CAS: 86780-90-7; Aranidipine

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CAS号86780-89-4 2,2-ethylenedio... | CAS号86780-80-5 2,2-ethylenedio... | CAS号39562-27-1 3-酮基-2-邻硝亚苄基-丁酰苯胺 | CAS号105-45-3 乙酰乙酸甲酯 | CAS号103785-52-0 2,2-ethylenedio... | CAS号552-89-6 邻硝基苯甲醛

📜2,2-Ethylenedioxypropyl Methyl 1,4-Dihydro-2,6-Dimethyl-4-(2-Nitrophenyl)-3,5-Pyridinedicarboxylate置于溶剂黄146体系中,用 水 作为反应溶剂,化学反应 10.0H,以92%的收率获得产物阿雷地平
参考文献:Synthesis Of Asymmetric 4-Aryl-1,4-Dihydro-2,6-Dimethyl-3,5-Pyridinedicarboxylates With Vasodilating And Antihypertensive Activities.
标题:Synthesis Of Asymmetric 4-Aryl-1,4-Dihydro-2,6-Dimethyl-3,5-Pyridinedicarboxylates With Vasodilating And Antihypertensive Activities.
摘要:合成了非对称的4-芳基-1,4-二氢-2,6-二甲基-3,5-吡啶二羧酸酯,其中含有2-乙烯二氧丙基,2-氧丙基或环丙基甲基作为酯基,以及相关衍生物,并进行了在麻醉开放胸腔犬中的扩血管活性及在意识清醒的自发性高血压大鼠中的抗高血压活性测试.环丙基甲基甲基1,4-二氢-2,6-二甲基-4-(3-硝基苯基)-3,5-吡啶二羧酸酯(5F,Mpc-2101)和甲基2-氧丙基1,4-二氢-2,6-二甲基-4-(2-硝基苯基)-3,5-吡啶二羧酸酯(8I,Mpc-1304)分别表现出强效的脑扩血管和抗高血压活性.在3.0 μg/kg的静脉给药后,5F对脊椎血流的最大增加为221.4%,而硝苯地平和尼卡地平氯化物分别为187.0%和166.3%.8I在0.3和1.0 Mg/kg口服给药后的收缩压最大下降分别为42.2和54.0 Mmhg,而硝苯地平,尼卡地平和肼苯噻啶氯化物在3.0 Mg/kg时的最大下降分别为23.3,16.8和24.5 Mmhg.5F和8I的显著扩血管和抗高血压效果持续时间比硝苯地平和尼卡地平更长.
DOI:10.1248/cpb.34.1589

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-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.

专利号:US-7235237-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 present invention provides methods of treating or preventing vascular diseases caused by nitric oxide (NO) insufficiency. The methods encompass administering a composition comprising an antioxidant, a compound to treat cardiovascular diseases, a nitrosated compound, a compound that donates, transfers or relases NO, or is a NO synthase substrate, or endogenously stimulates NO synthesis, or stimulates levels of endothelium derived relaxing factor. In the said composition, a hydralazine compound may be an antioxidant, isosorbide mono-or dinitrate may be the compound to donate, transfer, release, or stimulate endogenous NO synthesis. The isorsorbide may also elevate endogenous levels of endotherlium-derived relaxing factor, or be a NO synthase substrate and angiotensin enzyme inhibitor may be nitrosated compound. Disclosed in the invention is also a method to treat, or prevent Renaud's syndrome by administering a therapeutically effective amount of an antioxidant, a NO donor, a nitrosated compound and novel sustained-release formulations (e.g. a transdermal patch).