CAS: 139133-26-9; Lexipafant

该化合物是强力和选择性的小板球活性受体抗体,主要调查其在炎症和血栓条件下的治疗潜力,其行动机制包括竞争抑制PAF的束缚,从而调节炎症反应和聚盘.莱克西帕凡是PAF受体的高度亲近性,在急性胰腺炎,败血症和血清复发性伤害的临床前型模型中表现出了效力.该化合物的特点和药用动力特征使它成为瞄准PAF介导路径的有希望的候选物.其发展有助于加深了解PAF在病理学中的作用,为未来在关键护理和炎症中的治疗应用提供见解.

结构式图片

MSDS等安全信息

    合成工艺路线路线简述

      📜Ethyl (2S)-2-[[4-[[(3-Aminopyridin-4-yl)Amino]Methyl]Phenyl]Sulfonyl-Methylamino]-4-Methylpentanoate 以55的收率获得1,2-丙二醇,3-(2-乙氧基苯氧基)-,(S)-(9Ci)
      参考文献:4-(1H-2-Methylimidazo[4,5-C]Pyridinylmethyl)Phenylsulphonamide
      标题:4-(1H-2-Methylimidazo[4,5-C]Pyridinylmethyl)Phenylsulphonamide
      摘要:本发明涉及一般式i的化合物及其药学和兽医学上可接受的酸盐或水合物.本发明还涉及含有一般式i的化合物的药物和兽医学组合物.本发明的一般式i的化合物是血小板活化因子(paf)的拮抗剂.因此,本发明还涉及用于预防,治疗或缓解paf介导的各种疾病或生理状况的人类或哺乳动物的方法.

      海关参考信息

      专利信息


      专利号:US-2008287407-A1
      优先权日:2003-12-10
      标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
      发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
      权利人:NITROMED INC
      摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

      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: Oztürk H, Oztürk H, Dokucu AI, Otcu S. Effects of lexipafant (BB-882), a platelet activating factor receptor antagonist, on liver damage due to bile duct ligation in rats. Acta Gastroenterol Belg. 2006 Apr-Jun;69(2):197-202.
      4: Börjesson A, Wang X, Sun Z, Inghammar M, Truedsson L, Andersson R. Early treatment with lexipafant, a platelet-activating factor-receptor antagonist, is not sufficient to prevent pulmonary endothelial damage after intestinal ischaemia and reperfusion in rats. Dig Liver Dis. 2002 Mar;34(3):190-6. Review.
      12: Schwartz JD, Shamamian P, Grossi EA, Schwartz DS, Marcus SG, Steiner F, Jacobs CE, Tayyarah M, Eng K, Colvin SB, Galloway AC. Lexipafant inhibits platelet activating factor enhanced neutrophil functions. J Surg Res. 1997 May;69(2):240-8. Review. Review.

      合成参考文献


      参考文献:10.3109/00365529609104996
      摘要:Kingsnorth AN. Platelet-Activating Factor. Scandinavian Journal of Gastroenterology. 1996 Jan;31(sup219):28–31. doi: 10.3109/00365529609104996.
      参考文献:10.1080/135502801300069692
      摘要:Smith DG, Guillemin GJ, Pemberton L, Kerr S, Nath A, Smythe GA, Brew BJ. Quinolinic acid is produced by macrophages stimulated by platelet activating factor, Nef and Tat. J Neurovirol. 2001 Feb;7(1):56–60. doi: 10.1080/135502801300069692.
      参考文献:10.1021/jm010852p
      摘要:Carceller E, Salas J, Merlos M, Giral M, Ferrando R, Escamilla I, Ramis J, García-Rafanell J, Forn J. Novel azo derivatives as prodrugs of 5-aminosalicylic acid and amino derivatives with potent platelet activating factor antagonist activity. J Med Chem. 2001 Aug 30;44(18):3001–13. doi: 10.1021/jm010852p.
      参考文献:10.1016/s0016-5085(98)85715-6|10.1177/000313489906500703
      摘要:Liu Q, Djuricin G, Rossi H, Bewsey K, Nathan C, Gattuso P, Weinstein RA, Prinz RA. The effect of lexipafant on bacterial translocation in acute necrotizing pancreatitis in rats. Am Surg. 1999 Jul;65(7):611–6; discussion 617. doi: 10.1016/s0016-5085(98)85715-6.
      参考文献:10.1159/000052027
      摘要:McKay CJ. Recent developments in the management of acute pancreatitis. Dig Surg. 2002;19(2):129–34. doi: 10.1159/000052027.
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