1,2,3,4-tetrahydro-5,8-dimethoxynaphthalen-1-amine

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 1,2,3,4-tetrahydro-5,8-dimethoxynaphthalen-1-amine
• 英文别名: 5,8-dimethoxy-1,2,3,4-tetrahydronaphthalen-1-amine
• 化学式: C₁₂H₁₇NO₂
• 分子量: 207.272
• InChiKey: BFKGQFXJSRWVQK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  44.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1,2,3,4-tetrahydro-5,8-dimethoxynaphthalen-1-amine 、 2,4-二氟苯甲磺酮 在 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 以63%的产率得到N-(5-fluoro-2-(methylsulfonyl)phenyl)-1,2,3,4-tetrahydro-5,8-dimethoxynaphthalen-1-amine
  参考文献：
  名称：

  WO2006/81332

  摘要：

  公开号：
• 作为产物：
  描述：

  5,8-二甲氧基-1-四氢萘酮 在 titanium(IV) isopropylate 、 氨 、 sodium tetrahydroborate 、 盐酸 、 sodium hydroxide 作用下， 以 乙醇 为溶剂， 反应 9.16h， 以93%的产率得到1,2,3,4-tetrahydro-5,8-dimethoxynaphthalen-1-amine
  参考文献：
  名称：

  WO2006/81332

  摘要：

  公开号：

文献信息

• QUINOLINES
  申请人：Kolczewski Sabine

  公开号：US20080146567A1

  公开（公告）日：2008-06-19

  The present invention relates to 2-Aminoquinoline derivatives of general formula I and pharmaceutically-acceptable acid-addition salts thereof, wherein R 1 , R 2 and X are as defined in the specification. The compounds may be used as 5-HT 5A receptor antagonists. The present invention relates also to processes for making such a compound and a pharmaceutical composition comprising such a compound. Compounds of the present invention are useful in the prevention and/or treatment of anxiety depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders and gastrointestinal disorders.

  本发明涉及一般式I的2-氨基喹啉衍生物及其药用可接受的酸盐，其中R1、R2和X如规范中所定义。这些化合物可以用作5-HT5A受体拮抗剂。本发明还涉及制备这种化合物的方法以及包含这种化合物的药物组合物。本发明的化合物在预防和/或治疗焦虑抑郁症、焦虑障碍、精神分裂症、惊恐障碍、广场恐惧症、社交恐惧症、强迫症、创伤后应激障碍、疼痛、记忆障碍、痴呆症、饮食行为障碍、性功能障碍、睡眠障碍、戒除药物滥用、帕金森病等运动障碍、精神障碍和胃肠道障碍方面具有用处。
• Substituted arylamine compounds and methods of treatment
  申请人：Becker Oren

  公开号：US20060205737A1

  公开（公告）日：2006-09-14

  The invention relates to 5-HT 6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.

  本发明涉及5-HT6受体拮抗剂。揭示了新型芳胺化合物及其在治疗、调节和/或预防与血清素作用相关的生理状况中的应用，例如在治疗肥胖症和肥胖相关疾病（例如心血管疾病、消化系统疾病、呼吸系统疾病、癌症和2型糖尿病）以及精神障碍（如精神分裂症）中的应用。此外，还揭示了这些化合物及其制药组合物的用途。
• Quinolines
  申请人：Hoffmann-La Roche Inc.

  公开号：US07923561B2

  公开（公告）日：2011-04-12

  The present invention relates to 2-Aminoquinoline derivatives of general formula I and pharmaceutically-acceptable acid-addition salts thereof, wherein R1, R2 and X are as defined in the specification. The compounds may be used as 5-HT5A receptor antagonists. The present invention relates also to processes for making such a compound and a pharmaceutical composition comprising such a compound. Compounds of the present invention are useful in the prevention and/or treatment of anxiety depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders and gastrointestinal disorders.

  本发明涉及通式I的2-氨基喹啉衍生物及其药学上可接受的酸加成盐，其中R1、R2和X如规范中所定义。该化合物可用作5-HT5A受体拮抗剂。本发明还涉及制备这种化合物的方法和包含这种化合物的药物组合物。本发明的化合物对于预防和/或治疗焦虑抑郁症、焦虑症、精神分裂症、惊恐症、广场恐惧症、社交恐惧症、强迫症、创伤后应激障碍、疼痛、记忆障碍、痴呆症、饮食行为障碍、性功能障碍、睡眠障碍、药物滥用戒断、帕金森病等运动障碍、精神障碍和胃肠障碍方面是有用的。
• SUBSTITUTED ARYLAMINE COMPOUNDS AND METHODS OF TREATMENT
  申请人：Becker Oren

  公开号：US20120115850A1

  公开（公告）日：2012-05-10

  The invention relates to 5-HT 6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.

  本发明涉及5-HT6受体拮抗剂。本发明公开了新型芳基胺化合物及其在治疗、调节和/或预防与血清素作用相关的生理状况中的应用，例如治疗肥胖症以及与肥胖症相关的疾病，如心血管疾病、消化系统疾病、呼吸系统疾病、癌症和2型糖尿病；以及精神障碍，如精神分裂症的制备及其制药组合物。
• SUBSTITUTED ARYLAMINE COMPOUNDS AND THEIR USE AS 5-HT6 MODULATORS
  申请人：Epix Delaware, Inc.

  公开号：EP1856075A1

  公开（公告）日：2007-11-21