CAS: 87679-71-8; (2S,3Ar,7As)-1-[(2S)-2-[[(1S)-1-Carboxy-3-Phenylpropyl]Amino]Propanoyl]-2,3,3A,4,5,6,7,7A-Octahydroindole-2-Carboxylic Acid

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群多普利 Trandolapril 87679-37-6

📜群多普利置于recombinant Human Carboxylesterase 1,水体系中,用 Aq. Phosphate Buffer 作为反应溶剂,化学反应 0.17H,反应生成 群多普利
参考文献:In Vitro Drug Metabolism By Human Carboxylesterase 1: Focus On Angiotensin-Converting Enzyme Inhibitors
标题:In Vitro Drug Metabolism By Human Carboxylesterase 1: Focus On Angiotensin-Converting Enzyme Inhibitors
摘要:羧基酯酶 1(ces1)是人体肝脏中的主要水解酶.该酶参与了多种重要治疗药物,滥用药物和内源性化合物的代谢.然而,还没有研究描述过人 Ces1 在激活两种常用的血管紧张素转换酶抑制剂依那普利和雷米普利中的作用.在这里,我们研究了重组人 Ces1 和 Ces2 介导的依那普利和雷米普利原药酯的水解活化,并与已知底物曲托普利的活化进行了比较.依那普利,雷米普利和曲多普利很容易被 Ces1水解,但不被 Ces2水解.雷米普利和曲多普利表现出 Michaelis-Menten 动力学,而依那普利则表现出底物抑制动力学.雷米普利,曲妥拉普利和依那普利的内在清除率分别为 1.061,0.360 和 0.02 毫升/分钟/毫克蛋白质.此外,我们还筛选了一系列治疗药物和滥用药物,以评估它们对重组 Ces1 和人肝微粒体水解对硝基苯乙酸酯的抑制作用.筛选试验证实了几种已知的 Ces1 抑制剂,并发现了两种以前未报道过的抑制剂:二氢吡啶类钙拮抗剂异拉地平和免疫抑制剂他克莫司.ces1 在用于治疗高血压,充血性心力衰竭和糖尿病等常见疾病的多种药物的代谢过程中发挥作用,因此有可能发生临床相关的药物相互作用.本研究的发现可能有助于预测这种相互作用,从而为更安全的药物治疗提供可能.
DOI:10.1124/dmd.113.053512

专利信息

专利号:US-7973173-B2
优先权日:2005-07-05
标 题:Process for the synthesis of an ACE inhibitor
发明人：KANKAN RAJENDRA NARAYANRAO; RAO DHARMARAJ RAMACHANDRA; PHULL MANJINDER SINGH; SAWANT ASHWINI; BIRARI DILIP RAMDAS
权利人:CIPLA LTD
摘要:A process for the synthesis of trandolapril which comprises condensing N—[I—(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride with trans octahydro-1H-indole-2-carboxylic acid in a first organic solvent comprising a water immiscible inert organic solvent and in the presence of a base, and isolating trandolapril from a second organic solvent. N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride may also be condensed with (2S,3aR,7aS) octahydro-1H-indole-2-carboxylic acid in a first organic solvent and in the presence of a base, and trandolapril isolated. There is also provided a process for the resolution of racemic trans octahydro-1H-indole-2-carboxylc acid.

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-2007225505-A1
优先权日:2003-11-25
标题 :Method for the Preparation of (2S, 3AR, 7AS)-Octahydro-III-Indole-2-Carboxylic Acid as Key Intermediate in the Preparation of Trandolapril by Reacting a Cyclohexyl Aziridine with a Dialkyl Malonate
发明人：CID PAU
权利人:CID PAU
摘要:A method for the synthesis of a compound of formula I as a mixture of enantiomers, n n n(wherein R 1 is H or an acid protective group and H + A − indicates an optional acid with which the compound of formula I may form an ammonium salt) nsaid method comprising; A) reacting a cyclohexyl aziridine with a dialkyl malonate, whereby to provide a trans-fused 3-alkylcarbonyl-octahydro-indol-2-one; B) decarbonylation at the 3-position, conversion of the ketone of the resulting trans-octahydro-indol-2-one to an optionally protected carboxylic acid group; and C) optionally removing any N-substitution if necessary.

专利号:US-8288565-B2
优先权日:2009-07-16
标题 :Process for the synthesis of (2S,3AR,7AS)-octahydro-1H-indole carboxylic acid as an intermediate for trandolapril
发明人：CHEMBURKAR SANJAY R; REDDY RAJARATHNAM E; REAMER DOUGLAS M; PAVLINA JOHN T; ULREY STEPHEN S; KOTECKI BRIAN J
权利人:CHEMBURKAR SANJAY R; REDDY RAJARATHNAM E; REAMER DOUGLAS M; PAVLINA JOHN T; ULREY STEPHEN S; KOTECKI BRIAN J; ABBOTT LAB
摘要:A process for the preparation of (2S,3aR,7aS)-octahydro-1H-indole-20carboxylic acid hydrochloride.

专利号:US-2009069574-A1
优先权日:2005-07-05
标 题:Process for the synthesis of an ace inhibitor

专利号:CA-2614099-A1
优先权日:2005-07-05
标题 :Process for the synthesis of the ace inhibitor