2-amino-3-cyano-7,7-dimethyl-4-(2,4,6-trimethylphenyl)-5-oxo-5,6,7,8-tetrahydro-4H-1-benzopyran | 311773-22-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-amino-3-cyano-7,7-dimethyl-4-(2,4,6-trimethylphenyl)-5-oxo-5,6,7,8-tetrahydro-4H-1-benzopyran
• 英文别名: 2-amino-4-mesityl-7,7-dimethyl-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile；2-amino-7,7-dimethyl-5-oxo-4-(2,4,6-trimethylphenyl)-6,8-dihydro-4H-chromene-3-carbonitrile
• CAS: 311773-22-5
• 化学式: C₂₁H₂₄N₂O₂
• 分子量: 336.434
• InChiKey: LLJKCXGCZNAIPT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  25
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  76.1
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• SUBSTITUTED 5-OXO-5, 6, 7, 8-TETRAHYDRO-4H-1-BENZOPYRANS
  申请人：——

  公开号：US20040097581A1

  公开（公告）日：2004-05-20

  Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I: 1 or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is NH 2 , NHR, and NHCOR; Z is 0 and S; and R 1 , R 2 , R 3 , R 4 , and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula I.

  本发明涉及一种用于治疗对AMPA受体正性调节有反应的动物所患疾病的方法，包括向需要该治疗的动物施用公式I中的化合物1或其药学上可接受的盐或前药，其中：Y是NH2，NHR和NHCOR; Z为0和S; 而R1，R2，R3，R4和X在此被定义。这些化合物可用作认知增强剂，用于治疗神经退行性疾病，包括阿尔茨海默病、肌萎缩性侧索硬化症、亨廷顿病、帕金森病、艾滋病相关痴呆和唐氏综合征，以及用于治疗精神分裂症和肌阵挛症。还公开了用于治疗对AMPA受体正性调节有反应的疾病的药物组合物，以及公式I的新化合物。
• SUBSTITUTED 5-OXO-5,6,7,8-TETRAHYDRO-4H-1-BENZOPYRANS AND BENZOTHIOPYRANS AND THE USE THEREOF AS POTENTIATORS OF AMPA
  申请人：Euro-Celtique S.A.

  公开号：EP1189896A1

  公开（公告）日：2002-03-27
• US6680332B1
  申请人：——

  公开号：US6680332B1

  公开（公告）日：2004-01-20
• US6800657B2
  申请人：——

  公开号：US6800657B2

  公开（公告）日：2004-10-05
• [EN] SUBSTITUTED 5-OXO-5,6,7,8-TETRAHYDRO-4H-1-BENZOPYRANS AND BENZOTHIOPYRANS AND THE USE THEREOF AS POTENTIATORS OF AMPA<br/>[FR] 5-OXO-5,6,7,8-TETRAHYDRO-4H-1-BENZOPYRANNES ET BENZOTHIOPYRANNES SUBSTITUES ET UTILISATION DE CES SUBSTANCES COMME POTENTIALISATEURS DE AMPA
  申请人：COCENSYS INC

  公开号：WO2000075123A1

  公开（公告）日：2000-12-14

  Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula (I): or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is NH2, NHR, and NHCOR; Z is O and S; and R1, R2, R3, R4, and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula (I).