8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine;hydron;chloride

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶嗪类
• 英文名称: 8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine;hydron;chloride
• 化学式: C18H19Cl2N3O
• 分子量: 364.3
• InChiKey: JSXBVMKACNEMKY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.19
• 重原子数：
  24
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  28.1
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE<br/>[FR] COMPOSÉS PRÉSENTANT UNE ACTIVITÉ AU NIVEAU DU RÉCEPTEUR M1 ET LEURS UTILISATIONS EN MÉDECINE
  申请人：GLAXO GROUP LTD

  公开号：WO2009037294A1

  公开（公告）日：2009-03-26

  Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.

  提供具有公式(I)或其盐的化合物：其中R4、R5、R6、Q、A、Y和R按描述定义。披露了这些化合物作为药物的使用和在制造用于治疗精神病性障碍、认知障碍和阿尔茨海默病药物中的应用。本发明还公开了包含这些化合物的药物组合物。
• [EN] COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE<br/>[FR] COMPOSÉS AYANT UNE ACTIVITÉ AU NIVEAU DU RÉCEPTEUR M1 ET UTILISATIONS DE CES DERNIERS EN MÉDECINE
  申请人：GLAXO GROUP LTD

  公开号：WO2009037293A1

  公开（公告）日：2009-03-26

  Compounds of formula (I) and salts thereof are provided: formula (I) wherein R4, R5, R6, Q, A, and Y are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.

  提供了式（I）及其盐：式（I）其中R4、R5、R6、Q、A和Y如描述中所定义。公开了这些化合物作为药物以及用于治疗精神病、认知障碍和阿尔茨海默病的药物制造中的用途。该发明还公开了包含这些化合物的药物组合物。
• [EN] 7-PHENYLSULFONYL-TETRAHYDRO-3-BENZAZEPINE DERIVATIVES AS ANTIPSYCHOTIC AGENTS<br/>[FR] DERIVES DE LA 7-PHENYLSULFONYL-TETRAHYDRO-3-BENZAZEPINE AGENTS ANTIPSYCHOTIQUES
  申请人：GLAXO GROUP LTD

  公开号：WO2005051398A1

  公开（公告）日：2005-06-09

  The invention provides one or more chemical entities selected from a compound of formula (I): wherein R1 represents C1-6alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, halo, cyano, 5-methyl-1,2,4-oxadiazol-3-yl or a group -SO2X; R2 represents hydrogen, C1-6alkyl, C1-6alkoxy, halo or cyano; X is C1-6alkyl, -NR3R4 or morpholino; R3 and R4 independently represent hydrogen or C1-6alkyl; and a pharmaceutically acceptable salt and solvate thereof; with the proviso that the compound 8-[4-(4-fluoro-benzyl)-benzenesulfonyl]-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl}-dimethyl-amine is excluded. The compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof are useful in therapy, in particular as antipsychotic agents.

  该发明提供了一种或多种从化合物的化学实体，该化合物的结构如下（I）：其中R1代表C1-6烷基，C1-6烷氧基，三氟甲基，三氟甲氧基，卤素，氰基，5-甲基-1,2,4-噁二唑-3-基或基团-SO2X；R2代表氢，C1-6烷基，C1-6烷氧基，卤素或氰基；X代表C1-6烷基，-NR3R4或吗啡啉；R3和R4独立地代表氢或C1-6烷基；以及其药学上可接受的盐和溶剂；但化合物8-[4-(4-氟苄基)-苯甲磺酰]-3-甲基-2,3,4,5-四氢-1H-3-苯并哌啶-7-基}-二甲胺被排除。该式（I）的化合物及其药学上可接受的盐和溶剂在治疗中很有用，特别是作为抗精神病药物。
• [EN] INDOLE AND AZAINDOLE MODULATORS OF THE ALPHA 7 NACHR<br/>[FR] MODULATEURS INDOLES ET AZAINDOLES DU NACHR-?7
  申请人：PROXIMAGEN LTD

  公开号：WO2011045353A1

  公开（公告）日：2011-04-21

  This invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a pharmaceutically acceptable salt thereof.

  这项发明涉及利用式(I)的化合物或其药用可接受盐对α7尼古丁乙酰胆碱受体(nAChR)进行调节。
• [EN] AGONISTS AND ANTAGONISTS OF THE S1P5 RECEPTOR, AND METHODS OF USES THEREOF<br/>[FR] AGONISTES ET ANTAGONISTES DU RÉCEPTEUR S1P5, ET LEURS PROCÉDÉS D'UTILISATION
  申请人：ABBOTT LAB

  公开号：WO2010093704A1

  公开（公告）日：2010-08-19

  Disclosed are compounds that are agonists or antagonists of the S1P5 receptor, compositions comprising said compounds, and methods of using said compounds and compositions. In certain embodiments, said compounds are 1-benzylazetidine-3-carboxylic acid derivatives. In certain embodiments, said methods relate to the treatment of neuropatic pain and/or a neurodegenerative disorder. In certain embodiments, said compounds may be used in combination with a second therapeutic agent.

  本文披露了作为S1P5受体激动剂或拮抗剂的化合物，包括含有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。在某些实施例中，这些化合物是1-苄基氮杂环丙氨酸衍生物。在某些实施例中，这些方法涉及治疗神经痛和/或神经退行性疾病。在某些实施例中，这些化合物可以与第二治疗剂结合使用。