CAS: 304-20-1; 1-Hydrazinylphthalazine Hydrochloride

该化合物是一种主要用作抗血压抗血压剂的药物化合物,被归类为血管消毒剂,这意味着通过放松血管,从而减少心脏的工作量.氢盐酸的化学配方为C8H8N4HHl,表明它含有一种对生物活动至关重要的氢.该化合物一般是口服或静脉注射,以其迅速行动闻名.盐酸盐的特征是白色到非白晶状的外表,在水中溶解,适合各种配方.常见副作用可能包括头痛,痛楚和胃肠扰动.重要的是监测病人潜在的不良反应,例如象lupus一样的症状,特别是长期使用.

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CAS号1044569-46-1 1-hydrazinophth... | CAS号54687-66-0 3-HYDROXYMETHYL... | CAS号234-80-0 S-三唑并[3,4-α]酞嗪 | CAS号20062-41-3 3-甲基-1,2,4-噻唑并[... | CAS号119-39-1 2,3-二氮杂萘酮 | CAS号65846-18-6 N'-(4-oxo-3H-ph... | CAS号79364-48-0 3-(D-galacto-pe... | CAS号56173-18-3 N-(propan-2-yli... | CAS号103429-70-5 N-phthalazin-1-... | CAS号103429-71-6 1,1-di(phthalaz... | CAS号103429-73-8 1,1,2-tri(phtha...

合成工艺路线路线简述

    2-Formylphenyl Tosylate置于palladium(II) Trifluoroacetate,肼基甲酸叔丁酯,1,3-双(二苯基膦)丙烷,Magnesium Sulfate,Potassium Carbonate,三氯氧磷体系中,用 乙腈 作为反应溶剂,60.0~140.0 °C,1.0 Mpa 条件下,反应 23.5H,反应生成 盐酸肼屈嗪
    参考文献:通过钯催化的2-甲酰基芳基甲苯磺酸盐,肼和co的三组分环氨基羰基化反应获得邻苯二氮酮
    标题:通过钯催化的2-甲酰基芳基甲苯磺酸盐,肼和co的三组分环氨基羰基化反应获得邻苯二氮酮
    摘要:已经建立了用肼和一氧化碳进行钯催化的2-甲酰基芳基甲苯磺酸酯的三组分环氨基羰基化反应,这为合成取代的邻苯二氮酮提供了一种有效的方法.此外,通过将该方案用作关键步骤,可以轻松以65%的产率合成肼屈嗪.
    DOI:10.1016/j.Tet.2016.10.065

    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-7220858-B2
    优先权日:2003-12-23
    标 题 :Synthesis of hydrazine and chlorinated derivatives of bicyclic pyridazines
    发明人:NELSON DEANNA J
    权利人:BARBEAU PHARMA INC
    摘要:The present invention relates to both a novel method of preparing hydralazine hydrochloride and to a novel method of preparing hydrazine derivatives of compounds containing a pyridazine ring, including, for example, pyridazines, phthalazines and other compounds containing the pyridazine ring.

    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-4713383-A
    优先权日:1984-10-01
    标 题:Triazoloquinazoline compounds, and their methods of preparation, pharmaceutical compositions, and uses
    发明人:FRANCIS JOHN E; GELOTTE KARL O
    权利人:CIBA GEIGY CORP
    摘要:[1,2,4]triazolo[1,5-c]quinazoline compounds of the formula wherein R1 is optionally substituted phenyl, pyridyl, furyl thienyl, dihydro or tetrahydro furanyl or thienyl, pyranyl, or 0-ribofuranosyl; R2 is hydrogen or lower alkyl; X is oxygen or NR3, R3 is as defined in the claims, and ring A is unsubstituted or substituted as set forth in the claims. The compounds wherein X is N-R3 are especially useful as adenosine antagonists and for the treatment of asthma. The compounds wherein X is oxygen are useful as benzodiazepine antagonists and as intermediates in the synthesis of the compounds wherein X is N-R3.
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    主要参考文献


    1: Ruiz-Magaña MJ, Martínez-Aguilar R, Lucendo E, Campillo-Davo D, Schulze-Osthoff K, Ruiz-Ruiz C. The antihypertensive drug hydralazine activates the intrinsic pathway of apoptosis and causes DNA damage in leukemic T cells. Oncotarget. 2016 Mar 3. doi: 10.18632/oncotarget.7871. [Epub ahead of print] doi: 10.1016/j.vph.2015.07.009. Epub 2015 Jul 18. doi: 10.1161/CIRCHEARTFAILURE.115.002444.
    5: Flynn JT, Bradford MC, Harvey EM. Intravenous Hydralazine in Hospitalized Children and Adolescents with Hypertension. J Pediatr. 2016 Jan;168:88-92. doi: 10.1016/j.jpeds.2015.07.070. Epub 2015 Sep 1. doi: 10.1016/j.jpeds.2015.09.071. Epub 2015 Oct 17. doi: 10.1097/JNN.0000000000000170. doi: 10.1016/j.ijcard.2015.05.160. Epub 2015 Jun 3. doi: 10.1590/abd1806-4841.20153893.
    13: Yiginer O, Tokatli A, Haholu A, Ozmen N. The combination of hydralazine and isosorbide dinitrate: the only antioxidant treatment recommended in the guidelines. Eur Rev Med Pharmacol Sci. 2015 May;19(10):1745-6. doi: 10.1016/j.brainres.2015.01.049. Epub 2015 Feb 7. doi: 10.3797/scipharm.1505-03. eCollection 2015.

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    摘要:Makino H, Mukoyama M, Mori K, Suganami T, Kasahara M, Yahata K, Nagae T, Yokoi H, Sawai K, Ogawa Y, Suga S, Yoshimasa Y, Sugawara A, Tanaka I, Nakao K. Transgenic overexpression of brain natriuretic peptide prevents the progression of diabetic nephropathy in mice. Diabetologia. 2006 Oct;49(10):2514–24. doi: 10.1007/s00125-006-0352-y.
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