 3H-isobenzofuanones - used as analgesics and antiinflammatories, prepd. from 2-formyl benzoic acid and substd. aniline

摘要

Isobenzofuranones of formula (I) are new (where E1 is H or one or more substituents, pref. OH, OMe, OCOMe or -OCH2O-or -OCH2CH2O- an adjacent ring atoms; E2 is H or one or more substituents, pref. 1-4C alkyl, CO2Me or CO2H or its salts with pharmacologically acceptable bases; E3 is H, 1-4C alkyl or benzyl; A is CR1R2, -CH2R2, -CH2CH2 - or -CH(CH2X) CH2-; R1 and R2 are same or different H, 1-4C alkyl, aralkyl or cycloalkyl, or CR1R2 is a is not >7C alicyclic ring; X is halogen, OH, OCOMe, CH2CH2N , NH2, NHCONH2 or -N ; -N is a cyclic or acyclic sec. or tert.amine gp; B is a direct bond, or if E2 is H or 1-4C alkyl and A is CR1R2 then B may also be CR1R2). (I) have analgesic and antiinflammatory (esp. antioedema) activity, with low toxicity and good gastric tolerance (i.e. low ulcerogenic activity). They may be used in human or veterinary medicine, orally, rectally or percutaneously.