1207351-15-2Relevant articles and documents
4-ETHYLNYLPYRIDINE DERIVATIVES USEFUL AS GCN2 INHIBITORS
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Page/Page column 103-104, (2021/12/31)
The invention relates to compounds of formula I, wherein the substituents are as defined in more detail in the description. The compounds are potent inhibitors of GCN2 and have excellent pharmacokinetic properties. Compounds are useful for the treatment or prevention of various conditions, especially cancer. The invention further relates to pharmaceutical compositions comprising the compounds of the invention and uses of the compounds and compositions.
Novel substituted benzoyl compound and its pharmaceutically acceptable salt and preparation method and application (by machine translation)
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Paragraph 0299-0300; 0304-0305, (2019/11/13)
The invention relates to the general formula I shown novel substituted benzoyl compound and its pharmaceutically acceptable salt and preparation method and application. The invention also provides pharmaceutical compositions containing them, in vitro and in vivo anti-tumor effect results and acute toxicity study, the obtained anti-tumor drug model substituted benzoyl compound, has more excellent anti-tumor activity and safety, can be in the treatment of leukemia, lung cancer, colon cancer, ovarian cancer and renal carcinoma tumor in the application, so that the therapeutic window, so in the medical field as antitumor agents in the very application value. (by machine translation)
Novel S-type or R-type tetrahydronaphthalene amide compounds and pharmaceutically acceptable salts thereof, and preparation method and application thereof
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Paragraph 0311; 0316-0318; 0326; 0328-0330, (2019/11/29)
The invention relates to novel S-type or R-type tetrahydronaphthalene amide compounds and pharmaceutically acceptable salts thereof, and a preparation method and application thereof. The novel S-typeor R-type tetrahydronaphthalene amide compounds and the
Aryne as protein kinase inhibitors of such derivative and its medical uses
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Paragraph 0156-0158, (2016/10/08)
Disclosed is an aromatic alkyne derivative as a protein kinase inhibitor. The compound is a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4, ring A, ring B, L, m, n, p or q are as specifically defin
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
supporting information, 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.
Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl) benzamide derivatives as potent pan Bcr-Abl inhibitors including the threonine315←isoleucine315 mutant
Li, Yupeng,Shen, Mengjie,Zhang, Zhang,Luo, Jinfeng,Pan, Xiaofen,Lu, Xiaoyun,Long, Huoyou,Wen, Donghai,Zhang, Fengxiang,Leng, Fang,Li, Yingjun,Tu, Zhengchao,Ren, Xiaomei,Ding, Ke
, p. 10033 - 10046 (2013/01/16)
A series of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives were designed and synthesized as new Bcr-Abl inhibitors by using combinational strategies of bioisosteric replacement, scaffold hopping, and conformational constraint. The compounds displayed significant inhibition against a broad spectrum of Bcr-Abl mutants including the gatekeeper T315I and p-loop mutations, which are associated with disease progression in CML. The most potent compounds 6q and 6qo strongly inhibited the kinase activities of Bcr-AblWT and Bcr-AblT315I with IC50 values of 0.60, 0.36 and 1.12, 0.98 nM, respectively. They also potently suppressed the proliferation of K562, KU812 human CML cells, and a panel of murine Ba/F3 cells ectopically expressing either Bcr-AblWT or any of a panel of other Bcr-Abl mutants that have been shown to contribute to clinical acquired resistance, including Bcr-AblT315I, with IC50 values in low nanomolar ranges. These compounds may serve as lead compounds for further development of new Bcr-Abl inhibitors capable of overcoming clinical acquired resistance against imatinib.
5-ALKYNYL-PYRIMIDINES
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Page/Page column 14-15, (2012/02/06)
The present invention encompasses compounds of general formula (1) wherein R1 to R4 R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
5-ALKYNYL-PYRIMIDINES
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Page/Page column 14-15, (2012/02/06)
The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
5-ALKYNYL PYRIMIDINES AND THEIR USE AS KINASE INHIBITORS
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Page/Page column 38, (2011/08/21)
The present invention encompasses compounds of general formula (1) wherein R1 to R4 R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
5-ALKYNYL-PYRIMIDINES
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Page/Page column 19, (2010/04/03)
The present invention encompasses compounds of general Formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use th