📜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
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 %.
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.