盐酸洛非帕明 | 26786-32-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 中文名称: 盐酸洛非帕明
• 英文名称: 1-(4-Chlorophenyl)-2-[3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)propyl-methylamino]ethanone;hydron;chloride
• CAS: 26786-32-3
• 化学式: C26H28Cl2N2O
• 分子量: 455.4
• InChiKey: ZWZIQPOLMDPIQM-UHFFFAOYSA-N

物化性质

• 熔点：
  152-154°
• 闪点：
  9℃
• 溶解度：
  二甲基亚砜：~24 mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  6.11
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.269
• 拓扑面积：
  23.6
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• WGK Germany：
  2

文献信息

• [EN] PRODRUG COMPOSITIONS AND METHODS OF TREATMENT<br/>[FR] COMPOSITIONS DE PROMÉDICAMENT ET PROCÉDÉS DE TRAITEMENT
  申请人：AQUESTIVE THERAPEUTICS INC

  公开号：WO2021087359A1

  公开（公告）日：2021-05-06

  Pharmaceutical compositions include a prodrug of epinephrine are described.

  药物组合物包括表述的肾上腺素前药。
• BICYCLIC HETEROCYCLIC COMPOUND
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1961745A1

  公开（公告）日：2008-08-27

  A compound represented by the formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof: wherein X, Y, and W each independently represent a carbon atom or a nitrogen atom; Z represents CH or a nitrogen atom; R1 represents (1) C3-10 branched alkyl which may be substituted or (2) -(CH2)m-NR4R5; R2 and R3 each independently represent (1) a hydrogen atom, (2) C1-4 alkyl which may be substituted with a halogen atom, hydroxy which may be protected, amino which may be protected, or carboxyl which may be protected, (3) C2-4 alkenyl, (4) C2-4 alkynyl, (5) nitrile, (6) COOR6, (7) CONR7R8, (8) COR101, (9) S(O)nR102, or (10) a halogen atom, in which R6 represents a hydrogen atom or C1-4 alkyl, R7 and R8 each independently represent a hydrogen atom or C1-4 alkyl, R101 represents a hydrogen atom or C1-4 alkyl, R102 represents C1-4 alkyl, n represents 1 or 2; and Ar represents an aromatic ring which may be substituted, is useful as a pharmacologically active ingredient having a CRF antagonist action in preventing and/or treating neuropsychiatric diseases, diseases of peripheral organs or the like.

  公式（I）表示的化合物，其盐，其N-氧化物，其溶剂合物或其前药：其中X，Y和W分别独立表示碳原子或氮原子；Z表示CH或氮原子；R1表示（1）可能被取代的C3-10支链烷基或（2）-(CH2)m-NR4R5；R2和R3分别独立表示（1）氢原子，（2）可能被卤原子取代的C1-4烷基，可能被保护的羟基，可能被保护的氨基，或可能被保护的羧基，（3）C2-4烯基，（4）C2-4炔基，（5）腈基，（6）COOR6，（7）CONR7R8，（8）COR101，（9）S（O）nR102，或（10）卤原子，其中R6表示氢原子或C1-4烷基，R7和R8分别独立表示氢原子或C1-4烷基，R101表示氢原子或C1-4烷基，R102表示C1-4烷基，n表示1或2；Ar表示可能被取代的芳香环，用作在预防和/或治疗神经精神疾病，外周器官疾病等方面具有CRF拮抗作用的药理活性成分。
• Multi-functional ionic liquid compositions for overcoming polymorphism and imparting improved properties for active pharmaceutical, biological, nutritional, and energetic ingredients
  申请人：Rogers D. Robin

  公开号：US20070093462A1

  公开（公告）日：2007-04-26

  Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.

  揭示了离子液体及制备活性药物、生物、营养和能量成分的离子液体组合物的方法。还揭示了利用本文描述的组合物的方法，以克服多型性、克服溶解度和输送问题、控制释放速率、增加功能性、增强功效（协同作用）以及改善易用性和制造工艺。
• Combinations comprising alpha-2-delta ligands
  申请人：Dooley James David

  公开号：US20050059715A1

  公开（公告）日：2005-03-17

  The instant invention relates to a combination, particularly a synergistic combination, of an alpha-2-delta ligand and a dual serotonin-noradrenaline re-uptake inhibitor (DSNRI) or one or both of a selective serotonin re-uptake inhibitor (SSRI) and a selective noradrenaline re-uptake inhibitor (SNRI), and pharmaceutically acceptable salths thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain.

  该发明涉及一种组合，特别是α-2-δ配体和双重5-羟色胺-去甲肾上腺素再摄取抑制剂（DSNRI）或选择性5-羟色胺再摄取抑制剂（SSRI）和/或选择性去甲肾上腺素再摄取抑制剂（SNRI）的协同组合，以及其药学上可接受的盐，药物组合物及其在特别是神经痛治疗中的用途。
• [EN] INDOLIN-2-ONE OR PYRROLO-PYRIDIN-2-ONE DERIVATIVES<br/>[FR] DÉRIVÉS D'INDOLIN-2-ONE OU DE PYRROLOPYRIDIN-2-ONE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2015197567A1

  公开（公告）日：2015-12-30

  The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+-(O-); R1 is lower alkyl, halogen, cyano or cycloalkyl; Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+-(O-), or is benzo[b]thiophenyl; R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl; X is CH or N; n is 1 or 2; m is 1 or 2; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, epilepsy, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems.

  本发明涉及一般式（I）的2-氧代-2,3-二氢吲哚，其中Ar1为苯基或含有一个、两个或三个异原子（N、S或O）的五元或六元杂环芳基，其中杂环芳基中的N-异原子可以被氧化为N+-(O-)；R1为低碳基、卤素、氰基或环烷基；Ar2为含有一个、两个、三个或四个异原子（N、S或O）的五元或六元杂环芳基，其中杂环芳基中的N-异原子可以被氧化为N+-(O-)，或者为苯并[ｂ]噻吩基；R2为氢、低碳基、卤素、氰基、被羟基取代的低碳基、被卤素取代的低碳基、被氨基取代的低碳基、被烷氧基取代的低碳基、被酰胺取代的低碳基，或者为环烷基；X为CH或N；n为1或2；m为1或2；以及其药学上可接受的盐、消旋体混合物、或其对映体和/或光学异构体和/或立体异构体。这些化合物可用于治疗与精神病（精神病）、精神分裂症的阳性和阴性症状、物质滥用、酒精和药物成瘾、强迫症、认知障碍、躁郁症、情感障碍、重度抑郁症、治疗难治性抑郁症、焦虑障碍、阿尔茨海默病、自闭症、帕金森病、慢性疼痛、边缘人格障碍、神经退行性疾病、睡眠障碍、慢性疲劳综合征、僵硬、炎症性疾病、哮喘、亨廷顿病、注意力缺陷多动障碍、肌萎缩侧索硬化症、癫痫、关节炎作用、自身免疫疾病、病毒和真菌感染、心血管疾病、眼科学和炎症性视网膜疾病以及平衡问题相关的中枢神经系统疾病的治疗。