| 摘要 |
<p>The invention provides 2,3,4,5-tetrahydro-1H-3-benzazepines of general formula (I) wherein: R1 is hydrogen, halogen, C1-C4 alkyl, or CF3; R2 is hydrogen, methyl, or lower alkenyl of 3-5 carbon atoms; R3 and R4 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane or cyclohexane ring and R5 is hydrogen or R4 and R5 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane or cyclohexane ring and R3 is hydrogen; R6 is hydrogen, halogen, CF3, CN, NO2 or NH2; R7 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.</p> |
