CAS: 484-23-1; 1,4-Dihydrazinylphthalazine

该化合物是一种主要用作抗血压剂的药物化合物,属于氢氨衍生物,以其放松血管血管,从而降低血压的能力而著称,二氢氨的化学结构具有氢氨酸混合物,有助于其生物活动,通常以盐酸盐的形式施用,提高其溶性和生物利用率;二氢氨作为血管通气剂,抑制血管滑动肌肉的收缩,这可能导致血液流动增加和血管抗药性下降;常见副作用包括头痛,淋巴和胃肠扰动;由于其作用机制,二氢氨酸经常与其他抗血压药物结合使用,以更好地控制血压;重要的是监测病人可能受到的不利影响,特别是在先有心血管疾病的人.与任何药物一样,二氢氨的使用应当由保健专业人员指导,考虑到个别的病人因素和潜在的药物相互作用.

结构式图片

上下游产品

2,3-dihydro-phthalazine-1,4-dithione 1-Chloro-4-methoxyphthalazine 1-chloro-4-ethoxyphthalazine 1-chloro-4-hydrazinophthalazine1,4-bis-benzylidenehydrazino-phthalazine 1,4-Bis(5'-(4-chlorobenzylidene)-2'-methyl-4'-imidazolinone-3'-ylamino)phthalazine 1,4-Bis(5'-(2-chlorobenzylidene)-2'-methyl-4'-imidazolinone-3'-ylamino)phthalazine 1,4-Bis(5'-(3-methoxybenzylidene)-2'-methyl-4'-imidazolinone-3'-ylamino)phthalazine

合成工艺路线路线简述

    1-Chloro-4-Hydrazinophthalazine置于一水合肼体系中,化学反应生成 双肼酞嗪
    参考文献:De847748
    标题:De847748

    海关参考信息

    专利信息


    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:WO-2024061972-A1
    优先权日:2022-09-20
    标 题:Methods and platform for chemical synthesis
    发明人:CRONIN LEE; MANZANO SEBASTIÃ?N; ZALESSKIY SERGEY; KITSON PHILIP; WANG HSIN
    权利人:UNIV GLASGOW COURT
    摘要:The invention relates to a method and apparatus for performing and characterising a chemical synthesis, such as those performed with an automated chemical synthesis platform, including such that are portable platforms, the method comprising the steps of: performing a chemical synthesis in a chemical synthesiser; recording analytical data during the chemical synthesis, and developing a profile for the analytical data recorded over time; and comparing the profile for the chemical synthesis against a reference profile, which reference profile is the analytical data recorded over time for a reference chemical synthesis, wherein the chemical synthesis and the reference chemical synthesis share at least the same reagents and method steps for the same intended product, such as the chemical synthesis and the reference chemical synthesis sharing the same instruction set. The method and apparatus are for intended for use in replication of approved, chemical syntheses based on common reaction platforms.

    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).
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    主要参考文献


    1: Boulebd H, Khodja IA, Bay MV, Hoa NT, Mechler A, Vo QV. Thermodynamic and Kinetic Studies of the Radical Scavenging Behavior of Hydralazine and Dihydralazine: Theoretical Insights. J Phys Chem B. 2020 May 21;124(20):4123-4131. doi: 10.1021/acs.jpcb.0c02439. Epub 2020 May 6. 81(8):1147-1162. doi: 10.1007/s10337-018-3555-8. Epub 2018 Jun 25.
    3: Sridharan K, Sequeira RP. Drugs for treating severe hypertension in pregnancy: a network meta-analysis and trial sequential analysis of randomized clinical trials. Br J Clin Pharmacol. 2018 Sep;84(9):1906-1916. doi: 10.1111/bcp.13649. Epub 2018 Jul 8.
    4: Reinen J, Smit M, Wenker M. Evaluation of Strategies for the Assessment of Drug-Drug Interactions Involving Cytochrome P450 Enzymes. Eur J Drug Metab Pharmacokinet. 2018 Dec;43(6):737-750. doi: 10.1007/s13318-018-0485-7.

    合成参考文献


    摘要:Hagen, T. J.; Helgren, T. R., Science of Synthesis Knowledge Updates, (2015) 2, 162.
    摘要:United States Patent Document., #4376771
    摘要:Digestion., 27(47), 1983 []
    摘要:European Journal of Medicinal Chemistry--Chimie Therapeutique., 11(107), 1976
    参考文献:10.1007/bf00196814
    摘要:Meyer zum Büschenfelde KH, Dienes HP. Autoimmune hepatitis. Definition--classification--histopathology--immunopathogenesis. Virchows Arch. 1996 Sep;429(1):1–12. doi: 10.1007/bf00196814.
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