专利号:US-11319320-B2 优先权日:2017-11-06 标题:PIM kinase inhibitor compositions, methods, and uses thereof 发明人:BURK MARK J; CHEN BRANDON; LI JINGYI; BACHAN SHAWN 权利人:SNAP BIO INC 摘要:This application relates to compounds of formulae (I) and (II) and compositions thereof useful as inhibitors of PIM kinases. Also provided are methods of synthesis and methods of use of PIM inhibitors in treating individuals suffering from cancerous malignancies.
专利号:WO-2022162606-A1 优先权日:2021-01-30 标 题:Heterocyclic compounds as kinase inhibitor and uses thereof 发明人:YAN ZHIYU; WANG XIAOHUI; LIU HANLAN; KHAN PASHA M; PANPATIL DAYANAND; PUJALA BRAHMAM; PENDHARKAR DHANANJAY; JADHAVAR PRADEEP S; SAEED UZMA; KUMAR VIVEK 权利人:SPEROGENIX THERAPEUTICS LTD; INTEGRAL BIOSCIENCES PRIVATE LTD 摘要:The present disclosure relates generally to compounds useful in treatment of conditions associated with Checkpoint kinase (CHK), particularly CHK-1 enzymes. Specifically, the present invention discloses compound of formula (J), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes such as cancer, idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed. Formula (J)
1: Siu A, Virtanen C, Jongstra J. PIM kinase isoform specific regulation of MIG6 expression and EGFR signaling in prostate cancer cells. Oncotarget. 2011 Dec 22. [Epub ahead of print] doi: 10.1038/bjc.2011.426. Epub 2011 Oct 20. 4: Chen LS, Redkar S, Taverna P, Cortes JE, Gandhi V. Mechanisms of cytotoxicity to Pim kinase inhibitor, SGI-1776, in acute myeloid leukemia. Blood. 2011 Jul 21;118(3):693-702. Epub 2011 May 31. 5: Chang M, Kanwar N, Feng E, Siu A, Liu X, Ma D, Jongstra J. PIM kinase inhibitors downregulate STAT3(Tyr705) phosphorylation. Mol Cancer Ther. 2010 Sep;9(9):2478-87. Epub 2010 Jul 28.
合成参考文献
参考文献:10.1007/s00109-011-0788-5 摘要:Paulin R, Courboulin A, Barrier M, Bonnet S. From oncoproteins/tumor suppressors to microRNAs, the newest therapeutic targets for pulmonary arterial hypertension. J Mol Med (Berl). 2011 Nov;89(11):1089–101. doi: 10.1007/s00109-011-0788-5.