发明名称 Enhancer of zeste homolog 2 inhibitors
摘要 This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.;
申请公布号 US9562041(B2) 申请公布日期 2017.02.07
申请号 US201314400896 申请日期 2013.05.15
申请人 GlaxoSmithKline LLC 发明人 Burgess Joelle Lorraine;Knight Steven David
分类号 C07D211/86;C07D417/12;C07D213/64;C07D401/12 主分类号 C07D211/86
代理机构 代理人 Fitch Duke M.;Lutomski Kathryn A.;Gimmi Edward R.
主权项 1. A compound according to Formula (I): wherein: R1 is methyl; R2 is methyl; R3 is hydrogen; R4 is methyl; R5 is —NRaRb; R6 is phenyl, wherein said phenyl is optionally substituted by —(C1-C6)alkyl(Rc); Rc is —NRaRb; and Ra and Rb are each independently hydrogen, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C10)cycloalkyl, (C5-C8)cycloalkenyl, heterocycloalkyl, or aryl, wherein said (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or aryl group is optionally substituted by 1, 2 or 3 groups independently selected from the group consisting of halo, hydroxyl, (C1-C4)alkoxy, amino, (C1-C4)alkylamino, —N((C1-C4)alkyl)2, —CO2H, —CO2(C1-C4)alkyl, —CONH2, —CONH(C1-C4)alkyl, —CON((C1-C4)alkyl)2, —SO2(C1-C4)alkyl, —SO2NH2, —SO2NH(C1-C4)alkyl, and —SO2N((C1-C4)alkyl)2; and wherein said heterocycloalkyl is selected from the group consisting of pyrrolidinyl, tetrahydrofuranyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, and tetrahydropyranyl; or Ra and Rb taken together with the nitrogen to which they are attached represent a 5 or 6 membered saturated ring, optionally containing an additional heteroatom selected from oxygen, nitrogen, and sulfur, wherein said ring is optionally substituted by 1, 2 or 3 groups independently selected from the group consisting of (C1-C4)alkyl, (C1-C4)haloalkyl, amino, (C1-C4)alkylamino, ((C1-C4)alkyl)((C1-C4)alkyl)amino, hydroxyl, oxo, (C1-C4)alkoxy, and (C1-C4)alkoxy(C1-C4)alkyl; or a pharmaceutically acceptable salt thereof.
地址 Wilmington, New Castle DE US