6-(1'-oxo-2'S-t-butoxycarbonylaminopropylamino)-3-(4-pyridyl)-2-(4-fluorophenyl)-7-aza-indole | 208104-78-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 6-(1'-oxo-2'S-t-butoxycarbonylaminopropylamino)-3-(4-pyridyl)-2-(4-fluorophenyl)-7-aza-indole
• 英文别名: tert-butyl N-[(2S)-1-[[2-(4-fluorophenyl)-3-pyridin-4-yl-1H-pyrrolo[2,3-b]pyridin-6-yl]amino]-1-oxopropan-2-yl]carbamate
• CAS: 208104-78-3
• 化学式: C₂₆H₂₆FN₅O₃
• 分子量: 475.523
• InChiKey: RXDBWYKXNOSUNX-HNNXBMFYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  35
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  109
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  6-(1'-oxo-2'S-t-butoxycarbonylaminopropylamino)-3-(4-pyridyl)-2-(4-fluorophenyl)-7-aza-indole 生成 6-(1'-oxo-2'S-aminopropylamino)-3-(4-pyridyl)-2-(4-fluorophenyl)-7-aza-indole
  参考文献：
  名称：

  US6180643

  摘要：

  公开号：

文献信息

• Methods of treating or preventing weight gain, obesity, and related disorders
  申请人：Sepracor Inc.

  公开号：US20020188029A1

  公开（公告）日：2002-12-12

  Methods are disclosed for the treatment and prevention of disorders and conditions including, but are not limited to, erectile dysfunction, affective disorders, weight gain, cerebral functional disorders, pain, obsessive-compulsive disorder, substance abuse, chronic disorders, anxiety, eating disorders, migraines, and incontinence. The methods comprise the administration of a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Pharmaceutical compositions and dosage forms are also disclosed that comprise a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Preferred dopamine reuptake inhibitors are racemic or optically pure sibutramine metabolites and pharmaceutically acceptable salts, solvates, and clathrates thereof. Preferred additional pharmacologically active compounds include drugs that affect the central nervous system, such as 5-HT 3 antagonists.

  本发明揭示了用于治疗和预防多种疾病和症状的方法，包括但不限于勃起功能障碍、情感障碍、体重增加、脑功能障碍、疼痛、强迫症障碍、物质滥用、慢性疾病、焦虑、进食障碍、偏头痛和失禁。该方法包括给予多巴胺再摄取抑制剂和可选的其他药理活性化合物。本发明还揭示了包含多巴胺再摄取抑制剂和可选的其他药理活性化合物的制药组合物和剂型。优选的多巴胺再摄取抑制剂是外消旋或光学纯的西布曲明代谢物及其药学上可接受的盐、溶剂和包合物。优选的其他药理活性化合物包括影响中枢神经系统的药物，如5-HT3拮抗剂。
• Aryl and heteroaryl substituted fused pyrrole anti-inflammatory agents
  申请人：Amgen Inc.

  公开号：US20030096819A1

  公开（公告）日：2003-05-22

  The present invention comprises a new class of novel aryl and heteroaryl substituted fused pyrrole compounds useful for the prophylaxis and treatment of diseases or conditions, such as TNF-&agr;, IL-1&bgr; , IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. In particular, the compounds of the invention are useful for the prophylaxis and treatment of diseases or conditions involving inflammation. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of inflammation and other maladies, such as pain and diabetes, using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  本发明涉及一类新型的芳基和杂环芳基取代融合吡咯化合物，用于预防和治疗疾病或病症，例如TNF-α，IL-1β，IL-6和/或IL-8介导的疾病，以及其他疾病，如疼痛和糖尿病。特别地，本发明的化合物用于预防和治疗涉及炎症的疾病或病症。因此，本发明还包括包含本发明的化合物的制药组合物，使用本发明的化合物和组合物预防和治疗炎症和其他疾病或病症的方法，以及用于制备本发明化合物的中间体和过程。本发明还涉及制备这种化合物的过程以及在这些过程中有用的中间体。
• ARYL AND HETEROARYL SUBSTITUTED FUSED PYRROLE ANTIINFLAMMATORY AGENTS
  申请人：AMGEN INC.

  公开号：EP0948495A1

  公开（公告）日：1999-10-13
• US6180643B1
  申请人：——

  公开号：US6180643B1

  公开（公告）日：2001-01-30
• US6440973B1
  申请人：——

  公开号：US6440973B1

  公开（公告）日：2002-08-27