877149-80-9Relevant articles and documents
AMINOPYRIDINE COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
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Paragraph 0269-0271, (2021/11/04)
The present invention discloses an aminopyridine compounds, a preparation method and use thereof, particularly the aminopyridine compounds of formula (I), pharmaceutical compositions containing the same, the method for preparing the same and the use thereof in the prophylaxis or treatment of an adenosine A2a receptor related disease.
Design, synthesis, and structure activity relationship (SAR) studies of novel imidazo[1,2-a] pyridine derivatives as Nek2 inhibitors
Chen, Yunzhong,Du, Yijie,Duan, Yanhong,Gu, Xiaofan,Li, Hongyu,Ma, Mingliang,Ren, Ziwei,Wang, Haili,Wang, Shuting,Xi, Jianbei,Zhang, Xiongwen,Zhu, Tong
, (2020/10/02)
Never in mitosis (NIMA) related kinase 2 (Nek2) is involved in multiple cellular processes such as cell cycle checkpoint regulation, cell division, DNA damage response and cell apoptosis. Nek2 has been reported to be overexpressed in various tumors and correlated with poor prognosis. Herein, a series of imidazo[1,2-a] pyridines Nek2 inhibitors were designed, synthesized, and their biological activities were investigated. Besides, structure activity relationship analysis of these compounds were performed in the MGC-803 cell. The screening results are promising, and compound 28e shows good proliferation inhibitory activity with an IC50 of 38 nM. The results would be helpful to design and develop more effective Nek2 inhibitors for the treatment of gastric cancer.
PIPERIDINE DERIVATIVES AS INHIBITORS OF UBIQUITIN SPECIFIC PROTEASE 7
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Page/Page column 99, (2018/05/16)
The present invention concerns the identification of inhibitors of ubiquitin specific protease 7 (USP7), and methods of use thereof.
PYRAZOLOPYRIMIDINE DERIVATIVES
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Page/Page column 116; 117, (2017/11/10)
The present invention covers Pyrazolopyrimidine compounds of general formula (I), in which n, o, X, Y, R, Q, R1, R2, R3 and R4 are as defined herein, methods of preparing said compounds, intermediate compounds u
Imidazo[1,2-a]pyridine compound, and preparation method and applications thereof
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Paragraph 0110; 0112, (2017/08/28)
The invention discloses an imidazo[1,2-a]pyridine compound, and a preparation method and applications thereof. The imidazo[1,2-a]pyridine compound can inhibit the activity of NEK2 kinases as an NEK2 micro-molecular inhibitor with a novel structure. The in
HETEROARYL COMPOUNDS AND PHARMACEUTICAL APPLICATIONS THEREOF
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Paragraph 00686, (2016/01/25)
The present invention provides herein is a heteroaryl compound or a stereoisomer, a geometric isomer, a tautomer, a racemate, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, as well as a pharmaceutical composition containing the compound disclosed herein. The present invention also provides herein is use of the compound or the pharmaceutical composition thereof disclosed herein in the manufacture of a medicine for treating autoimmune diseases or proliferative diseases.
PROTEIN KINASE INHIBITORS
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Paragraph 0130, (2015/02/18)
A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
PYRAZINE DERIVATIVES AS FGFR INHIBITORS
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Paragraph 0257; 0258, (2014/03/21)
The present invention relates to pyrazine derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
4,5-DIHYDROISOXAZOLE DERIVATIVES AS NAMPT INHIBITORS
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Page/Page column 164; 167, (2014/08/06)
The present invention provides substituted 4,5-dihydroisoxazole derivatives of formula (I), which may be therapeutically useful, more particularly NAMPT inhibitors and in which R1 R2, Y, X, "Het" and "p" have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPT) in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted 4,5-dihydroisoxazole derivatives of formula (I) or a pharmaceutically acceptable salts or stereoisomers or N-oxide thereof.
USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3K-DELTA RELATED DISORDERS
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, (2014/09/16)
The present application provides methods of treating PI3Kδ related disorders using compounds of Formula I: or pharmaceutically acceptable salts thereof.