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    METHOD FOR PREPARING DIAZOXIDE
    1.
    发明申请
    METHOD FOR PREPARING DIAZOXIDE 有权

    公开(公告)号：US20230033450A1

    公开(公告)日：2023-02-02

    申请号：US17789474

    申请日：2019-12-29

    申请人： SOOCHOW UNIVERSITY

    发明人： Chunhua QIAO ,  Yiwen XU

    IPC分类号： C07D285/24

    摘要： A method for preparing diazoxide includes reacting o-aminobenzenesulfonamide with N-chlorosuccinimide in a chlorine solvent to obtain 2-amino-5-chlorobenzenesulfonamide, mixing the 2-amino-5-chlorobenzenesulfonamide, an imidazole salt and an amide solvent, then heating same for reaction so as to obtain diazoxide; or mixing o-aminobenzenesulfonamide, an imidazole salt and an amide solvent, then heating same for reaction to obtain a compound IV; then reacting the compound IV with N-chlorosuccinimide in a chlorine solvent to obtain diazoxide. The application of imidazole hydrochloride as a catalyst in preparing diazoxide is also disclosed. The present invention avoids the use of highly corrosive and toxic chlorosulfonyl isocyanate, a strong acid (sulfuric acid), and a high reaction temperature (240-250° C.), and the reaction steps are short; the total yield of the two steps is more than 90%, and compared with publicly disclosed preparation methods for diazoxide, the synthesis route overcomes numerous shortcomings, thus being more suitable for industrial production.

    C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use
    3.
    发明授权
    C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use 有权
    作为BACE抑制剂，组合物及其用途的C6-螺亚麻醇二氮杂二恶英

    公开(公告)号：US09580396B2

    公开(公告)日：2017-02-28

    申请号：US14653671

    申请日：2013-12-16

    申请人： Merck Sharp & Dohme Corp.

    发明人： Jared N. Cumming ,  Jack D. Scott, Jr. ,  Andrew W. Stamford ,  Ulrich Iserloh ,  Santhosh Francis Neelamkavil ,  Pengcheng Patrick Shao ,  Jonathan E. Wilson

    IPC分类号： C07D285/24 ,  C07D417/12 ,  C07D471/04 ,  C07D513/10 ,  C07D519/00 ,  C07D285/20

    CPC分类号： C07D285/24 ,  C07D285/20 ,  C07D417/12 ,  C07D471/04 ,  C07D513/10 ,  C07D519/00

    摘要： In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

    摘要翻译： 在其许多实施方案中，本发明提供某些C5-螺亚氨基二嗪二氧化物化合物，包括式（I）化合物：（结构表示）或其互变异构体及所述化合物的药学上可接受的盐，其中R1，R2，R3，X，Y ，s，环A，RA，m，-L1-和RL如本文所定义。 本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物，

    NITRIC OXIDE DONATING DIURETIC COMPOUNDS, COMPOSITIONS AND METHODS OF USE
    7.
    发明申请
    NITRIC OXIDE DONATING DIURETIC COMPOUNDS, COMPOSITIONS AND METHODS OF USE 失效
    硝酸氧化物滴定化合物，组合物和使用方法

    公开(公告)号：US20080255101A1

    公开(公告)日：2008-10-16

    申请号：US12136531

    申请日：2008-06-10

    申请人： David S. GARVEY ,  L. Gordon LETTS ,  Richard A. EARL ,  Maiko EZAWA ,  Xinqin FANG ,  Ricky D. GASTON ,  Subhash P. KHANAPURE ,  Chia-En LIN ,  Ramani R. RANATUNGE ,  Cheri A. STEVENSON ,  Shiow-Jyi WEY

    发明人： David S. GARVEY ,  L. Gordon LETTS ,  Richard A. EARL ,  Maiko EZAWA ,  Xinqin FANG ,  Ricky D. GASTON ,  Subhash P. KHANAPURE ,  Chia-En LIN ,  Ramani R. RANATUNGE ,  Cheri A. STEVENSON ,  Shiow-Jyi WEY

    IPC分类号： A61K31/549 ,  A61P9/00 ,  A61P13/00 ,  C07D285/24 ,  C07D417/04 ,  C07D513/10

    CPC分类号： C07D285/30 ,  C07D285/28 ,  C07D285/32 ,  C07D417/04 ,  C07D417/06 ,  C07D513/10

    摘要： The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia. The nitric oxide enhancing diuretic compounds comprise at least one nitric oxide enhancing group linked to the diuretic compound through one or more sites such as carbon, oxygen and/or nitrogen via a bond or moiety that cannot be hydrolyzed.

    摘要翻译： 本发明描述了包含至少一种一氧化氮增强利尿剂或其药学上可接受的盐，和任选的至少一种一氧化氮增强化合物和/或至少一种治疗剂的新型组合物和试剂盒。 本发明还提供了（a）处理由过量水和/或电解质滞留导致的条件的方法; （二）治疗心血管疾病; （c）治疗血管性疾病; （d）治疗糖尿病; （e）治疗由氧化应激引起的疾病; （f）治疗内皮功能障碍; （g）治疗由内皮功能障碍引起的疾病; （h）治疗肝硬化; （j）治疗先兆子痫; （k）治疗骨质疏松症; （l）治疗肾病; （m）治疗外周血管疾病; （n）治疗门静脉高压; （o）治疗中枢神经系统疾病; （p）治疗代谢综合征; （q）治疗性功能障碍; 和（r）高脂血症。 一氧化氮增强利尿化合物包含通过一个或多个位点如碳，氧和/或氮通过不能水解的键或部分与利尿剂化合物连接的至少一个一氧化氮增强基团。