| 摘要 |
The present invention provides a compound of Formula (I);;wherein
R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is 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, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl;A is
1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5 and unsubstituted or substituted with R6 and unsubstituted or substituted with NH2, or2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; andB is
1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8;
and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses. |
| 主权项 |
1. A compound of formula Ior a pharmaceutically acceptable salts thereof, wherein
R1 is H or C1-6 alkyl, R2, is H or C1-6 alkyl or CH2OH, R3 is H or C1-6 alkyl, and R4 is 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, then R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl or —CH2OH, and when R2, R3, and R4 are H, then R1 is C1-6 alkyl; A is
1) a 9-10 membered bicyclic heterocycle having 1-3 heteroatoms independently selected from N, S and O, which 9-10 membered bicyclic heterocycle is unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with NH2, or2) a 6-9 membered monocyclic or bicyclic carbocyclic ring system unsubstituted or substituted with R5, unsubstituted or substituted with R6, and unsubstituted or substituted with —CH2NH2; R5 is halogen; R6 is C1-6alkyl; B is
1) a 5- or 6-membered monocyclic heterocycle having 1 or 2 heteroatoms independently selected from N, S or O, which is unsubstituted or substituted on a carbon or nitrogen atom with R7, unsubstituted or substituted on a carbon or nitrogen atom with R8, and unsubstituted or substituted on a carbon or nitrogen atom with R9, or2) an 8- or 9-membered fused bicyclic heterocycle having 1, 2 or 3 nitrogen atoms which is unsubstituted or substituted on a carbon or nitrogen atom with R7, and unsubstituted or substituted on a carbon or nitrogen atom with R8; R7 is CF3, C1-6alkyl, C1-6alkanol, C3-8carbocycle, aryl, or a 5- or 6-membered heterocycle having 1 or 2 nitrogen atoms and zero or 1 oxygen atom, which heterocycle or C3-8carbocycle or aryl is unsubstituted or mono-, di-, tri- or tetra-substituted with a group independently selected from R10, R11, R12, R13, and R15; R8 is C1-6alkyl; R9 is halogen; R10 is CF3, CN, C(O)NH2, OCD3, OC1-6alkyl, OCH(CH2Cl)(CH2OH), —OC3-8cycloalkyl, or R11 is halogen, C1-6alkyl, CF3, CHF2, CN, or COOH; R12 is CF3, COOH, C(O)OC1-6alkyl, CN, halogen, OCF3, ═O, or SO2C1-6alkyl; R13 is C1-6alkyl, C(O)OC1-6alkyl, CN, CF3, OC1-6alkyl, N(C1-6alkyl)2, OC1-6alkyl, or OCHF2; and R15 is halogen, CF3, CHF2, C1-6alkyl, CN, or COOH. |
