美西平 | 27432-00-4

• 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: 美西平
• 中文别名: 麦泽平
• 英文名称: mezepine
• 英文别名: 3-(6,11-dihydrobenzo[c][1]benzazepin-5-yl)-N-methylpropan-1-amine
• CAS: 27432-00-4
• 化学式: C₁₈H₂₂N₂
• 分子量: 266.386
• InChiKey: UVWYAZFZHPZJOT-UHFFFAOYSA-N

物化性质

• 沸点：
  425.4±45.0 °C(Predicted)
• 密度：
  1.047±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  15.3
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933990090

文献信息

• BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS AND PRODRUGS THEREOF
  申请人：Bristol-Myers Squibb Company

  公开号：US20140087992A1

  公开（公告）日：2014-03-27

  Disclosed are compounds of Formula (I) and/or salts thereof: wherein R 1 is —CH 2 CH 2 CF 3 ; R 2 is —CH 2 CH 2 CF 3 or —CH 2 CH 2 CH 2 CF 3 ; R 3 is H, —CH 3 , or R x ; R 4 is H or R y ; Ring A is phenyl or pyridinyl; and R x , R y , R a , R b , y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.

  公开了公式(I)的化合物及/或其盐：其中R1为-CH2CH2CF3；R2为-CH2CH2CF3或-CH2CH2CH2CF3；R3为H，-CH3或Rx；R4为H或Ry；环A为苯基或吡啶基；Rx，Ry，Ra，Rb，y和z在此定义。还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物。这些化合物在治疗、预防或减缓多种治疗领域，如癌症的疾病或病症进展方面非常有用，或者作为这些化合物的前药。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• FLUOROALKYL DIBENZOAZEPINONE COMPOUNDS
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：US20150218104A1

  公开（公告）日：2015-08-06

  Disclosed are compounds of Formula (I): wherein R 1 is CH 2 CH2CF 3 or CH 2 CH2CH 3 ; R2 is CH 2 CH 2 CF 3 , CH 2 CH 2 CH 3 , CH 2 (cyclopropyl), phenyl, or; R3 is H; R a , R b , y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

  本发明涉及化合物的公式(I)： 其中R1为CH2CH2CF3或CH2CH2CH3；R2为CH2CH2CF3，CH2CH2CH3，CH2（环丙基），苯基或；R3为H；Ra，Rb，y和z在此定义。还公开了使用这种化合物来抑制Notch受体的方法以及包含这种化合物的制药组合物。这些化合物在治疗、预防或减缓多种治疗领域中的疾病或障碍方面非常有用，例如癌症。
• PRODRUGS OF 1,4-BENZODIAZEPINONE COMPOUNDS
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：US20150232491A1

  公开（公告）日：2015-08-20

  Disclosed are compounds of Formula (I) and salts thereof, wherein: a) R 1 is H or CH 3 , and R 2 is R y ; or b) R 1 is Rx and R 2 is H; wherein R x and R y are disclosed herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are prodrugs of compounds that are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

  本文公开了式（I）的化合物及其盐，其中：a）R1为H或CH3，R2为Ry；或b）R1为Rx且R2为H；其中Rx和Ry在此被公开。还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的制药组合物。这些化合物是有用于治疗、预防或减缓多种治疗领域（如癌症）疾病或紊乱的化合物的前药。
• TRICYCLIC HETEROCYCLE COMPOUNDS
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：US20150246930A1

  公开（公告）日：2015-09-03

  Disclosed are compounds of Formula (I), wherein: X is O or —NR 3 ; R 1 is —CH 2 CH 2 CH 3 , —CH 2 CF 3 , —CH 2 CH 2 CF 3 , —CH 2 CF 2 CH 3 , —CH 2 CH 2 CH 2 CF 3 , —CH 2 CH 2 CF 2 CH 3 , —CH 2 CH(CH 3 )CF 3 , —CH 2 CH 2 CH 2 F, or CH 2 (cyclopropyl); R 2 is —CH 2 CH 2 CH 3 , —CH 2 CF 3 , —CH 2 CH 2 CF 3 , —CH 2 CF 2 CH 3 , —CH 2 CH 2 CH 2 CF 3 , —CH 2 CH 2 CH 2 F, —CH 2 CH(CH 3 )CF 3 , CH 2 CH 2 CF 2 CH 3 , —CH 2 (cyclopropyl), —CH(CH 3 )(cyclopropyl), phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, pyridinyl, formula (i), formula (ii), formula (iii), formula (iv) or formula (v); Ring A is phenyl or pyridinyl; and R 3 , R a , R b , R c , y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

  本发明涉及化合物（I）的公式，其中：X是O或—NR3; R1是—CH2CH2CH3，—CH2CF3，—CH2CH2CF3，—CH2CF2CH3，—CH2CH2CH2CF3，—CH2CH2CF2CH3，—CH2CH(CH3)CF3，—CH2CH2CH2F或CH2（环丙烷）; R2是—CH2CH2CH3，—CH2CF3，—CH2CH2CF3，—CH2CF2CH3，—CH2CH2CH2CF3，—CH2CH2CH2F，—CH2CH(CH3)CF3，CH2CH2CF2CH3，—CH2（环丙烷），—CH（CH3）（环丙烷），苯基，氟苯基，氯苯基，三氟苯基，甲基异噁唑基，吡啶基，公式（i），公式（ii），公式（iii），公式（iv）或公式（v）; 环A是苯基或吡啶基; R3、Ra、Rb、Rc、y和z在此定义。本发明还涉及使用这些化合物来抑制Notch受体的方法，以及包含这些化合物的制药组合物。这些化合物在治疗、预防或减缓各种治疗领域的疾病或障碍方面非常有用，例如癌症。