CAS: 66104-23-2; Pergolide Mesylate

该化合物是含有多聚胺性活性药性特性的合成雌性衍生物,主要用于治疗帕金森氏病和超蛋白性贫血.其主要优势包括多巴胺D1和D2受体的高亲和性,以及血清素受体,这有助于其管理运动症状和荷尔蒙不平衡的功效. 间聚盐形式提高了溶性性和生物利用率,确保了一致的药用植物. Pergolide meylate展示了长期的动作,降低了剂量频率,提高了患者的合规性. 其选择性受体活动将负面影响减少到了非选择性的活性. 化合物研究周全,并制定了安全有效使用的临床规程.

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CAS号66104-22-1 培高利特 | CAS号63719-21-1 PERGOLIDE MESYL... | CAS号5878-43-3 9,10-二氢麦角酸 | CAS号75-75-2 甲基磺酸 | CAS号72821-83-1 6-propylergolin...

合成工艺路线路线简述

    培高利特置于甲烷磺酸体系中,用 甲醇 作为反应溶剂,化学反应生成 甲磺酸培高利特
    参考文献:Decyanation Of Pergolide Intermediate
    标题:Decyanation Of Pergolide Intermediate
    摘要:本发明提供了一种在酒精溶剂中,使用沸点大约在100摄氏度以上的碱金属氢氧化物对多巴胺受体激动剂中间体进行脱氰化的方法,温度范围在大约100摄氏度到175摄氏度之间.

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    专利信息


    专利号:US-7019140-B2
    优先权日:2002-03-15
    标 题:Process for the synthesis of pergolide
    发明人:CABRI WALTER; PAISSONI PAOLO; ROLETTO JACOPO; FONTE PIERA; OLMO SARA
    权利人:ANTIBIOTICOS SPA
    摘要:A process for the synthesis of pergolide (Formula (I)) (D-6-n-propyl-8βmethylmercaptomethylergo line) from acid 9,10-dihydrolysergic is herein disclosed. The process can be carried out without isolating most intermediates and is particularly convenient both from the yield and safety standpoint. Moreover, pergolide thereby obtained is highly pure and can be conveniently transformed into pergolide mesylate

    专利号:US-2009285888-A1
    优先权日:2005-05-13
    标题:Derivatives of dihydroxyphenylalanine
    发明人:SUSILO GISELA
    权利人:SUSILO GISELA
    摘要:The invention relates to derivatives of dihydroxyphenylalanine, to their synthesis and to pharmaceutical compositions containing said derivatives of dihydroxyphenylalanine. Furthermore, the invention relates to the use of said derivatives of dihydroxyphenylalanine and said pharmaceutical compositions for the treatment and prophylaxis of movement disorders, neurodegenerative diseases, Alzheimer's disease, Parkinson's disease, hemiparkinson-hemiatrophy, parkinsonian syndrome, Lewy body disease, frontotemporal dementia, Lytico-Bodig disease (parkinsonism/dementia/amyotrophic lateral sclerosis), striatonigral degeneration, Shy-Drager syndrome, sporadic olivopontocerebellar degeneration, progressive atrophy of the globus pallidus, progressive supranuclear palsy, Hallervorden-Spatz disease, Huntington's disease, X-linked dystonia-parkinsonism (Lubag), mitochondrial cytopathy with striatal necrosis, neuroacanthocytosis, restless legs syndrome, Wilson's disease.

    专利号:US-2004232390-A1
    优先权日:2003-04-07
    标 题 :Highly conductive carbon/inherently conductive polymer composites
    发明人:VISWANATHAN TITO
    摘要:This invention relates to composites of a highly conductive form of carbon, preferably graphite, and an inherently conducting polymer that exhibits higher conductivity than the conductivities of the individual components and the synthesis of these composites.

    专利号:US-8697888-B2
    优先权日:2012-01-06
    标题 :Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors
    发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; CHEUNG YIU-YIN
    权利人:UNIV VANDERBILT
    摘要:In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    专利号:US-9056875-B2
    优先权日:2012-08-31
    标 题 :Substituted pyrazolo[3′,4′:4,5]thieno[2,3-C]pyridazin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
    发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; SALOVICH JAMES M
    权利人:UNIV VANDERBILT
    摘要:In one aspect, the invention relates to substituted pyrazolo[3′,4′:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    专利号:US-9073935-B2
    优先权日:2011-11-11
    标 题:Substituted benzylspiroindolin-2-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1
    发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; HOPKINS COREY R; MELANCON BRUCE J; POSLUSNEY MICHAEL S
    权利人:UNIV VANDERBILT
    摘要:In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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    主要参考文献


    1: Volochanskyi O, Švecová M, Prokopec V. Detection and identification of medically important alkaloids using the surface-enhanced Raman scattering spectroscopy. Spectrochim Acta A Mol Biomol Spectrosc. 2019 Jan 15;207:143-149. doi: 10.1016/j.saa.2018.09.009. Epub 2018 Sep 9. doi: 10.15653/tpg-170574. Epub 2018 Aug 24. German. doi: 10.1002/brb3.1036. Epub 2018 Jun 29.
    4: Shotton JCR, Justice WSM, Salguero FJ, Stevens A, Bacci B. PITUITARY PARS INTERMEDIA DYSFUNCTION (EQUINE CUSHING'S DISEASE) IN NONDOMESTIC EQUIDS AT MARWELL WILDLIFE: A CASE SERIES. ONE CHAPMAN'S ZEBRA ( EQUUS QUAGGA CHAPMANI) AND FIVE PRZEWALSKI's HORSES ( EQUUS FERUS PRZEWALSKII). J Zoo Wildl Med. 2018 Jun;49(2):404-411. doi: 10.1638/2017-0149.1. doi: 10.1111/avj.12716. Epub 2018 Jun 3. Review. doi: 10.1002/mds.27260. Epub 2018 May 14. Review. doi: 10.1016/j.tvjl.2018.03.007. Epub 2018 Mar 23. International Parkinson and movement disorder society evidence-based medicine review: Update on treatments for the motor symptoms of Parkinson's disease. Mov Disord. 2018 Aug;33(8):1248-1266. doi: 10.1002/mds.27372. Epub 2018 Mar 23. Review. doi: 10.1021/acschemneuro.7b00460. Epub 2018 Mar 16. doi: 10.1038/npp.2017.301. Epub 2017 Dec 18.
    11: Carmalt JL, Waldner CL, Allen AL. Equine pituitary pars intermedia dysfunction: An international survey of veterinarians' approach to diagnosis, management, and estimated prevalence. Can J Vet Res. 2017 Oct;81(4):261-269.

    合成参考文献


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    摘要:Drugs in Japan, -(1265), 1995
    摘要:Gekkan Yakuji. Pharmaceuticals Monthly., 36(3350), 1994
    摘要:A2932: Blin O: The pharmacokinetics of pergolide in Parkinson's disease. Curr Opin Neurol. 2003 Dec;16 Suppl 1:S9-12.
    参考文献:10.1007/bf03343573
    摘要:Cannavò S, Curtò L, Squadrito S, Almoto B, Vieni A, Trimarchi F. Cabergoline: A first-choice treatment in patients with previously untreated prolactin-secreting pituitary adenoma. Journal of Endocrinological Investigation. 1999 May;22(5):354–9. doi: 10.1007/bf03343573.
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