Cis-2, 6-disubstituted tetrahydropyran derivatives and preparation method thereof
    22.
    发明授权
    Cis-2, 6-disubstituted tetrahydropyran derivatives and preparation method thereof 有权
    顺-2,6-二取代四氢吡喃衍生物及其制备方法

    公开(公告)号:US08115019B2

    公开(公告)日:2012-02-14

    申请号:US12243244

    申请日:2008-10-01

    IPC分类号: C07D309/06 C07D309/22

    CPC分类号: C07D309/06

    摘要: Disclosed are cis-2,6-disubstituted tetrahydropyran derivatives represented by Chemical Formula 1 and a preparation method thereof. The tetrahydropyran derivatives can be prepared by Prins-reacting tetrahydropyran derivatives with homopargylicalcohol derivatives in the presence of trimethylsilyltriflate. The tetrahydropyran derivatives with cis-substituents at both C2 and C6 positions of the tetrahydropyran ring are useful as intermediates for use in the synthesis and development of therapeutically effective, naturally occurring compounds. (wherein, R1, R2 and R3 are as defined in the specification.).

    摘要翻译: 公开了由化学式1表示的顺式-2,6-二取代四氢吡喃衍生物及其制备方法。 四氢吡喃衍生物可以通过Prins-在三甲基甲硅烷基三氟甲磺酸酯存在下将四氢吡喃衍生物与高官能醇衍生物反应来制备。 在四氢吡喃环的C2和C6位上具有顺式取代基的四氢​​吡喃衍生物可用作合成和开发治疗有效的天然存在的化合物的中间体。 (其中,R1,R2和R3如说明书中所定义)。

    Pyrazolopyrimidine derivatives having biological activity on serotonin receptor 5-HT2c
    23.
    发明授权
    Pyrazolopyrimidine derivatives having biological activity on serotonin receptor 5-HT2c 有权
    对5-羟色胺受体5-HT2c具有生物活性的吡唑并嘧啶衍生物

    公开(公告)号:US08232279B2

    公开(公告)日:2012-07-31

    申请号:US12575235

    申请日:2009-10-07

    CPC分类号: C07D487/04

    摘要: The present invention relates to a novel medicinal use of pyrazolopyrimidine compounds having superior effect as serotonin 5-HT2C receptor ligand thus being useful for the prevention and treatment of central nervous system (CNS) diseases. Accordingly, the pharmaceutical composition comprising pyrazolopyrimidine compounds and their pharmaceutically acceptable salts as active ingredients are useful for the prevention and treatment of serotonin 5-HT2C-related central nervous system diseases such as obesity, depression, anxiety and withdrawal symptoms due to drug abuse.

    摘要翻译: 本发明涉及作为5-羟色胺5-HT 2C受体配体具有优越作用的吡唑并嘧啶化合物的新药用,因此可用于预防和治疗中枢神经系统(CNS)疾病。 因此,包含吡唑并嘧啶化合物及其药学上可接受的盐作为活性成分的药物组合物可用于预防和治疗5-羟色胺5-HT2C相关的中枢神经系统疾病如肥胖症,抑郁症,由药物滥用导致的焦虑和戒断症状。

    METHOD OF PREPARING TETRABENAZINE AND DIHYDROTETRABENAZINE
    24.
    发明申请
    METHOD OF PREPARING TETRABENAZINE AND DIHYDROTETRABENAZINE 有权
    制备四氢萘啶酮和二氢吗啡酮的方法

    公开(公告)号:US20130197227A1

    公开(公告)日:2013-08-01

    申请号:US13617357

    申请日:2012-09-14

    IPC分类号: C07D455/06 C07F7/10

    CPC分类号: C07D455/06 C07F7/0812

    摘要: The present invention relates to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ), and more specifically to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ) by using simple and short reaction processes of using 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline and 4-methyl-2-(3-(trimethylsilyl)prop-1-ene-2-yl)pentane as starting materials to sequentially perform an alkylation reaction, an Aza-Prins cyclization reaction in the presence of an oxidant and an oxidation reaction.

    摘要翻译: 本发明涉及一种制备丁苯那嗪(TBZ)和二氢丁苯那嗪(DTBZ)的方法,更具体地涉及通过使用6,7-二甲氧基苯并咪唑的简单且短的反应方法制备丁苯那嗪(TBZ)和二氢丁苯那嗪(DTBZ)的方法 -1,2,3,4-四氢异喹啉和4-甲基-2-(3-(三甲基甲硅烷基)丙-1-烯-2-基)戊烷作为起始原料,以顺序进行烷基化反应,Aza-Prins环化反应 在氧化剂和氧化反应的存在下。

    Method of preparing tetrabenazine and dihydrotetrabenazine
    25.
    发明授权
    Method of preparing tetrabenazine and dihydrotetrabenazine 有权
    制备丁苯那嗪和二氢丁苯那嗪的方法

    公开(公告)号:US08993766B2

    公开(公告)日:2015-03-31

    申请号:US13617357

    申请日:2012-09-14

    IPC分类号: C07D455/06 C07F7/08

    CPC分类号: C07D455/06 C07F7/0812

    摘要: The present invention relates to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ), and more specifically to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ) by using simple and short reaction processes of using 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline and 4-methyl-2-(3-(trimethylsilyl)prop-1-ene-2-yl)pentane as starting materials to sequentially perform an alkylation reaction, an Aza-Prins cyclization reaction in the presence of an oxidant and an oxidation reaction.

    摘要翻译: 本发明涉及一种制备丁苯那嗪(TBZ)和二氢丁苯那嗪(DTBZ)的方法,更具体地涉及通过使用6,7-二甲氧基苯并咪唑的简单且短的反应方法制备丁苯那嗪(TBZ)和二氢丁苯那嗪(DTBZ)的方法 -1,2,3,4-四氢异喹啉和4-甲基-2-(3-(三甲基甲硅烷基)丙-1-烯-2-基)戊烷作为起始原料,以顺序进行烷基化反应,Aza-Prins环化反应 在氧化剂和氧化反应的存在下。