1256162-94-3Relevant academic research and scientific papers
Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9
Phillipson, Louisa J.,Segal, David H.,Nero, Tracy L.,Parker, Michael W.,Wan, Soo San,De Silva, Melanie,Guthridge, Mark A.,Wei, Andrew H.,Burns, Christopher J.
, p. 6280 - 6296 (2015)
The serine-threonine kinase CDK9 is a target of emerging interest for the development of anti-cancer drugs. There are multiple lines of evidence linking CDK9 activity to cancer, including the essential role this kinase plays in transcriptional regulation
Design, synthesis and biological evaluation of macrocyclic derivatives as TRK inhibitors
Cai, Shi,Guan, Dezhong,Li, Jinruo,Li, Pei,Xu, Lin,Zhang, Huibin,Zhao, Tong,Zhou, Jinpei
, (2021/11/11)
Tropomyosin receptor kinases (TRKA, TRKB, TRKC) are transmembrane receptor tyrosine kinases, which are respectively encoded by NTRK1, NTRK2, and NTRK3 genes. Herein, we reported the design, synthesis and Structure-Activity Relationship (SAR) investigation of a series of macrocyclic derivatives as new TRK inhibitors. Among these compounds, compound 9e exhibited strong kinase inhibitory activity (TRKG595R IC50 = 13.1 nM) and significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM) and compound 9e has shown a better inhibitory effect (IC50 = 0.646 μM) than control drug LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line. These results indicate that compound 9e is a potential TRK inhibitor for further investigation.
Macrocyclic compound, and preparation method and application thereof
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Paragraph 0203-0205; 0218-0222, (2021/06/23)
The invention discloses a macrocyclic kinase inhibitor, and a compound, or a stereoisomer or a pharmaceutically acceptable salt thereof as shown in a formula (I). Experiments show that the novel compound shown in the formula (I) shows good TRK inhibitory
Pyrazolo [1, 5 - a] pyrimidine compounds and their preparation method and medical use
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, (2017/08/02)
The invention relates to a pyrazolo[1,5-a]miazine compound and its preparation method and medical use. The invention relates to the preparation method of the pyrazolo[1,5-a]miazine compound shown in the general formula (I) and its salt, a pharmaceutical c
FUSED RING HETEROARYL COMPOUNDS AND THEIR USE AS TRK INHIBITORS
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, (2016/07/05)
The disclosure provides novel chemical compounds represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof. The compounds can be used as an inhibitor of Trk and are useful in the treatment of pain, cancer, inflammation, neurodegenerative disease and certain infectious diseases. In some compounds of Formula I, Q is —CH═CR3C(O)NR4R5, —C≡CC(O)NR4R5, or
HETEROAROMATIC COMPOUNDS AS PI3 KINASE MODULATORS AND METHODS OF USE
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Paragraph 0318; 0319, (2014/09/03)
The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
PHARMACEUTICALLY USEFUL HETEROCYCLE-SUBSTITUTED LACTAMS
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Page/Page column 76; 84, (2011/04/18)
The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, infections, and certain immunological disorders.
