CAS: 1508-65-2; 4-(Diethylamino)But-2-Yn-1-Yl 2-Cyclohexyl-2-Hydroxy-2-Phenylacetate Hydrochloride

该化合物是一种合成抗胆碱药物,主要用于治疗过活膀胱和尿尿失禁等相关症状,其作用是抑制膀胱肌肉受体的乙酰胆碱酯酶作用,导致膀胱肌肉放松,降低紧迫性.该化合物似乎是白色的,白色的晶状粉,在水中溶解,适合各种药物配方.其分子配方为C21H30ClN,其分子重量相对较低.氧化丁烷通常通过口服或转基因施用,剂量因地适应病人的需要.常见的副作用可能包括干口,内吸附和眩晕,反映其抗胆碱性特性.由于它的操作机制,对具有诸如青光眼或尿液保留等条件的病人采取谨慎态度.

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欧盟法规

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CAS号5633-20-5 奥昔布宁 | CAS号10575-25-4 4-二乙氨基-2-丁炔-1-醇 | CAS号4335-77-7 2-环己基-2-羟基苯乙酸

合成工艺路线路线简述

    奥昔布宁置于盐酸体系中,用 甲醇 用作溶剂,化学反应生成盐酸奥昔布宁
    参考文献:Substituted Phenylcyclohexylglycolates
    标题:Substituted Phenylcyclohexylglycolates
    摘要:本文揭示了基于取代苯基环己基甘醇酸酯的 Formula I 的肌氨酸乙酰胆碱受体调节剂,其制备方法,药物组合物及使用方法.

    海关参考信息

    专利信息


    专利号:US-6825378-B2
    优先权日:2003-03-28
    标 题 :Process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid
    发明人:KUMAR PRADEEP; FERNANDES RODNEY AGUSTINHO; GUPTA PRITI
    权利人:COUNCIL SCIENT IND RES
    摘要:The present invention provides a process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1). The present invention more particularly relates to a process using cyclohexylphenyl ketone for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1).

    专利号:US-10022366-B2
    优先权日:2013-04-23
    标 题:Extending and maintaining micropore viability of microneedle treated skin with lipid biosynthesis inhibitors for sustained drug delivery
    发明人:STINCHCOMB AUDRA L; GHOSH PRIYANKA
    权利人:STINCHCOMB AUDRA L; GHOSH PRIYANKA; UNIV MARYLAND; UNIV KENTUCKY RES FOUND
    摘要:Microneedles and their use as a physical skin permeation enhancement technique facilitate drug delivery across the skin in therapeutically relevant concentrations. Micropores created in the skin by MNs reseal because of normal healing processes of the skin, thus limiting the duration of the drug delivery window. Pore lifetime enhancement strategies can increase effectiveness of MNs as a drug delivery mechanism by prolonging the delivery window. Fluvastatin (FLU) was used to enhance pore lifetime by inhibiting the synthesis of cholesterol, a major component of the stratum corneum lipids. The skin recovered within a 30-45-min time period following the removal of occlusion, and there was no significant irritation observed due to the treatment compared to the control sites. Thus, it can be concluded that localized skin treatment with FLU can be used to extend micropore lifetime and deliver drugs for up to 7 days across MN-treated skin.

    专利号:US-9751877-B2
    优先权日:2012-09-21
    标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
    发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT
    权利人:PFIZER
    摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-5677346-A
    优先权日:1995-01-31
    标 题:Treating urinary incontinence using (S)-desethyloxybutynin
    发明人:ABERG GUNNAR; MCCULLOUGH JOHN R; FANG YUE
    权利人:SEPRACOR INC
    摘要:A method for treating urinary incontinence while avoiding concomitant liability of adverse effects associated with racemic oxybutynin is disclosed. The method comprises administering a therapeutically effective amount of (S)-oxybutynin, (S)-desethyloxybutynin or a pharmaceutically acceptable salt thereof, substantially free of the corresponding R enantiomer. Pharmaceutical compositions in the form of tablets and transdermal devices comprising (S)-oxybutynin or (S)-desethyloxybutynin and an acceptable carrier are also disclosed, as is a synthesis of desethyloxybutynin.

    专利号:US-2004192962-A1
    优先权日:2003-03-28
    标 题 :Process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid

    专利号:US-7993390-B2
    优先权日:2002-02-08
    标 题:Implantable or insertable medical device resistant to microbial growth and biofilm formation
    发明人:MILLER KATHLEEN M; BUCAY-COUTO WEENNA; LI JIANMIN
    权利人:BOSTON SCIENT SCIMED INC
    摘要:Disclosed are implantable or insertable medical devices that provide resistance to microbial growth on and in the environment of the device and resistance to microbial adhesion and biofilm formation on the device. In particular, the invention discloses implantable or insertable medical devices that comprise at least one biocompatible matrix polymer region, an antimicrobial agent for providing resistance to microbial growth and/or a microbial adhesion/biofilm synthesis inhibitor for inhibiting the attachment of microbes and the synthesis and accumulation of biofilm on the surface of the medical device. Also disclosed are methods of manufacturing such devices under conditions that substantially prevent preferential partitioning of any of said bioactive agents to a surface of the biocompatible matrix polymer and substantially prevent chemical modification of said bioactive agents.
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    主要参考文献


    1: Capalbo D, Guarino S, Di Sessa A, Esposito C, Grella C, Papparella A, Miraglia Del Giudice E, Marzuillo P. Combination therapy (desmopressin plus oxybutynin) improves the response rate compared with desmopressin alone in patients with monosymptomatic nocturnal enuresis and nocturnal polyuria and absence of constipation predict the response to this treatment. Eur J Pediatr. 2023 Jan 25. doi: 10.1007/s00431-023-04824-5. Epub ahead of print. 67(3):222-227. doi: 10.4103/ijd.IJD_799_20.
    5: Edwards BA, Joosten SA. Variability in the response to atomoxetine and oxybutynin for OSA: Highlighting the need for personalized medicine. Respirology. 2023 Mar;28(3):215-216. doi: 10.1111/resp.14395. Epub 2022 Oct 18. 28(3):273-280. doi: 10.1111/resp.14383. Epub 2022 Oct 2. Erratum in: Respirology. 2022 Oct 30;: 28(3):9-14. doi: 10.46292/sci21-00091. Epub 2022 Aug 17.
    8: Sun P, Wang Z, Wu T, Zuo S, Huang X, Cui Z, Zhang D. Injectable, Adhesive, and Self-Healing Composite Hydrogels Loaded With Oxybutynin Hydrochloride for the Treatment of Overactive Bladder in Rats. Front Bioeng Biotechnol. 2022 Jun 27;10:906835. doi: 10.3389/fbioe.2022.906835.

    合成参考文献


    参考文献:10.1007/s11255-011-0030-y
    摘要:Lehnert T, Weisser M, Till H, Rolle U. The effects of long-term medical treatment combined with clean intermittent catheterization in children with neurogenic detrusor overactivity. International Urology and Nephrology. 2011 Jul 21;44(2):335–41. doi: 10.1007/s11255-011-0030-y.
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