Pyrazolo[1,5-a]pyrimidine derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/505 (2006.01)

Patent

CA 2331468

The present invention provides pyrazolo[1,5- a]pyrimidine derivatives represented by the formula (1) (See formula I) wherein R1 represents lower alkyl or the like; one of R2 and R3 represents hydrogen and the other represents phenyl having lower alkoxy or the like, and R4 is hydrogen, carboxyl, lower alkoxy-carbonyl or the like. The derivatives of the invention have pharmacological effects such as analgesic action, inhibitory effect on nitrogen monoxide synthetase and the like and are useful as analgesics. The derivatives of the invention are also useful as therapeutic or prophylactic agents for septicemia, endotoxin shock, chronic articular rheumatism, etc.

L'invention concerne des dérivés de pyrazolo[1,5-a]pyrimidine représentés par la formule générale (1) ci-après, lesquels dérivés ont des effets pharmacologiques, notamment un effet analgésique et un effet inhibiteur vis-à-vis de la synthèse du monoxyde d'azote, et sont utiles comme agents analgésiques et comme remèdes et agents prophylactiques pour la septicémie, le choc endotoxinique, la polyarthrite rhumatoïde chronique, etc.. Dans cette formule, R<1> représente un alkyle inférieur, etc.; R<2> ou R<3> représente un hydrogène tandis que l'autre représente un phényle, etc. ayant un alkyle inférieur, etc.; et R<4> représente un hydrogène, un carboxy, un alcoxycarbonyle inférieur, etc.

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