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8 条记录 (耗时 0.013 秒)

    Acyclic nucleoside phosphonate derivatives and medical uses thereof
    2.
    发明授权
    Acyclic nucleoside phosphonate derivatives and medical uses thereof 有权
    非环型核苷膦酸衍生物及其医疗用途

    公开(公告)号：US09187507B2

    公开(公告)日：2015-11-17

    申请号：US13514749

    申请日：2010-06-21

    申请人： Bohua Zhong ,  Xinhua He ,  Yongguang Wang ,  He Liu

    发明人： Bohua Zhong ,  Xinhua He ,  Yongguang Wang ,  He Liu

    IPC分类号： C07F9/6561 ,  A61K31/683

    CPC分类号： C07F9/65616

    摘要： The present invention relates to an acyclic nucleoside phosphonate derivative and medical uses thereof. Specifically, the present invention relates to an acyclic nucleoside phosphonate derivative of Formula I having strong potency against viruses, such as hepatitis B virus, and low cytotoxicity, or a pharmaceutically acceptable salt, isomer, hydrate or solvate thereof, wherein R1 is H or methyl; each R2 is independently —R3 or —OR3, each R3 is independently C1-C8 alkyl, C3-C8 cycloalkyl. The present invention further relates to a process for preparing the compounds of Formula I, a pharmaceutical composition comprising the compound, and the medical uses of the compound. The acyclic nucleoside phosphonate derivative of the present invention has activity against virus such as hepatitis B virus and good in vivo behavioral traits.

    摘要翻译： 本发明涉及无环核苷膦酸衍生物及其医疗用途。 具体地说，本发明涉及对乙型肝炎病毒等病毒具有强效力和低细胞毒性的式I的无环核苷膦酸酯衍生物或其药学上可接受的盐，异构体，水合物或溶剂化物，其中R1是H或甲基 ; 每个R 2独立地是-R 3或-OR 3，每个R 3独立地是C 1 -C 8烷基，C 3 -C 8环烷基。 本发明还涉及制备式I化合物的方法，包含该化合物的药物组合物和该化合物的医学用途。 本发明的无环核苷膦酸酯衍生物具有抗乙型病毒等病毒的活性和体内行为特性良好的活性。

    POLY(GLUTAMIC ACID)-DRUG CONJUGATE WITH AN AMINO ACID AS A LINKER
    3.
    发明申请
    POLY(GLUTAMIC ACID)-DRUG CONJUGATE WITH AN AMINO ACID AS A LINKER 审中-公开
    多糖（GLUTAMIC ACID）-DRUG与氨基酸连接的连接子

    公开(公告)号：US20120041167A1

    公开(公告)日：2012-02-16

    申请号：US12521767

    申请日：2007-11-07

    申请人： Bohua Zhong ,  Jianxin Zhang ,  Lanfu Chen

    发明人： Bohua Zhong ,  Jianxin Zhang ,  Lanfu Chen

    IPC分类号： C08H1/00

    CPC分类号： A61K31/706 ,  A61K31/337 ,  A61K31/365 ,  A61K47/645

    摘要： A poly(glutamic acid)-drug conjugate with an amino acid as a linker, and nontoxic pharmaceutically acceptable salt thereof, are provided in the present invention. The drug is gemcitabine, paclitaxel or docetaxel. The α-carboxyl group in the amino acid is linked to 5′-hydroxy in gemcitabine molecule or linked to 2′-hydroxy in paclitaxel (docetaxel) molecule via an ester linkage. The α-amino group in the amino acid is linked to the carboxyl group in the poly-(L-glutamic acid) molecule via an amide linkage. The content of gemcitabine in the conjugate is 5-30% in weight, and the content of paclitaxel or docetaxel is 10-40% in weight.

    摘要翻译： 在本发明中提供了具有氨基酸作为连接体的聚（谷氨酸） - 药物偶联物及其无毒的药学上可接受的盐。 该药物是吉西他滨，紫杉醇或多西紫杉醇。 氨基酸中的α-羧基与吉西他滨分子中的5'-羟基连接，或通过酯键与紫杉醇（多西紫杉醇）分子中的2'-羟基连接。 氨基酸中的α-氨基通过酰胺键与聚（L-谷氨酸）分子中的羧基连接。 缀合物中吉西他滨的含量为5-30％，紫杉醇或多西紫杉醇的含量为10-40％。

    Oripavine derivatives and their uses as pharmaceuticals
    4.
    发明授权
    Oripavine derivatives and their uses as pharmaceuticals 有权
    奥哌拉滨衍生物及其作为药物的用途

    公开(公告)号：US07119100B2

    公开(公告)日：2006-10-10

    申请号：US10489656

    申请日：2002-09-13

    申请人： Bohua Zhong ,  Zehui Gong ,  Yaping Wang ,  Yongshao Liu

    发明人： Bohua Zhong ,  Zehui Gong ,  Yaping Wang ,  Yongshao Liu

    IPC分类号： A61K31/44

    CPC分类号： C07D489/12

    摘要： The present invention relates to oripavine derivatives of formula (I), wherein R1 is hydrogen or methyl, R2 is methyl, cyclopropyl methyl, cyclobutyl methyl or allyl, R3 is thiophenyl ethyl or cycloalkyl methyl where the cycloalkyl has 3 to 6 carbon atoms, or non-toxic pharmaceutically acceptable salts thereof. These compounds can be used for the preparation of analgesics or abstinence agents of opium habit-forming drugs.

