📜H-Ala-Obzl,(S)-2-Acetylthiomethyl-3-(3,4-Methylenedioxyphenyl)Propionic Acid置于h-Ala-Obzl体系中,用76的收率获得法西多曲 参考文献:Process For The Synthesis Of .Alpha.-Substituted Acrylic Acids And Their 标题:Process For The Synthesis Of .Alpha.-Substituted Acrylic Acids And Their 摘要:通式(I)的α-取代丙烯酸的合成过程及其应用于通式(II)的n-(巯基酰基)氨基酸衍生物的合成. ##str1##
专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:CN-1931854-A 优先权日:2005-09-16 标题:Intermediates used in the synthesis of facidotril and its use in the synthesis
专利号:EP-1836163-B1 优先权日:2004-12-23 标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin 发明人:BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER 权利人:NOVARTIS AG 摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.
专利号:EP-1205476-A1 优先权日:2000-11-09 标题:Process for the synthesis of N-(mercaptoacyl)-amino acids derivatives from alpha-substituted acrylic acids
专利号:TW-201518323-A 优先权日:2013-07-25 标题 :Synthesis of biological conjugates of APELIN polypeptides
1: Inoue M, Sasaki T, Takazawa H, Morita T, Narisawa A, Saito A, Midorikawa H, Nishijima M. Symptomatic vasospasm in elderly patients with aneurysmal subarachnoid hemorrhage: comparison with nonelderly patients. Acta Neurochir Suppl. 2013;115:281-4. doi: 10.1007/978-3-7091-1192-5_50. Review. Review. Review.
合成参考文献
参考文献:10.2165/00126839-199901040-00011 摘要:Kentsch M, Otter W. Novel neurohormonal modulators in cardiovascular disorders. The therapeutic potential of endopeptidase inhibitors. Drugs R D. 1999 Apr;1(4):331–8. doi: 10.2165/00126839-199901040-00011. 参考文献:10.2165/00126839-199901040-00012 摘要:Coleman SG, Duff R. Endopeptidase inhibitors. Summary and table. Drugs R D. 1999 Apr;1(4):339–40. doi: 10.2165/00126839-199901040-00012. 参考文献:10.2165/00126839-199901040-00015 摘要:Fasidotril. Aladotril, alatriopril, BP 1137. Drugs R D. 1999 Apr;1(4):346–7. doi: 10.2165/00126839-199901040-00015.