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    2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives having an effect on the C.N.S. and the heart
    10.
    发明授权
    2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives having an effect on the C.N.S. and the heart 失效
    2-（1,2,4-三唑-1-基）-1,3,4-噻二唑衍生物对C.N.S.有影响。 和心脏

    公开(公告)号：US06191152B1

    公开(公告)日：2001-02-20

    申请号：US09341362

    申请日：1999-09-20

    申请人： József Reiter ,  József Barkóczy ,  Gábor Berecz ,  Gyula Simig ,  András Egyed ,  Katalin Ivanicsné Megyeri ,  Sándor Drabant ,  Szabolcs Kertész ,  Anikó Miklósné Kovács ,  Ildikó Nagyné Gyönös ,  Mária Szécseyné Hegedüs ,  Gábor Szénási ,  János Wellmann ,  Katalin Pallagi ,  Éva Schmidt ,  Károly Tihanyi ,  Péter Trinka ,  Margit Csörgö

    发明人： József Reiter ,  József Barkóczy ,  Gábor Berecz ,  Gyula Simig ,  András Egyed ,  Katalin Ivanicsné Megyeri ,  Sándor Drabant ,  Szabolcs Kertész ,  Anikó Miklósné Kovács ,  Ildikó Nagyné Gyönös ,  Mária Szécseyné Hegedüs ,  Gábor Szénási ,  János Wellmann ,  Katalin Pallagi ,  Éva Schmidt ,  Károly Tihanyi ,  Péter Trinka ,  Margit Csörgö

    IPC分类号： C07D41704

    CPC分类号： C07D417/04

    摘要： The invention refers to novel 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives of formula (I) having an influence on the heart and the central nervous system, furthermore pharmaceutical compositions containing the above derivatives, and a process for the preparations of the novel compounds. In formula (I) R1 represents a hydrogen atom, a C1-4 alkyl group of a phenyl group optionally substituted by 1 to 3 substituents selected from the group defined in the application, Z stands for a hydrogen atom of a C1-4 alkoxy group, R0 means a group of the formula Alk—NR4R5 wherein Alk is a C1-6 straight of branched chain alkylene group, R4 and R5 represent, independently, a hydrogen atom, a C2-6 alkenyl group, a C1-8 alkyl group optionally substituted by a substituent selected from the group defined in the application or R4 and R5 form together with the adjacent nitrogen atom and optionally with one or more further nitrogen and/or oxygen and/or sulfur atom(s) a 5- to 10-membered saturated heterocyclic group, optionally substituted, one of R2 and R3 is an amino group, while the other stands for an amino group of a 5- to 10-membered saturated heterocyclic group containing one or more nitrogen and/or oxygen and/or sulfur atom(s) and being linked through its nitrogen atom, said heterocyclic group being optionally substituted or the latter one of R2 and R3 means a group of formula —SR wherein R represents a C1-8 alkyl group, a C2-6 alkenyl group or a C2-6 alkinyl group, wherein the alkyl group is optionally substituted by a phenyl group of a halophenyl group, and optionally one or both amino group(s) is/are substituted by 1 of 2 substituent(s) selected from the group consisting of a C1-6 alkyl group, a C2-6 alkenyl group, a phenyl(C1-4 alkyl) group or a halophenyl-(C1-4 alkyl) group.

    摘要翻译： 本发明涉及对心脏和中枢神经系统有影响的式（I）的新的2-（1,2,4-三唑-1-基）-1,3,4-噻二唑衍生物，此外还含有 上述衍生物，以及新型化合物的制备方法。 在式（I）中，R 1表示氢原子，任选被1至3个选自本申请所定义的基团的取代基取代的苯基的C 1-4烷基，Z表示C 1-4烷氧基的氢原子 R 0表示式Alk-NR4R5的基团，其中Alk是支链亚烷基的直链的C1-6，R4和R5独立地表示氢原子，C2-6烯基，C1-8烷基， 被选自本申请中所定义的基团或R4和R5形式的取代基与相邻的氮原子一起取代，并且任选地与一个或多个另外的氮和/或氧和/或硫原子一起形成5-至10-元 饱和杂环基，任选取代的，R 2和R 3中的一个是氨基，而另一个代表含有一个或多个氮和/或氧和/或硫原子的5至10元饱和杂环基的氨基 并且通过其氮原子连接，所述杂环 任选地被取代，或者R 2和R 3中的后一个表示式-SR的基团，其中R表示C 1-8烷基，C 2-6烯基或C 2-6炔基，其中烷基是任选的 被卤代苯基的苯基取代，并且任选地一个或两个氨基被2个选自以下的取代基取代：C 1-6烷基，C 2-6烯基 基团，苯基（C 1-4烷基）基团或卤代苯基 - （C 1-4烷基）基团。