CAS: 520-85-4; (6S,8R,9S,10R,13S,14S,17R)-17-Acetyl-17-Hydroxy-6,10,13-Trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-Dodecahydro-1H-Cyclopenta[a]Phenanthren-3(2H)-One

该化合物是一种源于 progneone 的合成蛋白质结构结构. 由于其长期的活动和可预测的药用植物基因特征,该化合物在激素治疗中被广泛使用. 该化合物的受体具有高度亲近性,能够有效控制异丙酮的扩散和抑制甲酸酯分泌. 它的主要优势包括口服生物利用率,代谢稳定性,以及临床应用(如避孕,荷尔蒙替代疗法和妇科病治疗)中具有清晰特征的安全特征. 最常见的乙酸甲酯(Medroxyprochesterone acetate)是其最常见的酯状,它提供仓库配方的持续释放,加强治疗的合规性. 化合物的多功能性和既定功效使它成为内分泌治疗的基石.

结构式图片

欧盟法规

ECHA物质ECHA物质C&L通报REACH预注册

上下游产品

CAS号113665-92-2 3β,5,17-trihydr... | CAS号3386-01-4 6β-Methyl-3,20-... | CAS号3386-00-3 17-hydroxypregn... | CAS号3496-78-4 (5α,6α)-Epoxy-1... | CAS号80996-18-5 17α-Hydroxy-6α-... | CAS号1863-39-4 Pregn-5-en-20-o... | CAS号3562-63-8 甲地孕酮 | CAS号595-33-5 醋酸甲地孕酮 | CAS号71-58-9 安宫黄体酮

合成工艺路线路线简述

  • 合成目标产物 Medroxyprogesterone 主要起始原料 Medroxyprogesterone Acetate
  • (文献来源)合成步骤主要原料 Medroxyprogesterone Acetate
醋酸甲羟孕酮置于水,Sodium Hydroxide体系中,用 甲醇 作为反应溶剂,化学反应 5.0H,反应生成 甲羟孕酮
参考文献: Novel Esters Of Medroxyprogesterone[fr] Nouveaux Esters De Médroxyprogestérone
标题: Novel Esters Of Medroxyprogesterone[fr] Nouveaux Esters De Médroxyprogestérone
摘要:本公开涉及醋酸甲羟孕酮的新酯形式,其制备方法以及包含其的药物组合物.本公开还涉及在激素疗法中使用这些新酯形式,例如避孕,激素替代疗法,子宫内膜异位症等.

海关参考信息

专利信息


专利号:US-2021220331-A1
优先权日:2016-05-03
标题:Inhibitors of ires-mediated protein synthesis
发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA
权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS
摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.

专利号:US-10975069-B2
优先权日:2014-04-01
标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
发明人:HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN
权利人:UNIV WASHINGTON
摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.

专利号:US-9573873-B2
优先权日:2014-06-03
标题:Catalytic method for dibenzocycloheptane synthesis and allocolchicinoid synthesis
发明人:GREEN JAMES; MEHDI MARIAM; DJURDJEVIC SINISA
权利人:UNIV OF WINDSOR
摘要:In a non-limiting embodiment, there is provided a compound of formula (I), which may permit for a method or use in treating or preventing a cancer, such as pancreatic cancer or leukemia. In one embodiment, there is also provide a method of preparing a compound of formula (Ia), the method including conducting a cyclization reaction of a compound of formula (III) to obtain a compound of formula (IV), wherein conducting the cyclization reaction comprises conducting a Michael reaction in the presence of a Lewis acid.

专利号:US-4150236-A
优先权日:1976-05-26
标 题 :Steroidal intermediates from the condensation product of dimethyl-3-ketoglutarate and glyoxal
发明人:WEISS ULRICH; RICE KENNER C
权利人:US HEALTH EDUCATION & WELFARE
摘要:Tricyclic aromatic compounds of the formula ##STR1## including those wherein: (A) R 1 is H, R 2 is carbomethoxy, and R 3 is methyl; n (b) R 1 is acetyl, R 2 is carbomethoxy, and R 3 is methyl; n (c) R 1 and R 3 are methyl and R 2 is carbomethoxy; n (d) R 1 , R 2 , and R 3 are hydrogen; and n (e) R 1 and R 3 are methyl and R 2 is hydrogen n Are intermediates for the total synthesis of steroids.

