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    2-CARBONYLTHIAZOLE DERIVATIVES AND USE OF THE SAME
    7.
    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。

    4-TETRAHYDROPYRIDYLPYRIMIDINE DERIVATIVES
    10.
    发明公开
    4-TETRAHYDROPYRIDYLPYRIMIDINE DERIVATIVES 失效
    4-四氢吡啶基嘧啶衍生物

    公开(公告)号：EP0976745A4

    公开(公告)日：2001-11-28

    申请号：EP98911002

    申请日：1998-03-25

    申请人： TAISHO PHARMA CO LTD

    发明人： NAKAZATO ATSURO ,  KUMAGAI TOSHIHITO ,  OKUBO TAKETOSHI ,  AIBE IZUMI ,  TANAKA HIDEO ,  CHAKI SHIGEYUKI ,  OKUYAMA SHIGERU ,  TOMISAWA KAZUYUKI

    IPC分类号： A61P25/08 ,  C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  A61K31/505

    CPC分类号： C07D401/04 ,  C07D405/14 ,  C07D409/14

    摘要： 4-Tetrahydropyridylpyrimidine derivatives of general formula (I); and medicinally acceptable salts thereof, wherein Ar is phenyl optionally substituted with one to three groups selected from among halogeno, C1-C5 alkyl, C1-C5 alkoxy and trifluoromethyl, thienyl or furanyl; R1 is hydrogen, C¿1?-C5 alkyl or amino optionally substituted with one or two C1-C5 alkyl groups; R?2 is C¿1-C5 alkyl, C4-C7 cycloalkylalkyl, C2-C5 alkenyl or C2-C5 alkynyl; and X?1, X2 and X3¿ are each independently hydrogen, halogeno, C¿1?-C5 alkyl, C1-C5 alkoxy, C1-C5 alkylthio or amino optionally substituted with one or two C1-C5 alkyl groups. These compounds are efficacious against diseases in which CRF is believed to be concerned, for example, melancholia, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, digestive diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immunologic diseases and so on.