PYRIMIDINOXYALKYLPIPERAZINES AND THEIR THERAPEUTIC USE
    3.
    发明申请
    PYRIMIDINOXYALKYLPIPERAZINES AND THEIR THERAPEUTIC USE 审中-公开
    吡咯烷酮氧基丙烯酸酯及其治疗用途

    公开(公告)号:WO2003002543A1

    公开(公告)日:2003-01-09

    申请号:PCT/EP2002/007183

    申请日:2002-06-28

    CPC classification number: C07D239/34

    Abstract: Pyrimidinoxyalkylpiperazines of the formula (I) in which n represents an integer from 2 to 6, R 1 represents H, C 1 -C 6 -alkyl or phenyl ( C 1 -C 6 )-alkyl in which the phenyl radical can be substituted by one or more substituents selected from C 1 -C 6 -alkyl and C 1 -C 6 -alkoxy, R 2 represents H, C 1 -C 4 -alkyl, OH, C 1 -C 6 -alkoxy, NH 2 or C 1 -C 6 -halogenoalkyl, R 3 and R 4 , independently of each other, represent H, C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 1 -C 6 -halogenoalkyl, pyrrolyl or phenyl, which latter can be substituted by one or more substituents selected from C 1 -C 6 -alkyl, C 1 -C 6 -hydroxyalkyl, C 1 -C 6 -alkoxy, OH, halogen or C 1 -C 6 -halogenoalkyl, phenyl, cyano or nitro. The compounds can be used for treating diseases which respond to modulation of the dopamine D 3 receptor and are characterized by a high degree of bioavailability.

    Abstract translation: 式(I)的嘧啶基亚烷基哌嗪,其中n表示2至6的整数,R 1表示H,C 1 -C 6 - 烷基或苯基(C 1 -C 6) - 烷基,其中苯基可以被一个或多个选自以下的取代基取代 C 1 -C 6烷基和C 1 -C 6烷氧基,R 2表示H,C 1 -C 4 - 烷基,OH,C 1 -C 6 - 烷氧基,NH 2或C 1 -C 6 - 卤代烷基,R 3和R 4彼此独立地表示H ,C 1 -C 6 - 烷基,C 1 -C 6 - 羟基烷基,C 1 -C 6 - 卤代烷基,吡咯基或苯基,后者可以被一个或多个选自C 1 -C 6烷基,C 1 -C 6羟基烷基,C 1 -C 6 - 烷氧基,OH,卤素或C 1 -C 6 - 卤代烷基,苯基,氰基或硝基。 该化合物可用于治疗对多巴胺D3受体的调节作出反应的疾病,其特征在于高度的生物利用度。

    TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
    6.
    发明申请
    TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 审中-公开
    适用于治疗多巴胺D3受体调节症状的三唑化合物

    公开(公告)号:WO2004108706A1

    公开(公告)日:2004-12-16

    申请号:PCT/EP2004/006139

    申请日:2004-06-07

    CPC classification number: C07D403/12

    Abstract: The invention relates to triazole compounds of the general formula I wherein R 1 is hydrogen or methyl, and R 2 is C 3 -C 4 alkyl or C 1 -C 2 fluoroalkyl, as well as the physiologically tolerated acid addition salts of these compounds. The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula (I) and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D 3 receptor antagonists or dopamine D 3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula (I) to a subject in need thereof.

    Abstract translation: 本发明涉及通式Ⅰ的三唑化合物,其中R 1为氢或甲基,R 2为C 3 -C 4烷基或C 1 -C 2氟烷基,以及这些化合物的生理上耐受的酸加成盐。 本发明还涉及包含至少一种式(I)的三唑化合物和/或至少一种生理上耐受的酸加成盐的药物组合物,还涉及治疗有益于多巴胺D3受体拮抗剂的病症的方法 或多巴胺三角体,所述方法包括向有需要的受试者施用有效量的至少一种式(I)的三唑化合物或生理学上耐受的酸加成盐。

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