发明名称 PIM KINASE INHIBITORS AND METHODS OF THEIR USE
摘要 New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
申请公布号 US2014249135(A1) 申请公布日期 2014.09.04
申请号 US201414273595 申请日期 2014.05.09
申请人 Burger Matthew;Lindvall Mika;Han Wooseok;Lan Jiong;Nishiguchi Gisele;Shafer Cynthia;Bellamacina Cornelia;Huh Kay;Atallah Gordana;McBride Christopher;Antonios-McCrea, JR. William;Zavorotinskaya Tatiana;Walter Annette;Garcia Pablo Dominguez 发明人 Burger Matthew;Lindvall Mika;Han Wooseok;Lan Jiong;Nishiguchi Gisele;Shafer Cynthia;Bellamacina Cornelia;Huh Kay;Atallah Gordana;McBride Christopher;Antonios-McCrea, JR. William;Zavorotinskaya Tatiana;Walter Annette;Garcia Pablo Dominguez
分类号 C07D401/12;A61K31/55;A61K31/497;A61K31/4545;A61K31/444;C07D491/113;C07D403/12;A61K31/506;C07D241/28;C07D401/14;C07D405/14;C07D409/14;C07D417/14;C07D497/04;C07D403/14;A61K31/553 主分类号 C07D401/12
代理机构 代理人
主权项 1. A compound of Formula I, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof,wherein, X1, X2, X3 and X4 are CR2 or X3 and X1 are N and X2 is CR2; Y is substituted or unsubstituted amino, alkoxy, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; Z1, Z2 and Z3 are independently selected from CR2 and N; provided that not more than one of Z1, Z2 and Z3 can be N; R1 is selected from the group consisting of hydrogen, halo, alkyl, cycloalkyl, —CN, —NO2, and —NHR3; each R2 is independently selected from the group consisting of hydrogen, halo, hydroxyl, nitro, cyano, SO3H and substituted or unsubstituted alkyl, alkenyl, alkynyl, alkoxy, amino, aminocarbonyl, aminothiocarbonyl, aminocarbonylamino, aminothiocarbonylamino, aminocarbonyloxy, aminosulfonyl, aminosulfonyloxy, aminosulfonylamino, amidino, carboxyl, carboxyl ester, (carboxyl ester)amino, (carboxyl ester)oxy, sulfonyl, sulfonyloxy, thioacyl, thiol, alkylthio, aryl, heteroaryl, cycloalkyl, hetero cycloalkyl, partially saturated cycloalkyl, aryloxy, heteroaryloxy, heterocyclyloxy, cycloalkyloxy, acyl, acylamino and acyloxy; R3 is selected from the group consisting of hydrogen, —CO—R4 and substituted or unsubstituted alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl; and R4 is selected from the group consisting of alkyl, substituted alkyl, alkoxy, substituted alkoxy, amino, substituted amino, and alkylamino.
地址 Emeryville CA US