CAS: 53882-12-5; 2,2'-((2-Chloro-5-Cyano-1,3-Phenylene)Bis(Azanediyl))Bis(2-Oxoacetic Acid)

该化合物是一种化学化合物,主要用作抗过敏剂,属于被称为甲状腺细胞稳定剂的化合物类别,其作用是阻止胸腔细胞释放甲胺和其他炎性调剂,这有助于缓解与过敏反应有关的症状,如结膜炎和鼻炎. Lodoxamide通常以眼滴的形式对眼科进行施用,或对呼吸过敏作鼻喷剂.该化合物的特点是水溶性较低,影响其配制和输送方法.此外,该化合物有一个特定的分子结构,有助于其药性,包括有选择地针对乳腺细胞的能力.通过临床研究建立了安全性和效率简介,在过敏管理中成为有价值的选择.与任何药物一样,潜在副作用可能发生,用户必须咨询保健专业人员,以便适当使用.

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CAS号53882-13-6 lodoxamide ethyl | CAS号1930-72-9 4-氯-3,5-二硝基苯甲腈 | CAS号34207-46-0 diethyl 2,2'-(2...

合成工艺路线路线简述

    📜4-氯-3,5-二硝基苯甲腈置于盐酸,Sodium Hydroxide,三乙胺,Tin(Ll) Chloride体系中,用 二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 诺朵腊酸
    参考文献:N,N'-(Phenylene)Dioxamic Acids And Their Esters As Antiallergy Agents
    标题:N,N'-(Phenylene)Dioxamic Acids And Their Esters As Antiallergy Agents
    摘要:A Series Of Dialkyl N,N'-(M-Phenylene)Dioxamates Was Synthesized By Treatment Of The Requisite M-Phenylenediamines With An Alkyloxalyl Chloride In The Presence Of Triethylamine. Hydrolysis With Sodium Hydroxide Solution Gave The Corresponding N,N'-(M-Phenylene)Dioxamic Acids. Several N,N'-(P-Phenylene)Dioxamic Acids Were Synthesized Also In The Same Manner Starting With The Requisite P-Phenylenediamines. These Compounds Were Tested In The Rat Passive Cutaneous Anaphylaxis (Pca) Assay. When Tested Iv,Activity Was Found In The N,N'-(M-Phenylene) Dioxamic Acids Up To 2500 Times That Shown By Disodium Cromoglycate [50% Inhibition At 0.001 Mg/kg For N,N'-(2-Chloro-5-Cyano-M-Phenylene)Dioxamic Acid (Compound 61)]. Oral Activity Was Seen In This Series Of Compounds With Duration Of Activity Up To 120 Min. Oral Activity Was Detected In Diethyl N,N'-(2-Chloro-5-Cyano-M-Phenylene)Dioxamate (Compound 38) At Levels Of Drug As Low As 0.1 Mg/kg.
    DOI:10.1021/jm00207A016

    海关参考信息

    专利信息


    专利号:US-6277489-B1
    优先权日:1998-12-04
    标题:Support for high performance affinity chromatography and other uses
    发明人:ABBOTT NICHOLAS; STROEVE PIETER; DUBROVSKY TIMOTHY B; HOU ZHIZHONG
    权利人:UNIV CALIFORNIA
    摘要:Multilayered particulate materials are formed by coating a particulate substrate with a metal and adsorbing an organic layer comprising a recognition moiety onto the metal film. The recognition moiety interacts with an analyte of interest allowing for its detection, purification, etc. Suitable recognition moieties can be selected from a range of species including, small molecules, polymers and biomolecules and the like. The novel particulate materials of the invention can be utilized in an array of methods including, ion-exchange, ion-selective ion-exchange, assays, affinity dialysis, size exclusion dialysis, as supports in solid phase synthesis, combinatorial synthesis and screening of compound libraries and the like.

    专利号:US-2009081274-A1
    优先权日:2003-10-17
    标题 :Mast cell-derived renin
    发明人:SILVER RANDI B; LEVI ROBERTO
    权利人:CORNELL RES FOUNDATION INC
    摘要:The invention relates to the discovery that renin is present in mast cells and can act in a localized manner to initiate and/or exacerbate a number of conditions. Thus, the invention provides methods for treating cardiac, vascular, lung, liver, cervical, intestinal, muscle, pancreatic, brain, kidney, skin and other conditions that involve inhibiting the synthesis and/or release of renin from mast cells and/or inhibiting the activity of renin after release from mast cells. The methods of the invention can also involve inhibiting elements of the local renin-angiotensin system (e.g. inhibiting ACE and angiotensin II receptors), thereby inhibiting angiotensin II produced locally from mast-cell-derived renin

    专利号:US-2011263650-A1
    优先权日:2007-07-20
    标 题:Tubulysin D Analogues
    发明人:ELLMAN JONATHAN A; PATTERSON ANDREW W; PELTIER HILLARY; SASSE FLORENZ
    权利人:HELMHOLTZ INFEKTIONSFORSCHUNG
    摘要:The present invention provides novel tubulysin analogues, methods of making and methods of using such analogues and conjugates thereof. The essential features for the potent cytotoxicity of tubulysin D have been established for the first time by the synthesis and evaluation of a series of analogues. By identifying functionality that surprisingly is not necessary for activity, highly potent cell-growth inhibitors have been developed that are smaller and considerably more stable than tubulysin D.

    专利号:US-2014315720-A1
    优先权日:2012-10-24
    标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
    发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
    权利人:CELANESE ACETATE LLC
    摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: MacKenzie AE, Caltabiano G, Kent TC, Jenkins L, McCallum JE, Hudson BD, Nicklin SA, Fawcett L, Markwick R, Charlton SJ, Milligan G. The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35. Mol Pharmacol. 2014 Jan;85(1):91-104. doi: 10.1124/mol.113.089482. Epub 2013 Oct 10.
    2: Das D, Khan M, Gul A, Alam R. Safety and efficacy of lodoxamide in vernal keratoconjunctivitis. J Pak Med Assoc. 2011 Mar;61(3):239-41. Comparison of lodoxamide 0.1% ophthalmic solution and levocabastine 0.05% ophthalmic suspension in vernal keratoconjunctivitis. Eur J Ophthalmol. 2001 Apr-Jun;11(2):120-5. Br J Ophthalmol. 1998 Oct;82(10):1135-8.
    7: Santos CI, Huang AJ, Abelson MB, Foster CS, Friedlaender M, McCulley JP. Efficacy of lodoxamide 0.1% ophthalmic solution in resolving corneal epitheliopathy associated with vernal keratoconjunctivitis. Am J Ophthalmol. 1994 Apr 15;117(4):488-97.

    合成参考文献


    参考文献:10.2165/11539460-000000000-00000
    摘要:Iskedjian M, Covert DW, Walker JH. Persistence with prostaglandin agonist use with and without adjunctive therapy for glaucoma patients: a Canadian population-based analysis. Patient. 2011;4(2):133–41. doi: 10.2165/11539460-000000000-00000.
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