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Substituted benzyl amine compounds and medical, in particular their use in the treatment of hepatitis C virus (HCV) infection

机译:取代的苄胺化合物和医药,尤其是其在治疗丙型肝炎病毒(HCV)感染中的用途

摘要

The present invention provides a compound having the formula (I): or a salt, N-oxide or tautomer thereof, wherein A is CH, CF or nitrogen; E is CH, CF Or R0 is hydrogen or C1-2 alkyl; R1a is CONH2; CO2H; an optionally substituted acyclic C1-8 hydrocarbon group; and 3 to 7 ring members, Selected from optionally substituted monocyclic carbocyclic or heterocyclic groups wherein 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S R2 is selected from hydrogen and the group R2a; R2a is an optionally substituted acyclic d-8 hydrocarbon group; has 3 to 7 ring members, of which 0, 1 or 2 The ring member is a heteroatom ring member selected from O, N and S; An optionally substituted monocyclic carbocyclic or heterocyclic group; and an optionally substituted bicyclic ring having 9 or 10 members, one or two of which are nitrogen atoms Selected from the formula heterocyclic groups; at least one of R 1 and R 2 is other than hydrogen; R 3 is zero, one, two or three heteroatom ring members selected from N, O and S Including, optionally substituted, 3 to 10 membered monocyclic or bicyclic carbocyclic or heterocyclic ring; R4a is halogen; cyano; optionally substituted with one or more fluorine atoms C 1-4 alkyl; selected from C 1-4 alkoxy optionally substituted with one or more fluorine atoms; hydroxy-C 1-4 alkyl; and C 1-2 alkoxy-C 1-4 alkyl; R 5 is hydrogen and substituent From R5a R 5a is C 1-2 alkyl optionally substituted with one or more fluorine atoms; C 1-3 alkoxy optionally substituted with one or more fluorine atoms; halogen; cyclopropyl; cyano; Selected from amino. This compound has activity against hepatitis C virus and can be used for prevention or treatment of hepatitis C virus infection. [Selection figure] None
机译:本发明提供了具有式(I)的化合物或其盐,N-氧化物或互变异构体,其中A为CH,CF或氮; E为CH,CF或R 0为氢或C 1-2烷基; R1a是CONH2; CO2H;任选取代的无环C 1-8烃基; 3至7个环成员,选自任选取代的单环碳环或杂环基团,其中0、1、2、3或4为选自O,N和S R2的杂原子环成员,选自氢和基团R2a;和R 2a是任选取代的无环d-8烃基;具有3至7个环成员,其中0、1或2。环成员是选自O,N和S的杂原子环成员;任选取代的单环碳环或杂环基;任选地被取代的具有9或10个成员的双环,其中一个或两个是选自式杂环基的氮原子; R 1和R 2中的至少一个不是氢。 R 3是选自N,O和S的零个,一个,两个或三个杂原子环成员,包括任选取代的3至10元单环或双环碳环或杂环; R4a是卤素;氰基;任选地被一个或多个氟原子C 1-4烷基取代;选自任选地被一个或多个氟原子取代的C 1-4烷氧基;羟基-C 1-4烷基; C 1-2烷氧基-C 1-4烷基; R 5是氢和取代基。从R 5a到R 5a是任选地被一个或多个氟原子取代的C 1-2烷基。任选地被一个或多个氟原子取代的C 1-3烷氧基;卤素;环丙基氰基;选自氨基。该化合物具有抗丙型肝炎病毒的活性,可用于预防或治疗丙型肝炎病毒感染。 [选择图]无

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