Benzoxazepinones and their use as squalene synthase inhibitors

Details Benzoxazepinones and their use as squalene synthase inhibitors Benzoxazepinones and their use as squalene synthase inhibitors

C - Chemistry, Metallurgy

07

D

C07D 267/14 (2006.01) A61K 31/553 (2006.01) A61P 3/06 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2413429

There is disclosed a compound represented by formula (I), wherein R1 is optionally substituted 1-carboxyethyl group, optionally substituted alkyl- sulfonyl group, optionally substituted (carboxy-cycloalkyl)-alkyl group, -X1- X2-Ar-X3-X4-COOH (wherein X1 and X4 are a bond or alkylene group, X2 and X3 are a bond, -O-, -S-, Ar is divalent aromatic group , etc.), R2 is alkyl group optionally substituted with alkanoyloxy group and/or hydroxy group, R3 is alkyl group, and W is halogen atom, etc., or a salt thereof. The compound has the cholesterol lowering activity and the triglyceride lowering activity and is useful for preventing and/or treating hyperlipidemia.

L'invention concerne un composé représenté par la formule (I): ou un sel dudit composé. Dans ladite formule, R?1¿ représente un groupe 1-carboxyéthyle éventuellement substitué, un groupe alkyl-sulfonyle éventuellement substitué, un groupe (carboxy-cycloalkyl)-alkyle éventuellement substitué, -X?1¿-X?2¿-Ar-X?3¿-X?4¿-COOH (où X?1¿ et X?4¿ désignent une liaison ou un groupe alkylène, X?2¿ et X?3¿ désignent une liaison, -O-, -S-, Ar désigne un groupe aromatique divalent, etc.), R?2¿ représente un groupe alkyle éventuellement substitué par un groupe alcanoyloxy et/ou un groupe hydroxy, R?3¿ représente un groupe alkyle et W désigne un atome d'halogène, etc. Le composé selon l'invention, qui possède une activité hypocholestérolémiante et qui abaisse les triglycérides, est utilisé dans la prévention et/ou le traitement de l'hyperlipidémie.

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