Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1985-08-14
1986-10-28
Friedman, Stanley J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514211, 514227, 514375, A61K 3142, A61K 3155, A61K 31395, A61K 31535
Patent
active
046199268
ABSTRACT:
The invention relates to pharmaceutical preparations for topical application which contain salts of alkanecarboxylic acids, in particular compounds of the formula ##STR1## wherein R.sub.1 is a group of the formula ##STR2## wherein X.sub.1 and X.sub.2 are hydrogen and X.sub.3 is isobutyl, or X.sub.1 and X.sub.3 are hydrogen and X.sub.2 is benzoyl, or X.sub.1 is hydrogen, X.sub.2 is chlorine, and X.sub.3 is 3-pyrrolin-1-yl, or X.sub.1 is hydrogen, X.sub.2 is a group of the formula --CH.dbd.CH--C(OCH.sub.3).dbd.CH--X.sub.4, and X.sub.3 together with X.sub.4 are a bond, and R.sub.2 is methyl, or X.sub.2 and X.sub.3 are hydrogen and X.sub.1 is 2,6-dichloroanilino, and R.sub.2 is hydrogen, or R.sub.1 is a group of the formula ##STR3## wherein X.sub.5 is the common bond with the methine group in formula I, X.sub.6 and X.sub.7 are hydrogen, X.sub.8 is p-methylbenzoyl, Y is a nitrogen atom, and X.sub.9 is a methyl group, or X.sub.5 is a methyl group, X.sub.6 is a common bond with the methine group in formula I, X.sub.7 is a group of the formula --CH.dbd.C(OCH.sub.3)--CH.dbd.CH--X.sub.10, X.sub.8 together with X.sub.10 are a bond, Y is a nitrogen atom and X.sub.9 is p-chlorobenzoyl, or X.sub.5 is a methyl group, X.sub.6 is the common bond with the methine group in formula I, X.sub.7 is a group of the formula --CH.dbd.C(F)--CH.dbd.CH--X.sub.11, X.sub.8 together with X.sub.11 are a bond, Y is a carbon atom and X.sub.9 is (p-methanesulfinylphenyl)methylene, and R.sub.2 is hydrogen, and each of R.sub.3, R.sub.4 and R.sub.5 independently is hydrogen, an aliphatic radical, or two of R.sub.3, R.sub.4 and R.sub.5 together are a bivalent aliphatic radical, unsubstituted or substituted or interrupted by aza, oxa or thia, with the proviso that at least one of R.sub.3, R.sub.4 and R.sub.5 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.
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Ciba-Geigy Corporation
Fishman Irving M.
Friedman Stanley J.
Glynn Michael W.
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