91591-69-4Relevant articles and documents
Site-Selective γ-C(sp3)?H and γ-C(sp2)?H Arylation of Free Amino Esters Promoted by a Catalytic Transient Directing Group
Lin, Hua,Wang, Chao,Bannister, Thomas D.,Kamenecka, Theodore M.
supporting information, p. 9535 - 9541 (2018/07/14)
The first selective PdII-catalysed γ-C(sp3)?H and γ-C(sp2)?H arylation of free amino esters using a commercially available catalytic transient directing group. A variety of free amino esters, including α-amino esters and β-amino esters, amino monoesters and amino bis-esters, are shown to react with a diverse range of simple aryl and heteroaryl iodide reagents.
PYRROLOPYRAZINE KINASE INHIBITORS
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Page/Page column 238; 239, (2013/03/28)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor
Tran, Joe A.,Jiang, Wanlong,Tucci, Fabio C.,Fleck, Beth A.,Wen, Jenny,Sai, Yang,Madan, Ajay,Ta, Kung Chen,Markison, Stacy,Foster, Alan C.,Hoare, Sam R.,Marks, Daniel,Harman, John,Chen, Caroline W.,Arellano, Melissa,Marinkovic, Dragan,Bozigian, Haig,Saunders, John,Chen, Chen
, p. 6356 - 6366 (2008/03/30)
Benzylamine and pyridinemethylamine derivatives were synthesized and characterized as potent and selective antagonists of the melanocortin-4 receptor (MC4R). These compounds were also profiled in rodents for their pharmacokinetic properties. Two compounds with diversified profiles in chemical structure, pharmacological activities, and pharmacokinetics, 10 and 12b, showed efficacy in an established murine cachexia model. For example, 12b had a Ki value of 3.4 nM at MC4R, was more than 200-fold selective over MC3R, and had a good pharmacokinetic profile in mice, including high brain penetration. Moreover, 12b was able to stimulate food intake in the tumor-bearing mice and reverse their lean body mass loss. Our results provided further evidence that a potent and selective MC4R antagonist with appropriate pharmacokinetic properties might potentially be useful for the treatment of cancer cachexia.