87808-11-5Relevant academic research and scientific papers
Interrupting the Barton?McCombie reaction: Aqueous deoxygenative trifluoromethylation of o-alkyl thiocarbonates
Liu, Zhi-Yun,Cook, Silas P.
supporting information, p. 808 - 813 (2021/02/01)
The site-selective trifluoromethylation of aliphatic systems remains an important challenge. This work describes a light-driven, copper-mediated trifluoromethylation of O-alkyl thiocarbonates. The reaction provides broad functional group tolerance (e.g., alkyne, alkene, phenol, free alcohol, electron-rich and -deficient arenes), thereby offering orthogonality and practicality for trifluoromethylation. A radical organometallic mechanism is proposed.
MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X4 AND RELATED PRODUCTS AND METHODS
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Page/Page column 254-255, (2020/10/18)
Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.
ANTICANCER COMPOUNDS
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Paragraph 0215, (2018/05/03)
The invention provides compounds having the general formula I: and salts thereof, wherein the variables RA, RB, RC, L1, L2, L3, A, B, C, X, Y, Z, E, m, n, and p have the meaning as describe
Design, synthesis, biological evaluation and molecular modeling of novel 2-amino-4-(1-phenylethoxy) pyridine derivatives as potential ROS1 inhibitors
Tian, Yuanxin,Zhang, Tingting,Long, Lifan,Li, Zhonghuang,Wan, Shanhe,Wang, Guangfa,Yu, Yonghuan,Hou, Ju,Wu, Xiaoyun,Zhang, Jiajie
, p. 182 - 199 (2017/11/27)
With the aim of discovering potential and selective inhibitors targeting ROS1 kinase, we rationally designed, synthesized and evaluated two series of novel 2-amino-pyridine derivatives with 1-phenylethoxy at C-3 and C-4 position. The enzymic assays results indicated that six of the new compounds 13b-13d and 14a-14c showed remarkably higher inhibitory activities against ROS1 kinase. The most promising compounds, 13d and 14c displayed the most desired ROS1 inhibitory activity with IC50 values of 440 nM and 370 nM respectively. Furthermore, 13d and 14c displayed ROS1 inhibitory selectivity of about 7-fold and 12-fold, relative to that of ALK sharing about 49% amino acid sequence homology in the kinase domains. They also showed good anti-proliferative effects against ROS1-addicted HCC78 cell lines with the IC50 values of 8.1 μM and 65.3 μM, respectively. Moreover, molecular docking and molecular dynamics simulation studies disclosed that compound 14c and 13d shared similar binding poses with Crizotinib except the selective binding site of ROS1. It also gave a probable molecular explanation for their activity and selectivity, which the methoxyl group in benzene ring was the crucial to the selectivity to ROS1 versus ALK.
3-(1-(aminopyridine oxy)ethyl)benzamide derivative, and synthesis method and application thereof
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Paragraph 0064; 0069-0071, (2017/07/19)
The invention discloses a 3-(1-(aminopyridine oxy) ethyl) benzamide derivative, and a synthesis method and application thereof. The 3-(1-(aminopyridine oxy)ethyl)benzamide derivative or pharmaceutically acceptable salts, hydrates, solvates, polymorphic su
SUBSTITUTED DICYANOPYRIDINES AND USE THEREOF
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Paragraph 0514-0517, (2013/08/28)
The present application relates to novel substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders.
Pharmaceutically active phenylcarboxylic acid derivatives
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, (2008/06/13)
Compounds which antagonize the slow-reacting substance of anaphylaxis or components thereof, e.g., leukotrienes, in warm blooded animals as well as intermediates and methods for their preparation, pharmaceutical compositions and methods for their administration. The compounds are diphenyl carboxylic acids with particular linking groups between the individual phenyl rings and the carboxylic acid moiety. Particular utilities are to relieve asthma and inflammation in man.
