发明名称 Heterocyclic compounds and uses thereof
摘要 Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
申请公布号 US9388183(B2) 申请公布日期 2016.07.12
申请号 US201414512262 申请日期 2014.10.10
申请人 Infinity Pharmaceuticals, Inc. 发明人 Ren Pingda;Liu Yi;Li Liansheng;Chan Katrina;Wilson Troy Edward;Castro Alfredo C.;Evans Catherine A.;Snyder Daniel A.
分类号 A61K31/519;C07D471/04;C07D487/04;C07D473/34;C07D401/12;C07D513/04;C07D519/00;C07D413/14 主分类号 A61K31/519
代理机构 Jones Day 代理人 Jones Day
主权项 1. A compound of Formula (Ia):or a pharmaceutically acceptable form thereof, wherein: W5 is N4 or CR4; R4 is hydrogen, alkyl, haloalkyl, heteroalkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkoxy, heterocycloalkyloxy, amido, amino, acyl, acyloxy, alkoxycarbonyl, sulfonamido, thio, sulfoxide, sulfone, halo, cyano, hydroxy, nitro, phosphate, urea, carbonate, or NR′R″ wherein R′ and R″ are taken together with nitrogen to form a cyclic moiety; Cy is aryl or heteroaryl substituted by 0-4 occurrences of R3; R1 is -(L)n-R1′; each L is independently absent, alkylene, or —O—; R1′ is —(C═O)—NRa1Ra2; Ra1 and Ra2 are each independently hydrogen, alkyl, heteroalkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkoxy, heterocycloalkyloxy, amido, amino, acyl, acyloxy, alkoxycarbonyl, sulfonamido, thio, sulfoxide, sulfone, halo, cyano, hydroxy, nitro, phosphate, urea, carbonate, or Ra1 and Ra2 are taken together with nitrogen to form a cyclic moiety; R2 is hydrogen, alkyl, cycloalkyl, heterocycloalkyl, heteroalkyl, aryl, or heteroaryl; each R3 is independently alkyl, heteroalkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkoxy, heterocycloalkyloxy, amido, amino, acyl, acyloxy, alkoxycarbonyl, sulfonamido, thio, sulfoxide, sulfone, halo, cyano, hydroxy, nitro, phosphate, urea, carbonate, or NR′R″ wherein R′ and R″ are taken together with nitrogen to form a cyclic moiety; X is absent or is —(CH(R10))z—; Y is absent, —O—, —S—, —S(═O)—, —S(═O)2—, —N(R9)—, —C(═O)—, —(CHR10)z—, —C(═O)—, —N(R9)—C(═O)13 , —C(═O)—N(R9)—, —N(R9)—C(═O)NH—, —N(R9)C(R10 )2—, —C(═O)—N(R9)—(CHR10)z—, or —P(═O)R2—; each z is an integer of 1, 2, 3, or 4; n is an integer of 0, 1, 2, 3, or 4; each R9 is independently hydrogen, alkyl, cycloalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroalkyl, aryl, or heteroaryl; Wd is  wherein Wd is optionally substituted with one or more Rb, R11, R12, and R13; each Rbis independently hydrogen, halo, phosphate, urea, carbonate, alkyl, alkenyl, alkynyl, cycloalkyl, heteroalkyl, or heterocycloalkyl; and each R10, R11, R12, and R13 is independently hydrogen, alkyl, heteroalkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkoxy, heterocyclyloxy, amido, amino, acyl, acyloxy, alkoxycarbonyl, sulfonamido, halo, haloalkyl, cyano, hydroxyl, nitro, phosphate, urea, carbonate, or NR′R″ wherein R′ and R″ are taken together with nitrogen to form a cyclic moiety.
地址 Cambridge MA US