Lactam inhibitors of fxa and method

Details Lactam inhibitors of fxa and method Lactam inhibitors of fxa and method

A - Human Necessities

61

K

A61K 31/40 (2006.01) A61K 31/4015 (2006.01) A61K 31/4412 (2006.01) A61P 7/00 (2006.01) A61P 9/00 (2006.01) C07D 207/273 (2006.01) C07D 211/76 (2006.01) C07D 223/12 (2006.01) C07D 401/06 (2006.01) C07D 403/06 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) C07D 409/12 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2360305

Caprolactam inhibitors are provided which have structure (I) including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrugs thereof, wherein n is 1 to 5; and Y, R1, R2, R3, R5, R5a, R6, R7, R8, R9 and R10 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.

L'invention concerne des inhibiteurs caprolactames de structure (I) qui comprend les sels pharmaceutiquement acceptables, tous les stéréo-isomères et les promédicaments de ces composés. Dans la formule de la structure (I) n vaut de 1 à 5, et Y, R?1¿, R?2¿, R?3¿, R?5¿, R?5a¿, R?6¿, R?7¿, R?8¿, R?9¿ et R?10¿ sont tels que définis dans les spécifications. Ces composés sont des inhibiteurs du facteur Xa et sont donc utiles en tant qu'anticoagulants. L'invention concerne aussi une méthode de traitement des maladies cardio-vasculaires associées aux thromboses.

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