81171-71-3Relevant academic research and scientific papers
Synthetic method of isothiocyanate liquid crystal monomers
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Paragraph 0033-0040, (2021/01/30)
The invention discloses a synthetic method of isothiocyanate liquid crystal monomers. The synthetic method comprises the following steps: taking a halogenated aniline as a raw material, firstly preparing an active intermediate of an isothiocyanate group, reacting with different coupling substrates, and then purifying to obtain a series of isothiocyanate liquid crystal monomers. The method comprises the steps of salifying, isothiocyanic acid esterification, coupling and purification to finally obtain the product. According to the method, the reaction paths and post-treatment are optimized, andhigh yield is achieved while the product purity is guaranteed.
GLP-1R AGONISTS AND USES THEREOF
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Page/Page column 59; 117; 118, (2020/10/21)
Provided herein are compounds of Formula (I) and pharmaceutical compositions thereof, for use in, e.g. treating type 2 diabetes mellitus, pre-diabetes, obesity, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and cardiovascular disease.
NOVEL BENZIMIDAZOLE BASED EGFR INHIBITORS
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Page/Page column 12, (2016/06/15)
The present invention disclosed a novel EGFR inhibitor compound of formula (I), process for preparation thereof and methods of treating abnormal cell growth in mammals by administering the compounds of formula (I). Wherein, R= -H, 3-CH3, 4-NO2, 4-Cl, 2-CH3, 4-CH3, 4-Br, 4-F R1= -H, -4-OCH3, -4-NO2,-2-NO2, -4-Cl, -2,4,6-CH3, -4-CH3, -2-F,4-Br, -4-CF3, -4-S-CH3, -4-Cl,-3-CF3, -3-S-CH3, -3,5-CF3, -2-S-CH3, -3-CF3,-4-OCF3, -Si-(CH3)3, -Si-(C2H5)3, (CH3)2-Si- C2H5.
Structural optimization and structure-activity relationships of N 2-(4-(4-methylpiperazin-1-yl)phenyl)- N 8-phenyl-9 H -purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations
Yang, Jiao,Wang, Li-Jiao,Liu, Jing-Jing,Zhong, Lei,Zheng, Ren-Lin,Xu, Yong,Ji, Pan,Zhang, Chun-Hui,Wang, Wen-Jing,Lin, Xing-Dong,Li, Lin-Li,Wei, Yu-Quan,Yang, Sheng-Yong
, p. 10685 - 10699 (2013/02/22)
This paper describe the structural optimization of a hit compound, N 2-(4-(4-methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine- 2,8-diamine (1), which is a reversible kinase inhibitor targeting both EGFR-activating and drug-resistance (T790M) mutations but has poor binding affinity. Structure-activity relationship studies led to the identification of 9-cyclopentyl-N2-(4-(4-methylpiperazin-1-yl)phenyl)-N 8-phenyl-9H-purine-2,8-diamine (9e) that exhibits significant in vitro antitumor potency against the non-small-cell lung cancer (NSCLC) cell lines HCC827 and H1975, which harbor EGFR-activating and drug-resistance mutations, respectively. Compound 9e was further assessed for potency and selectivity in enzymatic assays and in vivo anti-NSCLC studies. The results indicated that compound 9e is a highly potent kinase inhibitor against both EGFR-activating and resistance mutations and has good kinase spectrum selectivity across the kinome. In vivo, oral administration of compound 9e at a dose of 5 mg/kg caused rapid and complete tumor regression in a HCC827 xenograft model, and an oral dose of 50 mg/kg initiated a considerable antitumor effect in an H1975 xenograft model.
Novel 5- and 6-subtituted benzothiazoles with improved physicochemical properties: Potent S1P1 agonists with in vivo lymphocyte-depleting activity
Frohn, Mike,Cee, Victor J.,Lanman, Brian A.,Pickrell, Alexander J.,Golden, Jennifer,Rivenzon-Segal, Dalia,Middleton, Scot,Fiorino, Mike,Xu, Han,Schrag, Michael,Xu, Yang,McElvain, Michele,Muller, Kristine,Siu, Jerry,Bürli, Roland
supporting information; experimental part, p. 628 - 633 (2012/03/11)
An SAR campaign designed to increase polarity in the 'tail' region of benzothiazole 1 resulted in two series of structurally novel 5-and 6-substituted S1P1 agonists. Structural optimization for potency ultimately delivered carboxamide (+)-11f,
