专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-7034154-B2 优先权日:1999-08-10 标 题:Synthesis of substituted pyrazolopyrimidines 发明人:GROSS RAYMOND S; WILCOXEN KEITH M; OGLESBY RICHARD CHRISTOPHER 权利人:NEUROCRINE BIOSCIENCES INC 摘要:Methods of making substituted pyrazolopyrimidines generally and, more particularly, N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide. Such compounds have utility over a wide range of indications, including treatment of insomnia. In the practice of the present invention, improved techniques which do not require use and/or isolation of the pyrazole intermediate are disclosed, as well as improved techniques for making the reaction intermediates themselves. Such techniques offer significant advantages, including enhanced efficiency, particularly in the context of large scale manufacture.
专利号:US-7498434-B2 优先权日:2004-01-14 标题:Two-phase method for the synthesis of selected pyrazolopyrimidines 发明人:CANTRELL GARY LEE; MOSER FRANK WILLIAM; HALVACHS ROBERT EDWARD 权利人:MALLINCKRODT INC 摘要:An improved method of making a substituted pyrazolopyrimidine. The method comprises reacting a aminopyrazole compound or a salt thereof with a substituted 1-oxo-2-propenyl-arene(-heterocycle) or a salt thereof under acidic conditions in a reaction medium including a two-phase mixture of an aqueous solution and a water-immiscible organic liquid. Specific substituted pyrazolopyrimidines include N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide and N-methyl-N-(3-{3-[2-thienyl-carbonyl]-pyrazolo[1,5-a]-pyrimidin-7-yl}phenyl)acetamide.
专利号:US-7304069-B2 优先权日:2004-10-18 标题 :Hydrate of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5α]-pyrimidin-7-yl}phenyl)acetamide and processes and methods related thereto 发明人:ZOOK SCOTT E; HETTINGER DONALD 权利人:NEUROCRINE BIOSCIENCES INC 摘要:A novel hydrate form of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide (“Compound No. 1†) and processes related to the use thereof in the synthesis of a polymorphic form of Compound No. 1.
专利号:US-7309799-B2 优先权日:2004-06-01 标 题:Methods for the synthesis of milnacipran and congeners thereof 发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V 权利人:COLLEGIUM PHARMACEUTICAL INC 摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.
专利号:US-2018370905-A1 优先权日:2013-04-05 标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same
1: Shimizu M, Fukami T, Ito Y, Kurokawa T, Kariya M, Nakajima M, Yokoi T. Indiplon is hydrolyzed by arylacetamide deacetylase in human liver. Drug Metab Dispos. 2014 Apr;42(4):751-8. doi: 10.1124/dmd.113.056184. Epub 2014 Jan 24. doi: 10.1016/j.bmcl.2011.12.013. Epub 2011 Dec 9. 4: Marrs JC. Indiplon: a nonbenzodiazepine sedative-hypnotic for the treatment of insomnia. Ann Pharmacother. 2008 Jul;42(7):1070-9. doi: 10.1345/aph.1K683. Epub 2008 Jul 1. doi: 10.1185/030079908X273327. Epub 2008 Feb 6. 7: Lankford A. Indiplon in the treatment of sleep disorders. Neuropsychiatr Dis Treat. 2007 Dec;3(6):765-73.
合成参考文献
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