Anti-inflammatory substituted 2-benzyl-mercapto-imidazole and pyrimidine derivatives compositions and method of use therefor
AssigneeMerck & Co., Inc.
InventorsMilton L. Hammond, Robert A. Zambias
Life of this patent
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Abstract
Substituted 2-benzyl-mercapto-imidazoles and analogs were prepared from the nucleophlic substitution of an appropriately substituted benzoxyacetate with a 2-imidazole mercapto anion or an analog thereof. These compounds were found to be anti-inflammatory agents.
Claims9
A compound of formula (I) ##STR17## or a pharmaceutically acceptable salt thereof wherein
- Y is ##STR18## R is (a) H;
- (b) C.sub.1-6 alkyl;
- (c) phenyl or phenyl or substituted with one or more substituents selected from a group consisting of
- (1) hydrogen;
- (2) halo;
- (3) loweralkoxy;
- (4) loweralkylthio;
- (5) loweralkylsulfinyl;
- (6) loweralkylsulfonyl;
- (7) loweralkyl;
- (8) loweralkanoyl;
- (9) haloloweralkyl;
- (10) --COOH;
- (11) hydroxyloweralkyl;
- (12) halo loweralkyanoyl;
- or
- (13) loweralkanoyloxy;
- R.sup.1 and R.sup.2 independently are
- (a) H;
- (b) C.sub.1-6 alkyl;
- or
- (c) phenyl.
A pharmaceutical composition for treating topical inflammation comprising a pharmaceutical carrier and an antiinflammatory effective amount of a compound of formula (I) ##STR21## or a pharmaceutically acceptable salt thereof wherein
- Y is ##STR22## R is (a) H;
- (b) C.sub.1-6 alkyl;
- (c) phenyl or substituted phenyl with one or more substituents selected from a group consisting of
- (1) hydrogen;
- (2) halo;
- (3) loweralkoxy;
- (4) loweralkylthio;
- (5) loweralkylsulfinyl;
- (6) loweralkylsulfonyl;
- (7) loweralkyl;
- (8) loweralkanoyl;
- (9) haloloweralkyl;
- (10) --COOH;
- (11) hydroxyloweralkyl;
- (12) halo loweralkyanoyl;
- or
- (13) loweralkanoyloxy;
- R.sup.1 and R.sup.2 independently are
- (a) H;
- (b) C.sub.1-6 alkyl;
- or
- (c) phenyl.
A method of treating or decreasing topical inflammation comprising the administration to a mammalian species in need of such treatment an antiinflammatory amount of a compound of formula (I) ##STR25## or a pharmaceutically acceptable salt thereof wherein
- Y is ##STR26## R is (a) H;
- (b) C.sub.1-6 alkyl;
- (c) phenyl or substituted phenyl with one or more substituents selected from a group consisting of
- (1) hydrogen;
- (2) halo;
- (3) loweralkoxy;
- (4) loweralkylthio;
- (5) loweralkylsulfinyl;
- (6) loweralkylsulfonyl;
- (7) loweralkyl;
- (8) loweralkanoyl;
- (9) haloloweralkyl;
- (10) --COOH;
- (11) hydroxyloweralkyl;
- (12) halo loweralkyanoyl;
- or
- (13) loweralkanoyloxy;
- R.sup.1 and R.sup.2 independently are
- (a) H;
- (b) C.sub.1-6 alkyl;
- or
- (c) phenyl.
Dependencies are inferred from the claim text.