5-(2,6-Difluorophenyl)-7,11-diazatricyclo[7.3.1.02,7]trideca-2,4-dien-6-one

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 羽扇豆生物碱
• 英文名称: 5-(2,6-Difluorophenyl)-7,11-diazatricyclo[7.3.1.02,7]trideca-2,4-dien-6-one
• 化学式: C₁₇H₁₆F₂N₂O
• 分子量: 302.32
• InChiKey: BGGGFMGAUXAEKO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  22
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  32.3
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Pharmaceutical composition and method of modulating cholinergic function in a mammal
  申请人：Pfizer Inc.

  公开号：US20030008892A1

  公开（公告）日：2003-01-09

  A pharmaceutical composition and method of modulating cholinergic function in a mammal comprising administration of a NRPA compound or a pharmaceutically acceptable salt thereof; and an anti-emetic/anti-nausea agent or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier. The NRPA compound and the anti-emetic/anti-nausea agent are present in amounts that render the composition effective modulating cholinergic function or in the treatment of a diorder or condition selected from inflammatory bowel disease (including but not limited to ulcerative colitis, pyoderma gangrenosum and Crohn's disease), irritable bowel syndrome, spastic dystonia, chronic pain, acute pain, celiac sprue, pouchitis, vasoconstriction, anxiety, panic disorder, depression, bipolar disorder, autism, sleep disorders, jet lag, amyotrophic lateral sclerosis (ALS), cognitive dysfunction, hypertension, bulimia, anorexia, obesity, cardiac arrythmias, gastric acid hypersecretion, ulcers, pheochromocytoma, progressive supranuclear palsy, chemical dependencies and addictions (e.g., dependencies on, or addictions to nicotine (and/or tobacco products), alcohol, benzodiazepines, barbiturates, opioids or cocaine), headache, migraine, stroke, traumatic brain injury (TBI), obsessive-compulsive disorder (OCD), psychosis, Huntington's chorea, tardive dyskinesia, hyperkinesia, dyslexia, schizophrenia, multi-infarct dementia, age-related cognitive decline, epilepsy, including petit mal absence epilepsy, senile dementia of the Alzheimer's type (AD), Parkinson's disease (PD), attention deficit hyperactivity disorder (ADHD) and Tourette's Syndrome. The method of using these compositions is also disclosed.

  一种药物组合物及其在哺乳动物中调节胆碱能功能的方法，包括给予NRPA化合物或其药学上可接受的盐；以及抗恶心/抗呕吐剂或其药学上可接受的盐；和药学上可接受的载体。NRPA化合物和抗恶心/抗呕吐剂的含量使组合物能够有效调节胆碱能功能或用于治疗炎症性肠病（包括但不限于溃疡性结肠炎、化脓性坏疽和克罗恩病）、肠易激综合症、痉挛性肌张力障碍、慢性疼痛、急性疼痛、乳糜泻、袋炎、血管收缩、焦虑、惊恐障碍、抑郁症、躁郁症、自闭症、睡眠障碍、时差反应、肌萎缩侧索硬化症（ALS）、认知功能障碍、高血压、贪食症、厌食症、肥胖症、心脏心律失常、胃酸过多分泌、溃疡、嗜铬细胞瘤、进行性核上性麻痹、化学依赖和成瘾（例如对尼古丁（和/或烟草制品）、酒精、苯二氮卓、巴比妥类药物、阿片类药物或可卡因的依赖或成瘾）、头痛、偏头痛、中风、创伤性脑损伤（TBI）、强迫症、精神病、亨廷顿舞蹈症、迟发性运动障碍、过动症、阿尔茨海默病的老年性痴呆、帕金森病（PD）、注意力缺陷多动障碍（ADHD）和抽动症。还公开了使用这些组合物的方法。
• Pyridone-fused azabicyclic- or cytisine derivatives, their preparation and their use in addiction therapy
  申请人：——

  公开号：US20030065173A1

  公开（公告）日：2003-04-03

  Pyridone-fused azabicyclic compounds of the formula 1 and their pharmaceutically acceptable salts and prodrugs, wherein R 1 , R 2 and R 3 are defined below, intermediates and methods for their preparation. Compositions and methods for using compounds of the formula I in the treatment of neurological and mental disorders related to a decrease in cholinergic function such as nicotine addiction, Huntington's Chorea, tardive dyskinesia, hyperkinesia, mania, dyslexia, schizophrenia , analgesia, attention deficit disorder (ADD), multi-infarct demetia, age related cognitive decline, epilepsy, neurological and mental disorders related to a decrease in cholinergic function, senile dementia of the Alzheimer's type, Parkinson's disease, attention deficit hyperactivity disorder (ADHD), anxiety, obesity, Tourette's Syndrome and ulcerative colitis.

