Topical analgesic and antiinflammatory compsn. - contg. amine salt of aryl:alkanoic acid non-steroidal antiinflammatory

摘要

Topical formulation contains a salt of formula (I), or its isomer, together with standard auxiliaries and additives. R1 R2 CH-COO- +HNR3R4R5 (I). R1 can be a gp. (IIa) where X1 and X2 are each H and X3 is isobutyl; or X1 and X3 are both H and X2 is benzoyl; or X1 is H, X2 is chloro and X3 is 3-pyrrolin-1-yl; or X is H, X2 is -CH=CH. C(OCH3)=CH X4 and X3 completes a bond with X4; in all these cases R2 is methyl, or X2 and X3 are both H, X1 is 2,6-dichloroanilino and R2 is then H. R1 can also be a gp. (II)b X5 is a bond to the methine gp; X6 and X7 are both H, X8 is p-methylbenzoyl, Y is nitrogen and X9 is methyl; or X5 is methyl, X6 is a bond to methine, X7 is -CH=C(OCH3). CH=CH X10, X8 and X10 are together a bond; Y is nitrogen and X9 is p-chlorobenzoyl; or X5 is methyl, X6 is a bond to methine, X7 is -CH=CF. CH=CH X11, X8 and X11 are together a bond; Y is carbon and X9 is p- methanesulphinylphenylmethylene; in all these cases R2 is H. R3, R4 and R5 are each H or aliphatic gps. or two of them form an opt. substd. bivalent aliphatic gp. which can be interrupted by nitrogen, oxygen or sulphur, but not all 3 can be H. 11(B) Some (I) are also new cpds. (I) have analgesic and esp. antiinflammatory activities, and can be used in human or veterinary medicine. They have good percutaneous penetration and resorption, and topical applicn. avoids the gastro-intestinal side effects associated with oral administration of R1R2. CH. COOH or their base salts.