发明名称 MACROCYCLIC FACTOR VIIA INHIBITORS
摘要 The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments.;
申请公布号 US2016115159(A1) 申请公布日期 2016.04.28
申请号 US201414897764 申请日期 2014.06.11
申请人 BRISTOL-MYERS SQUIBB COMPANY 发明人 RICHTER Jeremy;BATES J. Alex;CHENEY Daniel L.
分类号 C07D413/12;C07D255/04;C07D245/04;C07D401/12 主分类号 C07D413/12
代理机构 代理人
主权项 1. A compound of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, or a solvate thereof, wherein: W is independently selected from: W is independently selected from: X is independently selected from: CR13 and N;L is independently C1-5 alkylene substituted with 0-2 R9 or C2-5 alkenylene substituted with 0-2 R9; optionally one of the carbon atoms of said alkylene and alkenylene may be replaced by O, S, SO2, NH, N(C1-4 alkyl), N(C1-4 fluoroalkyl), and N(—CH2—C3-6 carboycle);R9 is independently selected from: halogen, C1-4 alkyl, C1-4 haloalkyl, hydroxy, C1-4 alkoxy, and C1-4 haloalkoxy; optionally when two R9 groups are substituted on the same carbon atom of L, they may combine, with the carbon atom to which they are attached, to form a C3-6 cycloalkyl ring;R1 and R2 are independently selected from: H, OH, halogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, C2-4 alkenyl, C2-4 alkynyl, —(CH2)0-1—C3-6 carboycle and —O—(CH2)0-1—C3-6 carboycle;R3, R4 and R7 are independently selected from H, halogen, C1-2 alkyl, C1-2 alkoxy, and C1-2 haloalkoxy;R5 is independently selected from: H C1-2 alkyl, and C1-2 haloalkyl;R6 is independently selected from: H, CN, C1-4 alkyl, —CO2H, CO2(C1-4 alkyl), —CH2CO2H, and —CH2CO2(C1-4 alkyl);R8 is independently selected from: H, halogen, CN, OH, SH, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, C1-4 alkylthio, C1-4 haloalkylthio, —SO2(C1-4 alkyl), —SO2(C1-4 haloalkyl), —SO2(C3-6 cycloalkyl), —SO2NH2, —SO2NH(C1-4 alkyl), —SO2N(C1-4 alkyl)2, and —SO2(C3-6 cycloalkyl);R12 is independently selected from H, halogen, CN, —C(═NH)NH2, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2, CH2NH2, CH2NH(C1-4 alkyl), CH2N(C1-4 alkyl)2, C(O)NH2, C(O)NH(C1-4 alkyl), and C(O)N(C1-4 alkyl)2; andR13 and R14 are independently selected from: H, F, Cl, C1-2 alkyl, and C1-2 alkoxy.
地址 Princeton NJ US