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INHIBITEURS DE THROMBINE
专利权人:
MERCK SHARP & DOHME CORP.
发明人:
CHOBANIAN, HARRY,BIFTU, TESFAYE,PIO, BARBARA,WU, ZHICAI
申请号:
EP13857464
公开号:
EP2922535A4
申请日:
2013.11.15
申请国别(地区):
EP
年份:
2016
代理人:
摘要:
Compounds of the invention, which may be useful in inhibiting thrombin and associated thrombotic occlusions, have the following structure: or a pharmaceutically acceptable salt thereof, wherein m is 0 or 1; R is a heterocycle, —(CR8R9)1-2NH2, or —(CR8R9)1-2OH, wherein R8 and R9, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; W is a) —CHR1R2, where R1 is —C(CH3)3, and R2 is —(CH2)1-2OH, b) a 5- or 6-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N and O, wherein substituted heterocycle is substituted with R3, c) a 9- or 10-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N, O and S, wherein substituted heterocycle is mono-substituted with R3, or disubstituted with R3 and R4, or d) a 3-, 4-, or 5-membered carbocyclic ring which is unsubstituted, mono-substituted with R3, di-substituted with R3 and R4, or tri-substituted with R3, R4 and R5; R3 is —CF3, —COOH, —COOR7, —C(O)R6, —CH(OH)R6, —CH2R6, R6, =O, halogen, R7, —OH, —NH2, or —NHSO2R7; and R10 is H or C1-6 alkyl.
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