CAS: 636-54-4; 4-Chloro-N-(Cis-2,6-Dimethylpiperidin-1-yl)-3-Sulfamoylbenzamide

该化合物是一种主要用于治疗高血压和与心脏衰竭有关的水肿的磺酰胺二酸性药物,其作用是抑制钠重新吸附在肾脏分解管内,导致尿液输出增加,血液量减少. 氯帕米德的特征是化学配方,其中包括一种磺酰胺组,有助于其药理活动.该物质一般是口服的,并已知其与其他二酸性药物相比具有中等强度. 氯帕米德的半衰期相对较长,在许多情况下允许每天一次服用.其副作用可能包括电解不平衡,特别是低血糖,以及其磺酸结构可能造成的过敏反应. 与任何药物一样,它对于监测病人的不良影响和与其他药物的相互作用至关重要. 总的来说,氯帕米德是管理液体保留和高血压的有效剂,在适当使用时有助于改善心血管健康.

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    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-2008227851-A1
    优先权日:2007-03-12
    标题 :Laulimalide and laulimalide analogs
    发明人:WENDER PAUL A
    权利人:WENDER PAUL A
    摘要:Novel laulimalide analogs, methods for the treatment of proliferative disease and processes for the synthesis of laulimalide and novel laulimalide analogs are described.

    专利号:US-10814013-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

    专利号:US-2008107598-A1
    优先权日:2006-10-05
    标 题:Efficient Synthesis of Chelators for Nuclear Imaging and Radiotherapy: Compositions and Applications

    专利号:US-8933207-B2
    优先权日:2010-07-28
    标 题 :Drug-ligand conjugates, synthesis thereof, and intermediates thereto
    发明人:CHEN ZHIYU; LANCASTER THOMAS M; ZION TODD C
    权利人:CHEN ZHIYU; LANCASTER THOMAS M; ZION TODD C; SMARTCELLS INC
    摘要:The present invention relates to methods for synthesizing compounds of formula I or pharmaceutically acceptable salts thereof: I wherein each of X, Alk 1 , Alk 2 , and W are as defined and described herein.

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    主要参考文献


    1: Wise PH, Rihan Z, Dinwiddy G, Whichelow MJ, Butterfield WJ. Clopamide and carbohydrate metabolism. Med J Aust. 1969 Oct 18;2(16):795-8. doi: 10.5694/j.1326-5377.1969.tb107423.x. 7(16):13870-13877. doi: 10.1021/acsomega.2c00256.
    3: McNeil JJ, Conway EL, Drummer OH, Howes LG, Christophidis N, Louis WJ. Clopamide: plasma concentrations and diuretic effect in humans. Clin Pharmacol Ther. 1987 Sep;42(3):299-304. doi: 10.1038/clpt.1987.151. 150(11):646, 648, 651-2. 19(3):161-8. doi: 10.1177/000331976801900304. 10(1):34-7. doi: 10.1080/07315724.1991.10718123.
    125:236-44. doi: 10.1016/j.jpba.2016.03.051. Epub 2016 Mar 25. 1(8268):355-8. doi: 10.1016/s0140-6736(82)91390-3. 74(3):219-25. doi: 10.1159/000174200. 26(8):337-40. doi: 10.1111/j.1532-5415.1978.tb03680.x. 78(8):679-82. doi: 10.1002/jps.2600780815. 83(4-5):336-42. French. 46(8):654-69. Italian. 66(18):682-4.

    合成参考文献


    摘要:Vichi FL, da Silva EJ, Cesar EB, Machado RR, Gigante E. [Effect of DCR-515 essental arterial hypertension of moderate severity(preliminary communition)]. Hospital (Rio J). 1969 Jul;76(1):99–106.
    摘要:Bernik V. [Modern therapy of the stabilization of essential hypertension by using a new drug combination: Bridina]. Hospital (Rio J). 1969 Aug;76(2):589–99.
    摘要:Elizalde JE. [Clinical test using Brinaldix plus Hydergine]. Hospital (Rio J). 1967 Dec;72(6):1941–2.
    摘要:Flückiger E, Taeschler M. [Extrarenal effects of a salidiuretic]. Arzneimittelforschung. 1966 Sep;16(9):1183–6.
    摘要:Frank H, Dentler H. [Clinical experiences with Brinaldix]. Munch Med Wochenschr. 1966 Nov 04;108(44):2235–40.
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