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    • 1. 发明专利
    • BIPHENYL DERIVATIVES AND THEIR USE IN TREATING HEPATITIS C
    • IL195198D0
    • 2009-08-03
    • IL19519808
    • 2008-11-10
    • ARROW THERAPEUTICS LTDTHOMAS ALEXANDER JAMES FLOYDLUMLEY JAMESSALTER JAMES IAINCARTER MALCOLM CLIVEMATHEWS NEILPILKINGTON CHRISTOPHER JOHNFRASER IAN JOHN
    • Compounds of formula (I) are found to be active against HCV. wherein: R 1 is a moiety -A 1 -L 1 -A 1 ', -A 1 -L 1 -A 1 '-A 1 " or -A 1 -L 1 -A 1 '-Y 1 -A 1 "; A and B are the same or different and each represent a direct bond or a -CO- NR'-, -NR'-CO-, -NR'-CO-NR"-, -NR'-S(O) 2 -, -S(O) 2 -NR'- or -NR'- moiety, wherein R' and R" are the same or different and each represent hydrogen or C 1 -C 4 alkyl; R 2 and R 3 are the same or different and each represent C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, halogen, hydroxy, thio, -NR'R", -SO 2 -R'", -NR'-COR'" or -CO 2 R'", wherein R' and R" are the same or different and represent hydrogen or C 1 -C 4 alkyl and R'" represents C 1 -C 4 alkyl; n and m are the same or different and each represent 0, 1 or 2; R 4 is a C 1 -C 6 alkyl or C 1 -C 6 haloalkyl group or a moiety -A 4 , -A 4 -A 4 ', -L 4 -A 4 , -A 4 -L 4 -A 4 ', -A 4 -Het 4 -L 4 -Het 4 '-L 4 ' or -L 4 -Het 4 -L 4 ', - each A 1 , A 4 , A 1 ', A 1 " and A 4 ' are the same or different and represent a phenyl, 5- to 10- membered heteroaryl, 5- to 10- membered heterocyclyl or C 3 -C 6 carbocyclyl moiety; each L 1 and L 4 is the same or different and represents a C 1 -C 4 alkylene or a C 1 -C 4 hydroxyalkylene group; - Y 1 represents -CO-NR'-, -CO-( C 1 -C 4 alkylene)-, -CO-( C 1 -C 4 alkylene)-NR'-, -NR'-CO-, -CO-, -O-CO- or -CO-O-, wherein R' is hydrogen or C 1 -C 4 alkyl; L 4 ' represents hydrogen or a C 1 -C 4 alkyl group; Het 4 and Het 4 ' are the same or different and represent -O-, -S- or -NR'-, wherein R' is hydrogen or a C 1 -C 4 alkyl group; the phenyl, heteroaryl, heterocyclyl and carbocyclyl moieties in R 1 and R 4 being unsubstituted or substituted by (a) a single unsubstituted substituent selected from -CO 2 R', -SO 2 NR"R', -S(O) 2 -R', -CONR"R", -COR'", -CO-CO-OR''', -CO-( C 1 -C 4 alkylene)-OR", -CO-( C 1 -C 4 alkylene)-NR"R", -CO-( C 1 -C 4 alkylene)-NR"-CO-R''', -CO- (C 1 -C 4 alkylene)-CO-NR"R", -CO-( C 1 -C 4 alkylene)-SO 2 -R'", -CO-( C 1 -C 4 alkylene)-O- (C 1 -C 4 alkylene)-OR", -CO-( C 1 -C 4 alkylene)-O-( C 1 -C 4 alkylene)-NR"R", -CO-( C 1 -C 4 alkylene)-NR"-( C 1 -C 4 alkylene)-OR", -CO-( C 1 -C 4 alkylene)-NR"-( C 1 -C 4 alkylene)- NR"R", -SO 2 -( C 1 -C 4 alkylene)-OR", -NR"-SO 2 -R'", -( C 1 -C 4 alkylene)-CO-( C 1 -C 4 alkylene)-CO