(5-methyl-1H-indol-2-yl)(piperidin-1-yl)methanone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: (5-methyl-1H-indol-2-yl)(piperidin-1-yl)methanone
• 英文别名: (5-methyl-1H-indol-2-yl)-piperidin-1-ylmethanone
• 化学式: C₁₅H₁₈N₂O
• 分子量: 242.32
• InChiKey: IDLOUIFRZCNRBQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  36.1
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• [EN] N-ACYL CYCLIC AMINE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF<br/>[FR] DÉRIVÉ D'AMINE N-ACYLE CYCLIQUE OU SON SEL PHARMACEUTIQUEMENT ACCEPTABLE
  申请人：DAINIPPON SUMITOMO PHARMA CO

  公开号：WO2011111875A1

  公开（公告）日：2011-09-15

  The present invention provides compounds which show high effectiveness against positive symptoms, negative symptoms and cognitive dysfunction in schizophrenia and reduce conventional side-effect risks as well as have remarkable effects for central neurological diseases associated with cognitive dysfunction other than schizophrenia. N-Acyl cyclic amine derivatives of formula (1): wherein Ar1 and Ar2 are aryl or heteroaryl; V is nitrogen, or CR3; W1 is a single bond, -C(O)-, etc.; W2 is C1- alkylene; W3 is a single bond, methylene, -NH-, -CR4=CR5-, etc.; Ring Q is a group of formula (a) in which n is 0 or 1; m is 0 to 2; k is 1 to 3; Z is a single bond, methylene, oxygen, etc.; R1a, R1b and R1c are each, same or different, hydrogen, hydroxyl, halogen, cyano, C1-6 alkyl, etc.; or pharmaceutically acceptable salts thereof are provided.

  本发明提供了一种化合物，对于精神分裂症的阳性症状、阴性症状和认知功能障碍具有高效性，同时减少了传统的副作用风险，并对与精神分裂症以外的认知功能障碍相关的中枢神经系统疾病具有显著效果。提供了式（1）的N-酰基环胺衍生物，其中Ar1和Ar2是芳基或杂环芳基；V是氮或CR3；W1是单键，-C(O)-等；W2是C1-烷基；W3是单键，亚甲基，-NH-，-CR4=CR5-等；环Q是式（a）的一组，其中n为0或1；m为0到2；k为1到3；Z是单键，亚甲基，氧等；R1a、R1b和R1c分别是相同或不同的氢、羟基、卤素、氰基、C1-6烷基等；或其药用可接受盐。
• MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：US20130178471A1

  公开（公告）日：2013-07-11

  Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

  本发明的化合物及其药学上可接受的组合物，可用作ATP结合盒（“ABC”）转运蛋白或其片段的调节剂，包括囊性纤维化跨膜传导调节因子（“CFTR”）。本发明还涉及使用本发明的化合物治疗ABC转运蛋白介导的疾病的方法。
• Modulators of ATP-Binding Cassette Transporters
  申请人：VERTEX PHARMACEUTICALS INCORPORATED

  公开号：US20150094304A1

  公开（公告）日：2015-04-02

  Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

  本发明的化合物及其药学上可以接受的组合物，可用作ATP结合盒（“ABC”）转运蛋白或其片段的调节剂，包括囊性纤维化跨膜传导调节因子（“CFTR”）。本发明还涉及使用本发明的化合物治疗ABC转运蛋白介导疾病的方法。
• EBI2 MODULATORS
  申请人：SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE

  公开号：US20160214951A1

  公开（公告）日：2016-07-28

  Provided herein are small molecule Epstein-Barr virus-induced G-protein coupled receptor 2 (EBI2) modulator compounds, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds. EBI2 is a therapeutic target for the treatment of a variety of diseases or conditions. In some embodiments, EBI2 is a therapeutic target for the treatment of diseases or conditions such as, but not limited to, autoimmune diseases or conditions, cancer, and cardiovascular disease.

  本文提供了小分子埃普斯坦-巴尔病毒诱导的G蛋白偶联受体2（EBI2）调节剂化合物，包括这些化合物的组合物，以及使用这些化合物和组合物的方法。EBI2是治疗多种疾病或病症的治疗靶点。在某些实施例中，EBI2是治疗自身免疫性疾病或病症、癌症和心血管疾病等疾病或病症的治疗靶点。
• US8575209B2
  申请人：——

  公开号：US8575209B2

  公开（公告）日：2013-11-05