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    • 7. 发明申请
    • 3-[(1,2,3,4-TETRAHYDROISOQUINOLINE-2-YL)METHYL]-8-AZABICYCLO[3.2.1]OCTANE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS
    • 3 - [(1,2,3,4-四氢喹啉-2-基)甲基] -8-亚氨基] [3.2.1]月桂衍生物,其制备及其在治疗中的应用
    • WO1997038998A1
    • 1997-10-23
    • PCT/FR1997000634
    • 1997-04-10
    • SYNTHELABOSEVRIN, MireilleMARABOUT, BenoitGEORGE, PascalMERLY, Jean-Pierre
    • SYNTHELABO
    • C07D451/02
    • C07D451/02
    • Compounds of general formula (I) in which each of R1, R2 and R3 represents a hydrogen or halogen atom or a hydroxy, alkyl or alkoxy group, R4 represents a hydrogen or halogen atom or an alkyl, 2-methoxyethoxy, alkoxy, cycloalkylmethoxy or phenylmethoxy group, or R3 and R4 together form a methylenedioxy group, Z represents oxygen or two hydrogen atoms and R represents an ethoxy group when Z represents oxygen, or represents a phenyl group optionally substituted by one or more halogen atoms or alkyl, alkoxy or amino groups. The compounds have a strong affinity for dopamine receptors of D2 and D3 type and for serotonin receptors of 5-HT1A and 5-HT2 type and are mixed ligands. Other compounds have a strong affinity for the dopamine receptors of D3 type and a weak affinity for the dopamine receptors of D2 type and serotonin receptors of 5-HT1A and 5-HT2 and are therefore selective and specific ligands.
    • R 1,R 2和R 3各自表示氢或卤素原子或羟基,烷基或烷氧基的通式(I)的化合物,R 4表示氢或卤素原子或烷基,2-甲氧基乙氧基,烷氧基,环烷基甲氧基或 苯基甲氧基或R3和R4一起形成亚甲二氧基,Z表示氧或两个氢原子,当Z表示氧时R表示乙氧基,或表示任选被一个或多个卤素原子取代的苯基或烷基,烷氧基或氨基 组。 这些化合物对D2和D3型的多巴胺受体和5-HT1A和5-HT2型的血清素受体具有强烈的亲合力,并且是混合配体。 其他化合物对D3型多巴胺受体具有强亲和力,对5型HT1A和5-HT2的D2型和5-羟色胺受体的多巴胺受体具有弱亲和性,因此是选择性和特异性配体。