MERCK SHARP & DOHME CORP.;ISIS PHARMACEUTICALS, INC.
发明人:
CARROLL, STEVEN S.,LAFEMINA, ROBERT L.,HALL, DAWN L.,HIMMELBERGER, AMY L.,KUO, LAWRENCE C.,MACCOSS, MALCOLM,OLSEN, DAVID B.,RUTKOWSKI, CARRIE A.,TOMASSINI, JOANNE E.,AN, HAOYUN,BHAT, BALKRISHEN,BHAT,
申请号：
ES02709095
公开号：
ES2532836T3
申请日:
2002.01.18
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
The use of a compound of structural formula I having the stereochemical configuration: ** Formula ** or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for inhibiting HC5 NS5B polymerase, inhibiting HCV replication or treating HCV infection, in which B is: ** Formula ** Y is C1-10 alkylcarbonyl, P3O9H4, P2O6H3 or P (O) R9R10； R1 is hydrogen, C2-4 alkenyl, C2-4 alkynyl or C1-4 alkyl optionally substituted with amino, hydroxy or 1 to 3 fluorine atoms and one of R2 and R3 is hydroxy or C1-4 alkoxy and the other of R2 and R3 is selected from the group consisting of hydrogen； hydroxy, halogen； C1-4 alkyl optionally substituted with 1 to 3 fluorine atoms, C1-10 alkoxy optionally substituted with C1-3 alkoxy or 1 to 3 fluorine atoms, C2-6 alkenyloxy, C1-4 alkylthio, C1-8 alkylcarbonyloxy, aryloxycarbonyl, azido, amino, C1-4 alkylamino and di (C1-4 alkyl) amino； or R2 is hydrogen, C2-4 alkenyl, C2-4 alkynyl or C1-4 alkyl optionally substituted with amino, hydroxy, 1 to 3 fluorine atoms, and one of R1 and R3 is hydroxy or C1-4 alkoxy and the other from R1 and R3 is selected from the group consisting of hydrogen； hydroxy, halogen； C1-4 alkyl optionally substituted with 1 to 3 fluorine atoms, C1-10 alkoxy optionally substituted with hydroxy, C1-3 alkoxy, carboxy or 1 to 3 fluorine atoms, C2-6 alkenyloxy, C1-4 alkylthio, alkylcarbonyloxy C1-8, aryloxycarbonyl, azido, amino, C1-4 alkylamino and di (C1-4 alkyl) amino； or R1 and R2 together with the carbon atom to which they are attached form a 3 to 6-membered saturated monocyclic ring system that optionally contains a heteroatom selected from O, S and N0-4 alkyl； R4 and R6 are each independently H, OH, SH, NH2, C1-4 alkylamino, di (C1-4 alkyl) amino, C3-6 cycloalkylamino, halogen, C1-4 alkyl, C1-4 alkoxy or CF3； R5 is H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-4 alkylamino, CF3 or halogen； R14 is H, CF3, C1-4 alkyl, amino, C1-4 alkylamino, C3-6 cycloalkylamino or di (C1-4 alkyl) amino； R12 and R
