CAS: 115956-13-3; Rel-(5S,6R,8R,9As)-3-Oxooctahydro-1H-2,6-Methanoquinolizin-8-Yl 1H-Indole-3-Carboxylate Methanesulfonate

该化合物是一种主要用作抗乳剂的药物化合物,特别是用于预防与化疗和外科手术有关的恶心和呕吐;是一种选择性的血清素5-HT3受体抗体抗体,通过阻塞可引发恶心的...

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methanesulfonic acid dolasetron Indole-3-carbonyl chloride 3,8]-undecan-10-oneendo-5-hydroxy-8-azatricyclo[5.3.1.03,8]-undecan-10-one

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    专利号:US-2025289827-A1
    优先权日:2022-12-02
    标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
    发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
    权利人:C4 THERAPEUTICS INC
    摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

    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-11279734-B2
    优先权日:2017-12-01
    标 题:Solution-phase affinity selection of inhibitors from combinatorial peptide libraries
    发明人:PENTELUTE BRADLEY L; TOUTI FAYCAL
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:The present invention provides novel peptides (e.g., peptides, macrocyclic peptides, mini-proteins) that modulate protein-protein interactions or salts thereof, and methods of making and using the inventive peptides. In some embodiments, the peptides are high affinity inhibitors (e.g., K D of at most 100 nM, at most 10 nM, at most 1 nM) of a protein-protein interaction. In certain embodiments, these peptides interfere with p53-MDM2 binding interactions (e.g., by binding to MDM2 (GenBank® Gene ID: 4193)). In some embodiments, the peptides interfere with the dimerization of the C-terminal domain of the human immunodeficiency virus (HIV) capsid protein (C-CA), comprising residues 146-231 of the HIV capsid protein (e.g., by binding to the C-terminal domain of the HIV capsid protein (C-CA), thereby inhibiting the dimeric interface of HIV capsid protein, thereby inhibiting viral assembly). These inventive peptides were rapidly generated and identified using novel methods described herein comprising combinatorial peptide synthesis and/or solution affinity selection.

    专利号:US-2022411407-A1
    优先权日:2019-11-15
    标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof
    发明人:WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN
    权利人:UNIV NORTH CAROLINA CHAPEL HILL
    摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.

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    主要参考文献


    1: Carlisle J, Stevenson CA. WITHDRAWN: Drugs for preventing postoperative nausea and vomiting. Cochrane Database Syst Rev. 2017 Jul 17;7:CD004125. doi: 10.1002/14651858.CD004125.pub3. Review. doi: 10.1002/jat.3433. Epub 2017 Jan 31. Review. doi: 10.1186/s12916-016-0761-9. Review.
    4: Simino GP, Marra LP, Andrade EI, Acúrcio Fde A, Reis IA, De Araújo VE, Cherchiglia ML. Efficacy, safety and effectiveness of ondansetron compared to other serotonin-3 receptor antagonists (5-HT3RAs) used to control chemotherapy-induced nausea and vomiting: systematic review and meta-analysis. Expert Rev Clin Pharmacol. 2016 Sep;9(9):1183-94. doi: 10.1080/17512433.2016.1190271. Epub 2016 Jun 15. Review. doi: 10.3109/03602532.2015.1089885. Epub 2015 Sep 29. Review. doi: 10.1186/s12916-015-0379-3. Review.
    7: Tricco AC, Soobiah C, Hui W, Antony J, Struchkov V, Hutton B, Hemmelgarn B, Moher D, Straus SE. Interventions to decrease the risk of adverse cardiac events for patients receiving chemotherapy and serotonin (5-HT3) receptor antagonists: a systematic review. BMC Pharmacol Toxicol. 2015 Jan 26;16:1. doi: 10.1186/2050-6511-16-1. Review.

    合成参考文献


    摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).
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