Substituted thiazolo[3,2-a]azepine derivatives

Details Substituted thiazolo[3,2-a]azepine derivatives Substituted thiazolo[3,2-a]azepine derivatives

C - Chemistry, Metallurgy

07

D

C07D 513/04 (2006.01) A61K 31/55 (2006.01) C07C 227/00 (2006.01) C07D 211/60 (2006.01) C07D 277/06 (2006.01)

Patent

CA 2171334

The present invention relates to a substituted thiazolo[3,2-a]azepine derivative having inhibitory activity against angiotensin I converting enzyme and neutral endpeptidase. The above substituted thiazolo[3,2-a]azepine derivative is represented by the following general formula (I): Image (wherein R1 represents a hydrogen atom or a protecting group of a thiol group; R2 represents a hydrogen atom, a lower alkyl group, an aryl group which may have a substituent, a hetroaryl group which may have a substituent, a lower alkoxyl group or a lower alkylthio group; R3; R4 and R5 may be the same or different from one another and represent each a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a lower alkylthio group or the like, with the proviso that the case wherein all of R3, R4 and R5 are hydrogen atoms are excepted; R6 and R7 may be the same or different from each other and represent each a hydrogen atom or a lower alkyl group; R8 represents a hydrogen atom or a protecting group of a carboxyl group; and m and n are each independently 0 or, 1 or 2).

L'invention se rapporte à un dérivé de thiazolo[3,2- alpha ]azépine à substitution représenté par la formule (I) et ayant pour effet d'inhiber une enzyme convertissant l'angiotensine I et une hydrolase auriculaire de peptide natriurétique. Dans cette formule, R<1> représente hydrogène ou un groupe protecteur de thiol; R<2> représente hydrogène, alkyle inférieur, aryle éventuellemnt substitué, hétéroaryle éventuellement substitué, alcoxy inférieur ou alkylthio inférieur; R<3>, R<4> et R<5> représentent chacun, indépendamment, hydrogène, alkyle inférieur, alcoxy inférieur, alkylthio inférieur, etc., à l'exception du cas où les R<3>, R<4> et R<5> sont tous en même temps des atomes d'hydrogène; R<6> et R<7> représentene chacun, indépendamment, hydrogène ou alkyle inférieur; R<8> représente hydrogène ou un groupe protecteur de carboxyle, et m et n représentent chacun indépendamment 0, 1 ou 2.

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