1465-76-5Relevant articles and documents
Acrylate as an efficient dimethylamine trap for the practical synthesis of 1-tert-butyl-4-piperidone via transamination
Amato, Joseph S.,Chung, John Y. L.,Cvetovich, Raymond J.,Reamer, Robert A.,Zhao, Dalian,Zhou, George,Gong, Xiaoyi
, p. 939 - 941 (2004)
Efficient trapping of dimethylamine was the key to success in the transamination of 1,1-dimethyl-4-oxopiperidinium iodide with tert-butylamine to afford 1-tert-butylpiperidin-4-one in high yield. The use of sodium acrylate was found to provide an elegant way to both trap dimethylamine and provide a convenient method to allow purification in the subsequent extraction.
Fused tricyclic hepatitis virus inhibitor and application thereof
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, (2016/12/26)
The invention belongs to the field of medical chemistry, relates to a fused tricyclic hepatitis virus inhibitor and application thereof, and particularly, provides a compound of the general formula I or pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug thereof, and a medicine composition containing the compounds and application of the compounds or the composition in medicine preparation. The compound has the good inhibiting activity on hepatitis C virus, meanwhile has the low toxicity on host cells, and is high in effectiveness, good in safety and likely to become the medicine for treating and/or preventing diseases relevant to HCV infection.
SPIROALKENE CARBOXAMIDE DERIVATIVES AND THEIR USE AS CHEMOKINE RECEPTOR MODULATORS
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, (2012/10/18)
The present invention is directed to compounds of Formula (I) below, which are antagonists to the chemoattractant cytokine receptor 2 (CCR2), and/or 5 (CCR5), pharmaceutical compositions, and methods for use thereof.
5-Hydroxyindole-2-carboxylic acid amides: Novel histamine-3 receptor inverse agonists for the treatment of obesity
Pierson, Pascale David,Fettes, Alec,Freichel, Christian,Gatti-McArthur, Silvia,Hertel, Cornelia,Huwyler, J?rg,Mohr, Peter,Nakagawa, Toshito,Nettekoven, Matthias,Plancher, Jean-Marc,Raab, Susanne,Richter, Hans,Roche, Olivier,Sarmiento, Rosa María Rodríguez,Schmitt, Monique,Schuler, Franz,Takahashi, Tadakatsu,Taylor, Sven,Ullmer, Christoph,Wiegand, Ruby
supporting information; experimental part, p. 3855 - 3868 (2010/02/28)
Obesity is a major risk factor in the development of conditions such as hypertension, hyperglycemia, dyslipidemia, coronary artery disease, and cancer. Several pieces of evidence across different species, including primates, underscore the implication of the histamine 3 receptor (H3R) in the regulation of food intake and body weight and the potential therapeutic effect of H3R inverse agonists. A pharmacophore model, based on public information and validated by previous investigations, was used to design several potential scaffolds. Out of these scaffolds, the 5-hydroxyindole-2-carboxylic acid amide appeared to be of great potential as a novel series of H3R inverse agonist. Extensive structure-activity relationships revealed the interconnectivity of microsomal clearance and hERG (human ether-a-go-go-related gene) affinity with lipophilicity, artificial membrane permeation, and basicity. This effort led to the identification of compounds reversing the (R)-R-methylhistamine-induced water intake increase in Wistar rats and, further, reducing food intake in diet-induced obese Sprague-Dawley rats. Of these, the biochemical, pharmacokinetic, and pharmacodynamic characteristics of (4,4-difluoropiperidin- 1-yl)[1-isopropyl-5-(1-isopropylpiperidin-4-yloxy)-1H-indol-2-yl]-methanone 36 are detailed.