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    4-TETRAHYDROPYRIDYLPYRIMIDINE DERIVATIVES
    1.
    发明公开
    4-TETRAHYDROPYRIDYLPYRIMIDINE DERIVATIVES 失效
    4- TETRAHYDROPYRIDYLPYRIMIDIN衍

    公开(公告)号：EP0976745A1

    公开(公告)日：2000-02-02

    申请号：EP98911002.8

    申请日：1998-03-25

    申请人： TAISHO PHARMACEUTICAL CO. LTD

    发明人： NAKAZATO, Atsuro, Taisho Pharmaceutical Co., Ltd ,  KUMAGAI, Toshihito, Taisho Pharmaceutical Co., Ltd ,  OKUBO, Taketoshi, Taisho Pharmaceutical Co., Ltd ,  AIBE, Izumi, Taisho Pharmaceutical Co., Ltd ,  TANAKA, Hideo, Taisho Pharmaceutical Co., Ltd ,  CHAKI, Shigeyuki, Taisho Pharmaceutical Co., Ltd ,  OKUYAMA, Shigeru, Taisho Pharmaceutical Co., Ltd ,  TOMISAWA, Kazuyuki, Taisho Pharmaceutical Co., Ltd

    IPC分类号： C07D401/04 ,  A61K31/505

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

    摘要： A 4-tetrahydropyridylpyrimidine derivative represented by formula (I):
    wherein Ar represents a phenyl group substituted with 1 to 3 substituents selected from a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, and a trifluoromethyl group, a phenyl group, a thienyl group or a furanyl group; R 1 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms; R 2 represents an alkyl group having 1 to 5 carbon atoms, a cycloalkylalkyl group having 4 to 7 carbon atoms, an alkenyl group having 2 to 5 carbon atoms or an alkynyl group having 2 to 5 carbon atoms; and X 1 , X 2 , and X 3 , which may be the same or different, each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, an alkylthio group having 1 to 5 carbon atoms, an amino group or an amino group substituted with 1 or 2 alkyl groups having 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof.
    The invention provides a compound effective on diseases which CRF is considered to participate in, such as depression, anxiety, Alzheimer's disease, Parkinson's syndrome, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head wounds, inflammation, and immunity-associated diseases.

    摘要翻译： 由式（I）表示的4-四氢吡啶基嘧啶衍生物：其中Ar表示被1至3个选自卤素原子，具有1至5个碳原子的烷基，1至5个碳原子的烷氧基取代的苯基 碳原子和三氟甲基，苯基，噻吩基或呋喃基; R 1表示氢原子，碳原子数1〜5的烷基，氨基或被1或2个碳原子数1〜5的烷基取代的氨基。 R 2表示碳原子数1〜5的烷基，碳原子数4〜7的环烷基烷基，碳原子数2〜5的烯基或碳原子数2〜5的炔基。 X 1，X 2和X 3可以相同或不同，分别表示氢原子，卤原子，碳原子数为1〜5的烷基，烷氧基为1 至5个碳原子，具有1至5个碳原子的烷硫基，氨基或被1或2个具有1至5个碳原子的烷基取代的氨基或其药学上可接受的盐。 本发明提供了一种对CRF被认为参与抑郁，焦虑，阿尔茨海默病，帕金森综合征，亨廷顿氏舞蹈病，进食障碍，高血压，消化系统疾病，药物依赖，癫痫，脑梗塞，脑缺血， 脑水肿，头部创伤，炎症和免疫相关疾病。