专利号:US-4041055-A
优先权日:1975-11-17
标题:Process for the preparation of 17α-hydroxyprogesterones and corticoids from androstenes
发明人:SHEPHARD KENNETH PAUL; VAN RHEENEN VERLAN H
权利人:UPJOHN CO
摘要:This invention discloses a general process for the production of corticoids from androstenes. This invention provides an economically viable alternative synthesis of 17α-hydroxyprogesterones and the corticoids.

专利号:US-2010247433-A1
优先权日:2005-10-14
标题:Use of non-canonical amino acids as metabolic markers for rapidly-dividing cells
发明人:TIRRELL DAVID; DIETERICH DANIELA C; LINK AARON J; SCHUMAN ERIN
权利人:CALIFORNIA INST OF TECHN
摘要:The invention provides methods, reagents and systems to preferentially mark fast-proliferating cells/tissues (such as cancer), by incorporating non-natural amino acids into proteins, preferably in vivo, using the endogenous protein synthesis machinery of an organism. The incorporated non-natural amino acids contain reactive groups for further chemical reagents, which may serve as a “handleâ€? to for a number of uses, such as imaging of cancer cells, targeting drugs to preferentially kill cancer cells, and proteomic analysis in the context of large scale or high throughput screening for candidate drug leads that affects the proliferation of a target cell, etc.
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主要参考文献


1: Okojie AK, Oyekunle OA. Depo-provera effects on Wistar rat performance in the Y-maze. Metab Brain Dis. 2014 Jun;29(2):529-31. doi: 10.1007/s11011-013-9460-9. Epub 2013 Dec 13. doi: 10.3109/13697137.2013.850481. Epub 2013 Oct 28. doi: 10.1111/vde.12073. Epub 2013 Sep 2. doi: 10.1136/jfprhc-2012-100517. Review. Czech. doi: 10.1080/19440049.2013.848293. Epub 2013 Nov 20. doi: 10.1530/REP-15-0314. Epub 2015 Sep 30. doi: 10.1097/QAD.0000000000000660. doi: 10.1016/j.neuroscience.2012.01.031. Epub 2012 Jan 25. doi: 10.1016/j.hrthm.2012.02.029. Epub 2012 Mar 6. Chinese. doi: 10.1177/1933719115623643. Epub 2015 Dec 29. doi: 10.1089/aid.2009.0185.
19: Lam C, Murthy AS. Depo-Provera (depot medroxyprogesterone acetate) use after bariatric surgery. Open Access J Contracept. 2016 Sep 29;7:143-150. doi: 10.2147/OAJC.S84097. eCollection 2016. Review.
20: Dempsey A, Roca C, Westhoff C. Vaginal estrogen supplementation during Depo-Provera initiation: a randomized controlled trial. Contraception. 2010 Sep;82(3):250-5. doi: 10.1016/j.contraception.2010.04.003. Epub 2010 May 11.

合成参考文献


参考文献:10.1634/theoncologist.2009-0153
摘要:Mantovani G, Macciò A, Madeddu C, Serpe R, Massa E, Dessì M, Panzone F, Contu P. Randomized phase III clinical trial of five different arms of treatment in 332 patients with cancer cachexia. Oncologist. 2010;15(2):200–11.
参考文献:10.1155/2011/601434
摘要:Donohoe CL, Ryan AM, Reynolds JV. Cancer Cachexia: Mechanisms and Clinical Implications. Gastroenterology Research and Practice. 2011;2011():1–13. doi: 10.1155/2011/601434.
参考文献:10.4137/ccrep.s5346
摘要:Fadhlaoui A, Ben Hassouna J, Khrouf M, Zhioua F, Chaker A. Endometrial adenocarcinoma in a 27-year-old woman. Clin Med Insights Case Rep. 2010;3():31–9.
参考文献:10.1093/carcin/bgr134
摘要:Markosyan N, Chen EP, Ndong VN, Yao Y, Sterner CJ, Chodosh LA, Lawson JA, Fitzgerald GA, Smyth EM. Deletion of cyclooxygenase 2 in mouse mammary epithelial cells delays breast cancer onset through augmentation of type 1 immune responses in tumors. Carcinogenesis. 2011 Oct;32(10):1441–9.
参考文献:10.3109/13625187.2011.591456
摘要:Fraser IS, Parke S, Mellinger U, Machlitt A, Serrani M, Jensen J. Effective treatment of heavy and/or prolonged menstrual bleeding without organic cause: pooled analysis of two multinational, randomised, double-blind, placebo-controlled trials of oestradiol valerate and dienogest. The European Journal of Contraception & Reproductive Health Care. 2011 Jul 20;16(4):258–69. doi: 10.3109/13625187.2011.591456.
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