发明名称 PIM kinase inhibitors and methods of their use
摘要 The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer.;
申请公布号 US8829193(B2) 申请公布日期 2014.09.09
申请号 US201213447988 申请日期 2012.04.16
申请人 Novartis AG 发明人 Burger Matthew;Lan Jiong;Lindvall Mika;Nishiguchi Gisele;Tetalman Michelle
分类号 C07D417/14;A61K31/4545;A61K31/4439;C07D417/12 主分类号 C07D417/14
代理机构 代理人 Johnson Stephen
主权项 1. A method for treating multiple myeloma comprising administering to a patient in need of such treatment an effective amount of a compound of Formula II: or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein: R1 is selected from —NH—CO-alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; X represents CH or N; R2a is selected from —H, —OH, alkyl, alkoxy, haloalkyl, aminoalkyl, hydroxyalkyl, halo, amino and benzoate; R2b is selected from —H and alkyl; R3 is selected from H, OH, alkyl, alkoxy and halo; R4a is selected from —OH, alkyl, alkoxy, haloalkyl, aminoalkyl, hydroxyalkyl, halo and amino; and R4b is selected from H, alkyl and halo.
地址 Basel CH