CAS: 81486-22-8; [8-[2-Hydroxy-3-(Propan-2-Ylamino)Propoxy]-3,4-Dihydro-2H-Chromen-3-Yl] Nitrate

该化合物是一种非选择性乙型肾上腺素受体对立物,增加了甲型一型肾上腺阻塞活动,主要用于高血压和青光眼的管理.它的双重行动机制通过减少水力幽默生产和血管变异,可以有效减少体内压力和系统血压.该化合物呈现出一种有利的药用动能特征,包括良好的生物利用率和平衡的行动持续时间.Nipradol 的竞争性受体对立能确保有针对性的治疗效果,同时最大限度地减少不良反应.其化学稳定性和特征完善的合成途径进一步支持其药剂配方的效用.研究表明,由于其互补性的药用特性,它具有综合治疗的潜力.

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    CAS号2173-78-6 (2-methoxy-6-pr... | CAS号91520-04-6 (8-methoxy-3,4-... | CAS号91520-02-4 [2-methoxy-6-(o... | CAS号91520-01-3 3,4-二氢-8-甲氧基-2H... | CAS号81486-17-1 3,4-二氢-2H-1-苯并吡... | CAS号81486-20-6 3,4-Dihydro-2H-... | CAS号81486-21-7 3,4-dihydro-8-(... | CAS号75-31-0 异丙胺

    合成工艺路线路线简述

    • 合成目标产物 Nipradilol 主要起始原料 3,4-Dihydro-8-Methoxy-2H-1-Benzopyran-3-Ol
    • (文献来源)合成步骤主要原料 3,4-Dihydro-8-Methoxy-2H-1-Benzopyran-3-Ol
    📜3,4-二氢-8-甲氧基-2H-1-苯并吡喃-3-醇置于sodium Hydroxide,氢溴酸,硝酸,氯甲酸乙酯,乙酸酐,三乙胺体系中,用 甲醇 作为反应溶剂,化学反应 14.0H,反应生成 尼普地洛
    参考文献:苯并吡喃衍生物的合成及其降压活性.
    标题:苯并吡喃衍生物的合成及其降压活性.
    摘要:合成了一系列包含硝氧基的二氢苯并吡喃醇胺和二氢苯并吡喃乙醇胺.对这些化合物在麻醉犬中的心血管效果进行了研究.部分化合物表现出与β-肾上腺素受体拮抗和扩血管作用相结合的降血压活性.讨论了结构与活性之间的关系.
    DOI:10.1248/cpb.35.632

    海关参考信息

    专利信息


    专利号:US-9353057-B2
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
    权利人:XENOPORT INC
    摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

    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: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-2015158809-A9
    优先权日:2013-02-26
    标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
    发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
    权利人:XENOPORT INC
    摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献

    1. Tomita H, Nakazawa T, Sugano E, Abe T, Tamai M. Nipradilol inhibits apoptosis by preventing the activation of caspase-3 via S-nitrosylation and the cGMP-dependent pathway. Eur J Pharmacol. 2002 Oct 11;452(3):263-8. doi: 10.1016/s0014-2999(02)02329-4.

    合成参考文献


    摘要:Iyakuhin Kenkyu. Study of Medical Supplies., 20(228), 1989
    摘要:Oyo Yakuri. Pharmacometrics., 29(725), 1985
    参考文献:10.2165/00044011-199816030-00009
    摘要:Aramaki T, Katsuta Y, Sekiyama T, Tsutsui H, Kome-Ichi H, Ohsuga M, Satomura K, Yoshimura M. Effects of Aging and Liver Disease upon the Pharmacokinetics of Nipradilol. Clin Drug Investig. 1998;16(3):251–7. doi: 10.2165/00044011-199816030-00009.
    参考文献:10.1007/bf01745104
    摘要:Araki J, Takaki M, Matsushita T, Matsubara H, Suga H. Postextrasystolic transient contractile alternans in canine hearts. Heart Vessels. 1994;9(5):241–8. doi: 10.1007/bf01745104.
    参考文献:10.1007/bf02481741
    摘要:Mizuno J, Araki J, Iribe G, Maesako M, Morita T, Miyaji K, Imaoka T, Mohri S, Sano S, Ohe T, Hirakawa M, Suga H. Total Ca handling in canine mild Ca overload failing heart. Heart Vessels. 1999;14(1):38–51. doi: 10.1007/bf02481741.
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