(6β,7β,11α,17β)-9,11-epoxy-6,7-dihydro-17-hydroxy-3-oxo-3'H-cyclopropa[6,7]pregna-4,6-diene-21-carboxylic acid methyl ester | 95716-96-4

• 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: (6β,7β,11α,17β)-9,11-epoxy-6,7-dihydro-17-hydroxy-3-oxo-3'H-cyclopropa[6,7]pregna-4,6-diene-21-carboxylic acid methyl ester
• 英文别名: 9α,11α-epoxy-17β-hydroxy-6β,7β-methylene-3-oxo-17α-pregn-4-ene-21-carboxylic acid methyl ester；methyl 3-[(1R,2S,8R,10S,11S,12S,15R,16S,18R)-15-hydroxy-2,16-dimethyl-5-oxo-19-oxahexacyclo[9.8.0.01,18.02,7.08,10.012,16]nonadec-6-en-15-yl]propanoate
• CAS: 95716-96-4
• 化学式: C₂₄H₃₂O₅
• 分子量: 400.515
• InChiKey: UTTAVEFEKHDCAP-OORZMFNGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  76.1
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Nanoparticulate eplerenone compositions
  申请人：Pharmacia Corporation

  公开号：EP1527782A1

  公开（公告）日：2005-05-04

  There is provided a pharmaceutical composition comprising eplerenone in solid particulate form, wherein at least 90% of the eplerenone particles are smaller than about 15 µm, for example about 0.01 to about 1 µm, in diameter. The composition can be adapted for oral administration, for example as a tablet or capsule comprising eplerenone in a unit dosage amount of about 10 to about 1000 mg and one or more excipients.

  本发明提供了一种药物组合物，该组合物包含固体颗粒状的依普利酮，其中至少90%的依普利酮颗粒直径小于约15微米，例如约0.01至约1微米。该组合物可用于口服给药，例如作为片剂或胶囊，包含单位剂量约为 10 至约 1000 毫克的依普利酮和一种或多种赋形剂。
• Aldosterone antagonist composition for release during aldosterone acrophase
  申请人：——

  公开号：US20020132001A1

  公开（公告）日：2002-09-19

  A pharmaceutical composition is provided for administration to a subject mammal such as a human exhibiting a diurnal cycle of plasma aldosterone concentration, the composition comprising a delayed-release formulation of an aldosterone antagonist drug, e.g., eplerenone, in a therapeutically effective amount. The delayed-release formulation, when administered about 6 hours to about 12 hours prior to the acrophase, results in a profile of plasma drug concentration that corresponds substantially to the diurnal cycle of plasma aldosterone concentration.

  提供了一种药物组合物，用于给受试哺乳动物（如表现出血浆醛固酮浓度昼夜周期的人类）用药，该组合物包括治疗有效量的醛固酮拮抗剂药物（如依普利酮）的缓释制剂。延迟释放制剂在凋亡期前约6小时至约12小时给药时，可使血浆药物浓度曲线与血浆醛固酮浓度的昼夜周期基本一致。
• Controlled release eplerenone compositions
  申请人：——

  公开号：US20020136775A1

  公开（公告）日：2002-09-26

  The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.

  本发明涉及可用作醛固酮受体阻断剂的口服药物组合物，该组合物由活性剂微粉化依普利酮和一种或多种载体材料组成，活性剂微粉化依普利酮的用量约为 10 毫克至约 1000 毫克。
• Micronized eplerenone compositions
  申请人：G. D. Searle & Co.

  公开号：US20040192661A1

  公开（公告）日：2004-09-30

  The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.

  本发明涉及可用作醛固酮受体阻断剂的口服药物组合物，该组合物由活性剂微粉化依普利酮和一种或多种载体材料组成，活性剂微粉化依普利酮的用量约为 10 毫克至约 1000 毫克。
• MICRONIZED EPLERENONE COMPOSITIONS
  申请人：G.D. SEARLE & CO.

  公开号：EP1135139B1

  公开（公告）日：2003-09-10