88319-37-3Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of quinazoline derivatives with covalent reversible warheads as potential FGFR4 inhibitors
Che, Jinxin,Dong, Xiaowu,Du, Jiaming,Gao, Jian,He, Qiaojun,Lu, Yang,Luo, Mengxin,Luo, Peihua,Nie, Wenwen,Pan, Chenghao,Wang, Jiao,Zhu, Hong
, (2022/03/16)
Fibroblast growth factor receptor 4 (FGFR4) together with co-receptors modulate the activation of downstream proteins that regulate fundamental processes, and elevated FGFR4 activity is associated with Hepatocellular Carcinoma (HCC). Hence, FGFR4 is a promising therapeutic target for HCC. Based on BLU9931, we designed and synthesized a series of phenylquinazoline derivatives as novel inhibitors of FGFR4 through the covalent reversible strategy. Among them, a novel compound (C3) showed FGFR4 and cell proliferation inhibitory activity. Cellular mechanism studies demonstrated that compound C3 induced apoptosis via the FGFR4 signaling pathway blockage. Further mechanism study showed that C3 has the reversible covalent binding capacity, could be used as a reference for the development of novel FGFR4 covalent reversible inhibitors.
IMMUNOPROTEASOME INHIBITORS
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Paragraph 0237, (2018/08/20)
Provided herein are compounds, such as a compound of Formula (I), as described herein, or a pharmaceutically acceptable salt thereof, that are immunoproteasome (such as LMP2 and LMP7) inhibitors. The compounds described herein can be useful for the treatment of diseases treatable by inhibition of immunoproteasomes. Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
PYRAZOLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS
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Page/Page column 52, (2014/03/26)
The present disclosure provides compounds of Formula (LA) and/ or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of ty r-osine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and p h ar-maceutically acceptable salts thereof
Purinone Derivatives as Tyrosine Kinase Inhibitors
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Paragraph 0182-0183, (2014/05/25)
The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as autoimmune diseases, cancer and inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
TYROSINE KINASE INHIBITORS
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Page/Page column 108; 109, (2012/12/13)
The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, JAK3, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by
