1-(4-fluorophenyl)-4-(5,6,8,11-tetrahydro-4H-pyrido[3',4':4,5]pyrrolo[3,2,1-ij]quinolin-10(9H)-yl)-1-butanone | 313670-83-6

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-(4-fluorophenyl)-4-(5,6,8,11-tetrahydro-4H-pyrido[3',4':4,5]pyrrolo[3,2,1-ij]quinolin-10(9H)-yl)-1-butanone
• 英文别名: 4-(1,12-diazatetracyclo[7.6.1.05,16.010,15]hexadeca-5(16),6,8,10(15)-tetraen-12-yl)-1-(4-fluorophenyl)butan-1-one
• CAS: 313670-83-6
• 化学式: C₂₄H₂₅FN₂O
• 分子量: 376.474
• InChiKey: WLFFAKKXQWSLGG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  25.2
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  N-nitroso-1,2,3,4-tetrahydroquinoline 在 potassium carbonate 、 溶剂黄146 、 锌 作用下， 以 乙腈 为溶剂， 生成 1-(4-fluorophenyl)-4-(5,6,8,11-tetrahydro-4H-pyrido[3',4':4,5]pyrrolo[3,2,1-ij]quinolin-10(9H)-yl)-1-butanone
  参考文献：
  名称：

  [EN] FUSED TETRACYCLIC PYRIDO[4,3-B]INDOLE AND PYRIDO[3,4-B]INDOLE DERIVATIVES AND METHODS OF USE
  [FR] DÉRIVÉS DE PYRIDO[4,3-B]INDOLE ET PYRIDO[3,4-B]INDOLE TÉTRACYCLIQUE CONDENSÉS ET PROCÉDÉS D'UTILISATION

  摘要：

  公开号：

  WO2011103460A8

文献信息

• Substituted heterocycle fused gamma-carbolines
  申请人：Bristol-Myers Squibb Pharma Company

  公开号：US06548493B1

  公开（公告）日：2003-04-15

  The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

  本发明涉及由结构式（I）表示的某些新化合物或其药用可接受的盐形式，其中R1、R5、R6a、R6b、R7、R8、R9、X、b、k、m和n以及虚线在此处描述。本发明还涉及包含这些新化合物作为活性成分的药物配方，以及在治疗某些疾病中使用这些新化合物及其配方。本发明的化合物是5-羟色胺激动剂和拮抗剂，在控制或预防包括肥胖、焦虑、抑郁症、精神病、精神分裂症、睡眠障碍、性功能障碍、偏头痛、头痛相关疾病、社交恐惧症以及胃肠道疾病（如胃肠道运动功能障碍）等中枢神经系统疾病方面具有用处。
• Substituted heterocyle fused gamma-carbolines
  申请人：Robichaud J. Albert

  公开号：US20060178362A1

  公开（公告）日：2006-08-10

  The present invention is directed to compounds useful for treating addictive behavior and sleep disorders represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R 1 , R 5 , R 6a , R 6b , R 7 , R 8 , R 9 , X, b, k, m, and n, and the dashed lines are described herein. The compounds used in the method of treatment of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including addictive behavior and sleep disorders.

  本发明涉及用于治疗成瘾行为和睡眠障碍的化合物，其结构式表示为(I)，或其药学上可接受的盐形式，其中R1、R5、R6a、R6b、R7、R8、R9、X、b、k、m和n以及虚线如本文所述。本发明方法中使用的化合物是5-羟色胺激动剂和拮抗剂，并且对于控制或预防包括成瘾行为和睡眠障碍在内的中枢神经系统疾病是有用的。
• COMPOUNDS AND METHODS OF TREATING HYPERTENSION
  申请人：Protter Andrew Asher

  公开号：US20140303144A1

  公开（公告）日：2014-10-09

  Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor α 2B antagonists. The compounds may also bind to and antagonize adrenergic receptor α 2B . The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.

  本文介绍了氢化吡啶[4,3-b]吲哚、吡啶[3,4-b]吲哚和氮杂七环[4,5-b]吲哚。这些化合物可以与肾上腺素受体α2B结合并对其产生拮抗作用。这些化合物还可以与肾上腺素受体α2B结合并对其产生拮抗作用。这些化合物可以用于治疗，例如：（i）降低血压和/或（ii）促进肾脏血流和/或（iii）减少或抑制钠的重吸收。这些化合物还可以用于治疗对降低血压有反应或预计会有反应的疾病或病况。特别描述了这些化合物用于治疗心血管和肾脏疾病。
• FUSED TETRACYCLIC PYRIDO [4,3-B] INDOLE AND PYRIDO [3,4-B] INDOLE DERIVATIVES AND METHODS OF USE
  申请人：Chakravarty Sarvajit

  公开号：US20130210803A1

  公开（公告）日：2013-08-15

  This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

  本公开涉及熔合四环吡啶[4,3-b]吲哚和吡啶[3,4-b]吲哚。还提供了包含这些化合物的制药组合物，以及使用这些化合物进行多种治疗应用的方法，包括治疗认知障碍、精神障碍、神经递质介导的障碍和/或神经元障碍。
• COMPOUNDS AND METHODS OF TREATING DIABETES
  申请人：Protter Andrew Asher

  公开号：US20140228353A1

  公开（公告）日：2014-08-14

  Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor α 2A . The compounds may also bind to and are an antagonist of the adrenergic receptor α 2B ; or the compounds are not antagonists of the adrenergic receptor α 2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.

  介绍了氢化吡咯[4,3-b]吲哚、吡咯[3,4-b]吲哚和氮杂七环[4,5-b]吲哚。这些化合物可以结合并拮抗肾上腺素α2A受体。这些化合物也可以结合并拮抗肾上腺素α2B受体；或者这些化合物不是肾上腺素α2B受体的拮抗剂，并且这些化合物与第二种预计可以降低血压的药物一起使用。这些化合物可以用于治疗，例如调节血糖水平，增加胰岛素分泌并治疗对胰岛素产生增加反应的疾病或状况。特别描述了使用这些化合物治疗2型糖尿病的方法。