发明名称 Pyrazolopyrimidine compounds for the treatment of cancer
摘要 Compound of Formula (I): are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof in the treatment of cancer.;
申请公布号 US9290499(B2) 申请公布日期 2016.03.22
申请号 US201113641729 申请日期 2011.05.12
申请人 The University of North Carolina at Chapel Hill 发明人 Wang Xiaodong;Liu Jing;Yang Chao;Zhaug Weihe;Frye Stephen;Kireev Dmitri
分类号 C07D487/04;A61K31/519;A61K31/5377;A61K31/551;A61P35/00;A61P35/02 主分类号 C07D487/04
代理机构 Myers Bigel & Sibley, P.A. 代理人 Myers Bigel & Sibley, P.A.
主权项 1. A compound of Formula I:wherein: R1 is aryl, wherein the aryl is unsubstituted or substituted from 1 to 3 times with halo, alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclo, heterocycloalkyl, hydroxyl, alkoxy, alkenyloxy, alkynyloxy, haloalkoxy, cycloalkoxy, cycloalkylalkyloxy, aryloxy, arylalkyloxy, heterocyclooxy, heterocyclolalkyloxy, mercapto, alkyl-S(O)m, haloalkyl-S(O)m, alkenyl-S(O)m, alkynyl-S(O)m, cycloalkyl-S(O)m, cycloalkylalkyl-S(O)m, aryl-S(O)m, arylalkyl-S(O)m, heterocyclo-S(O)m, heterocycloalkyl-S(O)m, amino, carboxy, alkylamino, alkenylamino, alkynylamino, haloalkylamino, cycloalkylamino, cycloalkylalkylamino, arylamino, arylalkylamino, heterocycloamino, heterocycloalkylamino, disubstituted-amino, acylamino, acyloxy, ester, amide, sulfonamide, urea, alkoxyacylamino, aminoacyloxy, nitro or cyano where m=0, 1, 2 or 3; or R1 is heteroaryl, wherein the heteroaryl is unsubstituted or substituted from 1 to 3 times with halo, alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclo, heterocycloalkyl, hydroxyl, alkoxy, alkenyloxy, alkynyloxy, haloalkoxy, cycloalkoxy, cycloalkylalkyloxy, aryloxy, arylalkyloxy, heterocyclooxy, heterocyclolalkyloxy, mercapto, alkyl-S(O)m, haloalkyl-S(O)m, alkenyl-S(O)m, alkynyl-S(O)m, cycloalkyl-S(O)m, cycloalkylalkyl-S(O)m, aryl-S(O)m, arylalkyl-S(O)m, heterocyclo-S(O)m, heterocycloalkyl-S(O)m, amino, alkylamino, alkenylamino, alkynylamino, haloalkylamino, cycloalkylamino, cycloalkylalkylamino, arylamino, arylalkylamino, heterocycloamino, heterocycloalkylamino, disubstituted-amino, acylamino, acyloxy, ester, amide, sulfonamide, urea, alkoxyacylamino, aminoacyloxy, nitro or cyano where m=0, 1, 2 or 3; R2 is —R5R6, where R5 is a covalent bond or C1 to C3 alkyl and R6 is cycloalkyl, wherein R6 is optionally substituted from one to two times with independently selected polar groups; R3 is —NR7R8, where R7 and R8 are each independently selected from H, alkyl, arylalkyl, and alkoxyalkyl; wherein the alkyl, arylalkyl, or alkoxyalkyl is unsubstituted or substituted from 1 to 3 times with alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, aryl, or heteroaryl; and R4 is H, loweralkyl, halo, or loweralkoxy;or a pharmaceutically acceptable salt thereof.
地址 Chapel Hill NC US