C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/608, 260/207
C07D 295/027 (2006.01) A61K 31/195 (2006.01) A61K 31/205 (2006.01) C07C 57/30 (2006.01) C07C 57/58 (2006.01) C07C 59/64 (2006.01) C07C 59/84 (2006.01) C07D 209/28 (2006.01)
Patent
CA 1180008
Abstract of the Disclosure Process for the production of salts of alkanecarboxylic acids and of pharmaceutical preparations The invention relates to pharmacetuical preparations for topical application which contain salts of alkanecarboxylic acids, in part- icular compounds of the formula Image (I) wherein R1 is a group of the formula Image (IIa) where X1 and X2 are hydrogen and X3 is isobutyl, or X1 and X3 are hydrogen and X2 is benzol, or X1 is hydrogen, X2 is chlorine, and X3 is 3-pyrrolin-1-yl, or X1 is hydrogen, X2 is a group of the formula -CH=CH-C(OCH3)-CH-X4, and X3 together with X4 are a bond, and R1 is methyl, or X2 and X3 are hydrogen and X1 is 2,6-dichloro- anilino, and R2 is hydrogen, or R1 is a group of the formula Image (IIb) wherein X5 is the common bond with the methine group in formula I, X6 and X7 are hydrogen, X8 is p-methylbenzoyl, Y is a nitrogen atom, and X9 is a methyl group, or X5 is a methyl group, X6 is a common bond with the methine group in formula I, X7 is a group of the formula -CH-C(OCH3)-CH=CH-Xlc, X8 together with X10 are a bond, Y is a nitrogen atom and X9 is p-chlorobenzoyl, or X5 is a methyl group, X6 is the common bond with the methine group in formula I, X7 is a group of the formula -CH=C(F)-CH-X11, X8 together with X11 are a bond, Y is a carbon atom and X9 is (p-methanesulfinylphenyl)- methylene, and R2 is hydrogen, and each of R3, R4 and R5 independently is hydrogen, an aliphatic radical, or two of R3, R4 and R5 together are a bivalent aliphatic radical, unsubstituted or substituted or interrupted by aza, oxa or fhia, with the proviso that at least one of R3, R4 and R5 is different from hydrogen, optionally in the form of an isomer, together with conventional carriers and/or excipients for topical application. The invention also relates to the production of these preparations and also to novel compounds of the formula I and a process for their production. The compounds of the formula I are suitable for use as anti-inflammatory agents and/or analgesics for topical application.
371271
Fetherstonhaugh & Co.
Novartis Ag
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