Antiinflammatory azole derivatives
AssigneeMerck Patent GmbH
InventorsJohann Dahm, Joachim Borck, Albrecht Wild, Jan Willem Hovy
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Abstract
Azole derivatives of the formula ##STR1## wherein R.sub.1 is free or esterified carboxyl or other functionally modified carboxyl group, R.sub.2 and R.sub.3 each are aryl; A is C.sub.n H.sub.2n in which n is an integer from 1 to 10, inclusive; and Z is O or S; and the physiologically acceptable salts thereof, possess, with good compatibility, excellent antiphlogistic activity and, in particular, influence favorably the chronic progressive diseases of the joints, e.g., arthritis. They can be prepared from compounds of the formula ##STR2## wherein X.sub.1 is a group convertible into the group --S--A--R.sub.1, and R.sub.2 and R.sub.3 have the values given above.
Claims19
A pharmaceutical composition comprising, in admixture with a solid, liquid or semiliquid pharmaceutically acceptable carrier, an antinflammatorily effective amount per unit dosage of a compound of the formula ##STR5## wherein R.sub.1 is carboxyl, a physiologically acceptable C.sub.1-12 alkyl ester thereof, --CONH.sub.2 or --CN;
- R.sub.2 and R.sub.3 each are phenyl or phenyl mono- or di-substituted by at least one member selected from the group consisting of alkyl, alkoxy alkylmercapto, monoalkylamino, dialkylamino or alkanoylamino wherein the alkyl, alkoxy and alkanoyl are each of up to 4 carbon atoms, F, Cl, Br, I, CF.sub.3, OH, methylenedioxy, NH.sub.2 and NO.sub.2 ;
- A is C.sub.n H.sub.2n wherein n is an integer from 1 to 10 inclusive;
- and Z is O or S, or a physiologically acceptable salt thereof.
Dependencies are inferred from the claim text.