16-Phenyl-2-oxa-9,11,15-triazatetracyclo[17.3.1.13,7.09,13]tetracosa-1(22),3,5,7(24),10,12,19(23),20-octaene-4-carbonitrile

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 16-Phenyl-2-oxa-9,11,15-triazatetracyclo[17.3.1.13,7.09,13]tetracosa-1(22),3,5,7(24),10,12,19(23),20-octaene-4-carbonitrile
• 化学式: C₂₇H₂₄N₄O
• 分子量: 420.5
• InChiKey: UJJQJPGQYYHUMV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  32
• 可旋转键数：
  1
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  62.9
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Method of treating cancer
  申请人：——

  公开号：US20030220241A1

  公开（公告）日：2003-11-27

  The present invention relates to methods of treating cancer using a combination of a compound which is a PSA conjugate and a compound which is a inhibitor of prenyl-protein transferase, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at least two therapeutic agents selected from a group consisting of a compound which is a PSA conjugate and a compound which is a inhibitor of prenyl-protein transferase. The invention also relates to methods of preparing such compositions.

  本发明涉及使用一种PSA共轭物和一种前脂蛋白转移酶抑制剂的组合治疗癌症的方法，该方法包括向所述哺乳动物施用来自以下组中选择的至少两种治疗剂的量，所述组包括一种PSA共轭物和一种前脂蛋白转移酶抑制剂，所述治疗剂可以顺序给药或同时给药。该发明还涉及制备这种组合物的方法。
• Methods for the treatment of synucleinopathies (Lansbury)
  申请人：Lansbury T. Peter

  公开号：US20050277629A1

  公开（公告）日：2005-12-15

  Methods are provided of treating synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease and Multiple System Atrophy, comprising administering to a synucleinopathic subject one or more farnesyl transferase inhibitor compounds.
• Methods for the treatment of synucleinopathies
  申请人：Lansbury T. Peter

  公开号：US20070293539A1

  公开（公告）日：2007-12-20

  Methods are provided of treating synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease and Multiple System Atrophy, comprising administering to a synucleinopathic subject a farnesyl transferase inhibitor compound.
• US6358985B1
  申请人：——

  公开号：US6358985B1

  公开（公告）日：2002-03-19
• [EN] TREATMENT OF PROTEINOPATHIES USING A FARNESYL TRANSFERASE INHIBITOR<br/>[FR] TRAITEMENT DE PROTÉINOPATHIES UTILISANT UN INHIBITEUR DE FARNÉSYLE TRANSFÉRASE
  申请人：LINK MEDICINE CORP

  公开号：WO2010057028A9

  公开（公告）日：2010-09-02

  [EN] Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject in need thereof a therapeutically effective amount of a farnesyl transferase inhibitor, wherein the amount is effective to inhibit the farnesylation of a non-Ras FTase substrate involved in the autophagy pathway without substantially affecting the farnesylation of Ras or other oncology related substrates. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA anatagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant.
  [FR] La présente invention concerne des procédés et des compositions pharmaceutiques comprenant une faible dose d'un inhibiteur de farnésyle transférase utile dans le traitement de protéinopathies. Ces faibles doses sont au-dessous des doses utilisées dans des traitements oncologiques pour lesquels ces composés ont été initialement conçus. Le traitement comprend l'administration à un sujet nécessitant celui-ci d'une quantité thérapeutiquement efficace d'un inhibiteur de farnésyle transférase, où la quantité est efficace pour inhiber la farnésylation d'un substrat de FTase non-Ras impliqué dans la voie d'autophagie sans affecter sensiblement la farnésylation de Ras ou d'autres substrats de type oncologique. Des traitements selon la présente invention peuvent comprendre en outre un inhibiteur d'acétylcholinestérase, un activateur de récepteurs neurotrophiques, un antagoniste de NMDA, un inhibiteur de dépôt amyloïde, un agent antipsychotique, un antidépresseur, un anxiolytique, ou un antioxydant.