CAS: 249921-19-5; 2-Amino-N-[(2R)-1-[(3R)-3-Benzyl-3-[dimethylamino(Methyl)Carbamoyl]Piperidin-1-Yl]-3-(1H-Indol-3-yl)-1-Oxopropan-2-Yl]-2-Methylpropanamide

该化合物是一种选择性的grelin受体激动剂,旨在解决暗礁和肌肉消瘦问题,特别是在癌症患者中,它模仿grelin行动,刺激食欲,促进肌肉蛋白合成;在临床上,Anamorelin在提高瘦质体重和体重的同时,在改善营养参数方面表现出了效力;其机制针对grelin途径,而没有直接影响肿瘤生长,提供了集中的治疗方法;复合物展示了口服生物利用率和有利的药用动能特征,使之适合慢性病的治疗;研究强调了其在减轻与癌症有关的暗礁方面的潜力,保持肌肉质量和重量对于患者的结果至关重要;继续进一步研究,探索其在代谢紊乱方面的更广泛应用.

结构式图片

欧盟法规

C&L通报

上下游产品

(R,R)-{1-[2-[3-Benzyl-3-(N,N',N'-Trimethyl-Hydrazinocarbonyl)Piperidin-1-Yl]-1-(1H-Indol-3-Ylmethyl)-2-Oxo-Ethylcarbamoyl]-1-Methylethyl}Carbamic Acid Tert-Butyl Ester 339539-90-1
N-[n-[(1,1-二甲基乙氧基)羰基]-2-甲基丙氨酰]-D-色氨酸 (R)-2-(2-Tert-Butoxycarbonylamino-2-Methyl-Propionylamino)-3-(1H-Indol-3-yl)-Propionic Acid 159634-94-3

合成工艺路线路线简述

    📜D-色氨酸置于盐酸,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,三乙胺,3-羟基-1,2,3-苯并三嗪-4(3H)-酮体系中,用 二氯甲烷,乙酸乙酯 用作溶剂,化学反应 20.0H,反应生成阿拉莫林
    参考文献:A Practical Synthesis Of The Pseudotripeptide Rc-1291
    标题:A Practical Synthesis Of The Pseudotripeptide Rc-1291
    摘要:The Rapid Process Development Of A Scaleable Synthesis Of The Pseudotripeptide Rc-1291 For Preclinical And Clinical Evaluation Is Described. By Employing A Nontraditional N-To-C Coupling Strategy,The Peptide Chain Of Rc-1291 Was Assembled In High Yield,With Minimal Racemization And In An Economical Manner By Introducing The Most Expensive Component Last. A One-Pot Deprotection/crystallization Procedure Was Developed For The Isolation Of Rc-1291 Free Base,Which Afforded The Target Compound In Excellent Yield And With A Purity Of > 99.5% Without Chromatographic Purification.
    Doi:10.1021/op0502506

    海关参考信息

    专利信息


    专利号:IT-201800009235-A1
    优先权日:2018-10-08
    标题 :Process for the synthesis of exosomes containing heat shock proteins and their use for the treatment of muscle atrophy and cachexia

    专利号:EP-2644618-B1
    优先权日:2007-02-09
    标题 :tether intermediates for the synthesis of macrocyclic ghrelin receptor modulators

    专利号:EP-2644618-A1
    优先权日:2007-02-09
    标题:tether intermediates for the synthesis of macrocyclic ghrelin receptor modulators

    专利号:WO-2024114661-A1
    优先权日:2022-12-01
    标题 :7-azaindole compounds, preparation method therefor, and use thereof
    发明人:DONG XIAOCHUN; ZHANG XIONGWEN; ZHAO WEILI; Sun Weikuan; RUAN LI; WANG XIAOTING; FAN RONG; GU XIAOFAN
    权利人:UNIV FUDAN; UNIV EAST CHINA NORMAL
    摘要:Disclosed in the present invention are 7-azaindole compounds, a preparation method therefor, and the use thereof, belonging to the field of drug synthesis. The present invention particularly relates to 7-azaindole compounds containing pyrazole or indole substitution represented by general formula (I), a preparation method therefor, and the use thereof in medicine. The compounds of the present invention alleviate cancer cachexia skeletal muscle atrophy by means of inhibiting ActRIIB protein in the MSTN pathway, thereby achieving a remarkable anti-cancer-cachexia effect. Experimental results show that the compounds have good anti-cachexia activity and thus can further be used for preparing novel anti-cachexia drugs.

    专利号:CN-117384063-A
    优先权日:2023-08-29
    标题:A kind of synthesis process and product of trimethylhydrazine

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Matsukane R, Minami H, Fujimori N, Ueda K, Komori Y, Takamatsu Y, Ueda T, Kimura M, Matsuzaki C, Tanaka T, Morito A, Kuwahara S, Hashimoto M, Hirai S, Yokoyama T, Ishida S, Hirota T, Ogawa Y, Uchida M. Prospective study of anamorelin in pancreatic cancer cachexia: Clinical and translational insights into response heterogeneity. Clin Nutr. 2026 Jan 20;58:106581. doi: 10.1016/j.clnu.2026.106581. Epub ahead of print. 13(11):e70398. doi: 10.1002/rcr2.70398.
    4: Yamamoto K, Kurokawa Y, Miyazaki Y, Omori T, Yanagimoto Y, Shinno N, Takeno A, Kawabata R, Akamaru Y, Sugimura K, Matsuyama J, Kimura Y, Yamashita K, Saito T, Takahashi T, Yamada T, Eguchi H, Doki Y. Efficacy and safety of anamorelin for cancer cachexia in patients with unresectable or recurrent gastric cancer: a multicentre, open-label, randomised controlled trial. EClinicalMedicine. 2025 Sep 22;88:103500. doi: 10.1016/j.eclinm.2025.103500.
    5: Yoshida D, Ishimatsu M, Nakashima S, Nakano K, Ishida S, Orimoto H, Miyagahara T, Yada K, Matsumoto T, Kawanaka H. Impact of the Timing of Initial Anamorelin Administration in Advanced Gastrointestinal Cancer With Cancer Cachexia. In Vivo. 2025 Nov-Dec;39(6):3406-3411. doi: 10.21873/invivo.14137.

    合成参考文献


    摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).
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