Androst-4-en-3,11-dion | 570-29-6

• 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: Androst-4-en-3,11-dion
• 英文别名: Androst-4-ene-3,11-dione；(8S,9S,10R,13S,14S)-10,13-dimethyl-2,6,7,8,9,12,14,15,16,17-decahydro-1H-cyclopenta[a]phenanthrene-3,11-dione
• CAS: 570-29-6
• 化学式: C₁₉H₂₆O₂
• 分子量: 286.414
• InChiKey: LUGQRKYQVJFUBW-AEIBSFOJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  21
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.79
• 拓扑面积：
  34.1
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] 17-SUBSTITUTED STEROIDS USEFUL IN CANCER TREATMENT<br/>[FR] STEROÏDES SUBSTITUES-17 UTILES POUR LE TRAITEMENT DU CANCER
  申请人：BRITISH TECHNOLOGY GROUP LTD.

  公开号：WO1993020097A1

  公开（公告）日：1993-10-14

  (EN) Compounds of general formula (1) wherein X represents the residue of the A, B and C rings of a steroid, R represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, R14 represents a hydrogen atom and R15 represents a hydrogen atom or an alkyl or alkoxy group of 1-4 carbon atoms, or a hydroxy or alkylcarbonyloxy group of 2 to 5 carbon atoms or R14 and R15 together represent a double bond, and R16 represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, in the form of the free bases or pharmaceutically acceptable acid addition salts, with the proviso that 17-(3-pyridyl)androsta-5,14,16-trien-3$g(b)-ol and 15$g(b)-acetoxy-17-(3-pyridyl)androsta-5,16-dien-3$g(b)-ol and their 3-acetates and 3$g(b)-methoxy-17-(3-pyridyl)androst-16-ene are claimed only for use in therapy are useful for treatment of androgen-dependent disorders, especially prostatic cancer, and also oestrogen-dependent disorders such as breast cancer.(FR) Composés de formule générale (1) dans laquelle X représente le reste des cycles A, B et C d'un stéroïde, R représente un atome d'hydrogène ou un groupe alkyle comprenant de 1 à 4 atomes de carbone, R14 représente un atome d'hydrogène et R15 représente un atome d'hydrogène ou un groupe alkyle ou alcoxy comprenant de 1 à 4 atomes de carbone, ou un groupe hydroxy ou alkylcarbonyloxy comprenant de 2 à 5 atomes de carbone ou R14 et R15 représentent conjointement une liaison double, et R16 représente un atome d'hydrogène ou un groupe alkyle comprenant de 1 à 4 atomes de carbone, sous la forme de bases libres ou de sels d'addition acide pharmaceutiquement acceptables, à condition que 17-(3-pyridyle)androsta-5,14,16-triène-3$g(b)-ol et 15$g(b)-acétoxy-17-(3-pyridyle)androsta-5,16-diène-3$g(b)-ol et leurs 3-acétates et 3$g(b)-méthoxy-17-(3-pyridyle)androst-16-ène sont revendiqués seulement pour usage thérapeutique. Les composés de l'invention sont utiles pour le traitement des affections dépendant de l'androgène, notamment le cancer prostatique, et également des affections dépendant de l'oestrogène telles que le cancer du sein.

  (中文) 通式（1）中X代表类固醇的A，B和C环的残基，R代表氢原子或1至4个碳原子的烷基，R14代表氢原子，R15代表氢原子或1-4个碳原子的烷基或烷氧基，或2至5个碳原子的羟基或烷基羰氧基，或R14和R15共同表示双键，R16代表氢原子或1至4个碳原子的烷基，以自由碱或药学上可接受的酸加成盐的形式存在，但17-(3-吡啶基)雄烯-5,14,16-三烯-3$g(b)-醇和15$g(b)-乙酰氧基-17-(3-吡啶基)雄烯-5,16-二烯-3$g(b)-醇及其3-乙酸酯和3$g(b)-甲氧基-17-(3-吡啶基)雄烯-16-烯仅声称用于治疗，用于治疗雄激素依赖性疾病，特别是前列腺癌，以及雌激素依赖性疾病，如乳腺癌。
• Microbiological preparation of 9-alpha-hydroxy-17-keto steroids
  申请人：ROUSSEL-UCLAF

