19073-14-4Relevant academic research and scientific papers
An efficient, simple synthesis of 4-azidobenzaldehyde
Walton, Richard,Lahti, Paul M.
, p. 1087 - 1092 (1998)
A three-pot synthesis of 4-azidobenzaldehyde from 4-nitrobenzaldehyde in overall yield of 71% is described. The new synthesis is superior in its ease of reproducibility and reduction of waste side products.
ANTIBIOTIC COMPOUNDS
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Paragraph 00115, (2021/04/02)
Provided herein are lipidated glycopeptide compounds of formula (I); or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof. R1 is a lipid, R2 is -H or a lipid, and R3 and R4 are as defined herein. These compounds have antibiotic activity. Also provided are formulations comprising such compounds; as well as such compounds or formulations for use as a medicament. The compounds and formulations may also be used in the treatment of bacterial infection.
Discovery of tert-amine-based RORγt agonists
Qiu, Ruomeng,Yu, Mingcheng,Gong, Juwen,Tian, Jinlong,Huang, Yafei,Wang, Yonghui,Xie, Qiong
, (2021/07/26)
The nuclear receptor retinoic acid receptor-related orphan receptor gamma-t (RORγt) is a transcription factor regulating Th17 cell differentiation and proliferation from naive CD4+ T cells. Since Th17 cells have demonstrated the antitumor efficacy by eliciting remarkable activation of CD8+ T cells, RORγt agonists could be applied as potential small molecule therapeutics for cancer immunotherapy. Based on the previously reported RORγt agonist 1 and its resolved co-crystal structure, a series of new tertiary amines were designed, synthesized and biologically evaluated, yielding optimal moieties with improved chemical properties and biological responses. The combination of these optimal moieties resulted in identification of novel RORγt agonists such as 8b with further elevated RORγt agonism responses at a target-based level as well as in cell-based assays, which provided some structural knowledge for further optimization of RORγt agonists as small molecule therapeutics for cancer immunotherapy.
Tertiary amine derivative or salt thereof, preparation method and application thereof
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Paragraph 0109; 0129; 0130; 0131, (2019/01/24)
Belonging to the technical field of chemical medicine, the invention relates to a tertiary amine RORgamma t regulator, in particular to a new tertiary amine compound or salt thereof with RORgamma t inhibition or agonist activity shown as general formula I, a preparation method and a pharmaceutical composition thereof. The tertiary amine compound or a salt thereof provided by the invention can be used for preparation of drugs treating or preventing RORgamma t receptor related diseases.
Carboxylic acid ester derivative and medical uses thereof
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Paragraph 0221-0224, (2019/07/04)
The invention relates to a compound represented by a general formula (I) or a stereoisomer, a hydrate, a metabolite, a solvate, a pharmaceutically acceptable salt, an eutectic or a prodrug thereof, and a preparation method thereof, and applications in pre
Dithienopyrrole Derivatives with Nitronyl Nitroxide Radicals and Their Oxidation to Cationic High-Spin Molecules
Baumgarten, Martin,Kolanji, Kubandiran
, (2020/03/13)
Three 1 N-phenyl nitronyl nitroxide (NN) 4-substituted dithieno[3,2-b:2′,3′-d]pyrrole (DTP) derivatives with R1=4-phenyl-, 4H-, and 4-methylthiothiophenyl- (R12DTP-Ph-NN, R1=H, Ph and MeSTh) were designed, synthesized and
Preparation method of prucalopride succinate
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Paragraph 0044; 0046; 0054; 0056; 0064; 0066, (2019/01/08)
The invention provides a preparation method of prucalopride succinate. The method comprises the steps that 4-nitrobenzaldehyde is taken as an initial raw material, and protected by formyl group, nitroreduction, amino protection, aromatic hydrocarbon chlor
Discovery of tertiary amine and indole derivatives as potent RORγt inverse agonists
Yang, Ting,Liu, Qian,Cheng, Yaobang,Cai, Wei,Ma, Yingli,Yang, Liuqing,Wu, Qianqian,Orband-Miller, Lisa A.,Zhou, Ling,Xiang, Zhijun,Huxdorf, Melanie,Zhang, Wei,Zhang, Jing,Xiang, Jia-Ning,Leung, Stewart,Qiu, Yang,Zhong, Zhong,Elliott, John D.,Lin, Xichen,Wang, Yonghui
supporting information, p. 65 - 68 (2014/02/14)
A novel series of tertiary amines as retinoid-related orphan receptor gamma-t (RORγt) inverse agonists was discovered through agonist/inverse agonist conversion. The level of RORγt inhibition can be enhanced by modulating the conformational disruption of H12 in RORγt LBD. Linker exploration and rational design led to the discovery of more potent indole-based RORγt inverse agonists.
CRYSTALLINE OXALATE SALTS OF A DIAMIDE COMPOUND
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Page/Page column 8, (2012/04/11)
The invention relates to crystalline oxalate salts of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]-methyl}phenylcarbamoyl)butyl]methylcarbamoyl}ethyl)piperidin-4-yl ester. This invention al
Structure-based design of novel boronic acid-based inhibitors of autotaxin
Albers, Harald M. H. G.,Hendrickx, Loes J. D.,Van Tol, Rob J. P.,Hausmann, Jens,Perrakis, Anastassis,Ovaa, Huib
supporting information; experimental part, p. 4619 - 4626 (2011/09/14)
Autotaxin (ATX) is a secreted phosphodiesterase that hydrolyzes the abundant phospholipid lysophosphatidylcholine (LPC) to produce lysophosphatidic acid (LPA). The ATX-LPA signaling axis has been implicated in inflammation, fibrosis, and tumor progression