  公式1中的吡啶并咪唑化合物及其药学上可接受的盐和前药，其中R1、R2和R3的定义如下，以及它们的中间体和制备方法。公式I化合物在治疗与胆碱能功能降低有关的神经和精神障碍方面的组合物和方法，例如尼古丁成瘾、亨廷顿舞蹈病、迟发性运动障碍、多动症、躁狂症、阅读障碍、精神分裂症、镇痛、注意力缺陷障碍（ADD）、多发性梗塞性痴呆、与胆碱能功能降低有关的神经和精神障碍、阿尔茨海默病、帕金森病、注意力缺陷过动症（ADHD）、焦虑症、肥胖症、抽动症和溃疡性结肠炎的治疗中使用。
• Composition for the treatment and prevention of nicotine addiction containing a nicotine receptor agonist and an anti-depressant or anti-anxiety drug
  申请人：Pfizer Products Inc.

  公开号：EP1078637A2

  公开（公告）日：2001-02-28

  Pharmaceutical compositions are disclosed for the treatment of nicotine dependence or addiction, tobacco dependence or addiction, reduction of nicotine withdrawal symptoms or aiding in the cessation or lessening of tobacco use or substance abuse. The pharmaceutical compositions are comprised of a therapeutically effective combination of a nicotine receptor partial agonist and an anti-depressant or anxiolytic agent and a pharmaceutically acceptable carrier. The method of using these compounds is also disclosed.

  本发明公开了用于治疗尼古丁依赖或成瘾、烟草依赖或成瘾、减轻尼古丁戒断症状或帮助戒烟或减少烟草使用或药物滥用的药物组合物。这些药物组合物由尼古丁受体部分激动剂和抗抑郁剂或抗焦虑剂的治疗有效组合以及药学上可接受的载体组成。还公开了使用这些化合物的方法。
• A pharmaceutical composition for the treatment of obesity or to facilitate or promote weight loss, comprising a nicotine receptor partial agonist and an anti-obesity agent
  申请人：Pfizer Products Inc.

  公开号：EP1159970A2

  公开（公告）日：2001-12-05

  Pharmaceutical compositions are disclosed for the treatment of obesity, an overweight condition and compulsive overeating. The pharmaceutical compositions are comprised of a therapeutically effective combination of a nicotine receptor partial agonist and an anti-obesity agent or weight loss facilitator or promoter and a pharmaceutically acceptable carrier. The method of using these compounds is also disclosed.

  本发明公开了用于治疗肥胖症、超重症和强迫性暴饮暴食的药物组合物。这些药物组合物由尼古丁受体部分激动剂和抗肥胖剂或减肥促进剂或促进剂的治疗有效组合以及药学上可接受的载体组成。还公开了使用这些化合物的方法。
• A pharmaceutical composition for the treatment of attention deficit hyperactivity disorder(ADHD) comprising a nicotine receptor partial agonist and anti-ADHD agent
  申请人：Pfizer Products Inc.

  公开号：EP1177798A2

  公开（公告）日：2002-02-06

  Pharmaceutical compositions are disclosed for the treatment of attention deficit hyperactivity disorder (ADHD). The pharmaceutical compositions are comprised of a therapeutically effective combination of a nicotine receptor partial agonist and an anti-ADHD agent and a pharmaceutically acceptable carrier. The method of using these compounds is also disclosed.

  本发明公开了用于治疗注意缺陷多动障碍（ADHD）的药物组合物。这些药物组合物由尼古丁受体部分激动剂和抗多动症药物的治疗有效组合以及药学上可接受的载体组成。还公开了使用这些化合物的方法。