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    Bismacrocyclic compounds as hepatitis C virus inhibitors
    5.
    发明授权
    Bismacrocyclic compounds as hepatitis C virus inhibitors 有权
    双丙酰类化合物作为丙型肝炎病毒抑制剂

    公开(公告)号：US09193740B2

    公开(公告)日：2015-11-24

    申请号：US12907614

    申请日：2010-10-19

    申请人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

    发明人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

    IPC分类号： C07D498/22 ,  A61K38/12 ,  A61K38/21 ,  A61P31/14 ,  A61K31/495 ,  A61K45/06

    CPC分类号： C07D498/22 ,  A61K31/495 ,  A61K45/06

    摘要： The present invention discloses compounds of formula Ia or Ib or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

    摘要翻译： 本发明公开了式Ia或Ib的化合物或其药学上可接受的盐，酯或前药：其抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶的活性。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HCV感染的方法。

    BISMACROCYCLIC COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS
    6.
    发明申请
    BISMACROCYCLIC COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS 有权
    BISMACROCYCLIC化合物作为乙型肝炎病毒抑制剂

    公开(公告)号：US20110123496A1

    公开(公告)日：2011-05-26

    申请号：US12907614

    申请日：2010-10-19

    申请人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

    发明人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

    IPC分类号： A61K38/12 ,  C07K5/087 ,  C07D498/22 ,  A61P31/12 ,  A61P31/14 ,  A61K38/21 ,  A61K39/00 ,  C07K1/00 ,  C12N7/06

    CPC分类号： C07D498/22 ,  A61K31/495 ,  A61K45/06

    摘要： The present invention discloses compounds of formula Ia or Ib or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

    摘要翻译： 本发明公开了式Ia或Ib的化合物或其药学上可接受的盐，酯或前药：其抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶的活性。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HCV感染的方法。

    MACROCYCLIC COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS
    7.
    发明申请
    MACROCYCLIC COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS 有权
    大环化合物作为丙型肝炎病毒抑制剂

    公开(公告)号：US20110033420A1

    公开(公告)日：2011-02-10

    申请号：US12759132

    申请日：2010-04-13

    申请人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

    发明人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

    IPC分类号： A61K38/12 ,  C07K5/083 ,  A61P31/14 ,  A61K38/21 ,  A61P35/00 ,  A61P31/04 ,  A61P31/10

    CPC分类号： A61K38/21 ,  A61K45/06 ,  C07K5/06034 ,  C07K5/0808 ,  C07K5/0812 ,  A61K2300/00

    摘要： The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

    摘要翻译： 本发明公开了式I化合物或其药学上可接受的盐，酯或前药：其抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶的活性。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HCV感染的方法。

    Macrocyclic compounds as hepatitis C virus inhibitors
    8.
    发明授权
    Macrocyclic compounds as hepatitis C virus inhibitors 有权
    大环化合物作为丙型肝炎病毒抑制剂

    公开(公告)号：US08936781B2

    公开(公告)日：2015-01-20

    申请号：US12759132

    申请日：2010-04-13

    申请人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

    发明人： Yonghua Gai ,  Yat Sun Or ,  Guoqiang Wang

    IPC分类号： A61K38/12 ,  C07K5/083 ,  A61P31/14 ,  A61K38/21 ,  A61P35/00 ,  A61P31/04 ,  A61P31/10 ,  C07K5/087 ,  A61K45/06 ,  C07K5/062

    CPC分类号： A61K38/21 ,  A61K45/06 ,  C07K5/06034 ,  C07K5/0808 ,  C07K5/0812 ,  A61K2300/00

    摘要： The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

    摘要翻译： 本发明公开了式I化合物或其药学上可接受的盐，酯或前药：其抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶的活性。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HCV感染的方法。

    Spirocyclic bicyclolides
    9.
    发明授权
    Spirocyclic bicyclolides 有权
    螺环双环

    公开(公告)号：US07517859B2

    公开(公告)日：2009-04-14

    申请号：US11416739

    申请日：2006-05-03

    申请人： Yonghua Gai ,  Datong Tang ,  Ying Sun ,  Zhigang Chen ,  Yat Sun Or ,  Zhe Wang

    发明人： Yonghua Gai ,  Datong Tang ,  Ying Sun ,  Zhigang Chen ,  Yat Sun Or ,  Zhe Wang

    IPC分类号： A61K31/70 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

    摘要翻译： 本发明公开了式I化合物或其药学上可接受的盐，酯或前药：其表现出抗菌性质。 本发明还涉及包含上述化合物的药物组合物，用于给予需要抗生素治疗的受试者。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。 本发明还包括制备本发明化合物的方法。

    POLYMORPHIC FORMS OF 6-11 BICYCLIC KETOLIDE DERIVATIVES
    10.
    发明申请
    POLYMORPHIC FORMS OF 6-11 BICYCLIC KETOLIDE DERIVATIVES 审中-公开
    6-11双相胶体衍生物的多晶型

    公开(公告)号：US20080248105A1

    公开(公告)日：2008-10-09

    申请号：US12105482

    申请日：2008-04-18

    申请人： Datong Tang ,  Guoyou Xu ,  Yonghua Gai ,  Zhe Wang ,  Yat Sun Or ,  Hui-Yin Li

    发明人： Datong Tang ,  Guoyou Xu ,  Yonghua Gai ,  Zhe Wang ,  Yat Sun Or ,  Hui-Yin Li

    IPC分类号： A61K9/48 ,  C07H17/08 ,  A61K9/12 ,  A61P29/00 ,  A61K31/7052

    CPC分类号： C07H17/08

    摘要： The present invention includes EP-13420 polymorphic crystalline forms: Form I, Form II, Form Ia, and monohydrate and amorphous EP-13420 which posses distinct physical properties. In another embodiment of the present invention, there are provided methods of producing the various polymorphic forms in pure form or in combination with one another. The present invention also provides pharmaceutical compositions and formulations comprising the polymorphic and amorphous forms and methods of treating bacterial infections by administering the pharmaceutical compositions to a subject in need of such treatment.

    摘要翻译： 本发明包括具有不同物理性质的EP-13420多晶型形式：I型，II型，Ia型和一水合物和无定型EP-13420。 在本发明的另一个实施方案中，提供了以纯形式或彼此组合生产各种多晶形式的方法。 本发明还提供药物组合物和制剂，其包含多形态和无定形形式以及通过将药物组合物施用于需要这种治疗的受试者来治疗细菌感染的方法。