CAS: 189691-06-3; Bremelanotide

该化合物是一种合成的peptide,它是一种作为地中海素受体激动剂的合成peptide,主要被确认为在治疗性功能失常方面,特别是在患有低性欲障碍的妇女中,该物质可能被用于治疗性功能失常;该物质来自自然产生的peptide,目的是通过在大脑中激活特定的受体来刺激性刺激;PT-141与传统的勃起性功能障碍药物有区别,因为它主要不是在血管系统上工作,而是影响中央...

结构式图片

MSDS等安全信息

    上下游产品

    Fmoc-L-色氨酸(Boc)-Oh 3-[(S)-2-Carboxy-2-(9H-Fluoren-9-Ylmethoxycarbonylamino)Ethyl]Indole-1-Carboxylic Acid Tert-Butyl Ester 143824-78-6

    合成工艺路线路线简述

      N-Fmoc-N'-三苯甲基-L-组氨酸,N-[(9H-芴-9-甲氧基)羰基]-N'-[(2-丙烯氧基)羰基]-L-赖氨酸,Fmoc-L-天冬氨酸 4-烯丙酯,Fmoc-L-色氨酸(Boc)-Oh,Alkaline Earth Salt Of/the/ Methylsulfuric Acid 以23.9%的收率获得布雷默浪丹 Pt 141
      参考文献:Detection And Control Of Aspartimide Formation In The Synthesis Of Cyclic Peptides
      标题:Detection And Control Of Aspartimide Formation In The Synthesis Of Cyclic Peptides
      摘要:Extensive Two-Dimensional NMR Analysis Was Employed To Characterize The Structural Identity Of The Macrocyclic Peptide Lactam And The Imide Analog,A Major Side Reaction Product When Allyl Ester Was Used To Protect The Side Chain Of Aspartic Acid. A Straightforward Protocol Modification Was Developed To Minimize Aspartimide Formation During The Synthesis Of Cyclic Peptides. (C) 2004 Elsevier Ltd. All Rights Reserved.
      Doi:10.1016/j.Bmcl.2004.12.025

      海关参考信息

      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: Simon JA, Kingsberg SA, Portman D, Williams LA, Krop J, Jordan R, Lucas J, Clayton AH. Long-Term Safety and Efficacy of Bremelanotide for Hypoactive Sexual Desire Disorder. Obstet Gynecol. 2019 Nov;134(5):909-917. doi: 10.1097/AOG.0000000000003514.
      2: Kingsberg SA, Clayton AH, Portman D, Williams LA, Krop J, Jordan R, Lucas J, Simon JA. Bremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials. Obstet Gynecol. 2019 Nov;134(5):899-908. doi: 10.1097/AOG.0000000000003500.
      3: Dhillon S, Keam SJ. Bremelanotide: First Approval. Drugs. 2019 Sep;79(14):1599-1606. doi: 10.1007/s40265-019-01187-w. Review. Review. Available from http://www.ncbi.nlm.nih.gov/books/NBK544629/ doi: 10.1016/j.jsxm.2019.05.012. Epub 2019 Jul 2. doi: 10.1080/14656566.2019.1582644. Epub 2019 Feb 26. doi: 10.1080/14728214.2018.1527901. Epub 2018 Oct 11. Review. doi: 10.1097/AOG.0000000000002733. doi: 10.1016/j.sxmr.2018.01.003. Epub 2018 Mar 22. Review. doi: 10.1016/j.esxm.2018.01.004. Epub 2018 Mar 6. Review.
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