1197953-49-3Relevant academic research and scientific papers
DIMETHYLPHOSPHINE OXIDE COMPOUND
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Paragraph 0049, (2021/02/25)
Disclosed is an application of a series of dimethylphosphine oxide compounds in the preparation of an LRRK2 kinase activity inhibitor-related drug, specifically an application of the compound shown in formula (I) or a pharmaceutically acceptable salt thereof in the preparation of an LRRK2 kinase activity inhibitor-related drug.
Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFRT790M/C797SMutants
Ding, Jian,Ding, Ke,Lai, Mengzhen,Lei, Chong,Li, Shan,Lu, Xiaoyun,Pang, Zilu,Peng, Lijie,Ren, Xiaomei,Tong, Linjiang,Xie, Hua,Yun, Cai-Hong,Zhang, Tao,Zhu, Su-Jie
, (2022/02/07)
A series of brigatinib derivatives were designed and synthesized as new potent and selective EGFRT790M/C797S inhibitors. One of the most potent and selective compounds 18k strongly suppressed the EGFRL858R/T790M/C797S and EGFR19Del/T790M/C797S kinases wit
Preparation method of ALK inhibitor Brigatinib
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Paragraph 0048-0050, (2020/06/02)
The invention relates to the technical field of medicines, and relates to a preparation method of a medicine ALK inhibitor AP26113. The method comprises the following steps: (1) carrying out substitution reaction of aromatic amine on 2,4,5-trichloropyrimi
EGFR INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Page/Page column 33, (2020/07/31)
Provided are compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or inf
2, 4, 5-substituted pyrimidine compound and preparation method and application thereof
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Paragraph 0049-0050, (2020/08/06)
The invention relates to a preparation method of 2, 4-substituted pyrimidine compound and a preparation method and application thereof. The compound has a molecular structure shown as a formula I or pharmaceutically acceptable salt, solvate, stereoisomer or prodrug molecule thereof. The 2, 4, 5-substituted pyrimidine compound is low in cytotoxicity and has high selective inhibition on EGFR; the compound can inhibit the proliferation of EGFR drug-resistant mutant enzymes (such as T790M/L858R/C797S mutant enzymes) and cell strains thereof at a low concentration (such as nanomole concentration),so that the compound can be used for treating diseases caused by EGFR mutation, and is expected to be developed into a new generation of EGFR inhibitors.
EGFR INHIBITORS, COMPOSITIONS AND METHODS THERE OF
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Page/Page column 18-19, (2020/10/20)
The present invention relates to compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders s
2,4,5-substituted pyrimidine compound as well as preparation method and application thereof
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Paragraph 0060-0063, (2020/10/14)
The invention relates to a 2,4,5-substituted pyrimidine compound as well as a preparation method and application thereof, and provides pharmaceutically acceptable salt, solvate, stereoisomer or prodrug molecule thereof, wherein the molecular structure of the pharmaceutically acceptable salt, solvate, stereoisomer or prodrug molecule is shown in the specification. The provided 2,4,5-substituted pyrimidine compound is low in cytotoxicity, has high selective inhibition on EGFR, can inhibit the proliferation of EGFR drug-resistant mutant enzymes (such as T790M/L858R/C797S mutant enzymes) and cellstrains thereof at a low concentration (such as nano mole concentration), can be used for treating diseases caused by EGFR mutation, and can be made into a new generation of EGFR inhibitors.
DIPHENYLAMINOPYRIMIDINE AND TRIAZINE COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF
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Paragraph 0091; 0092, (2019/04/25)
The invention relates to a diphenylaminopyrimidine and triazine compound of Formula I, or a pharmaceutically acceptable salt, stereoisomer, hydrate or solvate thereof: wherein A is C or N; X and Y are independently selected from hydrogen, halo, cyano, trifluoromethyl, alkoxy, alkyl, aryl, alkenyl, alkynyl and nitro; or X and Y, together with the atoms to which they are attached, form a phenyl or an heteroaromatic ring; R1 is R2 is CD3 or CD2CD3; R3 is R4 is hydrogen, methyl, trifluoromethyl, cyano or halo; R5 is hydrogen, alkyl, substituted and unsubstituted phenyl, allyl or propargyl; R6 and R7 are independently selected from hydrogen, alkyl, substituted and unsubstituted phenyl, allyl and propargyl; or R6 and R7, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heterocycloalkyl group. The compound herein has excellent pharmacodynamic and pharmacokinetic properties and ALK kinase inhibitory activity.
Polymorphism of novel spiroarylphosphine oxide
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Paragraph 0114; 0121-0123, (2019/11/20)
The invention relates to a polymorphic substance of a compound (2-((5-chloro-2-((2-methoxyl-4-(9-methyl-3,9-diaza-sprio[5.5]hendecane-3-yl)phenyl)amino)pyrimidine-4-yl)amino)phenyl)dimethyl phosphineoxide (compound I). The invention further relates to a m
2-aminopyrimidine compound and application thereof
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Paragraph 0165; 0168; 0173-0176, (2019/10/17)
The invention relates to a 2-aminopyrimidine compound and application thereof. The structure of the 2-aminopyrimidine compound is shown as I. The compound can effectively inhibit the activity of EGFRprotein kinase resistance mutants (such as EGFRT790M and
