N,N-dimethyl-6-phenyl-11H-pyrido[2,3-b][1,4]benzodiazepine-11-propanamine fumarate | 83166-18-1

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N,N-dimethyl-6-phenyl-11H-pyrido[2,3-b][1,4]benzodiazepine-11-propanamine fumarate
• 英文别名: Tampramine fumarate；(E)-but-2-enedioic acid;N,N-dimethyl-3-(6-phenylpyrido[2,3-b][1,4]benzodiazepin-11-yl)propan-1-amine
• CAS: 83166-18-1
• 化学式: C₄H₄O₄*C₂₃H₂₄N₄
• 分子量: 472.544
• InChiKey: USQAILMOWHOBTK-WLHGVMLRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.37
• 重原子数：
  35
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  106
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  [2-[[3-(dimethylamino)propyl](3-nitro-2-pyridinyl)amino]phenyl]phenylmethanone 、 富马酸 在 sodium hydroxide 、 溶剂黄146 、 锌 作用下， 生成 N,N-dimethyl-6-phenyl-11H-pyrido[2,3-b][1,4]benzodiazepine-11-propanamine fumarate
  参考文献：
  名称：

  [2-[(Nitropyridinyl)amino]phenyl]arymethanones

  摘要：

  [2-[(硝基吡啶基)氨基]苯基]芳基甲酮作为化学中间体和/或具有抗抑郁活性，其化学式为：##STR1## 其中：B为羰基、硫代甲基、缩酮或硫代缩酮，R为氢或-烷基-Q，Q为氢、-NR^1R^2或卤素，在制备吡啶并[1,4]苯并二氮杂环己烷类化合物的过程中被揭示。

  公开号：

  US04480100A1

文献信息

• Aryl substituted pyrido[1,4]benzodiazepines and their use as
  申请人：A. H. Robins Company, Incorporated

  公开号：US04556667A1

  公开（公告）日：1985-12-03

  Novel [2-[(aminopyridinyl)amino]phenyl]arylmethanones and their thioxomethyl, ketal or thioketal analogs of the formula: ##STR1## wherein; R is selected from the group consisting of hydrogen, loweralkyl, --alk.sup.1 --halo, --alk.sup.1 --NR.sup.1 --NR.sup.1 R.sup.2 or --alk.sup.1 --N.dbd.CH--OC.sub.2 H.sub.5 ; R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen, loweralkyl, --C(O)O-loweralkyl or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom may form a heterocyclic residue selected from the group consisting of 1-piperidinyl, 1-phthalimido, 1-pyrrolidinyl, 4-morpholinyl, 1-piperazinyl and 4-substituted-1-piperazinyl; B is selected from carbonyl, thioxomethyl, ketal or thioketal; Ar is selected from the group consisting of 2, 3 and 4-pyridinyl, 2 or 3-thienyl, phenyl or phenyl substituted by 1 to 3 radicals selected from halo, loweralkyl, loweralkoxy, trifluoromethyl or nitro and may be the same of different; alk.sup.1 is a straight or branched hydrocarbon chain containing 1-8 carbon atoms; Z is selected from the group consisting of hydrogen, halogen, loweralkyl, loweralkoxy, hydroxy or nitro; Y is selected from the group consisting of hydrogen or 1-2 radicals selected from loweralkyl, loweralkoxy or hydroxy and may be the same of different, and the acid addition salts thereof. These compounds are intermediates in the preparation of novel aryl substituted pyrido[1,4]benzodiazepines having antidepression activity. Some of these intermediates are useful in treating depression.

