442847-52-1Relevant academic research and scientific papers
An improved synthesis approach of the HIV-1 inhibitor RDEA427, a pyrrolo[2,3-d]pyrimidine derivative
Huang, Boshi,Liu, Xinhao,Li, Wanzhuo,Chen, Zihui,Kang, Dongwei,Zhan, Peng,Liu, Xinyong
, p. 45 - 51 (2021)
The diarylpyrimidine-like derivative RDEA427 is a highly potent inhibitor against wild-type and a wide range of drug-resistant HIV-1 strains and has attracted much attention. However, the yield of its reported synthesis is too low and the route is less environment-friendly and uneconomic. In order to achieve a short and more economic synthesis of RDEA427, an investigation was carried out. The optimized synthesis approach of RDEA427 was accomplished in an increased overall yield (39%). Moreover, the new route is more environment-friendly and economic. This work will accelerate the drug discovery process.
HETEROCYCLE-FUSED PYRIMIDINE DERIVATIVE AND USE THEREOF
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Paragraph 0178-0179, (2022/04/03)
The present invention relates to a heterocycle-fused pyrimidine derivative compound or a pharmaceutically acceptable salt thereof, a pharmaceutical composition for preventing or treating diseases related to one or more protein kinases of FLT3, CDK4, CDK6 and HPK1, comprising the same as an active ingredient, and a method for preventing or treating diseases related to one or more protein kinases of FLT3, CDK4, CDK6 and using the same.
Pyrimidina-1,5(1,3)-dibenzenacycloheptaphane derivative as mutant epidermal growth factor receptor inhibitor
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Paragraph 0086; 0097-0099, (2021/04/20)
The present invention relates to a pyrimidinyl monobenzocycloheptazole derivative represented by chemical formula I, a solvate thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient, capable of effectively inhibiting the growth and drug resistance of cancer cells caused by the mutation of tyrosine kinase domain in epidermal growth factor receptor (Chem. I). .
NOVEL SULFONAMIDE DERIVATIVE WITH FUSED PYRIMIDINE SKELETON, HAVING EPIDERMAL GROWTH FACTOR RECEPTOR MUTATION INHIBITORY EFFECT
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Paragraph 0076; 0079, (2021/07/02)
The present invention relates to a novel fused pyrimidine based sulfonamide derivative represented by Formula I, a solvate thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including the same as an active ingredient. The novel fused pyrimidine based sulfonamide derivative of the present invention can effectively suppress the growth of cancer cells and resistance to drugs, which are induced by mutations in the tyrosine kinase domain of epidermal growth factor receptors, or the growth of cancer cells having such resistance.
CYANO-PYRIMIDINE INHIBITORS OF EGFR/HER2
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Page/Page column 78, (2021/07/17)
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with EGFR and/or HER2 activity.
Structure-Guided Optimization Provides a Series of TTK Protein Inhibitors with Potent Antitumor Activity
Elsner, Jan,Cashion, Dan,Robinson, Dale,Bahmanyar, Sogole,Tehrani, Lida,Fultz, Kimberly E.,Narla, Rama Krishna,Peng, Xiaohui,Tran, Tam,Apuy, Julius,Lebrun, Laurie,Leftheris, Katerina,Boylan, John F.,Zhu, Dan,Riggs, Jennifer R.
supporting information, p. 12670 - 12679 (2021/09/13)
TTK is an essential spindle assembly checkpoint enzyme in many organisms. It plays a central role in tumor cell proliferation and is aberrantly overexpressed in a wide range of tumor types. We recently reported on a series of potent and selective TTK inhibitors with strong antiproliferative activity in triple negative breast cancer (TNBC) cell lines (8: TTK IC50 = 3.0 nM; CAL-51 IC50 = 84.0 nM). Inspired by previously described potent tricyclic TTK inhibitor 6 (TTK IC50 = 0.9 nM), we embarked on a structure-enabled design and optimization campaign to identify an improved series with excellent potency, TTK selectivity, solubility, CYP inhibition profile, and in vivo efficacy in a TNBC xenograft model. These efforts culminated in the discovery of 25 (TTK IC50 = 3.0 nM; CAL-51 IC50 = 16.0 nM), which showed significant single-agent efficacy when dosed iv in a TNBC xenograft model without body weight loss.
HETEROARYL DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS ACTIVE INGREDIENT
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Paragraph 0079; 0080, (2021/12/07)
The present invention relates to a heteroaryl derivative and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient, and a compound according to an aspect of the present invention, a stereoisomer
Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies
Daelemans, Dirk,De Clercq, Erik,Gao, Ping,Ginex, Tiziana,Huang, Boshi,Jiang, Xiangyi,Kang, Dongwei,Liu, Xinyong,Luque, F. Javier,Pannecouque, Christophe,Zhan, Peng,Zhang, Jian
, p. 13604 - 13621 (2021/09/28)
Two series of new pyridyl-bearing fused bicyclic analogues designed to target the dual-tolerant regions of the non-nucleoside reverse transcriptase inhibitor (NNRTI)-binding pocket were synthesized and evaluated for their anti-HIV activities. Several comp
MOLECULES AND METHODS RELATED TO TREATMENT OF UNCONTROLLED CELLULAR PROLIFERATION
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Paragraph 00442, (2021/02/05)
The present disclosure relates to chemical compounds that modulate cellular proliferation for the treatment of uncontrolled cellular proliferation disorders (such as cancer), pharmaceutical compositions containing such compounds, and their use in treatment. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Oxy-fluoropiperidine Derivative as Kinase Inhibitor
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Paragraph 0088-0090; 0165-0167; 0187-0189, (2020/11/24)
The present invention relates to a compound represented by the following Chemical Formula 1, or a pharmaceutically acceptable salt thereof, and the compound according to the present invention can be usefully used for the prevention or treatm ent of diseas
