H2YL7BN3AK | 139113-48-7

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: H2YL7BN3AK
• 英文别名: (8S,13S,14S,17S)-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
• CAS: 139113-48-7
• 化学式: C₂₁H₂₆O₂
• 分子量: 310.4
• InChiKey: UBLKQAIAGHSEHR-ANULTFPQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  23
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Programmable genotoxic agents and uses therefor
  申请人：——

  公开号：US20030220311A1

  公开（公告）日：2003-11-27

  The compositions and methods disclosed herein provide heterobifunctional programmable genotoxic compounds that can be designed to kill selected cells present in a heterogenous cell population. The present compounds comprise a first agent that inflicts damage on cellular DNA, and a second agent that attracts a macromolecular cell component such as a protein, which in turn shields genomic lesions from repair. Unrepaired lesions therefore persist in the cellular genome and contribute to the death of selected cells. In contrast, lesions formed in nonselected cells, which lack the cell component, are unshielded and thus are repaired. As a result, compounds described herein are less toxic to nonselected cells. Compounds of this invention can be designed to cause the selective killing of transformed cells, viral-infected cells and the like.

  本文所披露的组合物和方法提供了异双功能可编程基因毒性化合物，可以设计用于杀死杂种细胞群落中的选择性细胞。目前的化合物包括第一种对细胞DNA造成损伤的药剂和第二种吸引大分子细胞组分（例如蛋白质）的药剂，该组分反过来又保护基因组损伤不受修复。因此，未修复的损伤会在细胞基因组中持续存在，并有助于选择性细胞的死亡。相比之下，形成在缺乏细胞组分的非选择性细胞中的损伤是未被保护的，因此会得到修复。因此，本文所述的化合物对非选择性细胞的毒性较小。本发明的化合物可以被设计用于选择性杀死转化细胞、病毒感染细胞等。
• Glucocorticoid inhibitors for treatment of prostate cancer
  申请人：Sloan-Kettering Institute for Cancer Research

  公开号：US10919929B2

  公开（公告）日：2021-02-16

  The present invention encompasses the recognition that reproducible and detectable changes in the level and or activity of Glucocorticoid Receptor (GR) are associated with incidence and/or risk of Castration Resistant Prostate Cancer (CRPC) and/or doubly resistant prostate cancer, specifically in individuals having prostate cancer and on antiandrogen therapy, and provides for the use of GR inhibitors to treat and/or reduce risk of CRPC and/or doubly resistant prostate cancer. In some embodiments, GR inhibitors also have Androgen Receptor (AR) inhibitory activity or are administered in conjunction with AR inhibitors. The present invention also provides technologies for identification and/or characterization of agents to treat and/or reduce risk of CRPC and/or doubly resistant prostate cancer; in some embodiments such agents alter level and/or activity of a GR. In some embodiments, provided agents show effects on a GR's activity of regulating transcription of one or more target genes. The present invention also provides systems for using such agents, for example to treat and/or reduce risk of CRPC and/or doubly resistant prostate cancer.

  本发明包括认识到糖皮质激素受体（GR）水平和/或活性的可重复和可检测的变化与阉割抗性前列腺癌（CRPC）和/或双重抗性前列腺癌的发病率和/或风险有关，特别是在患有前列腺癌并接受抗雄激素治疗的个体中，并提供了使用GR抑制剂治疗和/或降低CRPC和/或双重抗性前列腺癌风险的方法。在某些实施方案中，GR抑制剂还具有雄激素受体（AR）抑制活性，或与AR抑制剂联合使用。本发明还提供了用于治疗和/或降低 CRPC 和/或双重抗性前列腺癌风险的制剂的鉴定和/或表征技术；在某些实施方案中，此类制剂可改变 GR 的水平和/或活性。在一些实施方案中，所提供的制剂显示了对 GR 调节一个或多个靶基因转录的活性的影响。本发明还提供了使用此类制剂的系统，例如用于治疗和/或降低 CRPC 和/或双重抗性前列腺癌的风险。
• Methods for inhibiting cognitive deterioration in adults with down's syndrome
  申请人：Corcept Therapeutics, Inc.

  公开号：US20030064974A1

  公开（公告）日：2003-04-03

  This invention generally pertains to the field of psychiatry. In particular, this invention pertains to the discovery that agents capable of inhibiting the binding of cortisol to its receptors can be used in methods for preventing or reversing cognitive deterioration in adults with Down's syndrome. Mifepristone, a potent specific glucocorticoid receptor antagonist, can be used in these methods. The invention also provides a kit for preventing or reversing cognitive deterioration in a DS patient including a glucocorticoid receptor antagonist and instructional material teaching the indications, dosage and schedule of administration of the glucocorticoid receptor antagonist.

  本发明一般涉及精神病学领域。特别是，本发明涉及发现能够抑制皮质醇与其受体结合的制剂可用于预防或逆转患有唐氏综合征的成年人认知功能退化的方法。米非司酮是一种强效的特异性糖皮质激素受体拮抗剂，可用于这些方法中。本发明还提供了一种用于预防或逆转唐氏综合征患者认知功能退化的试剂盒，包括一种糖皮质激素受体拮抗剂和教导糖皮质激素受体拮抗剂的适应症、剂量和给药计划的指导材料。
• [EN] GLUCOCORTICOID INHIBITORS FOR TREATMENT OF PROSTATE CANCER<br/>[FR] INHIBITEURS DE GLUCOCORTICOÏDES POUR LE TRAITEMENT DU CANCER DE LA PROSTATE
  申请人：SLOAN KETTERING INST CANCER

  公开号：WO2015089338A9

  公开（公告）日：2015-08-20
• GLUCOCORTICOID RECEPTOR ANTAGONISTS FOR THE TREATMENT OF DEMENTIA
  申请人：THE BOARD OF TRUSTEES OFTHE LELAND STANFORD JUNIOR UNIVERSITY

  公开号：EP1076562A1

  公开（公告）日：2001-02-21