[(1R,2R,4S)-2-methoxy-4-[(2R)-2-[(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18,30-trihydroxy-19-methoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]cyclohexyl] 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 大环内酯内酰胺
• 英文名称: [(1R,2R,4S)-2-methoxy-4-[(2R)-2-[(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18,30-trihydroxy-19-methoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]cyclohexyl] 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate
• 化学式: C₅₅H₈₅NO₁₆
• 分子量: 1016.3
• InChiKey: CJDQIEOIQZFHOU-XJEVXKDBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  72
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  253
• 氢给体数：
  5
• 氢受体数：
  16

文献信息

• Rapamycin for the treatment of lymphangioleiomyomatosis
  申请人：AI Therapeutics, Inc.

  公开号：US10307371B2

  公开（公告）日：2019-06-04

  The present invention relates to methods and compositions for treating lymphangioleiomyomatosis in a human subject in need of such treatment. The methods comprise administering to the subject via inhalation an aerosol composition comprising rapamycin or a prodrug or derivative (including analog) thereof.

  本发明涉及在需要治疗的人体中治疗淋巴管瘤病的方法和组合物。这些方法包括通过吸入向受试者施用包含雷帕霉素或其原药或衍生物（包括类似物）的气溶胶组合物。
• Drug delivery and imaging chemical conjugate, formulations and methods of use thereof
  申请人：NanoPhagix LLC

  公开号：US11034701B2

  公开（公告）日：2021-06-15

  The present invention relates to compounds of Formula 1, and methods of use thereof, capable of entering macrophages. The invention further relates to compounds capable of modulating (for example inhibiting) the activity of the mammalian target of rapamycin (mTor), treating mTor-associated diseases, in particular, but not limited to, related to mTor in macrophages. The invention also relates to compounds capable of imaging mTor in a subject, in particular, but not limited to, mTor in macrophages. wherein Q is, in one embodiment,

  本发明涉及能够进入巨噬细胞的式 1 化合物及其使用方法。本发明还涉及能够调节（例如抑制）哺乳动物雷帕霉素靶标（mTor）活性、治疗与 mTor 相关疾病，特别是但不限于与巨噬细胞中的 mTor 相关疾病的化合物。本发明还涉及能够对受试者体内的mTor成像的化合物，特别是但不限于巨噬细胞中的mTor。 其中 Q 在一个实施方案中为
• 42-RAPAMYCIN HYDROXYESTER, PROCESS FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT
  申请人：Wyeth LLC

  公开号：EP0763039B3

  公开（公告）日：2017-04-05
• EP3310786B1
  申请人：——

  公开号：EP3310786B1

  公开（公告）日：2021-03-03
• An Inhalable Rapamycin Formulation for Treating Age-Related Conditions
  申请人：LAM Therapeutics, Inc.

  公开号：US20170014341A1

  公开（公告）日：2017-01-19

  The present invention relates to methods and compositions for anti-aging therapy and for the treatment and prophylaxis of age-related diseases and disorders in a human subject in need of such therapy or treatment, the methods comprising the pulmonary administration to the subject, preferably via inhalation, of composition comprising rapamycin, or a prodrug or derivative thereof.