4-Bromo-3,3-dimethylindoline | 1227418-26-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 4-Bromo-3,3-dimethylindoline
• 英文别名: 4-bromo-3,3-dimethyl-1,2-dihydroindole
• CAS: 1227418-26-9
• 化学式: C₁₀H₁₂BrN
• 分子量: 226.11
• InChiKey: WRJRWRRMADSCCD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• [EN] 5-HT2C RECEPTOR AGONISTS AND COMPOSITIONS AND METHODS OF USE<br/>[FR] AGONISTES DU RÉCEPTEUR 5-HT2C ET COMPOSITIONS ET PROCÉDÉS D'UTILISATION
  申请人：ARENA PHARM INC

  公开号：WO2015066344A1

  公开（公告）日：2015-05-07

  Provided are 5-HT2C receptor agonists. Also provided are methods for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, dyslipidemia, nonalcoholic fatty liver disease, obesity-related renal disease, and sleep apnea. Also provided are compositions comprising a selective 5-HT2C receptor agonist, optionally in combination with a supplemental agent, and methods for reducing the frequency of smoking tobacco in an individual attempting to reduce frequency of smoking tobacco; aiding in the cessation or lessening of use of a tobacco product in an individual attempting to cease or lessen use of a tobacco product; aiding in smoking cessation and preventing associated weight gain; controlling weight gain associated with smoking cessation by an individual attempting to cease smoking tobacco; reducing weight gain associated with smoking cessation by an individual attempting to cease smoking tobacco; treating nicotine dependency, addiction and/or withdrawal in an individual attempting to treat nicotine dependency, addiction and/or withdrawal; or reducing the likelihood of relapse use of nicotine by an individual attempting to cease nicotine use comprising administering a selective 5-HT2C receptor agonist, optionally in combination with a supplemental agent.

  提供了5-HT2C受体激动剂。还提供了用于体重管理、诱导饱腹感、减少食物摄入量、预防和治疗肥胖、抗精神病药物引起的体重增加、2型糖尿病、普拉德-威利综合征、烟草/尼古丁依赖、药物成瘾、酒精成瘾、病态赌博、奖赏缺乏综合征和性成瘾）、强迫症谱系障碍和冲动控制障碍（包括咬指甲和咬甲）、睡眠障碍（包括失眠、睡眠结构碎裂和慢波睡眠紊乱）、尿失禁、精神障碍（包括精神分裂症、厌食症和暴食症）、阿尔茨海默病、性功能障碍、勃起功能障碍、癫痫、运动障碍（包括帕金森病和抗精神病药物引起的运动障碍）、高血压、血脂异常、非酒精性脂肪肝病、肥胖相关肾脏疾病和睡眠呼吸暂停。还提供了包含选择性5-HT2C受体激动剂的组合物，可选地与辅助剂结合，以及用于减少个体尝试减少吸烟频率的吸烟频率；帮助个体戒除或减少使用烟草制品的个体戒除或减少使用烟草制品；帮助戒烟并预防相关体重增加；通过个体尝试戒烟来控制与戒烟相关的体重增加；通过个体尝试戒烟来减少与戒烟相关的体重增加；治疗尼古丁依赖、成瘾和/或戒断的个体尝试治疗尼古丁依赖、成瘾和/或戒断；或减少个体尝试戒除尼古丁使用的复发可能性，包括给予选择性5-HT2C受体激动剂，可选地与辅助剂结合。
• [EN] INHIBITORS OF FATTY ACID BINDING PROTEIN (FABP)<br/>[FR] INHIBITEURS DE LA PROTÉINE DE LIAISON AUX ACIDES GRAS (FABP)
  申请人：SCHERING CORP

  公开号：WO2010056631A1

  公开（公告）日：2010-05-20

  The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein ("FABP") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the present invention is shown below: (I)

  本发明涉及新型杂环化合物作为脂肪酸结合蛋白（"FABP"）抑制剂，包括该杂环化合物的药物组合物以及利用该化合物治疗或预防心血管疾病、代谢紊乱、肥胖或与肥胖相关的疾病、糖尿病、血脂异常、糖尿病并发症、糖耐量受损或空腹血糖受损的用途。本发明的一个示例化合物如下所示：（I）
• [EN] NEW PROPANAMINE DERIVATIVES FOR TREATING PAIN AND PAIN RELATED CONDITIONS<br/>[FR] NOUVEAUX DÉRIVÉS DE PROPANAMINE PERMETTANT DE TRAITER LA DOULEUR ET DES ÉTATS PATHOLOGIQUES ASSOCIÉS À LA DOULEUR
  申请人：ESTEVE PHARMACEUTICALS SA

  公开号：WO2019020792A1

  公开（公告）日：2019-01-31

  The present invention relates to new compounds of general formula (I) that show dual activity towards α2δ subunit of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit, and to the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

  本发明涉及一般式(I)的新化合物，该化合物对电压门控钙通道（VGCC）的α2δ亚基，特别是α2δ-1亚基，以及去甲肾上腺素转运蛋白（NET）显示双重活性。该发明还涉及制备所述化合物的方法，以及包含它们的组合物，并将其用作药物。
• INHIBITORS OF FATTY ACID BINDING PROTEIN (FABP)
  申请人：Shipps, JR. Gerald W.

  公开号：US20110237575A1

  公开（公告）日：2011-09-29

  The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the present invention is shown below: (I)

  本发明涉及新型杂环化合物作为脂肪酸结合蛋白（“FABP”）抑制剂，包括所述杂环化合物的制药组合物以及用于治疗或预防心血管疾病、代谢紊乱、肥胖或肥胖相关疾病、糖尿病、血脂异常、糖尿病并发症、糖耐量受损或空腹血糖受损的化合物的用途。本发明的一种说明性化合物如下：（I）
• NEW PROPANAMINE DERIVATIVES FOR TREATING PAIN AND PAIN RELATED CONDITIONS
  申请人：ESTEVE PHARMACEUTICALS, S.A.

  公开号：EP3658550A1

  公开（公告）日：2020-06-03