CAS: 122852-69-1; Alosetron Hydrochloride

该化合物是一种选择性的血清质5-HT3受体敌体,主要用于治疗有严重症状的妇女的肠胃炎综合症(IBS),通过调节胃肠道中的血清素活动,从而减少肠道功能,减轻腹部疼痛和腹泻等症状,化合物的特点是盐化盐形式,这增强了其溶解性和稳定性,它通常以口服方式施用,并因其在管理IBS方面的效力而著称,尽管它与潜在的副作用有关,包括消化和罕见的严重的胃肠并发症.由于这些风险,它的使用受到限制,在临床环境中受到监测.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    阿洛司琼置于盐酸体系中,用 甲醇,异丙醇 用作溶剂,化学反应生成盐酸阿洛司琼
    参考文献:Process For The Preparation Of Alosetron
    标题:Process For The Preparation Of Alosetron
    摘要:本发明提供了一种改进的方法,用于制备公式(i)的alosetron及其药学上可接受的盐.

    海关参考信息

    专利信息


    专利号:US-2025206743-A1
    优先权日:2022-03-25
    标 题:Tyk2 inhibitor synthesis and intermediates thereof
    发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
    权利人:TAKEDA PHARMACEUTICALS CO
    摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

    专利号:US-7807349-B2
    优先权日:2002-11-29
    标 题 :Protein synthesis monitoring (PSM)
    发明人:SMILANSKY ZEEV
    权利人:ANIMA CELL METROLOGY
    摘要:A method and a device are disclosed for monitoring the synthesis of proteins by the ribosome in real time, in vivo as well as in in-vitro. The ribosome is engineered to carry a donor fluorophore, and tRNA and/or amino acids and/or some other part of the ribosome are either engineered to carry acceptor fluorophores or else their natural fluorescent properties are utilized as acceptors. As the ribosomes mechanism processed the mRNA and tRNA molecules and synthesizes a polypeptide chain, a light source illuminates the ribosome, exciting the donor fluorophores and thereby the acceptor fluorophores whenever these are in sufficient proximity to a donor. The resulting signals are detected and used as a key for real-time database searching and identification of the protein being synthesized. The resulting data can be tabulated and interpreted in different ways. FIG. ( 1 ) describes the properties of a FRET pair and the dependence of FRET on pair distance.

    专利号:US-8442773-B2
    优先权日:2002-11-29
    标题:Protein synthesis monitoring (PSM)
    发明人:SMILANSKY ZEEV
    权利人:SMILANSKY ZEEV; ANIMA CELL METROLOGY
    摘要:A method and a device are disclosed for monitoring the synthesis of proteins by the ribosome, wherein the ribosome is bound to a first label, for example a donor fluorophore, and a tRNA and/or amino acid are is bound to a second label, for example an acceptor fluorophore, wherein the first and second labels together from a FRET pair. As the ribosome mechanism processes the mRNA and tRNA molecules and synthesizes a polypeptide chain, a light source illuminates the ribosome, exciting the donor fluorophores and thereby the acceptor fluorophores whenever these are in sufficient proximity to a donor. The resulting signals are detected and used as a key for database searching and identification of the protein being synthesized.

    专利号:CN-103173783-A
    优先权日:2011-12-23
    标题:Electrochemical carboxylation synthesis for obtaining intermediates useful for the synthesis of SPAN derivatives

    专利号:US-10906888-B2
    优先权日:2016-07-14
    标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-10308615-B2
    优先权日:2015-05-29
    标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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    主要参考文献


    1: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Alosetron. 2019 Feb 7. 59(3):511-8; discussion 519-20. doi: 10.2165/00003495-200059030-00008. 2023 Jan–. 36(9):595-607. doi: 10.1358/dot.2000.36.9.593776. 4(11):2089-98. doi: 10.1517/14656566.4.11.2089. 27(3):503-12. doi: 10.1185/03007995.2010.547933. Epub 2011 Jan 6. 163(1):137-151. doi: 10.1053/j.gastro.2022.04.017. 9(1):147-59. doi: 10.1517/13543784.9.1.147. 10(6):556-584. doi: 10.1002/ueg2.12259. Epub 2022 Jun 13.
    10: Hyman PE, Garvey TQ 3rd. Return of alosetron. Expert Opin Drug Saf. 2002 May;1(1):1-4. doi: 10.1517/14740338.1.1.1. 13 Suppl
    2:70-6. doi: 10.1046/j.1365-2036.1999.00009.x. 12(4):303-315. doi: 10.1136/flgastro-2019-101298.

    合成参考文献


    摘要:O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. 13th Edition, Whitehouse Station, NJ: Merck and Co., Inc., 2001., p. 57
    摘要:Full text:
    摘要:
    参考文献:10.1177/2168479017742858
    摘要:Patriarca PA, Van Auken RM, Kebschull SA. Analysis of the Risks and Benefits of New Chemical Entities Approved by the US Food and Drug Administration (FDA) and Subsequently Withdrawn From the US Market. Therapeutic Innovation & Regulatory Science. 2018 Sep;52(5):649–55. doi: 10.1177/2168479017742858.
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