发明名称 COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO KIT AND PDFGR
摘要 Compounds and compositions useful for treating disorders related to KIT and PDGFR are described herein.
申请公布号 US2017022206(A1) 申请公布日期 2017.01.26
申请号 US201615217503 申请日期 2016.07.22
申请人 BLUEPRINT MEDICINES CORPORATION 发明人 Hodous Brian L.;Wilson Kevin J.;Zhang Yulian
分类号 C07D487/04;A61K45/06;A61K31/53 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: W is selected from hydrogen andwherein Ring A is selected from monocyclic or bicyclic aryl, monocyclic or bicyclic heteroaryl, cycloalkyl and heterocyclyl; Z is selected from C1-C6 alkyl, cycloalkyl, monocyclic or bicyclic aryl, monocyclic or bicyclic aralkyl, monocyclic or bicyclic heteroaryl, monocyclic or bicyclic heterocyclyl, and monocyclic or bicyclic heterocyclylalkyl; wherein each of C1-C6 alkyl, cycloalkyl, monocyclic or bicyclic aryl, monocyclic or bicyclic aralkyl, monocyclic or bicyclic heteroaryl, monocyclic or bicyclic heterocyclyl, monocyclic and bicyclic heterocyclylalkyl is independently substituted with 0-5 occurrences of RC; L is selected from —N(R1)—C(O)—, —N(R1)C(O)N(R1)—, —N(R1)C(O)N(R1)—(C1-C6 alkylene)-, N(R1)—(C1-C6 alkylene)-, —N(R1)—C(O)—(C1-C6 alkylene)-, —N(R1)—S(O)2, and —N(R1)—S(O)2—(C1-C6 alkylene)-; wherein each alkylene is independently substituted with 0-5 occurrences of R2; each RA is independently selected from C1-C6 alkyl, C1-C6 alkoxy, halo, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, C1-C6 heteroalkyl, —N(R1)(R1), cyano, and —OR1; each RB is independently selected from hydrogen, C1-C6 alkyl, C1-C6 cycloalkyl, hydroxyl, halo, C1-C6 alkoxy, C1-C6 haloalkyl, —N(R1)(R1), and cyano; each RC is independently selected from C1-C6 alkyl, C1-C6 alkynyl, halo, C1-C6 heteroalkyl, C1-C6 haloalkyl, C1-C6 haloalkoxy, C1-C6 hydroxyalkyl, cycloalkyl, monocyclic or bicyclic aryl, monocyclic or bicyclic aryloxy, monocyclic or bicyclic aralkyl, monocyclic or bicyclic heterocyclyl, monocyclic or bicyclic heterocyclylalkyl, nitro, cyano, —C(O)R1, —OC(O)R1, —C(O)OR1, —SR1, —S(O)2R1, —S(O)2—N(R1)(R1), —(C1-C6 alkylene)-S(O)2—N(R1)(R1), —N(R1)(R1), —C(O)—N(R1)(R1), —N(R1)(R1)—C(O)R1, —(C1-C6 alkylene)-N(R1)—C(O)R1, —NR1S(O)2R1, —P(O)(R1)(R1), and —OR1; wherein each of heteroalkyl, haloalkyl, haloalkoxy, alkyl, alkynyl, cycloalkyl, aryl, aryloxy, aralkyl, heterocyclyl, heterocyclylalkyl is independently substituted with 0-5 occurrences of Ra; or 2 RC together with the carbon atom(s) to which they are attached form a cycloalkyl or heterocyclyl ring substituted with 0-5 occurrences of Ra; each RD is independently selected from halo, C1-C6 alkyl, C1-C6 cycloalkyl, hydroxyl, halo, C1-C6 alkoxy, C1-C6 haloalkyl, —N(R2)(R2), and cyano; each R1 is independently selected from hydrogen, hydroxyl, halo, thiol, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, C1-C6 thioalkyl, —NR″R″, cycloalkyl, cycloalkylalkyl, heterocyclyl, and heterocyclylalkyl, wherein each of C1-C6 alkyl, cycloalkyl and heterocyclyl is independently substituted with 0-5 occurrences of Rb; or 2 R1 together with the atom(s) to which they are attached form a cycloalkyl or heterocyclyl ring; each R2 is independently selected from hydroxyl, C1-C6 alkyl, C1-C6 alkoxyl, —NR′R′; or 2 R2 together with the atom(s) to which they are attached form a cycloalkyl or heterocyclyl ring; each Ra and Rb is independently selected from hydrogen, halo, cyano, hydroxyl, C1-C6 alkoxyl, —C(O)R″, C(O)OR′, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 heteroalkyl, C1-C6 hydroxyalkyl, —NR′R′, and cycloalkyl, wherein cycloalkyl is substituted with 0-5 occurrences of R′; each R′ is independently selected from hydrogen, C1-C6 alkyl, C1-C6 alkoxyl, C1-C6 heteroalkyl, halo, hydroxyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, cycloalkyl and cyano; or 2R′ together with the atom(s) to which they are attached form a cycloalkyl or heterocyclyl ring; each R″ is hydrogen, C1-C6 alkyl, —C(O)—C1-C6 alkyl, —C(O)—NR′R′; or —C(S)—NR′R′; and each q and r is independently 0, 1, 2, 3, or 4.
地址 Cambridge MA US