153037-40-2Relevant articles and documents
A kind of the heart fades the medicine Entresto key intermediate (R)- tert-butyl (1 - ([1, 1' - biphenyl] - 4 - yl) - 3 - hydroxy - 2 - yl) carbamate preparation method
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Paragraph 0064-0066, (2017/10/06)
The invention relates to a preparation method of a drug key intermediate, particularly a method for preparing (R)-tert-butyl-(1-([1,1'-biphenyl]-4-yl)-3-hydroxypropane-2-yl)carbamate by chiral resolution. The method has the advantages of cheap and accessible raw materials, low production cost, high separation yield and high chiral purity of the product, and is simple to operate, friendly to the environment and suitable for industrial production.
New thiazole carboxamides as potent inhibitors of Akt kinases
Chang, Shaohua,Zhang, Zhang,Zhuang, Xiaoxi,Luo, Jinfeng,Cao, Xianwen,Li, Honglin,Tu, Zhengchao,Lu, Xiaoyun,Ren, Xiaomei,Ding, Ke
supporting information; experimental part, p. 1208 - 1212 (2012/03/11)
A new series of 2-substituted thiazole carboxamides were identified as potent pan inhibitors against all three isoforms of Akt (Akt1, Akt2 and Akt3) by systematic optimization of weak screening hit N-(1-amino-3-phenylpropan-2-yl)- 2-phenylthiazole-5-carboxamide (1). One of the most potent compounds, 5m, inhibited the kinase activities of Akt1, Akt2 and Akt3 with IC50 values of 25, 196 and 24 nM, respectively. The compound also potently inhibited the phosphorylation of downstream MDM2 and GSK3β proteins, and displayed strongly antiproliferative activity in prostate cancer cells. The inhibitors might serve as lead compounds for further development of novel effective anticancer agents.
PHOSPHONO SUBSTITUTED TETRAZOLE DERIVATIVES AS ECE INHIBITORS
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, (2008/06/13)
The present invention relates to the N-phosphonomethyl substituted compounds of formula STR1
PHOSPHONO/BIARYL SUBSTITUTED AMINO ACID DERIVATIVES
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, (2008/06/13)
The present invention relates to the N-phosphonomethyl-biaryl substituted amino acid derivatives of formula I STR1 wherein X represents a direct bond, C 1-4-alkylene or C 2-C 4-alkenylene; R and R' represent independently hydrogen, carbocyclic aryl, 6-tet