8-氯-2,3,4,5-四氢-2-甲基-5-[2-(6-甲基-3-吡啶基)乙基]-1H-吡啶并[4,3-B]吲哚 | 21228-13-7

• 物质功能分类: 医药中间体 - 吡啶类化合物
• 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
• 中文名称: 8-氯-2,3,4,5-四氢-2-甲基-5-[2-(6-甲基-3-吡啶基)乙基]-1H-吡啶并[4,3-B]吲哚
• 英文名称: dorastine
• 英文别名: 8-Chlor-1,3,4,5-tetrahydro-2-methyl-5-<2-(6-methyl-3-pyridyl)-aethyl>-2H-pyrido<4,3-b>indol；8-chloro-2-methyl-5-[2-(6-methyl-pyridin-3-yl)-ethyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole；8-chloro-2,3,4,5-tetrahydro-2.methyl-5-(2-(6-methylpyridin-3-yl)ethyl)-1H-pyrido[4,3-b]indole；8-chloro-2-methyl-5-[2-(6-methylpyridin-3-yl)ethyl]-3,4-dihydro-1H-pyrido[4,3-b]indole
• CAS: 21228-13-7
• 化学式: C₂₀H₂₂ClN₃
• 分子量: 339.868
• InChiKey: WCTGYFWVYBPRGF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  21.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  对氯苯肼盐酸盐 、 5-(2-溴乙基)-2-甲基吡啶 、 三乙胺 、 1-甲基-4-哌啶酮盐酸盐 以 乙醇 为溶剂， 以to obtain 390 mg of 8-chloro-2,3,4,5-tetrahydro-2-methyl-5-(2-(6-methylpyridin-3-yl)ethyl)-1H-pyrido[4,3-b]indole after的产率得到8-氯-2,3,4,5-四氢-2-甲基-5-[2-(6-甲基-3-吡啶基)乙基]-1H-吡啶并[4,3-B]吲哚
  参考文献：
  名称：

  Tetracyclic compounds

  摘要：

  本披露涉及新的四环化合物，可用于调节个体中的组胺受体。在其中一种实施例中，化合物是四环[4,3-b]吲哚。还提供了包含该化合物的制药组合物，以及使用该化合物进行各种治疗应用的方法，包括治疗认知障碍、精神疾病、神经递质介导的疾病和/或神经元疾病。

  公开号：

  US08338408B2

文献信息

• [EN] NEW TETRACYCLIC COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS TÉTRACYCLIQUES
  申请人：MEDIVATION TECHNOLOGIES INC

  公开号：WO2009055828A1

  公开（公告）日：2009-04-30

  This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3- 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.

  这项披露涉及可能用于调节个体组织胺受体的新四环化合物。在一个实施例中，这些化合物是四环[4,3- b]吲哚类化合物。此外还提供了包含这些化合物的药物组合物，以及使用这些化合物进行各种治疗应用的方法，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。
• Impaired energy processing disorders and mitochondrial deficiency
  申请人：Shchepinov Mikhail S.

  公开号：US10058612B2

  公开（公告）日：2018-08-28

  Some aspects of the invention provide for a method of treating Impaired Energy Processing Disorders and Mitochondrial Deficiencies using polyunsaturated fatty acids which are modified in certain positions to attenuate oxidative damage by Reactive Oxygen Species (ROS) and/or suppress the rate of formation of reactive products and toxic compounds.

  该发明的某些方面提供了一种治疗能量处理障碍和线粒体缺陷的方法，使用在特定位置被修饰以减轻活性氧（ROS）氧化损伤和/或抑制反应产物和有毒化合物形成速率的多不饱和脂肪酸。
• SUBSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR USE THEREOF
  申请人：Ivachtchenko Alexandre Vasilievich

  公开号：US20190233409A1

  公开（公告）日：2019-08-01

  The present invention relates to compound of the formula 1.2, or a pharmaceutically acceptable salt, or hydrate thereof wherein R 1 is C 1 -C 5 alkyl; R 2 , is independently hydrogen, halogen, C 1 -C 3 alkyl, CF 3 , OCF 3 or OCH 3 ; i is 1, 2,3, or 4; Ar is unsubstituted phenyl or substituted phenyl substituted with halogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, a substituted amino group or trifluoromethyl; or Ar is a substituted or unsubstituted 6-membered aromatic heterocycle one or, with two nitrogen atoms in the heterocycle; excluding the compounds of the formulas A1-A4 The invention relates to the novel chemical compounds, methods for their preparation and use as antagonists of 5-HT 6 receptors, simultaneously regulating homeostasis of calcium ions in cells. The invention relates to the novel annelated azaheterocycles—2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles, to methods for their preparation, to pharmaceutical compositions, including these compounds as active substances, and to methods of treatment and profylaxis of various diseases.

