Flentge, Charles,Hutchinson, Douglas K,Betebenner, David A,Degoey, David A,Donner, Pamela L,Kati, Warren M,Krueger, Allan C,Liu, Dachun,Liu, Yaya,Longenecker, Kenton L,Maring, Clarence J,Motter, Chris
申请号:
ES12182277
公开号:
ES2592961T3
申请日:
2008.09.17
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A unit formulation comprising one or more compounds of formula I-L0 or salts thereof, and one or more additional therapeutic agents selected from the group consisting of interferon agents, ribavirin, HCV inhibitors and anti-HIV agents; wherein the formula I-L0 is: is selected from the group consisting of a single carbon-carbon lace and double carbon-carbon bond; R1 is selected from the group consisting of hydrogen and methyl; R2 is selected from the group consisting of hydrogen, halo, hydroxy, methyl, cyclopropyl and cyclobutyl; R3 is selected from the group consisting of hydrogen, halo, oxo and methyl; R4 is selected from the group consisting of halo, alkyl, alkenyl, alkynyl, nitro, cyano, azido, alkyloxy, alkenyloxy, alkynyloxy, amino, aminocarbonyl, aminosulfonyl, alkylsulfonyl, carbocyclyl and heterocyclyl, in which: (a) the amino , aminocarbonyl and aminosulfonyl are optionally substituted with: (1) one or two substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl and alkylsulfonyl, or (2) two substituents which, together with the amino nitrogen, form a heterocyclyl single ring, and (b) alkyl, alkenyl, alkynyl, alkyloxy, alkenyloxy, alkynyloxy and alkylsulfonyl, are optionally substituted with one or more substituents independently selected from the group consisting of halo, oxo, nitro, cyano, azido, hydroxy, amino, alkyloxy, trimethylsilyl, carbocyclyl and heterocyclyl, wherein: the amino is optionally substituted with: (1) one or two substituents selected inde slopingly between the group consisting of alkyl, alkenyl, alkynyl, alkylcarbonyl, alkylsulfonyl, alkyloxycarbonyl, carbocyclyl, heterocyclyl, carbocyclylalkyl and heterocyclylalkyl, or (2) two substituents which, together with the amino nitrogen, form a single ring heterocyclyl, and (c) carbocyclyl and heterocyclyl are optionally substituted with up to three substituents independently selected from the group consisting of alkyl, alkenyl, alkynyl, halo, oxo, nitro, cyano