CAS: 79547-78-7; (3S,4R)-1-[4-Cyano-4-(4-Fluorophenyl)Cyclohexyl]-3-Methyl-4-Phenylpiperidine-4-Carboxylic Acid,Hydrochloride

该化合物是一种选择性的甲胺H1受体对立物,主要用作眼科和鼻腔配方中的抗脑膜炎,对H1受体的高度亲近性能确保有效减轻过敏症状,如痒,红和犀牛.该化合物表现出快速的动作和持续时间,适合管理急性过敏反应.其低系统吸收能最大限度地减少不利影响风险,增强耐受性.氢氯化叶酸在化学上稳定,与普通药剂受体兼容,有利于配方开发.其特性和特性使得其在临床和OTC应用中选择定向过敏治疗为首选.

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欧盟法规

C&L通报

合成工艺路线路线简述

  • 459-22-3 = 79547-78-7
    反应条件:1.1 Reagents: Sodium Amide Solvents: Toluene; 20 - 25 °C1.2 0.5 H,20 - 25 °C1.3 1 H,20 - 25 °C; 25 °C -> 110 °C; 7 H,110 °C
    标题:Preparation Of (-)-{3S-[1(Cis)-3α,4β]}-1-[4-Cyano-4-(4-Fluorophenyl)Cyclohexyl]-3-Methyl-4-Phenyl-4-Piperidinecarboxylic Acid
    参考文献:Poland]

    = 79547-78-7
    反应条件:1.1 Reagents: Ammonium Formate,Palladium Hydroxide Solvents: Methanol,Dichloromethane; 3 H,Rt1.2 Reagents: Ammonia Solvents: Methanol; Rt1.3 Solvents: Methanol,Diisopropyl Ether; 1 H,Rt1.4 Reagents: Hydrochloric Acid Solvents: Methanol; Rt; 30 Min,Rt1.5 Solvents: Diisopropyl Ether; 1 H,Rt1.6 Solvents: Ethanol,Methanol; 6 H,50 °C
    标题:Practical And Sustainable Synthesis Of Optically Pure Levocabastine,A H1 Receptor Antagonist
    作者:Kang,Sung Kwon; Nam,Dong Hyuk; Ahn,Jaeseung; Lee,Jaemin; Sim,Jaehoon; Et Al
    参考文献:Molecules 日期:2017 卷标:22(11) 页码:1971/1-1971/10

海关参考信息

专利信息


专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

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.

专利号:US-11617758-B2
优先权日:2009-12-31
标 题 :Emulsion formulations
发明人:DHINGRA OM; BERNSTEIN JAMES S
权利人:MARIUS PHARMACEUTICALS LLC
摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic 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.

专利号:US-2013303495-A1
优先权日:2009-12-31
标题:Emulsion formulations
发明人:DHINGRA OM; BERNSTEIN JAMES S
权利人:SOV THERAPEUTICS; DIFFERENTIAL DRUG DEV ASSOCIATES LLC
摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic 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.

专利号:EP-1930323-A1
优先权日:2004-03-11
标 题:Biphenyl compounds useful in the synthesis of muscarinic receptor antagonists

专利号:EP-1930323-B1
优先权日:2004-03-11
标 题:Biphenyl compounds useful in the synthesis of muscarinic receptor antagonists

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主要参考文献


1: Gutnisky A, López Ordieres MG, Rodríguez de Lores Arnaiz G. The Administration of Levocabastine, a NTS2 Receptor Antagonist, Modifies Na(+), K(+)-ATPase Properties. Neurochem Res. 2016 Jun;41(6):1274-80. doi: 10.1007/s11064-015-1823-7. Epub 2016 Jan 7. doi: 10.5414/CP202389. doi: 10.1111/cea.12556. doi: 10.1016/j.jfo.2011.08.016. Epub 2012 Apr 10. French. doi: 10.1002/cpdd.218. Epub 2015 Dec 4. Review. Review. Review. doi: 10.1016/j.anl.2009.11.014. Epub 2010 Feb 6. Review.

合成参考文献


摘要:Gekkan Yakuji. Pharmaceuticals Monthly., 42(1661), 2000
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