| 摘要 |
The present invention provides a compound of Formula (I);;wherein
R1, R2, R3 and R4 are independently H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl, and when R2, R3, and R4 are H, R is C1-6 alkyl;
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 I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3 and R4 are independently H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl, and when R2, R3, and R4 are H, R1 is C1-6 alkyl; A 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, or2) 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, whereone 5-membered monocyclic heterocycle nitrogen is substituted with 6-membered monocyclic heterocycle having one or two nitrogen atoms, C1-6 alkyl, C3-8 carbocycle, or 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 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, or3) aryl, substituted with —C1-6 alkyl. |
