6200-36-8Relevant academic research and scientific papers
A paclitaxel and model phthalazine ketone BTK inhibitor combination pharmaceutical composition and its application (by machine translation)
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Paragraph 0033; 0035, (2019/02/04)
The invention provides a joint for paclitaxel and BTK inhibitor pharmaceutical composition comprising an active ingredient and a pharmaceutically acceptable auxiliary material, wherein the active ingredient by the taxol of formula (I) of a BTK inhibitors shown, the active ingredient of taxol in the formula (I) indicated by the molar ratio of BTK inhibitors (0.14 - 0.20): 1. The pharmaceutical composition can be used for preparing the prevention and/or treating the Bruton tyrosine kinase-related disease drug, the treatment effect is good. (by machine translation)
Pyridazinone BTK inhibitors and application thereof
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Paragraph 0037; 0038; 0039, (2019/01/23)
The invention relates to the field of medicinal chemistry, relates to pyridazinone BTK inhibitors and an application thereof, and concretely relates to pyridazinone BTK inhibitors represented by formula (I), a preparation method thereof, a medicinal composition containing the compounds, and a use of the compounds or the medicinal composition in the treatment of Bruton's tyrosine kinase-related diseases.
Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis
Scott, Jill M.,Baccei, Christopher,Bain, Gretchen,Broadhead, Alex,Evans, Jilly F.,Fagan, Patrick,Hutchinson, John H.,King, Christopher,Lorrain, Daniel S.,Lee, Catherine,Prasit, Peppi,Prodanovich, Pat,Santini, Angelina,Santini, Brian A.
scheme or table, p. 6608 - 6612 (2011/12/04)
Biphenylacetic acid (5) was identified through a library screen as an inhibitor of the prostaglandin D2 receptor DP2 (CRTH2). Optimization for potency and pharmacokinetic properties led to a series of selective CRTH2 antagonists. Compounds demonstrated potency in a human DP2 binding assay and a human whole blood eosinophil shape change assay, as well as good oral bioavailability in rat and dog, and efficacy in a mouse model of allergic rhinitis following oral dosing.
NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES
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Page/Page column 48, (2009/12/05)
The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group
Cai, Sui Xiong,Guan, Lufeng,Jia, Shaojuan,Wang, Yan,Yang, Wu,Tseng, Ben,Drewe, John
, p. 5295 - 5300 (2007/10/03)
The synthesis and biological evaluation of a group of N-protected Val-Asp-fmk as caspase inhibitors is reported. This article describes the synthesis and biological evaluation of a group of N-protected Val-Asp-fmk as caspase inhibitors. The protecting group was found to contribute to caspase-3 inhibiting activity, and compounds with a large group such as Cbz are more active than compounds with a small group such as Ac. Compounds with more hydrophobic protecting groups were found to be more active in cell apoptosis protection assays, probably due to increased cell permeability. MX1122, 2,4-di-Cl-Cbz-Val-Asp-fmk, is identified as a potent broad-spectrum caspase inhibitor and is selective for caspases versus other proteases, with good activity in the cell apoptosis protection assays as well as good efficacy in the mouse liver apoptosis model.
