(+/-)1-(3-Methyl-4-amino-phenyl)-4-methyl-7,8-methylenedioxy-4,5-dihydro-3-acetyl-2,3-benzodiazepine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 英文名称: (+/-)1-(3-Methyl-4-amino-phenyl)-4-methyl-7,8-methylenedioxy-4,5-dihydro-3-acetyl-2,3-benzodiazepine
• 英文别名: 1-[5-(4-amino-3-methylphenyl)-8-methyl-8,9-dihydro-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-7-yl]ethanone
• 化学式: C₂₀H₂₁N₃O₃
• 分子量: 351.4
• InChiKey: UCBJVNOYWSKEPO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  26
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  77.2
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• OPTICAL ISOMERS OF DIHYDRO-2,3-BENZODIAZEPINES AND THEIR STEREOSELECTIVE SYNTHESIS
  申请人：Ling Istvan

  公开号：US20090233913A1

  公开（公告）日：2009-09-17

  The present invention relates to dihydro-2,3-benzodiazepine compounds of high enantiomeric purity according to the general formula (I), which contain an asymmetric centre at the position 4 of the dihydro-2,3-benzodiazepine compound, and the preparation thereof and the used intermediates as well. These compounds have anti-convulsiveA muscle relaxant and neuroprotective effect due their non-competitive AMPA antagonistic properties.

  本发明涉及高对映纯度的二氢-2,3-苯并二氮平化合物，其通式为(I)，其中在二氢-2,3-苯并二氮平化合物的4位含有不对称中心，以及其制备方法和用作中间体。这些化合物具有抗惊厥、肌肉松弛和神经保护作用，因为它们具有非竞争性AMPA拮抗作用。
• 2,3-BENZODIAZEPINE DERIVATIVES
  申请人：Egis Gyogyszergyar Rt.

  公开号：EP1200442B8

  公开（公告）日：2003-08-20
• US7053082B1
  申请人：——

  公开号：US7053082B1

  公开（公告）日：2006-05-30
• [EN] NEW 2,3-BENZODIAZEPINE DERIVATIVES<br/>[FR] NOUVEAUX DERIVES DE 2,3-BENZODIAZEPINES
  申请人：EGYT GYOGYSZERVEGYESZETI GYAR

  公开号：WO2001004122A2

  公开（公告）日：2001-01-18

  The invention relates to new 2,3-benzodiazepine derivatives of general Formula (I), (wherein R1 stands for methyl, formyl, carboxy, cyano, -CH=NOH, -CH=NNHCONH¿2? or -NR?5R6¿, wherein R?5 and R6¿ independently from each other represent hydrogen or lower alkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R2 is nitro or amino; R3 stands for hydrogen, lower alkanoyl or CO-NR7R8, wherein R?7 and R8¿ independently from each other stand for hydrogen, lower alkoxy, lower alkyl or lower cycloalkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R4 is hydrogen or lower alkyl; the dotted lines have the following meaning: if R?3 and R4¿ are not present, the bond between positions C?8 and C9¿ is a single bond and the bond between positions C?8 and N7¿ is a double bond; if R?3 and R4¿ are present, the bonds between positions C?8 and C9¿ and between position C?8 and N7¿ are single bonds; and if R3 is present and R4 is missing, the bond between positions C?8 and C9¿ is a double bond and the bond between positions C?8 and N7¿ is a single bond) and salts thereof. The invention compounds have neuroprotective effect.
• [EN] OPTICAL ISOMERS OF DIHYDRO-2,3-BENZODIAZEPINES AND THEIR STEREOSELECTIVE SYNTHESIS<br/>[FR] ISOMERES OPTIQUES DE DIHYDRO-2,3-BENZODIAZEPINES ET LEUR SYNTHESE STEREOSELECTIVE
  申请人：EGIS GYOGYSZERGYAR NYRT

  公开号：WO2007077469A1

  公开（公告）日：2007-07-12

  [EN] The present invention relates to dihydro-2,3-benzodiazepine compounds of high enantiomeric purity according to the general formula (I), which contain an asymmetric centre at the position 4 of the dihydro-2,3-benzodiazepine compound, and the preparation thereof and the used intermediates as well. These compounds have anti-convulsiveA muscle relaxant and neuroprotective effect due their non-competitive AMPA antagonistic properties.
  [FR] La présente invention concerne des composés de dihydro-2,3-benzodiazépine de pureté énantiomérique élevée selon la formule générale (I), qui contiennent un centre asymétrique à la position 4 du composé de dihydro-2,3-benzodiazépine, et leur préparation ainsi que les intermédiaires utilisés. Ces composés ont un effet myorelaxant anticonvulsif neuroprotecteur en raison de leurs propriétés antagonistes d'AMPA non compétitives.