  本发明涉及公式1.2的化合物，或其药学上可接受的盐或水合物，其中R1为C1-C5烷基；R2独立地为氢、卤素、C1-C3烷基、CF3、O 或OCH3；i为1、2、3或4；Ar为未取代的苯基或取代的苯基，取代基为卤素、C1-C6烷基、C1-C6烷氧基、取代氨基或三氟甲基；或Ar为取代或未取代的6元芳杂环之一，其中异杂环中含有两个氮原子；但不包括A1-A4式的化合物。本发明涉及新的化学化合物、其制备方法以及作为5-HT6受体拮抗剂的用途，同时调节细胞内钙离子的稳态。本发明涉及新的螺合的氮杂环-2,3,4,5-四氢-1H-吡啶[4,3-b]吲哚化合物，以及其制备方法、包括这些化合物作为活性物质的制药组合物，以及各种疾病的治疗和预防方法。
• SUSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR USE THEREOF
  申请人：Alla Chem, LLC

  公开号：US20130217703A1

  公开（公告）日：2013-08-22

  The present invention relates to a method of antagonizing a 5-HT 6 serotonin receptor and simultaneously regulating Ca +2 ion homeostasis in a cell, comprising administering to the cell a compound of formula 1, or a pharmaceutically acceptable salt thereof, wherein: R 1 is a C 1 -C 5 alkyl; R 2 i is independently hydrogen, halogen, a C 1 -C 3 alkyl, CF 3 , OCF 3 or OCH 3 ; i is 1, 2, 3 or 4; Ar is an unsubstituted phenyl or a substituted phenyl substituted with halogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, substituted amino group or trifluoromethyl; or Ar is a substituted or unsubstituted 6-membered aromatic heterocycle with one or two nitrogen atoms in the heterocycle; and W is an ethylene group —CH 2 —CH 2 —, ethenyl group —CH═CH—, or ethynyl group —C≡C—. The invention also relates to new compounds selected from the group of compounds of the general formula 1, method for their preparation, pharmaceutical compositions and method for treating a cognitive disorder or neurodegenerative disease, or obesity in a subject in need thereof comprising administering an effective dose to the subject of a compound of formula 1 according to claim 1 , or a pharmaceutically acceptable salt thereof.

  本发明涉及一种拮抗5-HT6 5-羟色胺受体和同时调节细胞内Ca+2离子稳态的方法，包括向细胞中投与式1的化合物或其药学上可接受的盐，其中：R1是C1-C5烷基；R2独立地是氢、卤素、C1-C3烷基、CF3、O 或OCH3；i为1、2、3或4；Ar是未取代的苯基或取代的苯基，其被卤素、C1-C6烷基、C1-C6烷氧基、取代的氨基团或三氟甲基取代；或Ar是带有一个或两个氮原子的取代或未取代的6元芳香杂环；W是乙烯基—CH2— —、乙烯基—CH═CH—或乙炔基—C≡C—。本发明还涉及从式1的化合物组中选择的新化合物、其制备方法、制备药物组合物的方法以及治疗认知障碍或神经退行性疾病或肥胖症的方法，包括向需要治疗的受体中投与式1的化合物或其药学上可接受的盐的有效剂量。
• NEURODEGENERATIVE DISORDERS AND MUSCLE DISEASES IMPLICATING PUFAS
  申请人：Shchepinov Mikhail S.

  公开号：US20140147428A1

  公开（公告）日：2014-05-29

  Some aspects of the invention provide for a method of treating Alzheimer's Disease, Mild Cognitive Impairment, Frontotemperal Dementia, Amyotrophic Lateral Sclerosis and/or Multiple Sclerosis using polyunsaturated fatty acids which are modified in certain positions to attenuate oxidative damage by Reactive Oxygen Species (ROS) and/or suppress the rate of formation of reactive products and toxic compounds.

  该发明的某些方面提供了一种使用在特定位置被修饰的多不饱和脂肪酸来治疗阿尔茨海默病、轻度认知障碍、额颞型痴呆、肌萎缩侧索硬化和/或多发性硬化症的方法，以减轻反应性氧化物（ROS）所引起的氧化损伤和/或抑制反应性产物和有毒化合物的形成速率。