Pharmaceutical preparations for topical application which contai

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514455, A61K 3136, A61K 3140

Patent

active

045514755

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 an anti-inflammatory agents and/or analgesics for topical application.

REFERENCES:
patent: B514839 (1976-03-01), Sekhar
patent: 3592902 (1971-07-01), Sato et al.
patent: 3896157 (1975-07-01), Fried et al.
patent: 3936528 (1976-02-01), Katz
patent: 4048330 (1977-09-01), Fried et al.
patent: 4346105 (1982-08-01), Sollman
Chem. Abst., 84, 121470w (1976).
Belligno et al., Chem. Abst. 77, 5274s (1972).
Stradi et al., Chem. Abst. 95, 61781p (1981).
Chem. Abst., vol. 95-(1981), 97376z.

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