CAS: 80880-90-6; Telenzepine

该化合物是一种化学化合物,被归类为抗胆碱剂,主要用于治疗各种胃肠紊乱,其作用是抑制肌肉受体的乙酰胆碱,导致胃肠功能和分泌减少.Terenzepine以其选择性行动而著称,它最大限度地减少了通常与非选择性抗胆碱基有关的副作用.该化合物通常以口服形式施用,并研究其在管理诸如胃溃疡和肠胃炎综合症等条件方面的效力.其药用植物基因特征显示,吸收相对快,半衰期中度,允许有效的治疗剂量.此外,Telenzepine的化学结构具有独特的安排,有助于其药用特性.与许多药物一样,潜在的副作用可能包括口干燥,内分泌和模糊的视力,这些是抗胆碱药物的典型特征.

结构式图片

MSDS等安全信息

上下游产品

4,9-Dihydro-9-[(+)-Isopinocampheyloxymethyl]-3-Methyl-4-[(4-Methyl-1-Piperazinyl)-Acetyl]-10H-Thieno[3,4-B][1,5]Benzodiazepin-10-One 126828-45-3

合成工艺路线路线简述

    📜4,9-Dihydro-9-[(+)-Isopinocampheyloxymethyl]-3-Methyl-4-[(4-Methyl-1-Piperazinyl)-Acetyl]-10H-Thieno[3,4-B][1,5]Benzodiazepin-10-One置于盐酸体系中,用 甲酸,水 作为反应溶剂,化学反应生成 替仑西平
    参考文献:Thienotricylene For The Treatment Of Bronchial Diseases
    标题:Thienotricylene For The Treatment Of Bronchial Diseases
    摘要:该发明涉及使用替莫唑和(+)-替莫唑治疗支气管疾病.此外,该发明涉及(+)-替莫唑,其制备方法以及其制备中间体.

    海关参考信息

    专利信息


    专利号:US-2006167025-A1
    优先权日:2004-12-22
    标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs
    发明人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID
    权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID
    摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.

    专利号:US-2022233673-A1
    优先权日:2019-06-04
    标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
    发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
    权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
    摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

    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-4381301-A
    优先权日:1980-05-07
    标题 :Substituted tricyclic thieno compounds, their synthesis, their use, their compositions and their medicaments
    发明人:RAINER GEORG
    权利人:BYK GULDEN LOMBERG CHEM FAB
    摘要:Substituted thienobenzodiazepinones of the general formula I (I) [wherein R1 denotes a hydrogen atom (-H) or an alkyl radical with 1 to 4 carbon atoms; R2 represents a halogen atom (halo) or has one of the meanings of R1; R3 denotes a halogen atom (halo) or the group -N(R4)R5; R4 denotes an alkyl radical with 1 to 4 carbon atoms or an alkenyl radical with 3 to 5 carbon atoms; R5 has one of the meanings of R4 or represents the group -(CH2)m-N(R6)R7; or R4 and R5, together with the nitrogen atom to which both are bonded, denote a morpholino group, a pyrrolidino group, a piperidino group, a hexahydroazepin-1-yl group, a piperazin-1-yl group (which is optionally substituted in the 4-position by a methyl, ethyl or benzyl group), a 2,4-dimethylpiperazin-1-yl group, or a hexahydro-1H-1,4-diazepin-1-yl group (which is substituted in the 4-position by a methyl or ethyl group); R6 denotes an alkyl group with 1 to 4 carbon atoms; R7 denotes an alkyl group with 1 to 4 carbon atoms; A denotes a straight-chain or branched alkylene group with 1 to 5 carbon atoms; and m denotes 2 or 3] and their acid-addition salts are new compounds. They either have a protective action on the stomach and intestine and are suitable for treating illnesses based on disorders of the stomach or intestine, or they are intermediates for preparing products having protective action. Processes for the preparation of the new pharmacologically-active compounds and of the intermediate products are presented.

