C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 311/21 (2006.01) A61K 31/18 (2006.01) A61K 31/33 (2006.01) A61K 31/44 (2006.01) C07C 311/01 (2006.01) C07C 311/29 (2006.01) C07C 311/44 (2006.01) C07C 323/67 (2006.01) C07D 213/40 (2006.01) C07D 213/56 (2006.01) C07D 295/15 (2006.01) C07D 307/54 (2006.01) C07D 333/24 (2006.01) C07D 453/02 (2006.01)
Patent
CA 2223727
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 of structure (I) or pharmaceutically acceptable salts thereof; wherein R1 is alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 is one of hydrogen, alkyl, cycloalkyl or aryl; R3 is one of hydrogen, hydroxy or alkoxy; R4 is one of -NH2, phenyl or pyridyl, wherein said phenyl and said pyridyl are optionally substituted with one or two of halogen, hydroxy, hydroxyalkyl, alkoxy, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and/or dialkylaminoalkyl; X is one of -CH2- or -C(O)-; and n is from zero to eleven; provided that when R4 is -NH2, then R3 is hydrogen and n is other than zero; and also provided that when R3 is hydroxy or alkoxy, then R4 is other than -NH2, an n is other than zero.
L'invention concerne des inhibiteurs non peptidiques du facteur Xa utiles pour traiter les troubles occlusifs d'artères et de veines causés par des thromboses, les inflammations, le cancer et les maladies neurodégénératives. Les inhibiteurs du facteur Xa sont des composés de structure (I) ou des sels pharmaceutiquement acceptables de ceux-ci. Dans la formule, R?1¿ désigne alkyle, alkyle substitué, cycloalkyle, aryle, aryle substitué, hétéroaryle substitué ou non; R?2¿ désigne hydrogène, alkyle, cycloalkyle ou aryle; R?3¿ désigne hydrogène, hydroxy ou alcoxy; R?4¿ désigne -NH¿2?, phényle ou pyridyle le cas échéant substitués par un ou deux halogènes, hydroxy, hydroxyalkyle, alcoxyle, amino, monoalkylamino, dialkylamino, aminoalkyle, monoalkylaminoalkyle et/ou dialkylaminoalkyle; X désigne -CH¿2?- ou -C(O)-; et n vaut 0 à 11; à condition que, lorsque R?4¿ désigne -NH¿2?, R?3¿ désigne hydrogène et n ne soit pas nul; à condition également que, lorsque R?3¿ désigne hydroxy ou alcoxy, R?4¿ ne désigne pas -NH¿2? et n ne soit pas nul.
Illig Carl R.
Lu Tianbao
Salvino Joseph M.
Soll Richard M.
Subasinghe Nalin L.
3-Dimensional Pharmaceuticals Inc.
Mbm & Co.
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