Factor IXa Inhibitors

摘要

The present invention provides a compound of Formula (I);;where A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.

主权项

1. A compound of formula Ior a pharmaceutically acceptable salt thereof, whereinA is
1) a 9-10 membered bicyclic heterocycle having 2-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with ═O, —C(═NH)NH2, or pyrazole, or 2) a 12-, 13-, or 14-membered tricyclic heterocycle having 3-5 heteroatoms selected from N, S and O, which 12-, 13-, or 14-membered heterocycle is unsubstituted or substituted with ═O or NH2;B is
1) a 5-membered monocyclic heterocycle having 2 nitrogen atoms and 3 carbon atoms, where
one 5-membered monocyclic heterocycle nitrogen is substituted with
a) 6-membered monocyclic heterocyle having one or two nitrogen atoms or one oxygen atom,b) C1-6 alkyl,c) C 3-8 carbocycle, ord) aryl,
wherein heterocycle, alkyl, carbocycle and aryl are unsubstituted, mono-substituted, or independently di-substituted with CF3, OCH3, F, CN, —CHF2, or ═O,and one 5-membered monocyclic heterocycle carbon atom is unsubstituted or substituted with C1-6 alkyl, 2) a 6-membered monocyclic heterocycle having 1 nitrogen atom and 5 carbon atoms, where three carbon atoms are unsubstituted, and one or two carbon atoms are independently unsubstituted or independently substituted with CF3, —C(CH3)2OH, —OCHF2, —CH(CF3)OH, —C(CF3)(CH3)OH, F, or 3) aryl, substituted with —C1-6 alkyl.