9-chloro-5-(2,3-dihydro-1H-inden-5-yl)-3-methyl-1,2,4,5-tetrahydro-3-benzazepine-7,8-diol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: 9-chloro-5-(2,3-dihydro-1H-inden-5-yl)-3-methyl-1,2,4,5-tetrahydro-3-benzazepine-7,8-diol
• 化学式: C₂₀H₂₂ClNO₂
• 分子量: 343.8
• InChiKey: UUTNTBWYKFDEDO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  24
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  43.7
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• DOPAMINE D1 RECEPTOR AGONIST COMPOUNDS
  申请人：CeNeS Limited

  公开号：EP1157009A1

  公开（公告）日：2001-11-28
• [EN] DOPAMINE D1 RECEPTOR AGONIST COMPOUNDS<br/>[FR] COMPOSES AGONISTES DU RECEPTEUR D1 DE DOPAMINE
  申请人：CENES LTD

  公开号：WO2000049000A1

  公开（公告）日：2000-08-24

  The invention provides 2,3,4,5-tetrahydro-1H-3-benzazepines of general formula (I) wherein: R1 is hydrogen, halogen, C¿1?-C4 alkyl, or CF3; R?2¿ is hydrogen, methyl, or lower alkenyl of 3-5 carbon atoms; R?3 and R4¿ together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane or cyclohexane ring and R5 is hydrogen or R?4 and R5¿ together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane or cyclohexane ring and R3 is hydrogen; R6 is hydrogen, halogen, CF¿3?, CN, NO2 or NH2; R?7¿ is hydrogen, halogen, CF¿3?, CN, NO2 or NH2. The specific combination of substituents: R1 = H, R2 = H and R4 and R5 together forming a cyclohexane ring is excluded, namely 1-(5,6,7,8-tetrahydronaphthalen-2-yl)-2,3,4,5-tetrahydro-1H-benzol[d]azepine-7,8-diol. The compounds of the invention provide therapeutic agents that selectively interact positively with postsynaptic dopamine D1 receptors in the striatum, directly or in-directly (termed dopamine D1 agonists) and are particularly valuable as anti-Parkinsonian agents.
• [EN] DOPAMINE D1 RECEPTOR AGONIST PRO-DRUG COMPOUNDS & DERIVATIVES<br/>[FR] COMPOSES DE PRO-MEDICAMENT D'AGONISTE DU RECEPTEUR D1 DE LA DOPAMINE ET DERIVES DE CEUX-CI
  申请人：SHIRE PHARMACEUTICAL DEV LTD

  公开号：WO2003053936A1

  公开（公告）日：2003-07-03

  The invention provides a pro-drug compound of Formula (A): wherein: R1 = alkanoyl (2-6 carbon atoms), benzoyl, 2-methylbenzoyl, 3-methylbenzoyl, 4-methylbenzoyl, 2-methoxybenzoyl, 3-methoxybenzoyl, 4-methoxybenzoyl, thiophene-2-carbonyl, thiophene-3-carbonyl, phenylacetyl, 3-phenylpropanoyl, 3-phenylacryloyl; R2 = H, halogen, cyano, nitro, alkyl (1-4 carbon atoms), CF3, CONHR (R = H, alkyl (1-4 carbon atoms)); R3 = H, alkyl (1-4 carbon atoms), allyl; R4 and R5 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane, benzene, cyclohexane ring, or R5 = hydrogen and R5 and R6 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane, benzene, cyclohexane ring; R7 and R8 can independently be hydrogen, halogen, CF3, CN, NO2 or NH2; or a mono -hydroxy benzazepine derivative of Formula (B): wherein: R1 = H, halogen, cyano, nitro, alkyl (1-4 carbon atoms), CF3, CONHR (R = H, alkyl (1-4 carbon atoms)); R2 = H, alkyl (1-4 carbon atoms), allyl; R3 and R4 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane, benzene, cyclohexane ring, or R3 = hydrogen and R4 and R5 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane, benzene, cyclohexane ring; R6 and R7 can independently be hydrogen, halogen, CF3, CN, NO2 or NH2; R8 = hydrogen, methyl; and a pharmaceutical composition comprising or consisting of said compound or derivative together with a pharmaceutically acceptable excipient or carrier, for treatment of neurodegenerative disease, for example, Parkinson's disease.