CAS: 133-67-5; 6-Chloro-3-(Dichloromethyl)-3,4-Dihydro-2H-Benzo[e][1,2,4]Thiadiazine-7-Sulfonamide 1,1-Dioxide

该化合物是一种硫酸二甲酸酯,在治疗高血压和与各种医疗条件有关的水肿时常用,其特点是化学配方,包括氯和硫磺原子,有助于其药理特性.复合作用是抑制肾脏溶解管管中的钠再吸附,导致尿液产量增加和血液量下降.三氯甲基苯并二甲胺通常通过口服,以相对长的半衰期为名,在许多情况下允许每天一次服用.其在水中的溶解性有限,这可能影响其吸收和生物利用率.该物质还可能产生副作用,包括电解不平衡,特别是低血糖,在肾损伤的病人中应谨慎使用.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

chloraminophenamide dichloroacetaldehyde diethyl acetal 2,2-dichloroacetaldehydechloraminophenamide (+)-trichlormethiazide (-)-trichlormethiazide

合成工艺路线路线简述

    5-氯-2,4-二磺酰胺基苯胺,二氯乙醛置于盐酸体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应生成三氯噻嗪
    参考文献:Craveri; Zoni,Bollettino Chimico Farmaceutico,1961,Vol. 100,P. 956-971
    标题:Craveri; Zoni,Bollettino Chimico Farmaceutico,1961,Vol. 100,P. 956-971

    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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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Takihata M, Nakamura A, Kondo Y, Kawasaki S, Kimura M, Terauchi Y. Comparison of Azelnidipine and Trichlormethiazide in Japanese Type 2 Diabetic Patients with Hypertension: The COAT Randomized Controlled Trial. PLoS One. 2015 May 4;10(5):e0125519. doi: 10.1371/journal.pone.0125519. eCollection 2015.
    2: Schulze S, Reinhardt S, Freese C, Schmitt U, Endres K. Identification of trichlormethiazide as a Mdr1a/b gene expression enhancer via a dual secretion-based promoter assay. Pharmacol Res Perspect. 2015 Feb;3(1):e00109. doi: 10.1002/prp2.109. Epub 2015 Jan 5.
    3: Hase M, Babazono T, Ujihara N, Uchigata Y. Comparison of spironolactone and trichlormethiazide as add-on therapy to renin-angiotensin blockade for reduction of albuminuria in diabetic patients. J Diabetes Investig. 2013 May 6;4(3):316-9. doi: 10.1111/jdi.12029. Epub 2013 Jan 24.

    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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