发明名称 SMYD2 inhibitors
摘要 The present disclosure generally relates to compounds having cellular anti-proliferative activities, and more particularly relates to compounds which inhibit the activity of human SMYD2, a SET and MYND domain-containing protein lysine methyltransferase.
申请公布号 US9598381(B2) 申请公布日期 2017.03.21
申请号 US201514812726 申请日期 2015.07.29
申请人 AbbVie Inc. 发明人 Chiang Gary G.;Pappano William N.;Sweis Ramzi F.;Wang Zhi
分类号 C07D209/40;C07D265/36;C07D295/13;C07D487/04;C07D401/12;C07D471/04;C07C255/58 主分类号 C07D209/40
代理机构 代理人 Sun Changxia
主权项 1. A compound having a structure of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: each of R1, R2, R3, R4, R5, and R6 are independently hydrogen or C1-6 alkyl; x has a value from 0 to 1; y has a value from 0 to 3; R7 is a C4-C6 cycloalkyl; R8 is —OR9 or —NHR10; R9 is a C1-10 alkyl; R10 is a C1-2 alkyl substituted with a phenyl, wherein the phenyl is optionally further substituted with halogen; and, (i) R11 and R12 are taken together with the nitrogen atom to which they are bound to form an optionally substituted heterocyclic ring having a structure: wherein Rx is selected from hydrogen and methoxypyridinyl, and Ry is selected from hydrogen and indolinyl; or alternatively, (ii) one of R11 and R12 is hydrogen, and the other is selected from: (a) a pyrazolopyrimidinyl ring having a structure: and being optionally substituted with one or more C1-5 alkyl substituents; and,(b) a C1-3 substituted alkyl or a C1-3 substituted hydoxyalkyl, wherein said substituent is selected from the group consisting of piperidinyl, pyrrolidinyl, cyanophenyl, methylindolizinyl, and a moiety having a structure: wherein R13, R14, and R15 are each independently selected from hydrogen, halogen, hydroxyl, trifluoromethyl, cyano, carboxyl, C1-6 alkyl, C1-6 alkoxy, and C1-6 alkylcarbonyl; provided that if one of R11 and R12 is C1-3 substituted alkyl and R15 is hydroxyl, then R7 comprises a C4 or C5 unsubstituted cycloalkyl, or R8 is —OR9, or R8 is —NHR10, wherein R10 is methyl substituted with a phenyl, optionally further substituted with a halogen.
地址 North Chicago IL US