(E)-1-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N'-(3,5-dibromo-4-hydroxybenzylidene)piperidine-4-carbohydrazide | 1068707-82-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (E)-1-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N'-(3,5-dibromo-4-hydroxybenzylidene)piperidine-4-carbohydrazide
• 英文别名: 1-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]-N-[(E)-(3,5-dibromo-4-hydroxyphenyl)methylideneamino]piperidine-4-carboxamide
• CAS: 1068707-82-3
• 化学式: C₁₉H₁₆Br₂ClF₃N₄O₂
• 分子量: 584.618
• InChiKey: RWILRIJYQWRPRJ-FLUNURKVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  77.8
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• CFTR INHIBITOR COMPOUNDS AND USES THEREOF
  申请人：Russell Michael Geoffrey Neil

  公开号：US20080269206A1

  公开（公告）日：2008-10-30

  The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-6 or encompassed by formulas I-VI) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

  本发明涉及用于治疗动物中一种对抑制囊性纤维化跨膜传导调节因子（CFTR）多肽的功能反应的疾病的组合物和方法，通过向需要治疗该疾病的哺乳动物中给予本文所定义的化合物（包括表1-6中列出的化合物或被公式I-VI所包含的化合物）或其组合物的有效量，从而治疗该疾病。本发明特别涉及治疗腹泻和多囊肾病的方法。
• METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF DISORDERS OF GLUCOSE HOMEOSTASIS
  申请人：Scharfmann Raphael

  公开号：US20120219543A1

  公开（公告）日：2012-08-30

  The invention is in the field of disorders of glucose homeostasis therapy. In particular the invention relates to a CFTR inhibitor or an inhibitor of CFTR gene expression for use in the treatment of disorders of glucose homeostasis. The present invention also relates to an in vitro methods for increasing the pool of Ngn3+ endocrine progenitor cells, pancreatic endocrine cells, or β cell mass obtained from stem cells, wherein said methods comprises the step of contacting stem cells with a CFTR inhibitor or an inhibitor of CFTR gene expression. The present invention also relates to a method of testing a subject thought to have or be predisposed to having disorders of glucose homeostasis, which comprises the step of analyzing a sample of interest from said subject for: (i) detecting the presence of a mutation in the CFTR gene and/or its associated promoter, and/or (ii) analyzing the expression of the CFTR gene.

  本发明涉及葡萄糖稳态失调疗法领域。特别地，本发明涉及一种CFTR抑制剂或CFTR基因表达抑制剂，用于治疗葡萄糖稳态失调疾病。本发明还涉及一种体外方法，用于增加来源于干细胞的Ngn3+内分泌祖细胞、胰岛内分泌细胞或β细胞群，其中该方法包括将干细胞与CFTR抑制剂或CFTR基因表达抑制剂接触的步骤。本发明还涉及一种检测被认为患有或易患葡萄糖稳态失调疾病的受试者的方法，其中包括分析来自该受试者的感兴趣样本，以检测CFTR基因及/或其关联启动子的突变的存在和/或分析CFTR基因的表达。
• US8283351B2
  申请人：——

  公开号：US8283351B2

  公开（公告）日：2012-10-09
• [EN] CFTR INHIBITOR COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS INHIBITEURS DE CFTR ET LEURS UTILISATIONS
  申请人：INST ONEWORLD HEALTH

  公开号：WO2008121877A2

  公开（公告）日：2008-10-09

  [EN] The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-6 or encompassed by formulas I-VI) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
  [FR] La présente invention concerne des compositions et des procédés de traitement d'une maladie chez un animal, ladite maladie répondant à l'inhibition d'un polypeptide régulateur de la conduction transmembranaire de la fibrose kystique fonctionnelle (CFTR) par l'administration à un mammifère qui en a besoin, d'une quantité efficace d'un composé défini dans celle-ci (comprenant les composés définis dans les tableaux 1 à 6 ou compris dans les formules I à VI) ou des compositions de ceux-ci, traitant ainsi la maladie. La présente invention concerne en particulier un procédé de traitement des diarrhées et de la maladie rénale polykystique.
• [EN] METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF DISORDERS OF GLUCOSE HOMEOSTASIS<br/>[FR] MÉTHODES ET COMPOSITIONS PHARMACEUTIQUES POUR LE TRAITEMENT DES TROUBLES DE L'HOMÉOSTASIE DU GLUCOSE
  申请人：INST NAT SANTE RECH MED

  公开号：WO2011048070A1

  公开（公告）日：2011-04-28

  The invention is in the field of disorders of glucose homeostasis therapy. In particular the invention relates to a CFTR inhibitor or an inhibitor of CFTR gene expression for use in the treatment of disorders of glucose homeostasis. The present invention also relates to an in vitro methods for increasing the pool of Ngn3+ endocrine progenitor cells, pancreatic endocrine cells, or β cell mass obtained from stem cells, wherein said methods comprises the step of contacting stem cells with a CFTR inhibitor or an inhibitor of CFTR gene expression. The present invention also relates to a method of testing a subject thought to have or be predisposed to having disorders of glucose homeostasis, which comprises the step of analyzing a sample of interest from said subject for: (i) detecting the presence of a mutation in the CFTR gene and/or its associated promoter, and/or (ii) analyzing the expression of the CFTR gene.