CAS: 135-09-1; Hydroflumethiazide

该化合物是一种硫酸二甲酸二甲酯,主要用于管理高血压和与凝聚性心脏衰竭或肾病有关的水肿,其行动机制包括抑制溶解管管管中的钠再吸附,促进水和电解排泄,主要优势包括其可预测的药用动力学,允许持续剂量,并与其他抗血压剂的兼容性进行混合治疗.氢氟化二氮酸酯表现出适度的行动持续时间,平衡了电解不平衡的功效,与较强的二苯酸盐相比,降低了电解不平衡的风险.在监测适当时,该化合物的长期安全性固定特征尤其受到重视.该化合物以平板形式可供口服.

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合成工艺路线路线简述

    2.4-Bis-Chlorosulfon-5-Trifluormethyl-Anilin置于氨体系中,用 水 用作溶剂,化学反应生成氢氟噻嗪
    参考文献:Synthesis Of Potential Diuretic Agents. I. Derivatives Of 7-Sulfamyl-3,4-Dihydro-1,2,4-Benzothiadiazine 1,1-Dioxide
    标题:Synthesis Of Potential Diuretic Agents. I. Derivatives Of 7-Sulfamyl-3,4-Dihydro-1,2,4-Benzothiadiazine 1,1-Dioxide
    摘要:
    Doi:10.1021/ja01490A028

    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-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-12295961-B2
    优先权日:2009-12-31
    标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
    发明人:DHINGRA OM
    权利人:MARIUS PHARMACEUTICALS INC
    摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

    专利号:US-11617758-B2
    优先权日:2009-12-31
    标 题 :Emulsion formulations
    发明人:DHINGRA OM; BERNSTEIN JAMES S
    权利人:MARIUS PHARMACEUTICALS LLC
    摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

    专利号:US-2007287734-A1
    优先权日:2006-06-09
    标 题 :Preparation and utility of substituted pyrazole compounds with cannabinoid receptor activity
    发明人:GANT THOMAS G; SARSHAR SEPEHR
    权利人:AUSPEX PHARMACEUTICALS INC
    摘要:The present disclosure is directed to modulators of CB-1 type receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of the severity and duration of obesity, metabolic syndrome, dyslipidemia, glucose imbalance, the inability to maintain weight loss, insulin resistance, a cardiovascular disorder, memory loss, drug dependence, a depressive disorder, a panic disorder, an obsessive-compulsive disorder, anxiety, post-traumatic stress syndrome, and any other condition in which it is beneficial to inhibit, inversely agonize or modulate a cannabinoid receptor are described.
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    主要参考文献


    1: Ogola EN, Yonga GO. Comparative study of the efficacy and tolerability of hydroflumethiazide versus propranolol in Africans with mild to moderate hypertension. East Afr Med J. 1993 May;70(5):277-9. Danish. Japanese. Italian.

    合成参考文献


    参考文献:10.1007/s00216-010-3484-3
    摘要:Peters RJB, Oosterink JE, Stolker AAM, Georgakopoulos C, Nielen MWF. Generic sample preparation combined with high-resolution liquid chromatography–time-of-flight mass spectrometry for unification of urine screening in doping-control laboratories. Analytical and Bioanalytical Chemistry. 2010 Feb 16;396(7):2583–98. doi: 10.1007/s00216-010-3484-3.
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