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HIV-inhibited 5,6-substituted pyrimidines
专利权人:
JANSSEN R&D IRELAND
发明人:
GUILLEMONT, JÉRÔME EMILE GEORGES,MORDANT, CÉLINE ISABELLE,SCHMITT, BENOIT ANTOINE
申请号:
ES07858202
公开号:
ES2523863T3
申请日:
2007.12.28
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of the formula a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate or a stereochemically isomeric form thereof, wherein: each of R1 is independently hydrogen; aryl; formyl; C1-6 alkylcarbonyl; C1-6 alkyl; C1-6 alkyl oxycarbonyl; R2, R3, R7 and R8 are independently hydrogen; hydroxy; halo; C3-7 cycloalkyl; C1-6-oxy alkyl; carboxyl; C 1-6 alkyl oxycarbonyl; cyano; nitro; Not me; mono- or di- (C1-6 alkyl) amino; polyhalo-C 1-6 alkyl; polyhalo-C1-6-oxy alkyl; -C (>; = O) R10; C1-6 alkyl, optionally substituted with halo, cyano or -C (>; = O) R10; C2-6 alkenyl, optionally substituted with halo, cyano or -C (>; = O) R10; C2-6 alkynyl, optionally substituted with halo, cyano or -C (>; = O) R10; R4 and R9 are independently hydroxy; halo; C3-7 cycloalkyl; C1-6-oxy alkyl; carboxyl; C 1-6 alkyl oxycarbonyl; formyl; cyano; nitro; Not me; mono- or di- (C1-6 alkyl) amino; polyhalo-C 1-6 alkyl; polyhalo-C1-6-oxy alkyl; -C (>; = O) R10; cyano; -S (>; = O) rR10; -NH-S (>; = O) 2R10; -NHC (>; = O) H; -C (>; = O) NHNH2; -NHC (>; = 0) 2R10; Het; -Y-Het; C1-6 alkyl, optionally substituted with halo, cyano, amino; mono- or di- (C1-6 alkyl) amino, -C (>; = O) R10, Het or with C1-6-oxy alkyl; C2-6 alkenyl, optionally substituted with halo, cyano, amino; mono- or di- (C1-6 alkyl) amino, -C (>; = O) R10, Het, or with C1-6-oxy alkyl; C2-6 alkynyl, optionally substituted with halo, cyano, amino; mono- or di- (C1-6 alkyl) amino, -C (>; = O) R10, Het or with C1-6-oxy alkyl; R5 is C2-6 alkenyl or C2-6 alkynyl, both substituted with cyano, aminocarbonyl, mono- or di- (C1-6 alkyl) aminocarbonyl, aryl, pyridyl, thienyl, furanyl, or with one or two C1-6 alkyl groups -oxi; R6 is C1-6 alkoxy-C1-6 alkyl; each of R10, independently, is C1-6 alkyl, amino, mono- or di- (C1-6 alkyl) amino or polyhalo-C1-6 alkyl; X is -NR1-; each of r, independently, is 1 or 2; each of Het, independently, is pyridyl, thienyl, furanyl, oxazolyl, isoxazolyl, imidazolyl
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