1-(2-fluoro-phenylsulfonyl)-4-piperazin-1-yl-1H-indole | 431043-89-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-(2-fluoro-phenylsulfonyl)-4-piperazin-1-yl-1H-indole
• 英文别名: 1-(2-fluoro-benzenesulfonyl)-4-piperazin-1-yl-1H-indole；1-(2-Fluorophenyl)sulfonyl-4-piperazin-1-ylindole
• CAS: 431043-89-9
• 化学式: C₁₈H₁₈FN₃O₂S
• 分子量: 359.424
• InChiKey: KRMUPVIERMHPQE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  62.7
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• 4-piperazinylindole derivatives with 5-HT6 receptor affinity
  申请人：——

  公开号：US20030045527A1

  公开（公告）日：2003-03-06

  This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: 1 wherein R 3 is SO 2 —Ar, Ar is aryl or heteroaryl; and R 1 , R 2 , R 4 and R 5 are as defined herein; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

  这项发明涉及一类通常具有5-HT6受体亲和力的化合物，其由以下式I表示： 其中R3为SO2—Ar，Ar为芳基或杂环芳基；R1、R2、R4和R5如本文所定义；或其各个异构体、外消旋或非外消旋异构体混合物，或其药用可接受盐或溶剂化合物。该发明还涉及含有这类化合物的药物组合物，以及它们作为治疗剂的使用方法和其制备方法。
• [EN] NOVEL 4-(ARYL-4-SULFONYL)-6,6a,7,8,9,10-HEXAHYDRO-4H-4,8,10a-TRIAZA-ACEPHENANTHRYLENE AND 3-ARYLSULFONYL-6,6a,7,8,9,10-HEXAHYDRO-3H-3,8,10a-TRIAZA-CYCLOPENTA[C]FLUORENE DERIVATIVES AS SEROTONIN 5-HT6 LIGANDS<br/>[FR] NOUVEAUX DÉRIVÉS DE 4-(ARYL-4-SULFONYL)-6,6A,7,8,9,10-HEXAHYDRO-4H-4,8,10A-TRIAZA-ACÉPHÉNANTHRYLÈNE ET 3-ARYLSULFONYL-6,6A,7,8,9,10-HEXAHYDRO-3H-3,8,10A-TRIAZA-CYCLOPENTA[C]FLUORÈNE EN TANT QUE LIGANDS DE SÉROTONINE 5-HT6
  申请人：LUNDBECK & CO AS H

  公开号：WO2011088836A1

  公开（公告）日：2011-07-28

  This invention is directed to compounds of formula I or II, which are serotonin 5-HT 6 ligands. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I or II, or a pharmaceutically acceptable salt thereof. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I or II, or a pharmaceutically acceptable salt thereof. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I or II, or a pharmaceutically acceptable salt thereof.

  本发明涉及式I或II的化合物，它们是血清素5-HT6受体配体。本发明提供了一种药物组合物，其包含本发明的化合物以及药学上可接受的载体的治疗有效量。本发明还提供了制备式I或II的化合物或其药学上可接受的盐的方法。本发明进一步提供了一种治疗患有神经退行性疾病的受试者的方法，包括向该受试者施用式I或II的化合物或其药学上可接受的盐的治疗有效量。本发明还提供了一种治疗患有精神疾病的受试者的方法，包括向该受试者施用式I或II的化合物或其药学上可接受的盐的治疗有效量。
• INDOLEAMINE DERIVATIVES FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES
  申请人：Kolaczkowski Marcin

  公开号：US20140121216A1

  公开（公告）日：2014-05-01

  Indoleamine derivatives of formula (IA), R 1 represents benzyl unsubstituted or substituted with halogen atom, —OH, or C 1 -C 3 -alkyl; phenylsulphonyl unsubstituted or substituted in the phenyl ring with halogen atom, —OH or C 1 -C 3 -alkyl; G 1 represents phenoxyalkyl, heteroaryloxyalkyl- or heterocyclyloxyalkyl-piperazine moiety; and pharmaceutically acceptable salts and solvates thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.

  公式（IA）的吲哚胺衍生物，其中R1代表苄基未取代或取代为卤原子，-OH，或C1-C3-烷基；苯磺酰未取代或取代为苯环中的卤原子，-OH或C1-C3-烷基；G1代表苯氧基烷基，杂环氧基烷基-或杂环氧基烷基-哌嗪基；以及其药学上可接受的盐和溶剂合物。这些化合物可能对治疗和/或预防中枢神经系统疾病有用。
• Compositions and methods for treating cognitive disorders
  申请人：F. Hoffmann-La Roche AG

  公开号：EP2301625A2

  公开（公告）日：2011-03-30

  Use of selective antagonists of the 5-HT6 receptor and 5-HT2A receptors for the preparation of medicaments and corresponding pharmaceutical compositions useful for the treatment of cognitive disorders are presented.

  介绍了如何利用 5-HT6 受体和 5-HT2A 受体的选择性拮抗剂来制备治疗认知障碍的药物和相应的药物组合物。
• 4-PIPERAZINYLINDOLE DERIVATIVES WITH 5-HT6 RECEPTOR AFFINITY
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP1401812B1

  公开（公告）日：2006-06-28