(1R)-7-(4-Chlorophenyl)-2-(4-fluorophenyl)-7-hydroxy-1-(4-hydroxyphenyl)-2-azaspiro[3.5]nonan-3-one | 194423-53-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环丁烷
• 英文名称: (1R)-7-(4-Chlorophenyl)-2-(4-fluorophenyl)-7-hydroxy-1-(4-hydroxyphenyl)-2-azaspiro[3.5]nonan-3-one
• CAS: 194423-53-5
• 化学式: C₂₆H₂₃ClFNO₃
• 分子量: 451.9
• InChiKey: DPZUDTYEZMUJDW-GMUMFXLYSA-N

物化性质

• 熔点：
  >207oC (dec.)
• 溶解度：
  DMSO（微溶）、乙醇（微溶）、甲醇（微溶）

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  32
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  60.8
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Compositions of ezetimibe and methods for the treatment of cholesterol-associated benign and malignant tumors
  申请人：——

  公开号：US20040116358A1

  公开（公告）日：2004-06-17

  A method of prevention or treatment of a cholesterol-associated tumor is provided which comprises administering a therapeutically effective amount of an azetidinone-based cholesterol absorption inhibitor, preferably ezetimibe (SCH 58235) and/or its phenolic glucuronide, or at least one ezetimibe analog, e.g., SCH 48461 and SCH 58053, to a patient wherein the patient is either at risk of developing a cholesterol-associated tumor or already exhibits a cholesterol-associated tumor. Formulations of ezetimibe are also provided for the prevention or treatment of a cholesterol-associated tumor further comprising at least one other anticancer agent. An article of manufacture is also provided which comprises a container, instructions, and a composition, wherein the composition comprises a therapeutically effective amount of an azetidinone-based cholesterol absorption inhibitor, preferably ezetimibe or its phenolic glucuronide, and the instructions are for the administration of the composition for the prevention or treatment of a cholesterol-associated tumor.

  本发明提供了一种预防或治疗胆固醇相关肿瘤的方法，该方法包括向患者施用治疗有效量的氮杂环丁酮类胆固醇吸收抑制剂，优选依折麦布（SCH 58235）和/或其酚类葡萄糖醛酸苷，或至少一种依折麦布类似物，如SCH 48461和SCH 58053、或至少一种依折麦布类似物，如 SCH 48461 和 SCH 58053，给有可能患胆固醇相关肿瘤或已患胆固醇相关肿瘤的患者服用。还提供了用于预防或治疗胆固醇相关肿瘤的依折麦布制剂，该制剂进一步包含至少一种其他抗癌剂。还提供了一种制造品，它包括容器、说明书和组合物，其中组合物包含治疗有效量的基于氮杂环丁酮的胆固醇吸收抑制剂，优选依折麦布或其酚类葡萄糖醛酸苷，说明书用于施用组合物预防或治疗胆固醇相关肿瘤。
• COMPOSITIONS OF EZETIMIBE AND METHODS FOR THE TREATMENT OF CHOLESTEROL-ASSOCIATED BENIGN AND MALIGNANT TUMORS
  申请人：Karykion Inc.

  公开号：EP1545479B1

  公开（公告）日：2010-10-27
• TREATMENT WITH AZETIDINONE-BASED CHOLESTEROL ABSORPTION INHIBITORS AND OMEGA-3 FATTY ACIDS AND A COMBINATION PRODUCT THEREOF
  申请人：Reliant Pharmaceuticals, Inc.

  公开号：EP1919468A2

  公开（公告）日：2008-05-14
• NUTRACEUTICALS CONTAINING NITRO FATTY ACIDS
  申请人：Nitromega Corp.

  公开号：EP2384114A1

  公开（公告）日：2011-11-09
• Treatment with azetidinone-based cholesterol absorption inhibitors and omega-3 fatty acids and a combination product thereof
  申请人：Rongen M. L. Roelof

  公开号：US20070036862A1

  公开（公告）日：2007-02-15

  Combinations of one or more azetidinone-based cholesterol absorption inhibitors with mixtures of omega-3 fatty acids, methods of administering such combinations, and unit dosages of such combinations.