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Macrocyclic inhibitors of hepatitis C virus
专利权人:
MEDIVIR AB
发明人:
PIERRE JEAN-MARIE RABOISSON,HERMAN AUGUSTINUS DE KOCK,LILI HU,SANDRINE MARIE HELENE VENDEVILLE,ABDELLAH TAHRI,DOMINIQUE LOUIS NESTOR SURLERAUX,KENNETH ALAN SIMMEN,KARL MAGNUS NILSSON,BENGT BERTIL SAMU
申请号:
NI200800036
公开号:
NI200800036A
申请日:
2008.01.29
申请国别(地区):
NI
年份:
2016
代理人:
摘要:
Equation VHC (I) and the replication inhibitors of positive oxides, salts and stereoisomers, each dot line represents an optional duplex; X is n, CH, and when x has a double connection, it is C; R1 is n, ch; nh-so2r8; R2 is hydrogen; when x is C or CH, R2 may also be C1-6 tar; R3 is hydrogen, C1-6 tar, C1-6-c1-6-c1-6, cycloquilo c3-7; R4 is arilo or het; n is 3, 4, 5 or 6; R5 is halo, C1-6, hc-6, hydroxi, alcoxi C1-6, fenilo or het; R6 is alcox C1-6, or dimethamine; R7 is hydrogen; arilo; het; het; cyclo-7 is alternative to C1-6 tar; C1-6 is C1-6, or chemical cycloethane;R8 is arilo; het; c3-7 cyclopentadiene; C1-6 tar optional substitution; or C1-6 tar optional substitution for c3-7 cyclopentadiene or het; arilo is phenyl, optional substitution for 1, 2 or 3; het is saturated heterocyclic ring, 1. Partially unsaturated or unsaturated with 5 to 6 members of 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, optionally replaced by 1, 2 or 3 substitutes;1. Pharmaceutical compounds containing compound (I) and process for preparing compound (I). A bioavailable combination of formula (I) and ritonavir's VHC inhibitor is also provided.Inhibidor de la replicación del VHC de fórmula (I) y los N-óxidos, sales y esteroisómeros, donde cada línea punteada representa un doble enlace opcional; X es N, CH y y cuando X posee un doble enlace es C; R1 es -OR7, -NH-SO2R8; R2 es hidrógeno y cuando X es C o CH, R2 también puede ser alquilo C1-6; R3 es hidrógeno, alquilo C1-6, alcoxi C1-6-alquilo C1-6, cicloalquilo C3-7; R4 es arilo o Het; n es 3, 4, 5 o 6; R5 es halo, alquilo C1-6, hidroxi, alcoxi C1-6, fenilo o Het; R6 es alcoxi C1-6 o dimetilamino; R7 es hidrógeno; arilo; Het; cicloalquilo C3-7 sustituido opcionalmente con alquilo C1-6; o alquilo C1-6 sustituido opcionalmente con cicloalquilo C3-7, arilo o con Het; R8 es arilo; Het; cicloalquilo C3-7 sustituido opcionalmente con alquilo C1-6; o alquilo C1-6 sustituido opcionalmente con cicloalquilo C3-7, arilo o con Het; ar
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