Lactam inhibitors of factor xa and method

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 405/12 (2006.01) A61K 31/55 (2006.01) C07D 223/10 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 403/14 (2006.01) C07D 405/14 (2006.01) C07D 409/12 (2006.01) C07D 409/14 (2006.01) C07D 413/12 (2006.01) C07D 413/14 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2412216

Lactam inhibitors are provided which have the structure (I) including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrug esters thereof, wherein n is l to 5; and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R10a, R11 and R12 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.

La présente invention concerne des inhibiteurs de lactames qui comprennent dans leur structure (I) des sels pharmaceutiquement acceptables de ces derniers et tous leurs stéréoisomères et leurs esters de promédicament. Dans la structure (I), n est compris entre 1 et 5; et R¿1?, R¿2?, R¿3?, R¿4?, R¿5?, R¿6?, R¿7?, R¿8?, R¿9,? R¿10?, R¿10a?, R¿11? et R¿12? sont tels que définis dans l'invention. Ces composés sont des inhibiteurs du Facteur Xa et sont par conséquent utiles en tant qu'anticoagulants. L'invention concerne également un procédé de traitement des maladies cardio-vasculaires associées à des thromboses. Structure (I)

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