  公开号：EP0322081A1

  公开（公告）日：1989-06-28

  9α-hydroxy-17-keto steroids are prepared by fermenting steroids having a C-17 side chain of 5-10 carbon atoms inclusive, with the novel Mycobacterium species CBS 482.86. Starting from various substrates containing a 5-10 C carbon chain an C-17, 9α-hydroxyandrost-4-ene-3,17-dione, 7α,9α,12α-trihydroxyandrost-4-ene-3,17-dione or 9α-­hydroxyandrost-4,11-diene-3,17-dione are obtained in high yield. The resulting compounds are useful intermediates in the synthesis of therapeutically important steroids, particularly corticosteroids.

  新型分枝杆菌 CBS 482.86 通过发酵具有 5-10 个碳原子的 C-17 侧链的类固醇，制备出 9α-羟基-17-酮类固醇。 从含有 5-10 个碳原子的 C-17 侧链的各种底物开始，可以高产率地获得 9α-羟基雄甾-4-烯-3,17-二酮、7α,9α,12α-三羟基雄甾-4-烯-3,17-二酮或 9α-羟基雄甾-4,11-二烯-3,17-二酮。 所得化合物是合成具有重要治疗作用的类固醇，特别是皮质类固醇的有用中间体。
• Methods and compositions for treating cancer
  申请人：Cougar Biotechnology, Inc.

  公开号：EP2478907A2

  公开（公告）日：2012-07-25

  Methods and compositions for treating cancer are described herein. More particularly, the methods for treating cancer comprise administering a 17α-hydroxylase/C17,20-lyase inhibitor, such as abiraterone acetate (i.e., 3β-acetoxy-17-(3-pyridyl) androsta-5, 16-diene), in combination with at least one additional therapeutic agent such as an anti-cancer agent or a steroid. Furthermore, disclosed are compositions comprising a 17α-hydroxylase/C17,20-lyase inhibitor, and at least one additional therapeutic agent, such as an anti-cancer agent or a steroid.

  本文描述了治疗癌症的方法和组合物。更具体地说，治疗癌症的方法包括施用 17α- 羟化酶/C17,20-赖氨酸酶抑制剂，如醋酸阿比特龙（即 3β-乙酰氧基-17-(3-吡啶基) 雄甾-5,16-二烯），与至少一种额外的治疗剂如抗癌剂或类固醇结合使用。此外，还公开了包含 17α- 羟化酶/C17,20-裂解酶抑制剂和至少一种额外治疗剂（如抗癌剂或类固醇）的组合物。
• COMPOSITIONS FOR TREATING CANCER
  申请人：Janssen Oncology, Inc.

  公开号：EP3804730A1

  公开（公告）日：2021-04-14

  Methods and compositions for treating cancer are described herein. More particularly, the methods for treating cancer comprise administering a 17α-hydroxylase/C17,20-lyase inhibitor, such as abiraterone acetate (i.e., 3β-acetoxy-17-(3-pyridyl) androsta-5, 16-diene), in combination with at least one additional therapeutic agent such as an anti-cancer agent or a steroid. Furthermore, disclosed are compositions comprising a 17α-hydroxylase/C17,20-lyase inhibitor, and at least one additional therapeutic agent, such as an anti-cancer agent or a steroid.

  本文描述了治疗癌症的方法和组合物。更具体地说，治疗癌症的方法包括施用 17α- 羟化酶/C17,20-赖氨酸酶抑制剂，如醋酸阿比特龙（即 3β-乙酰氧基-17-(3-吡啶基) 雄甾-5,16-二烯），与至少一种额外的治疗剂如抗癌剂或类固醇结合使用。此外，还公开了包含 17α- 羟化酶/C17,20-裂解酶抑制剂和至少一种额外治疗剂（如抗癌剂或类固醇）的组合物。
• 17-SUBSTITUTED STEROIDS USEFUL IN CANCER TREATMENT
  申请人：BTG INTERNATIONAL LIMITED

  公开号：EP0633893B1

  公开（公告）日：1999-11-24