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    PROCESS FOR PREPARING BEPOTASTINE AND INTERMEDIATES USED THEREIN
    6.
    发明申请
    PROCESS FOR PREPARING BEPOTASTINE AND INTERMEDIATES USED THEREIN 审中-公开
    用于制备BEPOTASTINE及其中间体的方法

    公开(公告)号：US20100168433A1

    公开(公告)日：2010-07-01

    申请号：US12663983

    申请日：2008-06-05

    申请人： Tae Hee Ha ,  Chang Hee Park ,  Won Jeoung Kim ,  Soohwa Cho ,  Han Kyong Kim ,  Kwee Hyun Suh

    发明人： Tae Hee Ha ,  Chang Hee Park ,  Won Jeoung Kim ,  Soohwa Cho ,  Han Kyong Kim ,  Kwee Hyun Suh

    IPC分类号： C07D401/12

    CPC分类号： C07D401/12

    摘要： A process for stereospecific preparation of bepotastine of formula (I) and novel intermediates used therein having formulae (II) to (IV) are provided. The inventive process comprises subjecting (RS)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine to a reaction with a 4-halobutanoic acid l-menthyl ester, halo being chloro, bromo or iodo, in an organic solvent in the presence of a base to produce (RS)-bepotastine l-menthyl ester of formula (II), conducting a reaction of the compound of formula (II) with N-benzyloxycarbonyl L-aspartic acid in an organic solvent to induce selective precipitation of bepotastine l-menthyl ester.N-benzyloxycarbonyl L-aspartate of formula (III), filtering the precipitates formed in step 2) to isolate the compound of formula (III), treating the compound of formula (III) with a base to liberate bepotastine l-menthyl ester of formula (IV), and hydrolyzing the compound of formula (IV) in the presence of a base. The inventive process can provide bepotastine having a high optical purity of not less than 99.5% in a high yield, and thus, is useful in the development of anti-histamines and anti-allergic agents.

    摘要翻译： 提供了式（I）的贝他辛汀的立体特异性制备方法和其中使用的具有式（II）至（IV）的新型中间体。 本发明的方法包括使（RS）-4 - [（4-氯苯基）（2-吡啶基）甲氧基]哌啶与4-卤代丁酸1-薄荷酯，卤素为氯，溴或碘的有机反应 溶剂在碱的存在下反应以制备式（II）的（RS） - 贝斯塔司汀l-薄荷酯，在有机溶剂中进行式（II）化合物与N-苄氧基羰基L-天冬氨酸的反应，以诱导选择性 贝他辛汀1-薄荷酯的沉淀。式（III）的N-苄氧基羰基L-天冬氨酸盐，过滤步骤2）中形成的沉淀物以分离式（III）化合物，用碱将式（III）化合物 释放式（IV）的布他辛酯l-薄荷酯，并在碱的存在下水解式（IV）的化合物。 本发明方法可以以高产率提供具有不低于99.5％的高光学纯度的贝他斯汀，因此可用于抗组胺和抗过敏剂的开发。

    NOVEL PYRIMIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION INCLUDING SAME AS AN ACTIVE INGREDIENT
    8.
    发明申请
    NOVEL PYRIMIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION INCLUDING SAME AS AN ACTIVE INGREDIENT 审中-公开
    新型吡咯烷衍生物和药物组合物，包括作为活性成分的组合物

    公开(公告)号：US20140163226A1

    公开(公告)日：2014-06-12

    申请号：US14232667

    申请日：2012-06-29

    申请人： Chul Hyun Park ,  Won Jeoung Kim ,  Young Hee Jung ,  Nam Du Kim ,  Young Kil Chang ,  Maeng Sup Kim

    发明人： Chul Hyun Park ,  Won Jeoung Kim ,  Young Hee Jung ,  Nam Du Kim ,  Young Kil Chang ,  Maeng Sup Kim

    IPC分类号： C07D495/04 ,  C07D487/04

    CPC分类号： C07D495/04 ,  C07D487/04

    摘要： The present invention relates to a compound represented by formula (I) for inhibiting the activity of diacylglycerol O-acyltransferase type 1 (DGAT1), and pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising same as an active ingredient. The compound of the present invention may be used effectively in the treatment or prevention of a disease or condition mediated by the activity of DGAT1 such as obesity, type II diabetes, dyslipidemia, metabolic syndrome, and the like, without any adverse effects: wherein A, B, X, and R5 to R7 are the same as defined in the specification.

    摘要翻译： 本发明涉及一种抑制二酰基甘油O-酰基转移酶1型（DGAT1）的活性的式（I）表示的化合物及其药学上可接受的盐，以及含有该活性成分的药物组合物。 本发明的化合物可以有效地用于治疗或预防由诸如肥胖，II型糖尿病，血脂异常，代谢综合征等的DGAT1的活性介导的疾病或病症，而没有任何不利影响：其中A ，B，X和R5至R7与说明书中所定义相同。