    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.

    专利号:US-2025221964-A1
    优先权日:2020-03-13
    标题 :Substituted Isoxazoles as Selective Nav1.7 Inhibitors for Pain Treatment and Method of Pain Treatment
    发明人:FRANZ DOUG; NEFF ROBYNNE; DIBRELL SARA
    权利人:UNIV TEXAS
    摘要:Tri-substituted isoxazole compounds and compound synthesis is disclosed. Tri-substituted isoxazole compounds having sodium gate channel Nav7 selectivity that are tunable for selectivity over Nav1.5. In particular, structure-activity relationship (SAR) studies demonstrated that subtype selectivity (Nav1.7 vs. Nav1.5) is improved with methylation of the amide nitrogen or ortho-substitution on the phenyl ring in the 5-position.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Pelosi A, Menardy F, Popa D, Girault JA, Hervé D. Heterozygous Gnal mice are a novel animal model to study dystonia pathophysiology. J Neurosci. 2017 May 25. pii: 1529-16. doi: 10.1523/JNEUROSCI.1529-16.2017. [Epub ahead of print] doi: 10.1016/j.bbr.2017.04.023. [Epub ahead of print] doi: 10.1523/JNEUROSCI.0873-16.2016. doi: 10.1074/jbc.M115.712562. Epub 2016 Apr 14.
    5: Testa B, Vistoli G, Pedretti A. Mechanisms and pharmaceutical consequences of processes of stereoisomerisation - A didactic excursion. Eur J Pharm Sci. 2016 Jun 10;88:101-23. doi: 10.1016/j.ejps.2016.04.007. Epub 2016 Apr 8. Review. doi: 10.1007/s00213-015-4123-7. Epub 2015 Oct 31. doi: 10.1017/S1461145714000613. Epub 2014 May 12. doi: 10.1523/JNEUROSCI.1040-13.2014.
    9: Jin S, Sarkar KS, Jin YN, Liu Y, Kokel D, Van Ham TJ, Roberts LD, Gerszten RE, Macrae CA, Peterson RT. An in vivo zebrafish screen identifies organophosphate antidotes with diverse mechanisms of action. J Biomol Screen. 2013 Jan;18(1):108-15. doi: 10.1177/1087057112458153. Epub 2012 Sep 6.

    合成参考文献


    参考文献:10.1016/j.bbrc.2018.04.193
    摘要:Braga LEG, Miranda RL, Granja MG, Giestal-de-Araujo E, dos Santos AA. PKC delta activation increases neonatal rat retinal cells survival in vitro: Involvement of neurotrophins and M1 muscarinic receptors. Biochemical and Biophysical Research Communications. 2018 Jun;500(4):917–23. doi: 10.1016/j.bbrc.2018.04.193.
    参考文献:10.1021/bc00015a006
    摘要:Karton Y, Baumgold J, Handen JS, Jacobson KA. Molecular probes for muscarinic receptors: derivatives of the M1-antagonist telenzepine. Bioconjug Chem. 1992 May;3(3):234–40.
    参考文献:10.1111/j.1474-8673.1996.tb00362.x
    摘要:Martin JR. McN‐A‐343 increases renal sympathetic nerve activity and blood pressure by a muscarinic and a non‐muscarinic mechanism in the rat. Journal of Autonomic Pharmacology. 1996 Oct;16(5):281–92. doi: 10.1111/j.1474-8673.1996.tb00362.x.
    参考文献:10.1073/pnas.0907915107
    摘要:Hern JA, Baig AH, Mashanov GI, Birdsall B, Corrie JET, Lazareno S, Molloy JE, Birdsall NJM. Formation and dissociation of M 1 muscarinic receptor dimers seen by total internal reflection fluorescence imaging of single molecules. Proc. Natl. Acad. Sci. U.S.A. 2010 Jan 20;107(6):2693–8. doi: 10.1073/pnas.0907915107.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知