5-Alpha-二氢皮质酮 | 298-25-9

• 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: 5-Alpha-二氢皮质酮
• 中文别名: 5Α-孕甾-11Β,21-二醇-3,20-二酮；5Α-二氢皮质酮
• 英文名称: 5α-pregnane-11β,21-diol-3,20-dione
• 英文别名: 5α-pregnan-11β-21-diol-3,20-dione；5α-dihydrocorticosterone；dihydrocorticosterone；11β,21-dihydroxy-5α-pregnane-3,20-dione；11β,21-Dihydroxy-5α-pregnan-3,20-dion；11β.21-Dihydroxy-5α-pregnandion-(3.20)；5alpha-Dihydrocorticosterone；(5S,8S,9S,10S,11S,13S,14S,17S)-11-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-1,2,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-one
• CAS: 298-25-9
• 化学式: C₂₁H₃₂O₄
• 分子量: 348.483
• InChiKey: CTTOFMJLOGMZRN-DYWNTJRHSA-N

物化性质

• 熔点：
  190-193 °C
• 沸点：
  508.5±50.0 °C(Predicted)
• 密度：
  1.175±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  25
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.904
• 拓扑面积：
  74.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-Alpha-二氢皮质酮 在 potassium dichromate 、 硫酸 、 过碘酸 、 丙酮 作用下， 生成 (+)-3,11-dioxo-5α-androstanecarboxylic acid
  参考文献：
  名称：

  Behavioural observations of interactions in a free-ranging lynxLynx lynx family at kills

  摘要：

  The behaviour of a free-ranging female lynx Lynx lynx Linnaeus, 1758 and her kittens at 12 different kills was studied for 44 hours of observation from September 1996 to March 1997. The development of interactions at kills of a lynx family group showed the following pattern: until the end of September we often observed two lynx, usually both kittens, food from the kill at the same time. After the age of four months aggression between kittens was observed frequently, with the bigger kitten being dominant. From September the kittens were never again seen feeding together at the kill, However, we never observed fighting, and aggressive behaviour did not increase with the age of the, kittens. Whereas until December one of the kittens was always first at the kill, from January onwards it was mostly the adult female who ate first. She introduced her kittens to the home range of a neighbouring female where the family break-up occurred. The kittens were last seen together with their mother on 26 March. Dispersal seemed to be initiated by the female abandoning the kittens.

  DOI：

  10.1007/bf03192451
• 作为产物：
  描述：

  肾上腺酮 以 乙醇 为溶剂， 反应 96.0h， 以68%的产率得到5-Alpha-二氢皮质酮
  参考文献：
  名称：

  Biotransformation of corticosteroids by Penicillium decumbens ATCC 10436

  摘要：

  The biotransformation of a series of corticosteroids by the fungus Penicillium decumbens ATCC 10436 has been investigated. Conversion to the corresponding 5 alpha-dihydrosteroid was observed for all the Delta(4)-3-ketosteroids studied with the exception of deoxycorticosterone, which was converted to a Delta(1,4)-diene. Deoxycorticosterone acetate was, however, converted to a 5 alpha-dihydro product concomitant with ester hydrolysis. Other substrates carrying a C-21 acetoxy group were also hydrolyzed to the alcohol. In two cases (resulting from deoxycorticosterone acetate and 11-deoxycortisone) the 5 alpha-3-keto product was further reduced to the 3 beta-alcohol. No reduction of Delta(1,4)-dienes was observed.

  DOI：

  10.1016/0039-128x(95)00071-w

文献信息

• HETERODIMER COMPOSITIONS AND METHODS FOR THE TREATMENT OF OCULAR DISORDERS
  申请人：Ripple Therapeutics Corporation

  公开号：US20210347809A1

  公开（公告）日：2021-11-11

  Described herein are processable compositions comprising at least one moiety that is processable in its free form. Also described herein are compositions and methods for the treatment of ocular diseases or disorders including glaucoma, blepharitis, ocular inflammation, diabetic macular edema, posterior inflammation, anterior inflammation, macular degeneration (e.g., wet macular degeneration (AMD) or dry AMD), post-cataract surgery, and retinal vein occlusion. Said compositions and methods comprise steroids and prostaglandins which demonstrate anti-inflammatory activity, intraocular pressure (IOP) lowering, and/or other desirable activities. Injection of said compositions in the eye provides therapeutic benefit to patients suffering from ocular disorders.

