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    2-CARBONYLTHIAZOLE DERIVATIVES AND USE OF THE SAME
    4.
    发明公开
    2-CARBONYLTHIAZOLE DERIVATIVES AND USE OF THE SAME 失效
    2-CARBONYLTHIAZOLDERIVATE和IHRE VERWENDUNG

    公开(公告)号：EP0940401A4

    公开(公告)日：2001-04-11

    申请号：EP97940436

    申请日：1997-09-19

    申请人： TAISHO PHARMA CO LTD ,  NIHON NOHYAKU CO LTD

    发明人： NAKAZATO ATSURO ,  KUMAGAI TOSHIHITO ,  CHAKI SHIGEYUKI ,  TOMISAWA KAZUYUKI ,  NAGAMINE MASASHI ,  GOTOH MAKOTO ,  YOSHIDA MASANORI

    IPC分类号： A61K31/425 ,  C07D417/06 ,  A61K31/445

    CPC分类号： C07D417/06

    摘要： 2-Carbonylthiazole derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof (wherein Ar?1 and Ar2¿ represent each phenyl optionally having one or two substituents selected from among halogeno, C¿1-5? alkyl, trifluoromethyl, C1-5 alkoxy and hydroxy or thienyl; R?1¿ represents C¿1-5? alkoxy, hydroxy or amino represented by the formula N(R?3)R4¿ (wherein R?3 and R4¿ represent each hydrogen or C¿1-5? alkyl, or R?3 and R4¿ together with the nitrogen atom to which they are bonded may form pyrrolidino, piperidino, morphorino or piperazino optionally having one to four substituents selected from among C¿1-5? alkyl, C1-5 alkoxy and hydroxy); Y?1-Y2¿ represents CH-CO or C=C(R2) (wherein R2 represents hydrogen or C¿1-5? alkyl); and n is an integer of 1 to 4); drugs comprising the derivatives represented by the above general formula (I) or pharmaceutically acceptable salts thereof; and dopamine D4 receptor antagonists containing as the active ingredient the same. These drugs are useful as preventives and remedies for various diseases in which dopamine D4 receptors participate, for example, schizophrenia, cerebrovascular disorders and problematic behaviors accompanying senile dementia without showing any extrapyramidal disorders as the side effect.

    摘要翻译： （I）表示的2-羰基噻唑衍生物或其药学上可接受的盐（其中Ar 1和Ar 2代表各自任选具有一个或两个选自卤素，C 1-5烷基，三氟甲基， R 5代表C 1-5烷氧基，羟基或由式N（R 3）R 4表示的氨基（其中R 3和R 4各自代表氢或C 1 -5烷基或R 3和R 4与它们所连接的氮原子一起可形成吡咯烷基，哌啶子基，吗啉代或哌嗪子基，其任选地具有一至四个选自C 1-5 - 烷基，C 1-6 - 5烷氧基和羟基）; Y 1 -Y 2'代表CH-CO或C = C（R 2）（其中R 2代表氢或C 1-5-5烷基）;并且n是1至4的整数。 包含由上述通式（I）表示的衍生物或其药学上可接受的盐的药物; 和含有相同作为活性成分的多巴胺D4受体拮抗剂。 这些药物可用作多巴胺D4受体参与的各种疾病的预防和治疗药物，例如精神分裂症，脑血管障碍和伴随老年性痴呆的有问题的行为，而不显示任何锥体外系疾病作为副作用。

    PROCESS FOR PRODUCING BICYCLOCARBOXYLIC ACID DERIVATIVE
    10.
    发明公开
    PROCESS FOR PRODUCING BICYCLOCARBOXYLIC ACID DERIVATIVE 审中-公开
    VERFAHREN ZUR HERSTELLUNG VONBICYCLOCARBONSÄUREDERIVATEN

    公开(公告)号：EP1369408A4

    公开(公告)日：2005-12-28

    申请号：EP02702875

    申请日：2002-03-11

    申请人： TAISHO PHARMA CO LTD

    发明人： NAKAZATO ATSURO ,  KUMAGAI TOSHIHITO ,  SAKAGAMI KAZUNARI

    IPC分类号： C07C51/377 ,  C07C67/327 ,  C07C62/24 ,  C07C69/757

    CPC分类号： C07C51/377 ,  C07C67/327 ,  C07C2602/18 ,  Y02P20/55 ,  C07C62/24 ,  C07C69/757

    摘要： A process for producing a 2-oxobicyclo[3.1.0]hex-3-ene-6-carboxylic acid derivative represented by the formula (I) (wherein R1 represents hydrogen, C¿1-6? alkyl, C3-6 cycloalkyl, C1-6 alkyl substituted by C3-6 cycloalkyl, C1-6 alkyl substituted by optionally substituted phenyl, C1-6 alkyl substituted by C1-6 alkoxy, C1-6 hydroxyalkyl, C1-6 alkyl substituted by C1-6 alkylthio, C1-6 mercaptoalkyl, or optionally substituted phenyl), characterized by reacting a 4-hydroxy-2-oxobicyclo[3.1.0]hexane-6-carboxylic acid derivative represented by the formula (II) (wherein R?1¿ is the same as defined above; and R2 represents hydrogen or a hydroxyl-protecting group) in the presence of an acid or base. Also provided is a process for producing a compound useful in the efficient synthesis of a 2-amino-3-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative.

    摘要翻译： 一种制备式（I）代表的2-氧代双环[3.1.0]己-3-烯-6-羧酸衍生物的方法（式中R1代表氢，C1-6烷基，C3-6环烷基， 被C3-6环烷基取代的C1-6烷基，被任选取代的苯基取代的C1-6烷基，被C1-6烷氧基取代的C1-6烷基，C1-6羟烷基，被C1-6烷硫基取代的C1-6烷基，C1- 6巯基烷基或任选取代的苯基）的方法，其特征在于使式（II）代表的4-羟基-2-氧代双环[3.1.0]己烷-6-羧酸衍生物（其中R1和定义的相同） 以上;并且R 2表示氢或羟基保护基）在酸或碱的存在下进行。 还提供了生产用于有效合成2-氨基-3-氟二环[3.1.0]己烷-2,6-二羧酸衍生物的化合物的方法。