5-[(15-chloro-7,11,13-triazatetracyclo[8.7.0.02,7.012,17]heptadeca-1(10),12(17),13,15-tetraen-11-yl)methyl]-7,8-dihydro-6H-isoquinolin-5-ol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 5-[(15-chloro-7,11,13-triazatetracyclo[8.7.0.02,7.012,17]heptadeca-1(10),12(17),13,15-tetraen-11-yl)methyl]-7,8-dihydro-6H-isoquinolin-5-ol
• 化学式: C₂₄H₂₇ClN₄O
• 分子量: 422.9
• InChiKey: PMSPJPRRGPWSQG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  30
• 可旋转键数：
  2
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  54.2
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• PYRIDO[4,3-b]INDOLE AND PYRIDO[3,4-b]INDOLE DERIVATIVES AND METHODS OF USE
  申请人：Chakravarty Sarvajit

  公开号：US20140206711A1

  公开（公告）日：2014-07-24

  This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. The compounds may bind to and antagonize receptor α 2B , α 1B or α 2A . The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption, or to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. The compounds may also be used to treat diseases or conditions that are expected to be responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular, renal disorders or type 2 diabetes is particularly described.

  这份披露涉及吡啶并[4,3-b]吲哚和吡啶并[3,4-b]吲哚衍生物。提供了包括这些化合物的药物组合物，以及使用这些化合物进行各种治疗应用的方法，包括治疗认知障碍、精神障碍、神经递质介导的障碍和/或神经元障碍。这些化合物可以结合并拮抗受体α2B、α1B或α2A。这些化合物可以用于治疗，例如，（i）降低血压和/或（ii）促进肾血流和/或（iii）降低或抑制钠重吸收，或者调节血糖水平，增加胰岛素分泌，并治疗对增加胰岛素产生反应的疾病或状况。这些化合物还可以用于治疗预计会对降低血压产生反应的疾病或状况。特别描述了使用这些化合物治疗心血管、肾脏障碍或2型糖尿病的用途。
• PYRIDO[4,3-B]INDOLE AND PYRIDO[3,4-B]INDOLE DERIVATIVES AND METHODS OF USE
  申请人：Medivation Technologies, Inc.

  公开号：US20150258075A1

  公开（公告）日：2015-09-17

  This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. The compounds may bind to and antagonize receptor α2B, α1B or α2A. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption, or to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. The compounds may also be used to treat diseases or conditions that are expected to be responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular, renal disorders or type 2 diabetes is particularly described.

  本公开涉及吡啶并[4,3-b]吲哚和吡啶并[3,4-b]吲哚衍生物。所述化合物的制药组合物也提供，以及使用该化合物进行各种治疗应用的方法，包括治疗认知障碍、精神障碍、神经递质介导的障碍和/或神经元障碍。该化合物可能结合并拮抗α2B、α1B或α2A受体。该化合物可能用于治疗，例如：（i）降低血压和/或（ii）促进肾血流和/或（iii）减少或抑制钠重吸收，或调节血糖水平，增加胰岛素分泌并治疗预计对胰岛素产生增加反应的疾病或情况。该化合物还可用于治疗预计对血压降低有反应的疾病或情况。特别描述了使用该化合物治疗心血管、肾脏疾病或2型糖尿病的用途。
• US9035056B2
  申请人：——

  公开号：US9035056B2

  公开（公告）日：2015-05-19
• US9211287B2
  申请人：——

  公开号：US9211287B2

  公开（公告）日：2015-12-15