| 摘要 |
The invention provides 2,3,4,5-tetrahydro-1H-3-benzazepines of general formula (I) wherein: R<1> is hydrogen, halogen, C1-C4 alkyl, or CF3; R<2> is hydrogen, methyl, or lower alkenyl of 3-5 carbon atoms; R<3> and R<4> together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane or cyclohexane ring and R<5> is hydrogen or R<4> and R<5> together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane or cyclohexane ring and R<3> is hydrogen; R<6> is hydrogen, halogen, CF3, CN, NO2 or NH2; R<7> is hydrogen, halogen, CF3, 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.
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