957147-17-0Relevant academic research and scientific papers
KINASE INHIBITORS AND USES THEREOF
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, (2020/10/21)
This invention described herein relates to compounds of general formula (I) : (I), in which variable groups are as defined herein, and to their preparation and use. Uses for the compounds and for compositions containing them include treatment of cancer and other diseases mediated by protein kinases, such as Bcr-Abl kinase, and mutants thereof, such as the T315I mutant.
BCR-ABL kinase inhibitor and its application (by machine translation)
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, (2017/03/28)
The present invention relates to the field of chemical medicines, in particular to compounds as represented by formula I having BCR-ABL kinase inhibitory activity, or pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug thereof, and pharmaceutical composition containing the compounds, and application of the compounds or compositions in drug preparation. The compounds of the present invention have strong inhibitory effect on BCR-ABL kinase, and can be used to treat diseases such as tumors.
A drug treating chronic granulocytic leukemia method for the preparation of
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, (2017/04/28)
The invention relates to a preparation method of a drug for treating chronic granulocytic leukemia, belonging to the field of medical chemistry, and specifically relates to a preparation method of 3-[2-(imidazo[1,2-b] pyridazine-3-yl) acetenyl]-4-methyl-N
ALKYNYL HETEROAROMATIC RING COMPOUND AND APPLICATION THEREOF
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, (2015/08/03)
The present invention belongs to the field of pharmaceutical chemistry, and specifically relates to compounds having an alkynyl heteroaromatic ring structure and pharmaceutically acceptable salts, stereoisomers, N-oxides, solvates, or prodrugs thereof, an
HETEROARYL ALKYNE COMPOUND AND APPLICATION THEREOF
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, (2015/11/18)
The present invention belongs to the field of pharmaceutical chemistry. Specifically, the invention relates to compounds of general formula I having heteroaryl alkynyl moiety or pharmceutically acceptable salts, isomers, solvates, crystals or prodrugs the
ALKYNYL HETEROAROMATIC COMPOUND AND USE THEREOF
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, (2015/06/10)
The present invention belongs to the field of pharmaceutical chemistry, and specifically relates to compounds having an alkynyl heteroaromatic ring structure and pharmaceutically acceptable salts, stereoisomers, N-oxides, solvates, or prodrugs thereof, an
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib
Ren, Xiaomei,Pan, Xiaofen,Zhang, Zhang,Wang, Deping,Lu, Xiaoyun,Li, Yupeng,Wen, Donghai,Long, Huoyou,Luo, Jinfeng,Feng, Yubing,Zhuang, Xiaoxi,Zhang, Fengxiang,Liu, Jianqi,Leng, Fang,Lang, Xingfen,Bai, Yang,She, Miaoqin,Tu, Zhengchao,Pan, Jingxuan,Ding, Ke
, p. 879 - 894 (2013/03/28)
Bcr-AblT315I mutation-induced imatinib resistance remains a major challenge for clinical management of chronic myelogenous leukemia (CML). Herein, we report GZD824 (10a) as a novel orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including T315I. It tightly bound to Bcr-AblWT and Bcr-AblT315I with Kd values of 0.32 and 0.71 nM, respectively, and strongly inhibited the kinase functions with nanomolar IC50 values. The compound potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC 50 values of 0.2 and 0.13 nM, respectively. It also displayed good oral bioavailability (48.7%), a reasonable half-life (10.6 h), and promising in vivo antitumor efficacy. It induced tumor regression in mouse xenograft tumor models driven by Bcr-AblWT or the mutants and significantly improved the survival of mice bearing an allograft leukemia model with Ba/F3 cells harboring Bcr-AblT315I. GZD824 represents a promising lead candidate for development of Bcr-Abl inhibitors to overcome acquired imatinib resistance.
