CAS: 68844-77-9; Astemizole

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CAS号73736-50-2 O-去甲基阿司咪唑 | CAS号73735-36-1 1-methoxy-4-(2-... | CAS号75970-64-8 氢溴酸诺拉司咪唑 | CAS号67-66-3 氯仿 | CAS号84501-68-8 4-[[1-[(4-氟苯基)甲... | CAS号73734-07-3 4-(1H-苯并咪唑-2-基氨... | CAS号352-11-4 对氟氯苄 | CAS号51-17-2 苯并咪唑 | CAS号14425-64-0 4-(2-溴乙基)苯甲醚 | CAS号75970-99-9 norastemizole | CAS号73736-50-2 O-去甲基阿司咪唑 | CAS号75970-99-9 norastemizole | CAS号104472-65-3 6-Hydroxydesmet...

合成工艺路线路线简述

    4-(2-(4-((1-((4-氟苯基)甲基)-1H-苯并咪唑-2-基)氨基)-1-哌啶基)乙基)-苯酚置于sodium Hydroxide体系中,用 水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 0.42H,反应生成 阿司咪唑
    参考文献:Cardiovascular Safety Assay
    标题:Cardiovascular Safety Assay
    摘要:本发明提供了用于筛选试验化合物在受试者中引起心脏毒性能力的测定和试剂盒.所述测定和试剂盒基于这样的发现:利用astemizole与herg钾通道的相互作用,可以在新药物和其他药物代理的开发过程中预测化合物的心脏毒性.

    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-8653238-B2
    优先权日:2006-02-27
    标题:Compositions and methods for transport of molecules with enhanced release properties across biological barriers
    发明人:WENDER PAUL A; GOUN ELENA A; JONES LISA R
    权利人:WENDER PAUL A; GOUN ELENA A; JONES LISA R; UNIV LELAND STANFORD JUNIOR
    摘要:Conjugates of a cargo molecule with a transporter molecule are disclosed, where the cargo molecule and the transporter molecule are linked covalently by a releasable linker. The cargo of the conjugate can be a biologically active agent or a reporter molecule. The transporter modulates the transport of the cargo across a biological barrier (e.g., a cell membrane) compared to the transport of the unconjugated cargo. Releasable linkers suitable for rapid and facile conjugation to various types of cargo and transporters are also disclosed, along with methods for using the linkers in the synthesis of conjugates.

    专利号:US-7919505-B2
    优先权日:2006-07-11
    标题 :Xinafoate salt of a substituted 5-oxazol-2-yl-quinoline compound
    发明人:TING PAULINE C; LEE JOE F; FENG KUNG-I; REEDER MICHAEL R; TRZASKA SCOTT T; ZHU MAN; MAO CHEN; FILIPOV DIMITAR L; ZARKADAS DIMITRIOS N
    权利人:SCHERING CORP
    摘要:The present invention relates to the compound of the formula n nTo methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.

    专利号:US-2013035307-A1
    优先权日:2010-01-26
    标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
    发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
    权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
    摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

    专利号:US-2011003780-A1
    优先权日:2007-07-10
    标题:Hydrogen chloride salt of a substituted 5-oxazol-2-yl-quinoline compound and a process for the production thereof
    发明人:ZHU MAN
    权利人:SCHERING CORP
    摘要:The present invention relates to the compound of the Formula I: n n n n n n n n n n and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form. n IM=105109

    专利号:US-12295961-B2
    优先权日:2009-12-31
    标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
    发明人:DHINGRA OM
    权利人:MARIUS PHARMACEUTICALS INC
    摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.
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    主要参考文献


    1: Asai T, Adachi N, Moriya T, Oki H, Maru T, Kawasaki M, Suzuki K, Chen S, Ishii R, Yonemori K, Igaki S, Yasuda S, Ogasawara S, Senda T, Murata T. Cryo-EM Structure of K+-Bound hERG Channel Complexed with the Blocker Astemizole. Structure. 2021 Mar 4;29(3):203-212.e4. doi: 10.1016/j.str.2020.12.007. Epub 2021 Jan 14. 11(3):307-14. doi: 10.2174/187152011795347513.
    156:104929. doi: 10.1016/j.micpath.2021.104929. Epub 2021 Apr 29.
    4: Richards DM, Brogden RN, Heel RC, Speight TM, Avery GS. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28(1):38-61. doi: 10.2165/00003495-198428010-00003. 323(10):684. doi: 10.1056/NEJM199009063231016. 11(1):35-63. doi: 10.1007/BF02802293. 12(2):102-4. doi: 10.1097/00006565-199604000-00009. 104(6):893-4. doi: 10.1177/019459989110400623. 26(11):1388-9. 12(2):025017. doi: 10.1088/1758-5090/ab6d36. 11(5):219-29. 22(6):233-41. French. 10(4):513-516. doi: 10.1039/c8md00562a.

    合成参考文献


    参考文献:10.2147/copd.s21071
    摘要:Wilson R, Anzueto A, Miravitlles M, Arvis P, Faragó G, Haverstock D, Trajanovic M, Sethi S. A novel study design for antibiotic trials in acute exacerbations of COPD: MAESTRAL methodology. Int J Chron Obstruct Pulmon Dis. 2011;6():373–83.
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