Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors

摘要

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: <IMAGE> 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, and n is other than zero.