CAS: 170851-70-4; (2S)-6-Amino-2-[[(2R)-2-[[(2R)-2-[[(2S)-2-[(2-Amino-2-Methylpropanoyl)Amino]-3-(4H-Imidazol-4-yl)Propanoyl]Amino]-3-Naphthalen-2-Ylpropanoyl]Amino]-3-Phenylpropanoyl]Amino]Hexanamide

该化合物是一种合成的五溴二苯醚,被归类为生长激素秘室(GHS) . 它有选择地刺激通过grelin受体(GHSR-1a)释放生长激素(GHH),但不会显著影响皮质素或蛋白素水平. 它的机制模仿了内生的grelin , 提倡肺脏动物GH分泌, 同时又保持生理反馈调节. Ipamorelin 表现出高度的特殊性, 最低目标外效应, 以及由于它的短半衰期和可预测的药用植物基因技术而具有有利的安全特征. 研究凸显了它在研究GHH缺乏和代谢监管方面的潜力. 它的稳定性和选择性行动使得它成为内分泌研究的宝贵工具, 在不干扰其他荷尔蒙轴的情况下提供与GHG有关路径的洞察力.

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      专利信息


      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-2020354404-A1
      优先权日:2019-05-09
      标 题 :Peptidomimetic agents, synthesis and uses thereof
      发明人:AL-ABED YOUSEF
      权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
      摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

      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-2022372022-A1
      优先权日:2019-05-09
      标 题:Compounds for use in synthesis of peptidomimetics

      专利号:US-10919882-B2
      优先权日:2019-05-09
      标题:Compounds for use in synthesis of peptidomimetics

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      主要参考文献


      1: Semenistaya E, Zvereva I, Thomas A, Thevis M, Krotov G, Rodchenkov G. Determination of growth hormone releasing peptides metabolites in human urine after nasal administration of GHRP-1, GHRP-2, GHRP-6, Hexarelin, and Ipamorelin. Drug Test Anal. 2015 Oct;7(10):919-25. doi: 10.1002/dta.1787. . Prospective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients. Int J Colorectal Dis. 2014 Dec;29(12):1527-34. doi: 10.1007/s00384-014-2030-8. doi: 10.2147/JEP.S35396.
      4: Venkova K, Mann W, Nelson R, Greenwood-Van Meerveld B. Efficacy of ipamorelin, a novel ghrelin mimetic, in a rodent model of postoperative ileus. J Pharmacol Exp Ther. 2009 Jun;329(3):1110-6. doi: 10.1124/jpet.108.149211.

      合成参考文献


      参考文献:10.2165/00126839-199901030-00001
      摘要:Reginster JY, Henrotin Y, Gosset C. Promising new agents in osteoporosis. Drugs R D. 1999 Mar;1(3):195–201. doi: 10.2165/00126839-199901030-00001.
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