CAS: 1706738-98-8; 4-(2-(Cyclopropylmethoxy)-5-(Methylsulfonyl)Phenyl)-2-Methylisoquinolin-1(2H)-One
该化合物是针对基因转录所涉的遗传调节器的小型分子溴素和绝缘蛋白抑制剂.它通过有选择地约束蛋白质,调节了主要的肿瘤和炎症调节器的表达方式,使它成为肿瘤学和炎症研究的有前途的候选体.它在临床前研究中展示了对BRD4的高度选择性和强烈抑制性活动,显示了血解恶性肿瘤和固态肿瘤的潜在效果.Trotabresib的精美化药性皮肤特征和可管理的安全数据支持其在临床环境中的进一步调查.该化合物为研究相互依赖的途径及其治疗影响提供了宝贵的工具.
- 英文名称4-(2-(Cyclopropylmethoxy)-5-(Methylsulfonyl)Phenyl)-2-Methylisoquinolin-1(2H)-One
- 中文名称4-(2-(环丙基甲氧基)-5-(甲基磺酰基)苯基)-2-甲基异喹啉-1(2H)-酮
- IUPAC名称Trotabresib
- CAS编号1706738-98-8
- MFCD编号:MFCD32874157
- FDA UNII编号:K424WH3WU0
- 分子式:C21H21NO4S分子量:383.47
- 产品CID: 870202
- 产品分类Inhibitors/Agonists → Epigenetics → Epigenetic Reader Domain
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- 2905121000-正丙醇
2933310010-吡啶
2905141000-异丁醇
2908199090-其他酚的卤化衍生物 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
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专利信息
专利号:US-11566004-B2
优先权日:2018-07-23
标题 :Process for the preparation of bromodomain inhibitor
发明人：TRAVERSE JOHN FITZGERALD; YONG KELVIN HIN-YEONG; FERRETTI ANTONIO CHRISTIAN; ALITE HEKLA; MOSELEY JONATHAN; RUDA ANTONIO MARIA; PRIMER DAVID; PHILP STEVEN
权利人:CELGENE QUANTICEL RES INC
摘要:The present invention provides processes of synthesis and purification of a bromodomain inhibitor, Compound 1, which compound includes crystalline forms, amorphous forms, solvates, and hydrates thereof. Embodiments of the disclosure relate to chemical synthesis routes of Compound 1 that provide a scalable method that results in highly pure final product. A further embodiment relates to methods to isolate the most stable polymorph of Compound 1 by crystallization from formic acid and water.
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主要参考文献
Moreno V, Sepulveda JM, Vieito M, Hernández-Guerrero T, Doger B, Saavedra O, Ferrero O, Sarmiento R, Arias M, De Alvaro J, Di Martino J, Zuraek M, Sanchez-Pérez T, Aronchik I, Filvaroff EH, Lamba M, Hanna B, Nikolova Z, Braña I. Phase I study of CC-90010, a reversible, oral BET inhibitor in patients with advanced solid tumors and relapsed/refractory non-Hodgkin's lymphoma. Ann Oncol. 2020 Jun;31(6):780-788. doi: 10.1016/j.annonc.2020.03.294. Epub 2020 Mar 30.11:621093. doi: 10.3389/fphar.2020.621093. Pearson AD, DuBois SG, Buenger V, Kieran M, Stegmaier K, Bandopadhayay P, Bennett K, Bourdeaut F, Brown PA, Chesler L, Clymer J, Fox E, French CA, Germovsek E, Giles FJ, Bender JG, Hattersley MM, Ludwinski D, Luptakova K, Maris J, McDonough J, Nikolova Z, Smith M, Tsiatis AC, Vibhakar R, Weiner S, Yi JS, Zheng F, Vassal G. Bromodomain and extra-terminal inhibitors-A consensus prioritisation after the Paediatric Strategy Forum for medicinal product development of epigenetic modifiers in children-ACCELERATE. Eur J Cancer. 2021 Mar;146:115-124. doi: 10.1016/j.ejca.2021.01.018. Epub 2021 Feb 16.
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