60230-33-3Relevant academic research and scientific papers
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.
Identification of N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a potent and selective proviral insertion site of Moloney murine leukemia (PIM) 1, 2, and 3 kinase inhibitor in clinical trials for hematological malignancies
Burger, Matthew T.,Nishiguchi, Gisele,Han, Wooseok,Lan, Jiong,Simmons, Robert,Atallah, Gordana,Ding, Yu,Tamez, Victoriano,Zhang, Yanchen,Mathur, Michelle,Muller, Kristine,Bellamacina, Cornelia,Lindvall, Mika K.,Zang, Richard,Huh, Kay,Feucht, Paul,Zavorotinskaya, Tatiana,Dai, Yumin,Basham, Steve,Chan, Julie,Ginn, Elaine,Aycinena, Alex,Holash, Jocelyn,Castillo, Joseph,Langowski, John L.,Wang, Yingyun,Chen, Min Y.,Lambert, Amy,Fritsch, Christine,Kauffmann, Audry,Pfister, Estelle,Vanasse, K. Gary,Garcia, Pablo D.
, p. 8373 - 8386 (2015/11/25)
Pan proviral insertion site of Moloney murine leukemia (PIM) 1, 2, and 3 kinase inhibitors have recently begun to be tested in humans to assess whether pan PIM kinase inhibition may provide benefit to cancer patients. Herein, the synthesis, in vitro activity, in vivo activity in an acute myeloid leukemia xenograft model, and preclinical profile of the potent and selective pan PIM kinase inhibitor compound 8 (PIM447) are described. Starting from the reported aminopiperidyl pan PIM kinase inhibitor compound 3, a strategy to improve the microsomal stability was pursued resulting in the identification of potent aminocyclohexyl pan PIM inhibitors with high metabolic stability. From this aminocyclohexyl series, compound 8 entered the clinic in 2012 in multiple myeloma patients and is currently in several phase 1 trials of cancer patients with hematological malignancies.
CYCLIC ETHER COMPOUNDS USEFUL AS KINASE INHIBITORS
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Page/Page column 60, (2012/02/01)
The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof, as further described herein. Also provided are formulations comprising compounds of formula I, and a method to use such compounds for treating a disease or condition mediated by Provirus Integration of Maloney Maloney Kinase (PIM Kinase), GSK3, PKC, KDR, PDGFRa, FGFR3, FLT3, or cABL.
Pim kinase inhibitors and methods of their use
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Page/Page column 44, (2010/09/05)
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.
PIM KINASE INHIBITORS AND METHODS OF THEIR USE
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Page/Page column 103, (2009/10/22)
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 pharmac
A mild and versatile synthesis of thioamides
Mahammed,Jayashankara,Premsai Rai,Mohana Raju,Arunachalam
experimental part, p. 2338 - 2340 (2009/12/08)
Aliphatic and aromatic nitriles react with thioacetic acid in the presence of calcium hydride to give the corresponding thioamides in good to excellent yields. The examples studied include haloaryl nitriles in which the halogen is facile towards SNAr reactions under other conditions. Georg Thieme Verlag Stuttgart.
3-(substituted phenyl)-5-(substituted heterocyclyl)-1,2,4-triazole compounds
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, (2008/06/13)
3-(Substituted phenyl)-5-(substituted heterocyclyl)-1,2,4-triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.
3-(substituted phenyl)-5-(thienyl or furyl)-1, 2, 4-triazole compounds
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, (2008/06/13)
3-(Substituted phenyl)-5-(thienyl or furyl)-1,2,4-triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.