  新型[2-[(氨基吡啶基)氨基]苯基]芳基甲酮及其硫羰甲基、缩酮或硫代缩酮类似物，其通式为：##STR1## 其中：R选自氢、低级烷基、--alk^1--卤素、--alk^1--NR^1--NR^1R^2或--alk^1--N=CH--OC2H5；R^1和R^2选自氢、低级烷基、--C(O)O-低级烷基，或者R^1和R^2与相邻的氮原子一起可以形成选自1-哌啶基、1-邻苯二甲酰亚胺、1-吡咯烷基、4-吗啉基、1-哌嗪基和4-取代的1-哌嗪基的杂环残基；B选自羰基、硫羰甲基、缩酮或硫代缩酮；Ar选自2、3和4-吡啶基、2或3-噻吩基、苯基或被1至3个选自卤素、低级烷基、低级烷氧基、三氟甲基或硝基的取代基取代的苯基，这些取代基可以相同或不同；alk^1是含有1-8个碳原子的直链或支链烃链；Z选自氢、卤素、低级烷基、低级烷氧基、羟基或硝基；Y选自氢或1-2个选自低级烷基、低级烷氧基或羟基的取代基，这些取代基可以相同或不同，以及它们的酸加成盐。这些化合物是制备具有抗抑郁活性的新型芳基取代的吡啶并[1,4]苯并二氮杂卓的中间体。其中一些中间体可用于治疗抑郁症。
• [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。
• 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。
• Aryl substituted pyrido[1,4]benzodiazepines
  申请人：A. H. Robins Company, Inc.

  公开号：US04447361A1

  公开（公告）日：1984-05-08

  Pyrido[1,4]benzodiazepines having antidepressant activity of the formula ##STR1## wherein Ar is 2, 3 and 4-pyridinyl, 2 or 3-thienyl, phenyl or a substituted phenyl; R is hydrogen, loweralkyl or an amine on the end of a hydrocarbon chain; Z is hydrogen, halogen, trifluoromethyl, loweralkyl, loweralkoxy, hydroxy or nitro; and Y is hydrogen, loweralkyl, loweralkoxy or hydroxy; and the pharmaceutical salts are prepared from [2-[(aminopyridinyl)amino]phenyl]arylmethanones which also have antidepressant activity.

  具有抗抑郁活性的吡啶并[1,4]苯二氮卓类化合物，其结构式如##STR1##所示，其中Ar为2、3和4-吡啶基，2或3-噻吩基，苯基或取代苯基；R为氢、低级烷基或位于碳氢链末端的胺；Z为氢、卤素、三氟甲基、低级烷基、低级烷氧基、羟基或硝基；Y为氢、低级烷基、低级烷氧基或羟基；以及由[2-[(氨基吡啶基)氨基]苯基]芳基甲酮制备的药用盐，这些化合物也具有抗抑郁活性。
• Aryl substituted pyrido[1,4]benzodiazepines for treatment of depression
  申请人：A. H. Robins Company, Incorporated

  公开号：US04495183A1

  公开（公告）日：1985-01-22

  Pyrido[1,4]benzodiazepines having antidepressant activity of the formula ##STR1## wherein Ar is 2, 3 and 4-pyridinyl, 2 or 3-thienyl, phenyl or a substituted phenyl; R is hydrogen, loweralkyl or an amine on the end of a hydrocarbon chain; Z is hydrogen, halogen, trifluoromethyl, loweralkyl, lower-alkoxy, hydroxy or nitro; and Y is hydrogen, loweralkyl, loweralkoxy or hydroxy; and the pharmaceutical salts are prepared from [2-[(aminopyridinyl)amino]phenyl]arylmethanones which also have antidepressant activity.

  具有抗抑郁活性的吡啶并[1,4]苯二氮卓类化合物，其结构式如上所示，其中Ar为2,3和4-吡啶基、2或3-噻吩基、苯基或取代苯基；R为氢、低级烷基或位于烃链末端的胺；Z为氢、卤素、三氟甲基、低级烷基、低级烷氧基、羟基或硝基；Y为氢、低级烷基、低级烷氧基或羟基；以及由[2-[(氨基吡啶基)氨基]苯基]芳基甲酮制备的药用盐，这些化合物也具有抗抑郁活性。