1338718-21-0Relevant articles and documents
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma
Wang, Xiaojing,Blackaby, Wesley,Allen, Vivienne,Chan, Grace Ka Yan,Chang, Jae H.,Chiang, Po-Chang,Diène, Coura,Drummond, Jason,Do, Steven,Fan, Eric,Harstad, Eric B.,Hodges, Alastair,Hu, Huiyong,Jia, Wei,Kofie, William,Kolesnikov, Aleksandr,Lyssikatos, Joseph P.,Ly, Justin,Matteucci, Mizio,Moffat, John G.,Munugalavadla, Veerendra,Murray, Jeremy,Nash, David,Noland, Cameron L.,Del Rosario, Geoff,Ross, Leanne,Rouse, Craig,Sharpe, Andrew,Slaga, Dionysos,Sun, Minghua,Tsui, Vickie,Wallweber, Heidi,Yu, Shang-Fan,Ebens, Allen J.
supporting information, (2019/03/07)
Pim kinases have been targets of interest for a number of therapeutic areas. Evidence of durable single-agent efficacy in human clinical trials validated Pim kinase inhibition as a promising therapeutic approach for multiple myeloma patients. Here, we report the compound optimization leading to GDC-0339 (16), a potent, orally bioavailable, and well tolerated pan-Pim kinase inhibitor that proved efficacious in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models and has been evaluated as an early development candidate.
PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE
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Page/Page column 115, (2011/10/19)
Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
