SUBSTITUTED 1,2,3,4-TETRAHYDRONAPHTHALENE DERIVATIVES
    4.
    发明公开
    SUBSTITUTED 1,2,3,4-TETRAHYDRONAPHTHALENE DERIVATIVES 失效
    替代物1,2,3,4-四氢萘基衍生物

    公开(公告)号:EP0888319A1

    公开(公告)日:1999-01-07

    申请号:EP97914727.0

    申请日:1997-03-20

    申请人: Astra Aktiebolag

    摘要: New piperidinyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having formula (I) wherein X is N or CH; Y is NR2CH2, CH2-NR2, NR2-CO, CO-NR2 or NR2SO2; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, where aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted; n is 0-4; as (R)-enantiomer, (S)-enantiomer or a racemate in the form of the free base or a pharmaceutically acceptable salt or hydrate thereof; a pharmaceutical formulation containing the compounds, use of the compounds in the treatment of 5-hydroxytryptamine mediated disorders, processes for the preparation of the compounds and intermediates for the preparation of the compounds.

    摘要翻译: 具有肟基X的新的哌啶基或哌嗪基 - 取代-1,2,3,4-四氢萘衍生物为N或CH; Y为NR2CH2,CH2-NR2,NR2-CO,CO-NR2或NR2SO2; R1为H,C1- C6烷基或C3-C6环烷基; R3是C1-C6烷基,C3-C6环烷基或(CH2)n-芳基,其中芳基是苯基或含有一个或两个选自N,O和S的杂原子的杂芳环, 作为(R) - 对映异构体,(S) - 对映异构体或游离碱形式的外消旋物或其药学上可接受的盐或水合物; n为0-4; 含有这些化合物的药物制剂,该化合物在治疗5-羟色胺介导的病症中的用途,制备化合物的方法和用于制备化合物的中间体。