CAS: 167305-00-2; (4S,7S,10As)-4-((S)-2-Mercapto-3-Phenylpropanamido)-5-Oxooctahydro-7H-Pyrido[2,1-B][1,3]Thiazepine-7-Carboxylic Acid

上下游产品

(3S,7S,11S)-1-Aza-3-Benzyloxycarbonylamino-11-Methoxycarbonyl-2-Oxo-6-Thiabicyclo[5.4.0]Undecane 167305-43-3
[4S-(4α,7α,10Aβ)]-4-Amino-Octahydro-5-Oxo-7H-Pyrido[2,1-B] [1,3]Thiazepine-7-Carboxylic Acid, Methyl Ester 167304-98-5

📜L-6-羟基正亮氨酸置于n-甲基吗啉,盐酸,甲醇,Sodium Hydroxide,草酰氯,碘代三甲硅烷,Sodium Methylate,(Benzotriazo-1-Yloxy)Tris(Dimethylamino)Phosphonium Hexafluorophosphate,1-羟基苯并三唑,二甲基亚砜,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,三乙胺,三氟乙酸体系中,用 甲醇,二氯甲烷 用作溶剂,化学反应 50.67H,反应生成奥马曲拉
参考文献:Dual Metalloprotease Inhibitors: Mercaptoacetyl-Based Fused Heterocyclic Dipeptide Mimetics As Inhibitors Of Angiotensin-Converting Enzyme And Neutral Endopeptidase
标题:Dual Metalloprotease Inhibitors: Mercaptoacetyl-Based Fused Heterocyclic Dipeptide Mimetics As Inhibitors Of Angiotensin-Converting Enzyme And Neutral Endopeptidase
摘要:A Series Of 7,6-And 7,5-Fused Bicyclic Thiazepinones And Oxazepinones Were Generated And Incorporated As Conformationally Restricted Dipeptide Surrogates In Mercaptoacyl Dipeptides. These Compounds Are Potent Inhibitors Of Angiotensin-Converting Enzyme (Ace) And Neutral Endopeptidase (Nep) Both In Vitro And In Vivo. Compound 1A,A 7,6-Fused Bicyclic Thiazepinone,Demonstrated Excellent Blood Pressure Lowering In A Variety Of Animal Models Characterized By Various Levels Of Plasma Renin Activity And Significantly Potentiated Urinary Sodium,Anp,And Cgmp Excretion In A Cynomolgus Monkey Assay. On The Basis Of Its Potency And Duration Of Action,Compound 1A (Bms-186716) Was Advanced Into Clinical Development For The Treatment Of Hypertension And Congestive Heart Failure.
Doi:10.1021/jm970041E

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:WO-2024103123-A1
优先权日:2022-11-17
标题 :The synthesis of omapatrilat
发明人：VITALE ROMINA; MARTIN VINCENT ALEXANDRE; FABER WIJNAND; SOMMER ROMAN
权利人:ENDOTHELIUM SCANNING NANOTECHNOLOGY LTD
摘要:Described herein are improved methods of making Compound 1 (4S,7S,10aS)-4-((S)-2- mercapto-3-phenylpropanamido)-5-oxooctahydro-7H-pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid, or Omapatrilat, and purified Omapatrilat obtained from the improved methods.

专利号:US-6300503-B1
优先权日:1999-12-17
标 题 :Hydantoin intermediates for the synthesis of omapatrilat and methods for producing and using the same
发明人：RONGIONE JOSEPH C; BROWN ROBERT E; RAFF DWIGHT E
权利人:DIXIE CHEMICAL CO
摘要:Omapatrilat (I) is a potent inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP) both in vitro and in vivo and is currently undergoing large scale clinical trials as an anti-hypertensive. Omapatrilat may be synthesized using the S-stereoisomer of compound (V). Compound (V) may be prepared from a novel hydantoin (III). The hydantoin may be prepared from a monoacetal (XI) or via a dinitrile (V).

专利号:US-6284901-B1
优先权日:1999-12-17
标题:Dinitrile intermediates for the synthesis of omapatrilat and methods for producing same
发明人：RONGIONE JOSEPH C; BROWN ROBERT G; RAFF DWIGHT E
权利人:DIXIE CHEMICAL CO
摘要:Omapatrilat (I) is a potent inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP) both in vitro and in vivo and is currently undergoing large scale clinical trials as an anti-hypertensive. Omapatrilat may be synthesized using the S-stereoisomer of a racemic mixture. The racemic mixture may be prepared from a hydantoin (III). The hydantoin may be prepared from a novel dinitrile compound (IV):The dinitrile may be produced by reacting a monoacetal with a non-carbonate ammonium salt and an alkali cyanide.

专利号:WO-0217958-A1
优先权日:2000-08-29
标 题:Agent for influencing angiogenesis
发明人：BADER MICHAEL; PESQUERO JOAO BOSCO; MADEDDU PAOLO; EMAMUELI COSTANCA
权利人:MAX DELBRUECK CENTRUM; BADER MICHAEL; PESQUERO JOAO BOSCO; MADEDDU PAOLO; EMAMUELI COSTANCA
摘要:The invention relates to an agent for influencing angiogenesis, i.e. the new formation of blood vessels. The application areas for this agent are the medical field and the pharmaceutical industry. The aim of the invention is to discover new agents for influencing angiogenesis and to provide corresponding substances that can be used in the medical field to produce said agents. The inventive agent is characterised in that it influences angiogenesis, i.e. promotes or inhibits the latter. The promotion of angiogenesis is achieved, for example, by increasing the synthesis of the B1 receptor (transcription-mediated amplification, e.g. by cytokines), or by increasing its activity (agonistic substances). The inhibition of angiogenesis is achieved, for example, by antagonists of the kinin B1 receptor, such as des-Arg<9>-Leu<8>-bradykinin (DALBK) or non-peptide substances and by inhibiting the synthesis of the protein, e.g. using glucucorticoids.

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.