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    Oxazolidone compound, preparing method and application thereof
    134.
    发明授权
    Oxazolidone compound, preparing method and application thereof 有权
    恶唑烷酮化合物，其制备方法和应用

    公开(公告)号：US09382265B2

    公开(公告)日：2016-07-05

    申请号：US14761843

    申请日：2013-12-30

    Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  ZHE JIANG JUTAI PHARMACEUTICAL CO., LTD.

    Inventor： Yushe Yang ,  Tao Xue ,  Shi Ding ,  Bin Guo

    IPC: C07D498/04 ,  C07D519/00

    CPC classification number: C07D498/04 ,  C07D519/00

    Abstract: The present invention relates to the field of a pharmaceutical compound, and more specifically, relates to a new oxazolidone compound, an enantiomer, a diastereoisomer and a raceme thereof, and a mixture thereof, and a pharmaceutically acceptable salt thereof, a preparation method thereof, an application thereof as a bioactive substance in a drug. The compound in the present invention has strong anticoagulant activity, does not affect the activity of thrombin, and can reduce the risk of hemorrhage. A pharmacokinetics experiment shows that the compound in the present invention further has good metabolic characteristics, and has a far better oral bioavailability than a positive contrastive agent rivaroxaban.

    Abstract translation: 本发明涉及药物化合物的领域，更具体地，涉及新的恶唑烷酮化合物，对映异构体，非对映异构体和其外消旋物及其混合物及其药学上可接受的盐，其制备方法， 其作为药物中的生物活性物质的应用。 本发明化合物具有较强的抗凝血活性，不影响凝血酶的活性，可降低出血的风险。 药代动力学实验表明，本发明的化合物还具有良好的代谢特征，并且具有比阳性对照剂利伐沙班更好的口服生物利用度。

    (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone and preparation method and use thereof
    135.
    发明授权
    (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone and preparation method and use thereof 有权
    （2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯及其制备方法和用途

    公开(公告)号：US09376410B2

    公开(公告)日：2016-06-28

    申请号：US14434563

    申请日：2013-10-10

    Applicant: TOPHARMAN SHANGHAI CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA , CHINESE ACADEMY OF SCIENCES ,  TOPHARMAN SHANDONG CO., LTD.

    Inventor： Guan Wang ,  Xiangrui Jiang ,  Xudong Gong ,  Weiming Chen ,  Fuqiang Zhu ,  Rongxia Zhang ,  Xianguo Zhao

    IPC: C07D307/00 ,  C07D307/33 ,  C07D413/12

    CPC classification number: C07D307/33 ,  C07D413/12

    Abstract: This invention disclose (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone in a single configuration and preparation method and use thereof. The (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone, or a pharmaceutically acceptable salt, an ester, a prodrug or a solvate thereof according to the invention are important intermediates of a variety of anti-viral and anti-tumor active ingredients. A compound obtained from (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone via an acylation reaction can be directly used for preparing various anti-viral and anti-tumor drugs. The Chiral synthesis method and the spontaneous resolution method of the compound of (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone according to the invention have the following advantages: the reaction routes are short and simple with high yield and low cost, which are suitable for industrial application.

    Abstract translation: 本发明公开了单一构型的（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯及其制备方法和用途。 根据本发明的（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯或其药学上可接受的盐，酯，前药或溶剂化物是各种抗 - 病毒和抗肿瘤活性成分。 通过酰化反应从（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯获得的化合物可以直接用于制备各种抗病毒和抗肿瘤药物。 根据本发明的（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯化合物的手性合成方法和自发拆分方法具有以下优点：反应路线短而简单 产量高，成本低，适合工业应用。

