CAS: 87269-97-4; (2S,3As,6As)-1-(((S)-1-Carboxy-3-Phenylpropyl)-L-Alanyl)Octahydrocyclopenta[b]Pyrrole-2-Carboxylic Acid

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Ramipril

雷米普利置于porcine Liver Esterase体系中,用 Phosphate Buffer 作为反应溶剂,化学反应生成 雷米普利
参考文献:在血管紧张素转化酶抑制剂的体外比较试验中,卡托普利抑制由髓过氧化物酶引起的载脂蛋白b-100的氧化修饰.
标题:在血管紧张素转化酶抑制剂的体外比较试验中,卡托普利抑制由髓过氧化物酶引起的载脂蛋白b-100的氧化修饰.
摘要:低密度脂蛋白(ldl)的氧化修饰是形成动脉粥样硬化病变的关键事件.实际上,氧化衍生物在血管壁中积聚并促进局部炎症过程,从而触发动脉粥样斑块的进展.髓过氧化物酶(mpo)被认为是该氧化过程的主要贡献者.它参与脂质通过氯化和过氧化的氧化以及载脂蛋白b-100的氧化.基于对几种抗炎药和含硫醇药物的最新观察,本研究旨在检验以下假设:来自血管紧张素转化酶(ace)抑制剂组的抗高血压药可抑制apo B-100引起的氧化修饰mpo.卡托普利,雷米普利,依那普利,赖诺普利和福辛普利通过以下方法进行评估:测量它们对mpo / H(2)o(2)/ Cl(-)系统的抑制作用,化合物ii的积累,这反映了hocl的合成和ldl氧化的抑制作用mpo存在几种浓度的ace抑制剂.只有卡托普利(一种含硫醇的ace抑制剂)能够以剂量依赖的方式显着降低ldl的氧化修饰,而这是通过清除hocl来实现的.因此,这种有效的降压药似乎
DOI:10.1016/j.Ejphar.2006.03.022

专利信息

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:UA-77527-C2
优先权日:2002-06-20
标题:Benzoic acid derivatives as modulators of ppar alpha and ppar gamma, method of synthesis, pharmaceutical composition, intermediate

专利号:UA-77987-C2
优先权日:2001-12-19
标题:Substituted derivatives of phenylpropionic acid as agonists of peroxisome proliferators activated alpha receptor, method for synthesis, pharmaceutical composition, intermediate (variants)