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    PRODRUG OF FLUORINE-CONTAINING AMINO ACID
    5.
    发明申请
    PRODRUG OF FLUORINE-CONTAINING AMINO ACID 有权
    含氟氨基酸的制备

    公开(公告)号：US20150141669A1

    公开(公告)日：2015-05-21

    申请号：US14403790

    申请日：2013-05-31

    申请人： TAISHO PHARMACEUTICAL CO., LTD.

    发明人： Takashi Hashihayata ,  Norikazu Otake ,  Naoki Miyakoshi ,  Kazunari Sakagami

    IPC分类号： C07D317/50 ,  C07D317/40 ,  C07C229/50

    CPC分类号： C07D317/50 ,  A61K31/265 ,  A61K31/357 ,  C07C229/50 ,  C07C237/04 ,  C07C237/20 ,  C07C271/24 ,  C07C323/60 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/18 ,  C07C2603/74 ,  C07D207/08 ,  C07D307/88 ,  C07D317/40

    摘要： Provided are a fluorine-containing amino acid prodrug represented by general formula (I) that makes a fluorine-containing amino acid which is a group 2 metabotropic glutamate receptor agonist into a prodrug, or a pharmaceutically acceptable salt thereof. More specifically, provided is a prodrug that increases the in vivo exposure and enhances the oral absorbability and other mucosal absorbability of a parent compound that acts on group 2 metabotropic glutamate receptors as an agent for the treatment or prevention of diseases in which group 2 metabotropic glutamate receptors are said to be involved, such as: schizophrenia, anxiety disorder and its related diseases, depression, bipolar disorder, epilepsy, developmental disorders, sleep disorders, and other neuropsychiatric diseases; and drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, movement disorders associated with muscular rigidity, cerebral ischemia, cerebral insufficiency, spinal cord disorders, cephalopathy, and other neurological diseases.

    摘要翻译： 本发明提供一种通式（I）所示的含氟氨基酸前药，其为前体药物中含有2族代谢型谷氨酸受体激动剂的含氟氨基酸或其药学上可接受的盐。 更具体地，提供了增加体内暴露并增强作用于第2组代谢型谷氨酸受体的母体化合物的口服吸收性和其它粘膜吸收性的前药，其作为治疗或预防其中组2代谢型谷氨酸的疾病 受体被称为涉及，如：精神分裂症，焦虑症及其相关疾病，抑郁症，双相情感障碍，癫痫，发育障碍，睡眠障碍和其他神经精神疾病; 药物依赖，认知障碍，阿尔茨海默病，亨廷顿氏舞蹈病，帕金森氏病，与肌肉紧张相关的运动障碍，脑缺血，脑功能不全，脊髓障碍，头痛和其他神经系统疾病。