Ethyl 2-((S)-2-Benzyl-3-((3R,4R)-4-(3-Hydroxyphenyl)-3,4-Dimethylpiperidin-1-yl)Propanamido)Acetate Hydrochloride置于水,Sodium Hydroxide体系中,用 异丙醇 用作溶剂,化学反应 1.0H,以88.6 G的收率获得爱维莫潘 参考文献: An Improved Process For The Preparation Of [[2(S)-[[4(R)-(3-Hydroxy Phenyl)-3(R),4-Dimethyl-1-Piperidinyl]Methyl]-1-Oxo-3-Phenylpropyl] Amino]Acetic Acid Dihydrate[fr] Procédé Amélioré De Préparation De Dihydrate D'Acide [[2(S)-[[4(R)-(3-Hydroxyphényl)-3(R),4-Diméthyl-1-Pipéridinyl]Méthyl]-1-Oxo-3-Phénylpropyl]Amino]Acétique 标题: An Improved Process For The Preparation Of [[2(S)-[[4(R)-(3-Hydroxy Phenyl)-3(R),4-Dimethyl-1-Piperidinyl]Methyl]-1-Oxo-3-Phenylpropyl] Amino]Acetic Acid Dihydrate[fr] Procédé Amélioré De Préparation De Dihydrate D'Acide [[2(S)-[[4(R)-(3-Hydroxyphényl)-3(R),4-Diméthyl-1-Pipéridinyl]Méthyl]-1-Oxo-3-Phénylpropyl]Amino]Acétique 摘要:本发明涉及一种改进的制备[[2(S)-[[4(R)-(3-羟基苯基)-3(R),4-二甲基-1-哌啶基]甲基]-1-氧代-3-苯基丙基]氨基]乙酸二水合物的方法,其结构式如下:
专利号:US-2012165520-A1 优先权日:2010-12-23 标题:Process for the synthesis of prodrugs of opioids 发明人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.
专利号:US-9765027-B2 优先权日:2014-08-22 标题 :Substituted 1-arylethyl-4-acylaminopiperidine derivatives as opioid/alpha-adrenoreceptor modulators and method of their preparation 发明人:VARDANYAN RUBEN S; HRUBY VICTOR J 权利人:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZAONA; UNIV ARIZONA 摘要:The invention provides compounds that bind with high affinities to the μ-, δ- and κ-opioid receptors and α 2 -adrenoreceptor. In addition to providing these compounds with novel pharmacological binding properties, the invention also describes detailed novel methods for the preparation of representative compounds and a scheme for the synthesis of related compounds that bind to the opioid receptors and/or α 2 -adrenoreceptor.
专利号:US-9580409-B2 优先权日:2011-11-07 标 题:Modulators of opioid receptors and methods of use thereof 发明人:MALCOLM SCOTT; BOWEN CARRIE; MELNICK LAURENCE; XIE LINGHONG 权利人:SUNOVION PHARMACEUTICALS INC; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., μ-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
专利号:US-2023407258-A1 优先权日:2019-09-16 标 题:Treatment of disc degenerative disease and stimulation of proteoglycan synthesis by fibroblast conditioned media and formulations thereof
专利号:WO-2021055448-A1 优先权日:2019-09-16 标题:Treatment of disc degenerative disease and stimulation of proteoglycan synthesis by fibroblast conditioned media and formulations thereof
专利号:CA-3154063-A1 优先权日:2019-09-16 标 题 :Treatment of disc degenerative disease and stimulation of proteoglycan synthesis by fibroblast conditioned media and formulations thereof
1: Adam MA, Sun Z, Kim J, Thacker JK. Reply to Letter: Alvimopan Is Associated With Improved Outcomes and Cost Savings in Enhanced Recovery Colorectal Surgery Protocols. Ann Surg. 2016 Jun 8. [Epub ahead of print] doi: 10.1016/j.jamcollsurg.2016.01.051. Epub 2016 Feb 5. 5: Shah KN, Waryasz G, DePasse JM, Daniels AH. Prevention of Paralytic Ileus Utilizing Alvimopan Following Spine Surgery. Orthop Rev (Pavia). 2015 Sep 28;7(3):6087. doi: 10.4081/or.2015.6087. eCollection 2015 Sep 28. 6: Cui Y, Chen H, Qi L, Zu X, Li Y. Effect of alvimopan on accelerates gastrointestinal recovery after radical cystectomy: A systematic review and meta-analysis. Int J Surg. 2016 Jan;25:1-6. doi: 10.1016/j.ijsu.2015.11.013. Epub 2015 Nov 18. Review. doi: 10.1097/SLA.0000000000001428. doi: 10.1586/17474124.2015.1095637. Epub 2015 Oct 21.
合成参考文献
参考文献:10.2165/00126839-200607040-00004 摘要:Alvimopan: ADL 8-2698, ADL 82698, Entrareg, LY 246736. Drugs R D. 2006;7(4):245–53. doi: 10.2165/00126839-200607040-00004. 参考文献:10.1111/j.1365-2982.2011.01709.x 摘要:Tack J, Müller-Lissner S, Stanghellini V, Boeckxstaens G, Kamm MA, Simren M, Galmiche JP, Fried M. Diagnosis and treatment of chronic constipation--a European perspective. Neurogastroenterol Motil. 2011 Aug;23(8):697–710.