发明名称 TRIAZOLOPYRIMIDINE COMPOUNDS AND USES THEREOF
摘要 A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder:;;wherein R1, R2, R3, R4, R5, and n are as defined herein.
申请公布号 US2016176882(A1) 申请公布日期 2016.06.23
申请号 US201514977273 申请日期 2015.12.21
申请人 CHAN Ho Man;GU Xiang-Ju Justin;HUANG Ying;LI Ling;MI Yuan;QI Wei;SENDZIK Martin;SUN Yongfeng;WANG Long;YU Zhengtian;ZHANG Hailong;ZHANG Ji Yue (Jeff);ZHANG Man;ZHANG Qiong;ZHAO Kehao 发明人 CHAN Ho Man;GU Xiang-Ju Justin;HUANG Ying;LI Ling;MI Yuan;QI Wei;SENDZIK Martin;SUN Yongfeng;WANG Long;YU Zhengtian;ZHANG Hailong;ZHANG Ji Yue (Jeff);ZHANG Man;ZHANG Qiong;ZHAO Kehao
分类号 C07D487/04;A61K31/551;A61K31/5377;A61K31/541;A61K31/519;A61K45/06 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of Formula (I):or a pharmaceutically acceptable salt thereof, wherein: is a single bond or a double bond; R1 and R2 are independently H or halogen; R3 is independently selected from: halogen, phenyl, and a 5- to 6-membered heteroaryl comprising carbon atoms and 1-4 heteroatoms selected from N, NRa, O, and S(O)p; wherein said phenyl and heteroaryl are substituted with 0-3 R3A; each R3A is independently selected from: halogen, CN, —(O)m—(C1-C6 alkyl substituted with 0-1 R3B), C1-C6 haloalkyl, C1-C6 haloalkoxy, R3C, —OR3C, —C(═O)R3D, NR3ER3F, —C(═O)NR3ER3F, —NHC(═O)R3D, —S(═O)2R3D, —S(═O)2NR3ER3F, —NHS(═O)2(C1-C4 alkyl), and —CR3CR3ER3G; R3B is independently selected from: OH, NReRf, C1-C4 alkoxy, —C(═O)NReRf, —S(═O)2(C1-C4 alkyl), —NHC(═O)(C1-C4 alkyl), and a 5- to 6-membered heterocycloalkyl comprising carbon atoms and 1-2 heteroatoms selected from N, NRa, O, and S(O)p; wherein said heterocycloalkyl is substituted with 0-2 Rc; each R3C is independently selected from: C3-C6 cycloalkyl, phenyl, and a 4- to 7-membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, NRa, O, and S(O)p; wherein each moiety is substituted with 0-2 Rc; each R3D is independently selected from: C1-C4 alkyl and R3C; R3E and R3G are, at each occurrence, independently selected from: H and C1-C4 alkyl; each R3F is independently selected from: H and C1-C4 alkyl substituted with 0-1 Rd; R4 is independently selected from: H, halogen and C1-C4 alkyl; R5 is independently selected from OH and C1-C4 alkyl; each Ra is independently selected from: H, →O, C1-C4 alkyl substituted with 0-1 Rb, —C(═O)H, —C(═O)(C1-C4 alkyl), —CO2(C1-C4 alkyl), C3-C6 cycloalkyl, and benzyl; Rb is independently selected from: halogen, OH and C1-C4 alkoxy; each Rc is independently selected from: ═O, halogen, OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy; Rd is independently selected from: OH and NReRf; Re and Rf are, at each occurrence, independently selected from: H and C1-C4 alkyl; each p is independently selected from 0, 1 and 2; and m and n are, at each occurrence, independently selected from 0 and 1.
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