📜1H-吲哚-1-胺置于sodium Hydride体系中,用 异丙醇 用作溶剂,化学反应 4.0H,反应生成贝西吡啶 参考文献:Synthesis And Structure−activity Relationships Of N-Propyl-N-(4-Pyridinyl)-1H-Indol-1-Amine (Besipirdine) And Related Analogs As Potential Therapeutic Agents For Alzheimer'S Disease 标题:Synthesis And Structure−activity Relationships Of N-Propyl-N-(4-Pyridinyl)-1H-Indol-1-Amine (Besipirdine) And Related Analogs As Potential Therapeutic Agents For Alzheimer'S Disease 摘要:A Series Of Novel N-(4-Pyridinyl)-1H-Indol-1-Amines And Other Heteroaryl Analogs Was Synthesized And Evaluated In Tests To Determine Potential Utility For The Treatment Of Alzheimer'S Disease. From These Compounds,N-Propyl-N-(4-Pyridinyl)-1H-Indol-1-Amine (Besipirdine,4C) Was Selected For Clinical Development Based On In-Depth Biological Evaluation. In Addition To Cholinomimetic Properties Based Initially On In Vitro Inhibition Of [h-3]Quinuclidinyl Benzilate Binding,In. Vivo Reversal Of Scopolamine-Induced Behavioral Deficits,And Subsequently On Other Results,4C Also Displayed Enhancement Of Adrenergic Mechanisms As Evidenced In Vitro By Inhibition Of [h-3]Clonidine Binding And Synaptosomal Biogenic Amine Uptake,And In Vivo By Reversal Of Tetrabenazine-Induced Ptosis. The Synthesis,Structure-Activity Relationships For This Series,And The Biological Profile Of 4C Are Reported. Doi:10.1021/jm9506433
专利号:US-6512125-B1 优先权日:1994-05-13 标 题 :Preparation of 1H-indol-1-amines 发明人:LEE THOMAS B; GOEHRING KEITH E 权利人:AVENTIS PHARMA INC 摘要:The synthesis of memory enhancing, analgetic, and antidepressant N-alkyl-N-pyridinyl-1H-indol-1-armines is described.
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: Pérez-Martínez FC, Vela-Navarrete R, Virseda J, Ocaña AV, Lluel P, Rekik M, Bienaymé H, Ferté J, Attali P, Palea S. Halothane-anesthetized rabbit: a new experimental model to test the effects of besipirdine and duloxetine on lower urinary tract function. Urol Int. 2011;86(2):210-9. doi: 10.1159/000321226. 5: Huff FJ. Preliminary evaluation of besipirdine for the treatment of Alzheimer's disease. Besipirdine Study Group. Ann N Y Acad Sci. 1996 Jan 17;777:410-4. Erratum in: Drug Metab Dispos 1997 Aug;25(8):1016.
合成参考文献
参考文献:10.1016/0361-9230(96)00163-3|10.1016/s0361-9230(96)00163-3 摘要:Woods-Kettleberger AT, Smith CP, Corbett R, Szewczak MR, Roehr JE, Bores GM, Klein JT, Kongsamut S. Besipirdine (HP 749) reduces schedule-induced polydipsia in rats. Brain Research Bulletin. 1996;41(2):125–30. doi: 10.1016/0361-9230(96)00163-3.