发明名称 COMBINATION THERAPY FOR TREATING CANCER
摘要 The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents, particularly anticancer agents such as prednisone, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.
申请公布号 US2015051163(A1) 申请公布日期 2015.02.19
申请号 US201314394463 申请日期 2013.04.12
申请人 EPIZYME, INC. 发明人 Keilhack Heike;Knutson Sarah Kathleen;Kuntz Kevin Wayne
分类号 C07D405/12;A61K31/573;A61K31/4745;A61K31/704;A61K31/5377;A61K31/675 主分类号 C07D405/12
代理机构 代理人
主权项 1. A composition comprising a compound of Formula (IIa):or a pharmaceutically acceptable salt thereof, and one or more other therapeutic agents, wherein each of Ra and Rb, independently, is H or C1-C6 alkyl optionally substituted with one or more -Q3-T3, in which Q3 is a bond or unsubstituted or substituted C1-C3 alkyl linker, and T3 is H, halo, 4 to 7-membered heterocycloalkyl, C1-C3 alkyl, ORd, COORd, —S(O)2Rd, or —NRdRe, in which each of Rd and Re is independently H or C1-C6 alkyl, or -Q3T3 is oxo; R7 is isopropyl or C1-C6 alkyl, C3-C8 cycloalkyl, piperidinyl, tetrahydropyran, tetrahydro-2H-thiopyranyl, cyclopentyl, or cyclohexyl, or 4 to 12-membered heterocycloalkyl, each optionally substituted with one or more -Q5-T5, in which Q5 is a bond, C(O), C(O)NRk, NRkC(O), S(O)2, or C1-C3 alkyl linker, Rk being H or C1-C6 alkyl, and T5 is H, halo, C1-C6 alkyl, hydroxyl, cyano, C1-C6 alkoxyl, amino, mono-C1-C6 alkylamino, di-C1-C6 alkylamino, C3-C8 cycloalkyl, C6-C10 aryl, 4 to 12-membered heterocycloalkyl, 5- or 6-membered heteroaryl, or S(O)qRq in which q is 0, 1, or 2 and Rq is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C6-C10 aryl, 4 to 12-membered heterocycloalkyl, or 5- or 6-membered heteroaryl, and T5 is optionally substituted with one or more substituents selected from the group consisting of halo, C1-C6 alkyl, hydroxyl, cyano, C1-C6 alkoxyl, amino, mono-C1-C6 alkylamino, di-C1-C6 alkylamino, C3-C8 cycloalkyl, C6-C10 aryl, 4 to 12-membered heterocycloalkyl, and 5- or 6-membered heteroaryl except when T5 is H, halo, hydroxyl, or cyano; or -Q5-T5 is oxo; and R8 is H, methyl, or ethyl.
地址 CAMBRIDGE MA US