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    Pharmaceutical compositions containing pyrazole derivatives for treating as serotonin antagonist
    3.
    发明申请
    Pharmaceutical compositions containing pyrazole derivatives for treating as serotonin antagonist 审中-公开
    含有用作5-羟色胺拮抗剂治疗的吡唑衍生物的药物组合物

    公开(公告)号：US20080312253A1

    公开(公告)日：2008-12-18

    申请号：US12213067

    申请日：2008-06-13

    申请人： Ghil Soo Nam ,  Hye Whon Rhim ,  Ae Nim Pae ,  Kyung II Choi ,  Hyun Ah Choo ,  Seung Yeol Nah

    发明人： Ghil Soo Nam ,  Hye Whon Rhim ,  Ae Nim Pae ,  Kyung II Choi ,  Hyun Ah Choo ,  Seung Yeol Nah

    IPC分类号： A61K31/496 ,  A61P25/16 ,  A61P25/28 ,  A61P25/18

    CPC分类号： A61K31/496

    摘要： The present invention relates to a pharmaceutical composition containing a pyrazole derivative as an active ingredient, which has antagonistic activity against serotonin 5-HT3A and is effective for the prevention and treatment of central nervous system (CNS) diseases, including emesis, nausea, alcoholism, drug abuse, depression, compulsive neurosis, anxiety, seizure, Alzheimer's disease, Parkinson's disease, Huntington's chorea, psychosis, schizophrenia, suicidal tendency, sleep disorder, appetite disorder and migraine.

    摘要翻译： 本发明涉及含有吡唑衍生物作为活性成分的药物组合物，其对5-羟色胺5-HT3A具有拮抗作用，对预防和治疗中枢神经系统（CNS）疾病有效，包括呕吐，恶心，酒精中毒， 药物滥用，抑郁症，强迫性神经症，焦虑症，癫痫发作，阿尔茨海默病，帕金森病，亨廷顿舞蹈病，精神病，精神分裂症，自杀倾向，睡眠障碍，食欲障碍和偏头痛。

    Method for preparing 1-N-ethylsisomicin
    4.
    发明授权
    Method for preparing 1-N-ethylsisomicin 失效
    1-N-乙基丙基肌氨酸的制备方法

    公开(公告)号：US5696244A

    公开(公告)日：1997-12-09

    申请号：US559671

    申请日：1995-11-20

    申请人： Joong-Hyup Kim ,  Sung Hoon Kim ,  Ghil Soo Nam ,  Ha Young Kim ,  Hyen Joo Son

    发明人： Joong-Hyup Kim ,  Sung Hoon Kim ,  Ghil Soo Nam ,  Ha Young Kim ,  Hyen Joo Son

    IPC分类号： C07H15/26 ,  A61K31/70 ,  A61K31/7028 ,  A61P31/04 ,  C07H15/12 ,  C07H15/236 ,  C07H1/00

    CPC分类号： C07H15/12

    摘要： 1-N-ethylsisomicin represented by the following structural formula I and pharmaceutically acceptable salts thereof are useful antibacterial agents and can be prepared in high yields by a characteristic method comprising the steps of: chelating sisomicin with a chelating agent in a protic solvent; protecting the 3-,2'-and 6'-amino groups of the chelated sisomicin derivative with an acylating reagent; removing the chelating metal from the sisomicin derivative by use of ammonia water, to obtain a 3, 2', 6-N-trisubstituted sisomicin derivative; reacting the trisubstituted sisomicin derivative with an ethylating reagent in an aprotic organic solvent, to selectively ethylate the 1-amino group of the trisubstituted sisomicin derivative; and deprotecting the ethylated sisomicin derivative: ##STR1##

    摘要翻译： 由以下结构式I表示的1-N-乙基缩水甘油酯及其药学上可接受的盐是有用的抗菌剂，可通过特征性方法制备高收率，包括以下步骤：用质子溶剂中的螯合剂螯合西索米星; 用酰化试剂保护螯合的西索米星衍生物的3，2'-和6'-氨基; 通过使用氨水从西索米星衍生物中除去螯合金属，得到3'，2'，6-N-三取代的西索米星衍生物; 使三取代的西索米星衍生物与乙基化试剂在非质子有机溶剂中反应，选择性地使三取代的西索米星衍生物的1-氨基乙基化; 并使乙基西索米星衍生物脱保护：（I）