发明名称 Hepatitis C inhibitor compounds
摘要 A compound of formula (I) useful for the treatment or prevention of hepatitis C viral infection, (Formula (I)) wherein: X1 and X2 are each independently CRB or N; RB is H, (C1-6)alkyl, (C1-6)haloalkyl, halo. —O—(C1-6)alkyl, NH2, NH(C1-6)alkyl or N((C1-6)alkyl)2; R1 and R2 are each independently (C1-6)alkyl optionally mono- or di-substituted with —O—(C1-6)alkyl, NH2, NH(C1-6)alkyl or N((C1-6)alkyl)2; or R1 and R2, together with the carbon to which they are attached, are linked to form a (C3-7)cycloalkyl group or a 3- to 7-membered heterocyclyl, said cycloalkyl and heterocyclyl being optionally mono- or di-substituted with —(C1-6)alkyl; RA is —C(═O)N(R3)(R4), —C(═O)O(R4), heterocyclyl or heteroaryl, wherein each said heterocyclyl and heteroaryl is optionally substituted 1 to 3 times with R41; R5 and R6 are each independently H or (C1-6)alkyl optionally mono- or di-substituted with —O—(C1-6)alkyl, NH2, NH(C1-6)alkyl or N((C1-6)alkyl)2; or R5 and R6, together with the carbon to which they are attached, are linked to form a (C3-7)cycloalkyl group or a 3- to 7-membered heterocyclyl, said cycloalkyl and heterocyclyl being optionally mono- or di-substituted with —(C1-6)alkyl; and n is 0, 1 or 2.;
申请公布号 US9340539(B2) 申请公布日期 2016.05.17
申请号 US201214240641 申请日期 2012.08.22
申请人 Boehringer Ingelheim International GmbH 发明人 Brochu Christian;Grand-Maitre Chantal;Fader Lee;Kuhn Cyrille;Bertrand-Laperle Megan;Pesant Marc
分类号 C07D487/04;A61K45/06;A61K31/403;C07D471/04;C07D403/12;C07D401/14;C07D405/14;C07D413/14;C07D401/12;C07D403/06;C07D403/14;C07D409/12;C07D409/14;C07D413/04;C07D417/14;C07D491/107;A61K31/4155;A61K31/4178;A61K31/4196;A61K31/433;A61K31/437;A61K31/4439;A61K31/497;C07D405/12 主分类号 C07D487/04
代理机构 代理人 Morris Michael P.;Lazer Edward S.
主权项 1. A compound of Formula (I) or salt thereof: wherein: X1 and X2 are each CRB; RB is H, (C1-6)alkyl, (C1-6)haloalkyl, halo, —O—(C1-6)alkyl, NH2, NH(C1-6)alkyl or N((C1-6)alkyl)2; R1 and R2 are each independently (C1-6)alkyl optionally mono- or di-substituted with —O—(C1-6)alkyl, NH2, NH(C1-6)alkyl or N((C1-6)alkyl)2; or R1 and R2, together with the carbon to which they are attached, are linked to form a (C3-7)cycloalkyl group or a 3- to 7-membered heterocyclyl, said cycloalkyl and heterocyclyl being optionally mono- or di-substituted with —(C1-6)alkyl; RA is —C(═O)N(R3)(R4), —C(═O)O(R4), heterocyclyl or heteroaryl, wherein each said heterocyclyl and heteroaryl is optionally substituted 1 to 3 times with R41; R3 is H or (C1-6)alkyl optionally mono- or di-substituted with —O—(C1-6)alkyl, NH2, NH(C1-6)alkyl, N((C1-6)alkyl)2, —C(═O)—(C1-6)alkyl, —SO2NH2, —SO2—NH(C1-6)alkyl, —SO2—N((C1-6)alkyl)2, —SO2(C1-6)alkyl, —C(═O)—NH2, —C(═O)—NH(C1-6)alkyl or —C(═O)—N((C1-6)alkyl)2; R4 is H, (C1-6)alkyl, (C3-7)cycloalkyl, —(C1-6)alkyl-aryl, —(C1-6)alkyl-heterocyclyl,—(C1-6)alkyl-heteroaryl, aryl, heterocyclyl or heteroaryl, wherein each said alkyl, cycloalkyl, aryl or heterocyclyl, either alone or in combination with another radical, is optionally substituted 1 to 3 times with R41, and each heteroaryl is mono-substituted with —C(═O)—R42; or R3 and R4, together with the N atom to which they are attached, are linked to form a heterocyclyl or heteroaryl, wherein said heterocyclyl and heteroaryl are optionally substituted 1 to 3 times with R41; R41 is each independently selected from the group consisting of halo, oxo, cyano, nitro, R42, —C(═O)—R42, —C(═O)OR42, —OR42, —SR42, —SOR42, —SO2R42, —N(R43)R42, —C(═O)—N(R43)R42, —N(R43)—C(═O)R42, —O—C(═O)—N(R3)R42 and —SO2—N(R43)R42; R42 is each independently selected from the group consisting of H, (C1-6)alkyl, (C3-7)cycloalkyl, —(C1-6)alkyl-aryl, —(C1-6)alkyl-heterocyclyl, —(C1-6)alkyl-heteroaryl, aryl, heterocyclyl and heteroaryl, wherein each said alkyl, cycloalkyl, aryl, heterocyclyl and heteroaryl, either alone or in combination with another radical, is optionally substituted with 1 to 3 substituents each independently selected from the group consisting of: halo, cyano, OH, —COOH, —O—(C1-6)alkyl, (C3-7)cycloalkyl, (C1-6)haloalkyl, —C(═O)—(C1-6)alkyl, —SO2NH2, —SO2—NH(C1-6)alkyl, —SO2—N((C1-6)alkyl)2, —SO2(C1-6)alkyl, —C(═O)—NH2, —C(═O)—NH(C1-6)alkyl, —C(═O)—N((C1-6)alkyl)2, —NH2, —NH(C1-6)alkyl, —N((C1-6)alkyl)2, —NH—C(═O)(C1-6)alkyl and (C1-6)alkyl optionally mono- or di-substituted with OH or —O—(C1-6)alkyl; R43 is H or (C1-6)alkyl; R5 and R6 are each independently H or (C1-6)alkyl optionally mono- or di-substituted with —O—(C1-6)alkyl, NH2, NH(C1-6)alkyl or N((C1-6)alkyl)2; or R5 and R6, together with the carbon to which they are attached, are linked to form a (C3-7)cycloalkyl group or a 3- to 7-membered heterocyclyl, said cycloalkyl and heterocyclyl being optionally mono- or di-substituted with —(C1-6)alkyl; and n is 1.
地址 Ingelheim am Rhein DE