    摘要翻译： 本发明涉及式（I）的oripavine衍生物，其中R 1是氢或甲基，R 2是甲基，环丙基甲基，环丁基甲基或烯丙基， 其中环烷基具有3至6个碳原子的噻吩基乙基或环烷基甲基，或其无毒的药学上可接受的盐。 这些化合物可用于制备鸦片习性形成药物的止痛剂或禁欲剂。

    Acyclic Nucleoside Phosphonate Derivatives and Medical Uses Thereof
    5.
    发明申请
    Acyclic Nucleoside Phosphonate Derivatives and Medical Uses Thereof 有权
    无环核苷磷酸衍生物及其用途

    公开(公告)号：US20120322764A1

    公开(公告)日：2012-12-20

    申请号：US13514749

    申请日：2010-06-21

    申请人： Bohua Zhong ,  Xinhua He ,  Yongguang Wang ,  He Liu

    发明人： Bohua Zhong ,  Xinhua He ,  Yongguang Wang ,  He Liu

    IPC分类号： C07F9/6561 ,  A61P31/12 ,  A61P31/20 ,  A61K31/683

    CPC分类号： C07F9/65616

    摘要： The present invention relates to an acyclic nucleoside phosphonate derivative and medical uses thereof. Specifically, the present invention relates to an acyclic nucleoside phosphonate derivative of Formula I having strong potency against viruses, such as hepatitis B virus, and low cytotoxicity, or a pharmaceutically acceptable salt, isomer, hydrate or solvate thereof, wherein R1 is H or methyl; each R2 is independently —R3 or —OR3, each R3 is independently C1-C8 alkyl, C3-C8 cycloalkyl. The present invention further relates to a process for preparing the compounds of Formula I, a pharmaceutical composition comprising the compound, and the medical uses of the compound. The acyclic nucleoside phosphonate derivative of the present invention has activity against virus such as hepatitis B virus and good in vivo behavioral traits.

    摘要翻译： 本发明涉及无环核苷膦酸衍生物及其医疗用途。 具体地说，本发明涉及对乙型肝炎病毒等病毒具有强效力和低细胞毒性的式I的无环核苷膦酸酯衍生物或其药学上可接受的盐，异构体，水合物或溶剂化物，其中R1是H或甲基 ; 每个R 2独立地是-R 3或-OR 3，每个R 3独立地是C 1 -C 8烷基，C 3 -C 8环烷基。 本发明还涉及制备式I化合物的方法，包含该化合物的药物组合物和该化合物的医学用途。 本发明的无环核苷膦酸酯衍生物具有抗乙型病毒等病毒的活性和体内行为特性良好的活性。

    SELECTIVE M4 RECEPTOR ANTAGONIST AND ITS MEDICAL USE
    6.
    发明申请
    SELECTIVE M4 RECEPTOR ANTAGONIST AND ITS MEDICAL USE 审中-公开
    选择性M4受体拮抗剂及其医疗用途

    公开(公告)号：US20110306633A1

    公开(公告)日：2011-12-15

    申请号：US12521859

    申请日：2007-11-07

    申请人： Bohua Zhong ,  Jianquan Zheng ,  Liyun Wang ,  He Liu ,  Lanfu Chen ,  Keliang Liu

    发明人： Bohua Zhong ,  Jianquan Zheng ,  Liyun Wang ,  He Liu ,  Lanfu Chen ,  Keliang Liu

    IPC分类号： A61K31/439 ,  A61P25/16 ,  C07D221/22

    CPC分类号： C07D221/22

    摘要： The present invention provides a selective M4 receptor antagonist, levorotatory demethylated phencynonate or its nontoxic pharmaceutically acceptable salt, a pharmaceutical composition comprising this compound, and a use thereof in the manufacture of a medicament for the treatment of motion dysfunction, such as, tremor, rigor and the like caused by Parkinson's disease (PD). The structure, of the compound is shown in Formula IIa:

    摘要翻译： 本发明提供选择性M4受体拮抗剂，左旋去甲基化的苯甲酸盐或其无毒的药学上可接受的盐，包含该化合物的药物组合物及其在制备用于治疗运动功能障碍的药物中的用途，例如颤抖，严重性 和类似因素引起的帕金森病（PD）。 该化合物的结构如式IIa所示：

    Oripavine derivatives and their uses as medicines
    7.
    发明申请
    Oripavine derivatives and their uses as medicines 有权
    奥曲连衍生物及其作为药物的用途

    公开(公告)号：US20050070564A1

    公开(公告)日：2005-03-31

    申请号：US10489656

    申请日：2002-09-13

    申请人： Bohua Zhong ,  Zehui Gong ,  Yaping Wang ,  Yongshao Liu

    发明人： Bohua Zhong ,  Zehui Gong ,  Yaping Wang ,  Yongshao Liu

    IPC分类号： B42F1/00 ,  C07D489/12 ,  A61K31/485

    CPC分类号： C07D489/12

    摘要： The present invention relates to oripavine derivatives of formula (I), wherein R1 is hydrogen or methyl, R2 is methyl, cyclopropyl methyl, cyclobutyl methyl or allyl, R3 is thiophenyl ethyl or cycloalkyl methyl where the cycloalkyl has 3 to 6 carbon atoms, or nontoxic pharmaceutically acceptable salts thereof. These compounds can be used for the preparation of analgesics or abstinence agents of opium habit-forming drugs.

    摘要翻译： 本发明涉及式（I）的oripavine衍生物，其中R 1是氢或甲基，R 2是甲基，环丙基甲基，环丁基甲基或烯丙基，R 3是噻吩基乙基或环烷基甲基，其中 环烷基具有3至6个碳原子，或其无毒的药学上可接受的盐。 这些化合物可用于制备鸦片习性形成药物的止痛剂或禁欲剂。