[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.