CAS: 151126-32-8; Pramlintide

该化合物是一种合成的人类阿米林类仿真物,一种用胰岛素与胰岛素共同保存的酸激素.它旨在模仿阿米林的生理影响,主要是在葡萄糖管制中.Pramlintide慢化胃空洞,抑制后春光葡萄素分泌,促进对使用食用胰岛素的1型或2型糖尿病患者的讽刺,使之成为一种宝贵的辅助疗法.它的机制通过处理后性高血糖病,而不增加剂量适当时的低血糖风险来补充胰岛素.Pramlintide是低血糖的亚,在减少淋病变异性方面特别有效.它的临床使用表明,如HbA1c测量的那样,长期的血清控制有所改善,同时支持糖尿病患者的体重管理.

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      专利号:US-12351573-B2
      优先权日:2019-05-09
      标 题:Compounds for use in synthesis of peptidomimetics
      发明人:AL-ABED YOUSEF; CHENG KAI FAN
      权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
      摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

      专利号:US-2023159450-A1
      优先权日:2020-05-08
      标 题 :Dimers for use in synthesis of peptidomimetics
      发明人:AL-ABED YOUSEF; ALTITI AHMAD
      权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
      摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

      专利号:US-2023212216-A1
      优先权日:2019-12-20
      标 题:Synthesis of lactone derivatives and their use in the modification of proteins
      发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH
      权利人:GENIE BIOTECH UK LTD
      摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.

      专利号:US-11440881-B2
      优先权日:2019-05-09
      标题 :Thiosemicarbazates and uses thereof
      发明人:AL-ABED YOUSEF; ALTITI AHMAD
      权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
      摘要:Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.

      专利号:US-2012010186-A1
      优先权日:2009-03-23
      标题:Heterocyclic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
      发明人:LACHANCE NICOLAS; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; TRANMER GEOFFREY K; MARTINS EVELYN; GAREAU YVES
      权利人:LACHANCE NICOLAS; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; TRANMER GEOFFREY K; MARTINS EVELYN; GAREAU YVES; MERCK FROSST CANADA LTD
      摘要:Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.

      专利号:US-2022372022-A1
      优先权日:2019-05-09
      标 题:Compounds for use in synthesis of peptidomimetics
      北京翔宇恒天医药技术有限公司
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      合成参考文献


      参考文献:10.1016/s0026-0495(99)90232-9
      摘要:Nyholm B, Orskov L, Hove KY, Gravholt CH, Møller N, Alberti KG, Moyses C, Kolterman O, Schmitz O. The amylin analog pramlintide improves glycemic control and reduces postprandial glucagon concentrations in patients with type 1 diabetes mellitus. Metabolism. 1999 Jul;48(7):935–41. doi: 10.1016/s0026-0495(99)90232-9.
      参考文献:10.1046/j.1365-2982.2002.00311.x
      摘要:Vella A, Lee JS, Camilleri M, Szarka LA, Burton DD, Zinsmeister AR, Rizza RA, Klein PD. Effects of pramlintide, an amylin analogue, on gastric emptying in type 1 and 2 diabetes mellitus. Neurogastroenterol Motil. 2002 Apr;14(2):123–31. doi: 10.1046/j.1365-2982.2002.00311.x.
      参考文献:10.1016/s1098-3597(09)60008-9
      摘要:Green DE. New therapies for diabetes. Clin Cornerstone. 2007;8(2):58–63; discussion 64. doi: 10.1016/s1098-3597(09)60008-9.
      参考文献:10.1007/s11883-007-0061-0
      摘要:Neff LM, Aronne LJ. Pharmacotherapy for obesity. Curr Atheroscler Rep. 2007 Dec;9(6):454–62. doi: 10.1007/s11883-007-0061-0.
      摘要:Rybka J. [Analogues of amylin, alpha-glucosidase inhibitors and the digestive system in homeostasis regulation]. Vnitr Lek. 2011 Apr;57(4):381–7.
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