Azacycloalkanone serine protease inhibitors

Details Azacycloalkanone serine protease inhibitors Azacycloalkanone serine protease inhibitors

C - Chemistry, Metallurgy

07

D

C07D 211/76 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) C07D 207/26 (2006.01) C07D 401/12 (2006.01) C07D 409/14 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2384247

The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula (I) or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1-3 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1, R2 and R3 are independently hydrogen or C1-3 alkyl.

L'invention concerne des inhibiteurs du facteur Xa non peptidique, utiles au traitement de troubles d'occlusion thrombotiques artériels et veineux, d'inflammations, de cancer et de maladies neurodégénératives. Les inhibiteurs du facteur Xa produisent des composés de la formule (I) ou des sels de ceux-ci pharmaceutiquement acceptables. Q est phényle, benzyle, pyridyle, indolyle, quinolinyle, benzothiényle, biphénylyle ou imidazolyle, qui peuvent indifféremment renfermer au moins un substituant facultatif indépendamment choisi parmi halo, trifluorométhyle, hydroxy, amino, nitro, cyano, C¿1-3? alcoxy, C¿1-3? alkyle, méthylènedioxy, carboxamido, acétamido ou amidino; X représente méthylène, carbonyle ou sulfonyle; Z représente méthylène, éthylène ou propylène; M représente méthylène ou éthylène et R?1¿, R?2¿ et R?3¿ représentent individuellement hydrogène ou C¿1-3? alkyle.

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