发明名称 MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
摘要 Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
申请公布号 US2015315148(A1) 申请公布日期 2015.11.05
申请号 US201514707874 申请日期 2015.05.08
申请人 Constellation Pharmaceuticals, Inc. 发明人 Albrecht Brian K.;Audia James Edmund;Gagnon Alexandre;Harmange Jean-Christophe;Nasveschuk Christopher G.
分类号 C07D213/64;C07D213/81;C07D401/12;C07D405/12 主分类号 C07D213/64
代理机构 代理人
主权项 1. A compound having structural Formula I: or a pharmaceutically acceptable salt thereof, wherein: Z is ═C(R2)—; each of X1, X2 and X3 is independently selected from ═N— and ═C(R3)—; X4 is selected from ═N—, —C(═O)— and ═C(R3)—; X5 is no more than two of X1, X2, X3, X4, and X5 are ═N— or each R1 and R2 is independently selected from hydrogen, halo, —OH, —CN, C1-C4 alkyl, —O—(C1-C4 alkyl), N(R7)2, —(C0-C4 alkylene)-aryl, —(C0-C4 alkylene)-heteroaryl, —(C0-C4 alkylene)-heterocyclyl, —(C0-C4 alkylene)-carbocyclyl, —O—(C0-C4 alkylene)-aryl, —O—(C0-C4 alkylene)-heteroaryl, —O—(C0-C4 alkylene)-heterocyclyl, and —O—(C0-C4 alkylene)-carbocyclyl; each R3 is independently selected from hydrogen, halo, —OH, —CN, C1-C4 alkyl, C2-C4 alkenyl or alkynyl, —O—(C1-C4 alkyl), N(R7)2, —(C0-C4 alkylene)-aryl, —(C0-C4 alkylene)-heteroaryl, —(C0-C4 alkylene)-heterocyclyl, —(C0-C4 alkylene)-carbocyclyl, —O—(C0-C4 alkylene)-aryl, —O—(C0-C4 alkylene)-heteroaryl, —O—(C0-C4 alkylene)-heterocyclyl, —O—(C0-C4 alkylene)-carbocyclyl, —C(O)OR9, —C(O)N(R9)2, —S(O)R8, —S(O)2R8 and —S(O)2N(R9)2; R4—H is selected from hydrogen and CH3; R5—H is selected from —CH3, —CH(CH3)2, —(CH2)2CH3, —CH2CH3, —OCH2CH3, —OCH(CH3)2, —OCH3, —OCH2CH(CH3)2, —OH, —CH2OH, —(CH2)2OH, —(CH2)2—O—CH3, —NH—C(═O)—CH3, —(CH2)2—NH—CH3, —(CH2)2—NH—C(═O)—CH3, —CH2—C(═O)NH2, —NH—S(═O)2—CH3, and —NH—C(═O)—NH—CH3 R6 is hydrogen or methyl; each R7 is independently selected from hydrogen, —(C0-C4 alkylene)-R9, —(C2-C4 alkylene)-O—R9, C2-C4 haloalkyl, —S(O)2—R8, —C(═O)—R8, —C(═O)—N(R9)(R9), —(C2-C4 alkylene)-O—C(═O)—R8 and —(C0-C4 alkylene)-C(═O)—O—R9; or two R7 are taken together with the nitrogen atom to which they are commonly bound to form an optionally substituted heterocyclyl or heteroaryl; R8 is selected from C1-C4 alkyl, aryl, heteroaryl, carbocyclyl and heterocyclyl; each R9 is independently selected from hydrogen and R8; and represents a single or double bond; wherein unless otherwise designated any alkyl, alkylene, alkenyl, alkenylene, alkynyl, alkynylene, aryl, heteroaryl, heterocyclyl or carbocyclyl portion of the compound is optionally substituted.
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