地仑雄酮 | 63014-96-0

• 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
• 中文名称: 地仑雄酮
• 中文别名: 待兰特绒
• 英文名称: 1α-Methylandrosta-4,16-dien-3-on
• 英文别名: 1α-methyl-androsta-4,16-dien-3-one；Delanterone；(1S,8S,9S,10R,13R,14S)-1,10,13-trimethyl-1,2,6,7,8,9,11,12,14,15-decahydrocyclopenta[a]phenanthren-3-one
• CAS: 63014-96-0
• 化学式: C₂₀H₂₈O
• 分子量: 284.442
• InChiKey: GDONNNQFENTLQC-VWTPSIDOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  21
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  17.1
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  地仑雄酮 生成 1α-Methyl-6β-chlorandrosta-4,16-dien-3-on
  参考文献：
  名称：

  DE2631915

  摘要：

  公开号：
• 作为产物：
  描述：

  17beta-羟基-1alpha-甲基雄甾-4-烯-3-酮 生成 地仑雄酮
  参考文献：
  名称：

  DE2631915

  摘要：

  公开号：

文献信息

• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• Combination of an antiandrogen with a vitamin K antagonist or with a gamma-glutamyl carboxylase inhibitor for the therapy of androgen receptor positive cancer
  申请人：CeMM—Forschungszentrum für Molekulare Medizin GmbH

  公开号：US10864190B2

  公开（公告）日：2020-12-15

  The present invention relates to the combination of an antiandrogen with a vitamin K antagonist or with a γ-glutamyl carboxylase inhibitor for use in the treatment or prevention of an androgen receptor positive cancer, such as prostate cancer, or a hyperactive androgen receptor signaling disease/disorder. The invention also relates to a vitamin K antagonist or a γ-glutamyl carboxylase inhibitor for use in resensitizing an antiandrogen-resistant prostate cancer to the treatment with an antiandrogen. The invention further provides a pharmaceutical composition comprising an antiandrogen, a vitamin K antagonist or a γ-glutamyl carboxylase inhibitor, and a pharmaceutically acceptable excipient.

  本发明涉及一种抗雄激素与维生素K拮抗剂或与γ-谷氨酰羧化酶抑制剂的组合，用于治疗或预防雄激素受体阳性癌症，如前列腺癌，或雄激素受体信号亢进疾病/紊乱。本发明还涉及一种维生素 K 拮抗剂或γ-谷氨酰羧化酶抑制剂，用于使抗雄激素耐药的前列腺癌对抗雄激素治疗重新敏感。本发明进一步提供了一种药物组合物，它包含一种抗雄激素、一种维生素 K 拮抗剂或一种 γ-谷氨酰羧化酶抑制剂和一种药学上可接受的赋形剂。
• PHARMACEUTICAL PREPARATION COMPRISING AN ACTIVE DISPERSED ON A MATRIX
  申请人：ALTANA Pharma AG

  公开号：EP1341527A1

  公开（公告）日：2003-09-10