  本文描述了可加工的组合物，其中至少包含一个可在其自由形式下加工的成分。本文还描述了用于治疗眼部疾病或障碍的组合物和方法，包括青光眼、眼睑炎、眼部炎症、糖尿病性黄斑水肿、后部炎症、前部炎症、黄斑变性（如湿性黄斑变性（AMD）或干性AMD）、白内障手术后和视网膜静脉阻塞。所述组合物和方法包括表现出抗炎活性、降低眼内压力（IOP）和/或其他理想活性的类固醇和前列腺素。将所述组合物注射到眼中可为患有眼部障碍的患者提供治疗益处。
• 5 alpha reduced glucocorticoid metabolites for the treatment of inflammation
  申请人：THE UNIVERSITY OF EDINBURGH

  公开号：EP1808176A2

  公开（公告）日：2007-07-18

  The present invention relates to the modulation of glucocorticoid metabolism. In particular, the invention relates to the modulation of the functional activity of the glucocorticoid receptor by 5α reduced metabolic breakdown products of glucocorticoids.

  本发明涉及糖皮质激素代谢的调节。特别是，本发明涉及通过 5α 还原糖皮质激素的代谢分解产物来调节糖皮质激素受体的功能活性。
• Glass formulations and uses thereof
  申请人：Ripple Therapeutics Corporation

  公开号：US10632075B2

  公开（公告）日：2020-04-28

  The disclosure features pharmaceutical compositions formed from prodrug dimers for the extended delivery of a drug and for the treatment of a disease or condition.

  本公开的特征是由原药二聚体形成的药物组合物，用于延长给药时间和治疗疾病或病症。
• Heterodimer compositions and methods for the treatment of ocular disorders
  申请人：Ripple Therapeutics Corporation

  公开号：US11279729B2

  公开（公告）日：2022-03-22

  Described herein are processable compositions comprising at least one moiety that is processable in its free form. Also described herein are compositions and methods for the treatment of ocular diseases or disorders including glaucoma, blepharitis, ocular inflammation, diabetic macular edema, posterior inflammation, anterior inflammation, macular degeneration (e.g., wet macular degeneration (AMD) or dry AMD), post-cataract surgery, and retinal vein occlusion. Said compositions and methods comprise steroids and prostaglandins which demonstrate anti-inflammatory activity, intraocular pressure (IOP) lowering, and/or other desirable activities. Injection of said compositions in the eye provides therapeutic benefit to patients suffering from ocular disorders.

  本描述涉及一种可处理组合物，所述组合物包含至少一个以自由形式可处理的单元。此外，本描述还涉及用于治疗眼科疾病或紊乱（包括青光眼、眼睑炎、眼部炎症、糖尿病性黄斑水肿、后部炎症、前部炎症、黄斑变性（例如湿性黄斑变性（AMD）或干性AMD）、白内障手术后和视网膜静脉阻塞）的组合物和方法。所述组合物和方法包含具有抗炎活性、降低眼内压以及/或其它有益活性的类固醇和前列腺素。将所述组合物注射入眼中，为患有眼科疾病患者带来治疗益处。
• Selective 11beta-HSD inhibitors and methods of use thereof
  申请人：——

  公开号：US20030148987A1

  公开（公告）日：2003-08-07

  Methods for treating glucocorticoid associated states using selective 11&bgr;-HSD1-dehydrogenase, 11&bgr;-HSD1-reductase and 11&bgr;-HSD2 dehydrogenase modulating compounds are described.

  描述了使用选择性 11&bgr;-HSD1-脱氢酶、11&bgr;-HSD1-还原酶和 11&bgr;-HSD2 脱氢酶调节化合物治疗糖皮质激素相关状态的方法。