11,19-环氧孕甾-4-烯-3,20-二酮 | 1913-28-6

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 11,19-环氧孕甾-4-烯-3,20-二酮
• 英文名称: 11,19-Oxidoprogesterone
• 英文别名: (1S,6S,7S,10S,11S,19S)-7-acetyl-6-methyl-3-oxapentacyclo[9.7.1.01,14.04,19.06,10]nonadec-14-en-16-one
• CAS: 1913-28-6
• 化学式: C₂₁H₂₈O₃
• 分子量: 328.4
• InChiKey: OXOOIWULQIFUDQ-SLGDTRQESA-N

物化性质

• 熔点：
  167-170 °C(Solv: ethyl ether (60-29-7))
• 沸点：
  493.5±45.0 °C(Predicted)
• 密度：
  1.18±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  24
• 可旋转键数：
  1
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.81
• 拓扑面积：
  43.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (1S,6S,7S,10S,11S,19S)-7-acetyl-6-methyl-3-oxapentacyclo[9.7.1.01,14.04,19.06,10]nonadec-13-en-16-one 生成 11,19-环氧孕甾-4-烯-3,20-二酮
  参考文献：
  名称：

  BRACHET-COTA, ADRIANA L.;BURTON, GERARDO, Z. NATURFORSCH. B , 45,(1990) N, C. 711-715

  摘要：

  DOI：

文献信息

• 21-Hydroy-6,19-oxidoprogesterone (210h-60p) as antiglucocorticoid
  申请人：Applied Research Systems ARS Holding N.V.

  公开号：EP0903146A1

  公开（公告）日：1999-03-24

  The conformationally highly bent steroid 21-hydroxy-6,19- oxidoprogesterone (21OH- 6OP) has been found to be a selective antiglucocorticoid virtually lacking mineralococortioid or glucocorticoid properties as well as affinity for MR or PR and is used for the treatment of diseases associated with an excess of glucocorticoids in the body, such as the Cushing's syndrome or depression.

  研究发现，构象高度弯曲的类固醇 21-羟基-6,19-氧化黄体酮（21OH- 6OP）是一种选择性的抗糖皮质激素，实际上缺乏矿物皮质激素或糖皮质激素的特性以及对 MR 或 PR 的亲和力，可用于治疗与体内糖皮质激素过多有关的疾病，如库欣综合征或抑郁症。
• Pharmaceutical formulations for the treatment and prevention of trauma-induced neuropathology and neurodegeneration
  申请人：Sapna Life Sciences Corporation

  公开号：US10201569B2

  公开（公告）日：2019-02-12

  Novel multi-component formulations, procedures and methods for use in treating neuropathology and neurodegeneration incident to trauma are provided. Multi-component formulations of the invention comprise biologically active forms of any two, any three, or all four of at least one neurosteroid or neuroactive steroid, such as progesterone or synthetic progestin, at least one anti-epileptic or anticonvulsant, such as gabapentin, pregabalin or valproic acid, at least one NK-1 receptor antagonist, such as aprepitant, casopitant or vestipitant, at least one lithium-containing or lithium-related drug. The provided formulations are configured or adapted to prevent or reduce the incidence and severity of neurological damage caused by trauma, or the risk of such damage. Formulations, procedures and methods of the invention advantageously effect both neuroprotective actions to prevent or reduce secondary injuries, and neurotrophic actions to repair and restore cells and tissues affected by the trauma, and are especially useful in treating injury or trauma to nerve cells, to neural support cells and to neural support tissues.

  本发明提供了用于治疗创伤引起的神经病理学和神经变性的新型多组分制剂、程序和方法。本发明的多组分制剂包括至少一种神经类固醇或神经活性类固醇（如黄体酮或合成孕激素）、至少一种抗癫痫药或抗惊厥药（如加巴喷丁、普瑞巴林或丙戊酸）、至少一种NK-1受体拮抗剂（如阿普瑞坦、卡索匹坦或马替匹坦）、至少一种含锂药物或与锂相关的药物的任意两种、任意三种或全部四种的生物活性形式。所提供的制剂经配置或调整后可预防或降低创伤引起的神经损伤的发生率和严重程度，或降低这种损伤的风险。本发明的制剂、程序和方法既能起到预防或减少二次损伤的神经保护作用，又能起到修复和恢复受创伤影响的细胞和组织的神经营养作用，特别适用于治疗神经细胞、神经支持细胞和神经支持组织的损伤或创伤。
• BRACHET-COTA, ADRIANA L.;BURTON, GERARDO, Z. NATURFORSCH. B , 45,(1990) N, C. 711-715
  作者：BRACHET-COTA, ADRIANA L.、BURTON, GERARDO

  DOI：——

  日期：——
• 21-HYDROXY-6,19-OXIDOPROGESTERONE (21OH-6OP) AND ITS USE AS MEDICAMENT FOR TREATING EXCESS OF GLUCOCORTICOIDS
  申请人：Applied Research Systems ARS Holding N.V.

  公开号：EP1033990B1

  公开（公告）日：2002-04-03
• MULTIPLE-COMPONENT PHARMACEUTICAL FORMULATIONS AND METHODS FOR THEIR USE IN TREATING NEUROPATHOLOGY AND NEURODEGENERATION CAUSED BY TRAUMATIC INJURY
  申请人：HENRY James Lorne

  公开号：US20140194397A1

  公开（公告）日：2014-07-10

  Novel two-component formulations, procedures and methods for use in treating neuropathology and neurodegeneration incident to trauma are provided. Two-component formulations of the invention comprise biologically active forms of at least one neurosteroid or neuroactive steroid, such as progesterone or synthetic progestin, and at least one anti-epileptic or anticonvulsant, such as pregabalin. The provided formulations are configured or adapted to prevent or reduce the incidence and severity of neurological damage caused by trauma. Formulations, procedures and methods of the invention advantageously effect both neuroprotective actions to prevent or reduce secondary injuries, and neurotrophic actions to repair and restore cells and tissues affected by the trauma, and are especially useful in treating neurological trauma, such as those caused by sports injuries, chemical weapons, vehicle collisions and improvised explosive devices in combat.