    PHARMACEUTIC OSMOTIC PUMP PREPARATION
    139.
    发明申请
    PHARMACEUTIC OSMOTIC PUMP PREPARATION 审中-公开
    药用动力泵的制备

    公开(公告)号：US20150245992A1

    公开(公告)日：2015-09-03

    申请号：US14436235

    申请日：2013-10-16

    Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

    Inventor： Jiwen Zhang ,  Li Wu ,  Xianzhen Yin ,  Zhen Guo ,  Haiyan Li

    IPC: A61K9/00 ,  G01N23/04 ,  A61K31/7052 ,  A61K31/40 ,  A61K47/32 ,  A61K31/192

    CPC classification number: A61K9/0004 ,  A61K9/2853 ,  A61K9/2866 ,  A61K31/192 ,  A61K31/205 ,  A61K31/40 ,  A61K31/401 ,  A61K31/407 ,  A61K31/513 ,  A61K31/519 ,  A61K31/522 ,  A61K31/64 ,  A61K31/7052 ,  A61K31/7056 ,  A61K47/32 ,  G01N23/046

    Abstract: Provided in the present invention is a pharmaceutic osmotic pump preparation comprising a tablet core, wherein the tablet core contains drugs (or pharmaceutically active ingredients) and materials forming a chamber structure; and a coating film coating the tablet core where a drug release hole is set; wherein when the pharmaceutic osmotic pump preparation releases drugs in water or an aqueous medium, the materials forming the chamber structure lead to the formation of a superfine chamber structure in the coating film, and the total volume of the superfine chamber structure Vb gradually increases over the releasing time, but the releasing rate R (or release amount A) of the pharmaceutically active ingredients is proportional to Vb. The osmotic pump preparation of the present invention is suitable for water-soluble drugs and water-insoluble drugs, and especially is suitable for the controlled release of low solubility drugs or pH dependent drugs.

    Abstract translation: 本发明提供了包含片芯的药物渗透泵制剂，其中片芯含有药物（或药物活性成分）和形成室结构的材料; 以及涂布药片释放孔的片芯的涂膜; 其中当药物渗透泵制剂在水或水介质中释放药物时，形成室结构的材料导致在涂膜中形成超细腔室结构，并且超细腔室结构Vb的总体积逐渐增加 释放时间，但是药物活性成分的释放速度R（或释放量A）与Vb成比例。 本发明的渗透泵制剂适用于水溶性药物和水不溶性药物，特别适用于低溶解度药物或pH依赖性药物的控制释放。

    HEXAHYDRODIBENZO[A,G]QUINOLIZINE COMPOUND, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION AND USE THEREOF
    140.
    发明申请
    HEXAHYDRODIBENZO[A,G]QUINOLIZINE COMPOUND, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION AND USE THEREOF 审中-公开
    六氢呋喃并[A，G]喹啉化合物，其制备方法，药物组合物及其用途

    公开(公告)号：US20140088130A1

    公开(公告)日：2014-03-27

    申请号：US14091979

    申请日：2013-11-27

    Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences

    Inventor： Hong LIU ,  Xin XIE ,  Xuechu ZHEN ,  Haifeng SUN ,  Jing LI ,  Liyuan ZHU ,  Zeng LI ,  Ying CHEN ,  Hualiang JIANG ,  Kaixian CHEN

    IPC: C07D491/147 ,  C07D491/22 ,  C07D455/03

    CPC classification number: C07D491/153 ,  C07C69/736 ,  C07C231/14 ,  C07D217/20 ,  C07D311/20 ,  C07D455/03 ,  C07D491/056 ,  C07D491/147 ,  C07D491/22

    Abstract: The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on.

    Abstract translation: 本发明涉及由通式（I）表示的新型六氢二苯并[a，g]喹啉化合物及其衍生物，对映体，非对映异构体，外消旋及其混合物，以及其药学上可接受的盐。 本发明还涉及一种制备该化合物的方法，该化合物对神经系统疾病，特别是与多巴胺受体和5-羟色胺受体相关的疾病具有良好的预防和治疗作用。 生物活性实验表明，该化合物预计将发展成为一种新颖有力的化学实体，用于治疗与多巴胺受体和5-羟色胺受体，特别是精神分裂症，帕金森病，药物成瘾，偏头痛等有关的疾病。

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