CP-615003 | 329016-45-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: CP-615003
• 英文别名: 4-Oxo-4,5,6,7-tetrahydro-1H-indole-3-carboxylic acid [3-fluoro4-(2-propylamino-ethoxy)-phenyl]-amide；N-[3-fluoro-4-(2-n-propylaminoethoxy)phenyl]-4-oxo-4,5,6,7-tetrahydro-1H-indole-3-carboxamide；n-(3-Fluoro-4-(2-(propylamino)ethoxy)phenyl)-4,5,6,7-tetrahydro-4-oxo-1h-indole-3-carboxamide；N-[3-fluoro-4-[2-(propylamino)ethoxy]phenyl]-4-oxo-1,5,6,7-tetrahydroindole-3-carboxamide
• CAS: 329016-45-7
• 化学式: C₂₀H₂₄FN₃O₃
• 分子量: 373.427
• InChiKey: YZHJISPIBWKWGY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  27
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  83.2
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  [2-(2-Fluoro-4-[(4-oxo-4,5,6,7-tetrahydro-1H-indole-3-carbonyl)-amino]-phenoxy)-ethyl]-propyl-carbamic acid tert-butyl ester 生成 CP-615003
  参考文献：
  名称：

  US2002/151718

  摘要：

  公开号：

文献信息

• Fused pyrrolecarboxamides: GABA brain receptor ligands
  申请人：Albaugh Pamela

  公开号：US20050014939A1

  公开（公告）日：2005-01-20

  Substituted pyrrolecarboxamide compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABA A brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABA A brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Alzheimer's dementia, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABA A receptors in tissue samples.

  揭示了取代吡咯甲酰胺化合物。这些化合物是高度选择性的GABAA脑受体的激动剂、拮抗剂或逆向激动剂，或者是GABAA脑受体的激动剂、拮抗剂或逆向激动剂的前药，因此在焦虑、抑郁、阿尔茨海默病痴呆、睡眠和癫痫障碍、苯二氮卓类药物过量以及增强记忆的诊断和治疗中非常有用。此外，还提供了包括包装的药物组合物在内的制药组合物。该发明的化合物还可用作定位组织样本中GABAA受体的探针。
• Fused pyrrolecarboxamides; a new class of GABA brain receptor ligands
  申请人：Neurogen

  公开号：US20010029299A1

  公开（公告）日：2001-10-11

  Disclosed are compounds of the formula: 1 or the pharmaceutically acceptable non-toxic salts thereof wherein: G, X, T, n, and R 3 -R 6 are as defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

  本发明涉及以下公式的化合物：1或其药学上可接受的非毒性盐，其中：G、X、T、n和R3-R6的定义如本文所述，这些化合物是高度选择性的GABAa脑受体的激动剂、拮抗剂或反向激动剂，或是GABAa脑受体的激动剂、拮抗剂或反向激动剂的前药。这些化合物在焦虑、睡眠和癫痫障碍的诊断和治疗、苯二氮卓类药物过量和增强记忆方面有用。
• Methods, kits and compositions for using pyrrole derivatives against anxiety
  申请人：WARNER-LAMBERT COMPANY

  公开号：EP1254660A2

  公开（公告）日：2002-11-06

  The present invention provides methods and kits for treating obsessive-compulsive disorder, acute stress disorder, post traumatic stress disorder, social anxiety disorder, somatization disorder, specific social phobia, premenstrual dysphoric disorder, anxiety associated with a medical condition, adjustment disorder with anxious mood, dysthymia, specific phobia or fibromyalgia using a compound of Formula I or a pharmaceutically acceptable salt, optical isomer or prodrug thereof The present invention also provides compositions comprising a compound of Formula I or a pharmaceutically acceptable salt, optical isomer or prodrug thereof and an additional compound useful to treat the aforementioned conditions.

  本发明提供了使用式 I 化合物或其药学上可接受的盐、光学异构体或原药治疗强迫症、急性应激障碍、创伤后应激障碍、社交焦虑障碍、躯体化障碍、特定社交恐惧症、经前期情感障碍、与疾病相关的焦虑、焦虑情绪的适应障碍、癔症、特定恐惧症或纤维肌痛的方法和试剂盒。 本发明还提供了由式 I 化合物或其药学上可接受的盐、光学异构体或原药和另一种用于治疗上述病症的化合物组成的组合物。
• Methods and kits for treating depression or preventing deterioration of cognitive function
  申请人：Pfizer Products Inc.

  公开号：EP1254662A2

  公开（公告）日：2002-11-06

  The present invention provides methods and kits for treating depression, perimenopausal depression, schizophrenia, anxiety, panic attacks, binge eating, social phobia, or preventing deterioration of cognitive function by administering to a patient in need thereof a therapeutically effect amount of an estrogen agonist /antagonist of formula I

  本发明提供了治疗抑郁症、围绝经期抑郁症、精神分裂症、焦虑症、恐慌症、暴食症、社交恐惧症或预防认知功能退化的方法和试剂盒，其方法是向有需要的患者施用具有治疗效果的式 I 的雌激素激动剂/拮抗剂。
• Methods, kits and compositions for using pyrrole derivatives
  申请人：——

  公开号：US20030022915A1

  公开（公告）日：2003-01-30

  The present invention provides methods and kits for treating obsessive-compulsive disorder, acute stress disorder, post traumatic stress disorder, social anxiety disorder, somatization disorder, specific social phobia, premenstrual dysphoric disorder, anxiety associated with a medical condition, adjustment disorder with anxious mood, dysthymia, specific phobia or fibromyalgia using a compound of Formula I or a pharmaceutically acceptable salt, optical isomer or prodrug thereof 1 The present invention also provides compositions comprising a compound of Formula I or a pharmaceutically acceptable salt, optical isomer or prodrug thereof and an additional compound useful to treat the aforementioned conditions.

  本发明提供了使用式 I 化合物或其药学上可接受的盐、光学异构体或原药治疗强迫症、急性应激障碍、创伤后应激障碍、社交焦虑障碍、躯体化障碍、特定社交恐惧症、经前期情感障碍、与疾病相关的焦虑、焦虑情绪的适应障碍、癔症、特定恐惧症或纤维肌痛的方法和试剂盒。 1 本发明还提供了由式 I 化合物或其药学上可接受的盐、光学异构体或原药和另一种用于治疗上述病症的化合物组成的组合物。