CAS: 111011-63-3; 2-(Benzyl(Phenyl)Amino)Ethyl 5-(5,5-Dimethyl-2-Oxido-1,3,2-Dioxaphosphinan-2-yl)-2,6-Dimethyl-4-(3-Nitrophenyl)-1,4-Dihydropyridine-3-Carboxylate

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CAS号1005-69-2 2-methoxy-5,5-d... | CAS号111011-80-4 2-acetonyl-5,5-... | CAS号126-30-7 新戊二醇(NPG)

📜2-丙酮基-5,5-二甲基-2-氧代-1,3,2-二氧杂磷杂环己烷置于哌啶,溶剂黄146体系中,用 甲苯,苯 用作溶剂,化学反应 11.5H,反应生成依福地平
参考文献:Synthesis Of 1,4-Dihydropyridine-5-Phosphonates And Their Calcium-Antagonistic And Antihypertensive Activities. Novel Calcium-Antagonist 2-(Benzyl(Phenly)Amino)Ethyl 5-(5,5-Dimethyl-2-Oxo-1,3,2-Dioxaphosphorinan-2-yl)-1,4-Dihydro-2,6-Dimethyl-4-(3-Nitrophenyl)-3-Pyridinecarboxylate Hydrochloride Ethanol(Nz-105) And Its Crystal Structure.
标题:Synthesis Of 1,4-Dihydropyridine-5-Phosphonates And Their Calcium-Antagonistic And Antihypertensive Activities. Novel Calcium-Antagonist 2-(Benzyl(Phenly)Amino)Ethyl 5-(5,5-Dimethyl-2-Oxo-1,3,2-Dioxaphosphorinan-2-yl)-1,4-Dihydro-2,6-Dimethyl-4-(3-Nitrophenyl)-3-Pyridinecarboxylate Hydrochloride Ethanol(Nz-105) And Its Crystal Structure.
摘要:研究了3-羧酸酯变体在2,2-二甲基三甲基烯-3-烷氧羰基-4-芳基-1,4-二氢-2,6-二甲基-5-吡啶膦酸酯(1)中与钙拮抗和降压活性相关的影响:合成了含有不超过12个碳的烷基和羧酸酯部分含有氨基功能团的类似物,以检测其生物活性.其中,2-[苄基(苯基)氨基]乙基5-(5,5-二甲基-2-氧-1,3,2-二氧膦杂环己烷-2-基)-1,4-二氢-2,6-二甲基-4-(3-硝基苯基)-3-吡啶羧酸酯盐酸盐乙醇(Nz-105)显示出特别有益的活性,并被选中进行进一步的药理学研究和临床开发.描述了通过x射线晶体学分析获得的nz-105的结构-活性关系和固态结构的一些方面.
Doi:10.1248/cpb.40.2362

专利信息

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-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-7708989-B2
优先权日:1999-10-29
标题 :Methods of treating vascular diseases characterized by nitric oxide insufficiency
发明人：LOSCALZO JOSEPH; VITA JOSEPH A; LOBERG MICHAEL D; WORCEL MANUEL
权利人:NITROMED INC
摘要:The invention provides methods of treating and/or preventing vascular diseases characterized by nitric oxide insufficiency by administering a therapeutically effective amount of at least one nitrosated angiotensin-converting enzyme inhibitor, nitrosated beta-adrenergic blocker, nitrosated cholesterol reducer, nitrosated calcium channel blocker, nitrosated endothelin antagonist, nitrosated angiotensin II receptor antagonist, nitrosated renin inhibitor, and optionally at least one compound used to treat cardiovascular diseases and/or at least one antioxidant, or a pharmaceutically acceptable salt thereof, and/or 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. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The 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 may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The vascular diseases characterized by nitric oxide insufficiency include a cardiovascular disease and a disease resulting from oxidative stress.

专利号:EP-3967330-A1
优先权日:2020-09-10
标 题:Methods for the synthesis of bioactivated metal nanocluster and their medical application
发明人：MARCHI VALÉRIE; CHIECHIO REGINA MARIA; EVEN-HERNANDEZ PASCALE
权利人:UNIV RENNES; CENTRE NAT RECH SCIENT; INSTITUT NAT DES SCIENCES APPLIQUEES DE RENNES; ECOLE NAT SUPERIEURE DE CHIMIE DE RENNES
摘要:The present invention relates to a bioactivated metal nanocluster comprising a mixture of ligands linked to a fluorescent metallic nanocluster, their synthesis methods, and their medical applications.

专利号:US-7384976-B2
优先权日:2001-05-02
标 题:Nebivolol and its metabolites in combination with nitric oxide donors, compositions and methods of use
发明人：GARVEY DAVID S
权利人:NITROMED INC
摘要:The invention describes novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a 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 may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and/or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and/or preventing Raynaud's syndrome; and for treating and/or preventing cardiovascular diseases or disorders.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人：GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.