943320-60-3Relevant academic research and scientific papers
N-(3-(IMIDAZO[1,2-B]PYRIDAZIN-3-YLETHYNYL)-4-METHYLPHENYL)-5-PHENYL-4,5-DIHYDRO-1H-PYRAZOLE-1-CARBOXAMIDE DERIVATIVE, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT FOR TREATING KINASE-RELATED DISEASES
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Paragraph 0254-0256, (2021/09/17)
The N-(3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methylphenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide derivative exhibits excellent inhibitory activity against at least one kinase selected from the group consisting of ABL1, ABL2, AURKB, BRK, CDK11
Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an o-Aminopyridyl Alkynyl Scaffold as Potential Treatment for Inflammatory Disorders
Xie, Zhicheng,Wu, Bing,Liu, Yingqiang,Ren, Wenming,Tong, Linjiang,Xiang, Caigui,Wei, Aihuan,Gao, Yuanzhuo,Zeng, Limin,Xie, Hua,Tang, Wei,Hu, Youhong
, p. 1397 - 1414 (2020/02/04)
Colony-stimulating factor 1 receptor (CSF-1R) is involved in inflammatory disorders as well as in many types of cancer. Based on high-throughput screening and docking results, we performed a detailed structure-activity-relationship study, leading to the d
COMPOUNDS USEFUL FOR INHIBITING RAF DIMERS
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Paragraph 0151; 0153, (2020/09/12)
The disclosure provides compounds of Formula I (Formula I) (c) And the pharmaceutically acceptable salts thereof. The A, B, C, and D rings and the variables, RA, RB, RC, RD, L0, L1, L2
BTK Inhibitors and uses thereof
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Paragraph 1587-1592, (2020/05/02)
The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease
Kaiser, Thomas M.,Dentmon, Zackery W.,Dalloul, Christopher E.,Sharma, Savita K.,Liotta, Dennis C.
supporting information, p. 491 - 496 (2020/04/30)
Parkinson's disease (PD) is a debilitating and common neurodegenerative disease. New insights implicating c-Abl activation as a driving force in PD have opened a new drug development avenue for PD treatment beyond the symptomatic relief by L-DOPA. BCR-Abl inhibitors, which include nilotinib and ponatinib, have been found to inhibit this process, and nilotinib has shown improvement in outcomes in a 12-patient, nonrandomized trial. However, nilotinib is a potent inhibitor of hERG, a cardiac K+ channel whose inhibition increases risk of sudden death. We used our machine learning approach to predict novel molecules that would inhibit c-Abl while also having minimal liability against hERG. Of our six novel compounds tested, we identified two that had c-Abl potencies comparable to nilotinib, but with significantly improved profiles regarding the hERG channel. Our best compound exhibited a hERG IC50 of 12.1 μM (compared to nilotinib with an IC50 of 0.45 μM and ponatinib with IC50 of 0.767 μM). This work is a step forward for a machine learning enabled, multiparameter optimization of a chemical space and represents a significant advance in the development of novel Parkinson's therapies.
Preparation method of
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Paragraph 0004; 0049-0051; 0058-0060, (2020/05/01)
The invention discloses a preparing method of ponatinib. The preparing method of ponatinib comprises the steps of building a reaction system in copper salt and alkaline organic solvent with 3-halogen-parazole [1,5-a]pyrimidine being the starting point, with trimethylsilylacetylene, tetrabutylammonium fluoride and the like being raw materials in sequence and with acridine salt being a photocatalyst, and thus indirectly building a synthesizing path of ponatinib. The synthesis conditions are mild, the cost is low, and the yield of ponatinib is high.
benzo[b][1,4]oxazepin derivatives and pharmaceutical composition for use in preventing or treating kinase-related disease
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Paragraph 0288-0289; 0291-0293, (2020/10/20)
The present invention relates to a benzo[b][1,4]oxazepine derivative represented by the following chemical formula 1, and a pharmaceutical composition for treating kinase-related diseases including the same as an active ingredient. The benzo[b][1,4]oxazep
ABELSON NON-TYROSINE KINASE COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
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Page/Page column 20-21, (2020/10/28)
The present disclosure relates to compounds for the use of treating neurodegenerative diseases and, in particular, to compounds targeting the Abelson non-tyrosine kinase (c-Abl) protein for such treatment. The neurological disorders and conditions include Parkinson's disease, Alzheimer's disease and the like. It also relates to pharmaceutical compositions and methods of treatment of such neurological disorders involving the c-Abl protein kinase.
Novel substituted benzoyl compound and its pharmaceutically acceptable salt and preparation method and application (by machine translation)
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Paragraph 0043; 0048; 0050-0051, (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 0108; 0122; 0126-0130, (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
