1374507-25-1Relevant articles and documents
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors
Chang, Xiayun,Gao, Yong,He, Xiangyi,Lu, Peng,Ren, Jing,Shi, Wei,Wang, Qinglin,Wang, Xiaojin,Xu, Hongjiang,Zhang, Xiquan,Zhang, Yinsheng,Zhao, Damin
, (2019)
Bruton's tyrosine kinase (BTK) and Janus kinase 3 (JAK3) are very promising targets for hematological malignancies and autoimmune diseases. In recent years, a few compounds have been approved as a marketed medicine, and several are undergoing clinical trials. By recombining the dominant backbone of known active compounds, constructing a foused library, and screening a broad panel of kinases, we found a class of compounds with dual activities of anti-BTK and anti-JAK3. Some of the compounds have shown 10-folds more active in the enzyme and cell-based assays than a known active compound. Furthermore, liver microsome stability experiments show that these compounds have better stability than ibrutinib. These explorations offered new clues to discover benzoxaborole fragment and pyrimidine scaffold as more effective BTK and JAK3 dual inhibitors.
BTK (Bruton's tyrosine kinase) inhibitors
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Paragraph 0106; 0107; 0108, (2018/08/28)
The invention belongs to the field of medicinal chemistry and particularly relates to compounds shown as formula (I) in the description, medically acceptable salts of the compounds, a preparation method of the compounds and pharmaceutical composition containing the compounds. The invention further relates to an application of the compounds, the medically acceptable salts of the compounds and the pharmaceutical composition containing the compounds to treatment of BTK (Bruton's tyrosine kinase) related diseases.
A including a spiro ring or bridge of the pyrimidines
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, (2017/08/25)
The invention discloses a spiral ring or bridged ring containing pyrimidine compound. The compound has a structure shown as formula I, and also can be an enantiomer, a diastereomer, a pharmaceutically acceptable salt, a prodrug molecule, a solvate, a taut
Deuterated diphenylaminopyrimidine compound
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, (2017/05/10)
The invention belongs to the field of medicine, and relates to a deuterated diphenylaminopyrimidine compound or a pharmaceutically acceptable salt thereof, and more particularly to a compound of the formula (I) or a pharmaceutically acceptable salt thereof, a preparation process thereof, a pharmaceutical composition thereof and application thereof in the treatment of a cell proliferative disease.
2,4-dibasic miazines compound
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, (2017/08/29)
The invention belongs to the field of medical chemistry, relates to a 2,4-dibasic miazines compound and specifically relates to a compound shown as formula (I) or a pharmaceutically acceptable salt thereof, a drug compound thereof and an application thereof in treating EGFR or/and ALK mediated diseases.
Tyrosine Kinase Inhibitor And Uses Thereof
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Paragraph 0421-0422, (2017/05/15)
Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.
Compounds possessing kinase inhibition activity, preparation method and uses
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, (2016/10/10)
Compounds possessing kinase inhibition activity, a preparation method and uses are disclosed. The invention discloses the compounds shown as a general formula I, or pharmaceutically-acceptable salts thereof, or enantiomers, diastereomers, tautomerisms, solvates, polymorphic substances or prodrugs thereof, the preparation method of the above compounds, and application of the above compounds to medicines, and the groups in the general formula I are defined as the specification. The compounds possess relatively excellent kinase inhibition activity, and especially EGFR and ALK kinases and mutants thereof possessses relative good medicinal prospect.
Pyrimidine derivative, preparation method therefor and application thereof in medicine
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Paragraph 0192;0197; 0198; 0199; 0200; 0201, (2016/10/07)
The invention relates to a pyrimidine derivative, a preparation method therefor and an application thereof in medicine. Particularly, the invention relates to a compound as shown in general formula (M) or a stereisomer, an aquo-complex, a metabolic product, a solvate, a pharmaceutically acceptable salt, a co-crystallization or a prodrug thereof; the preparation method thereof; and the application of the medicine composition thereof and the compound medicine compound in the medicine, particularly the application as an EGFR target spot inhibitor, wherein the definition of each substituent group in the general formula (M) is the same as that of the specification.
Substituted aminopyrimidine derivative, preparation method therefor and pharmaceutical application thereof
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, (2016/10/07)
The invention relates to a substituted aminopyrimidine derivative as shown in general formula (I) and (II), an optical isomer, a pharmaceutically acceptable salt or co-crystallization thereof, a preparation method and application in preparation of tumor m
Heteroaryl compounds and uses thereof
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Page/Page column 25, (2016/02/08)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.