专利号:US-11040938-B2 优先权日:2016-07-27 标 题 :Continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts 发明人:MA BING; PAN SHUAI 权利人:SHANGHAI HYBRID—CHEM TECH; SHANGHAI HYBRID CHEM TECH 摘要:The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.
专利号:US-2007287734-A1 优先权日:2006-06-09 标 题 :Preparation and utility of substituted pyrazole compounds with cannabinoid receptor activity 发明人:GANT THOMAS G; SARSHAR SEPEHR 权利人:AUSPEX PHARMACEUTICALS INC 摘要:The present disclosure is directed to modulators of CB-1 type receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of the severity and duration of obesity, metabolic syndrome, dyslipidemia, glucose imbalance, the inability to maintain weight loss, insulin resistance, a cardiovascular disorder, memory loss, drug dependence, a depressive disorder, a panic disorder, an obsessive-compulsive disorder, anxiety, post-traumatic stress syndrome, and any other condition in which it is beneficial to inhibit, inversely agonize or modulate a cannabinoid receptor are described.
专利号:US-6132953-A 优先权日:1996-07-02 标 题 :Combinatorial synthesis on soluble polyvalent supports having a discrete architecture 发明人:CHAPMAN KEVIN T; HUTCHINS STEVEN M; KIM RONALD M; MANNA MAHUA 权利人:MERCK & CO INC 摘要:The present invention is directed to the use of a soluble polyvalent support for the preparation of combinatorial libraries of compounds. The resultant combinatorial libraries are useful in screening for biologically active moieties in the drug discovery process or in developing compounds with desired physical and chemical properties.
专利号:US-8461184-B2 优先权日:2006-05-31 标题 :Sulphur containing pyrazole derivatives as selective cannabinoid CB1 receptor antagonists 发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; VLIET VAN BERNARD J 权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; VLIET VAN BERNARD J; SOLVAY PHARM BV 摘要:The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB 1 receptor antagonists having a high CB 1 /CB 2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) n nwherein the symbols have the meanings given in the specification.
专利号:WO-2007138050-A1 优先权日:2006-05-31 标题:Sulphur containing pyrazole derivatives as selective cannabinoid cb1 receptor antagonists 发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; VAN VLIET BERNARD J 权利人:SOLVAY PHARM BV; LANGE JOSEPHUS H M; KRUSE CORNELIS G; VAN VLIET BERNARD J 摘要:The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
专利号:US-8044203-B2 优先权日:2002-05-10 标 题 :Chiral indole intermediates and their fluorescent cyanine dyes containing functional groups 发明人:MUJUMDAR RATNAKER B; WEST RICHARD MARTIN 权利人:UNIV CARNEGIE MELLON; GE HEALTHCARE UK LTD 摘要:This invention relates to the functionalized cyanine dyes and more particularly, to the synthesis of chiral 3-substituted 2,3′-dimethyl-3H-indole and its derivatives as intermediates for preparation of cyanine dyes, to methods of preparing these dyes and the dyes so prepared.
摘要:Sapeta, K.; Kerr, M. A., Science of Synthesis Knowledge Updates, (2011) 1, 18. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 35. 摘要:H.H. Stroh and G. Westphal. Chem. Ber. 97, 83 (1964).