发明名称 Tyrosine kinase inhibitors containing a zinc binding moiety
摘要 The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
申请公布号 US9169244(B2) 申请公布日期 2015.10.27
申请号 US201313845885 申请日期 2013.03.18
申请人 Curis, Inc. 发明人 Cai Xiong;Qian Changgeng;Gould Stephen;Zhai Haixiao
分类号 A61K31/506;C07D419/12;C07D417/12;C07D417/14;C07D419/14 主分类号 A61K31/506
代理机构 Elmore Patent Law Group, P.C. 代理人 Elmore Patent Law Group, P.C. ;Harlan Edgar W.;Elmore, Esq. Carolyn S.
主权项 1. A method of treating a cancer which is susceptible to inhibition of one or more of Src, Bcr-Abl and HDAC, in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I):or a pharmaceutically acceptable salt or solvate thereof, wherein Cz is pyrimidine or substituted pyrimidine; Ar is phenyl or substituted phenyl; X3 is NH; Z2 is S; Y2 is N; R21 is hydrogen; B is a direct bond or straight- or branched-, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkylarylalkyl, alkylarylalkenyl, alkylarylalkynyl, alkenylarylalkyl, alkenylarylalkenyl, alkenylarylalkynyl, alkynylarylalkyl, alkynylarylalkenyl, alkynylarylalkynyl, alkylheteroarylalkyl, alkylheteroarylalkenyl, alkylheteroarylalkynyl, alkenylheteroarylalkyl, alkenylheteroarylalkenyl, alkenylheteroarylalkynyl, alkynylheteroarylalkyl, alkynylheteroarylalkenyl, alkynylheteroarylalkynyl, alkylheterocyclylalkyl, alkylheterocyclylalkenyl, alkylheterocycloalkynyl, alkenylheterocyclylalkyl, alkenylheterocyclylalkenyl, alkenylheterocyclylalkynyl, alkynylheterocyclylalkyl, alkynylheterocyclylalkenyl, alkynylheterocyclylalkynyl, alkylaryl, alkenylaryl, alkynylaryl, alkylheteroaryl, alkenylheteroaryl, or alkynylhereroaryl, in which one or more methylenes can be interrupted or terminated by O, S, S(O), SO2, N(R8), C(O), substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic; R8 is hydrogen, acyl, aliphatic or substituted aliphatic; C iswhere W is O; Y is absent; Z is N; R7 is absent; and R9 is OR′, wherein R′ is hydrogen.
地址 Lexington MA US