PROCESSES FOR THE PREPARATION OF O-[5-(4-AMINO-THIAZOL-2-YL)-PYRIDIN-2-YLMETHYL]-HYDROXYLAMINE
    91.
    发明申请
    PROCESSES FOR THE PREPARATION OF O-[5-(4-AMINO-THIAZOL-2-YL)-PYRIDIN-2-YLMETHYL]-HYDROXYLAMINE 有权
    制备O- [5-(4-氨基 - 噻唑-2-基) - 吡啶-2-基]甲基] - 羟基甲酰胺的方法

    公开(公告)号:US20090281324A1

    公开(公告)日:2009-11-12

    申请号:US12437636

    申请日:2009-05-08

    IPC分类号: C07D417/04

    CPC分类号: C07D417/04

    摘要: The present invention relates generally to novel methods for the synthesis of O-[5-(4-amino-thiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine which is an essential reagent in the synthesis of one of the bridged erythromycin derivatives and their respective pharmaceutically acceptable salts in PCT Application WO 03/097659 A1. In particular, the present invention relates to processes and intermediates for the preparation of a compound of formula (Ia):

    摘要翻译: 本发明一般涉及合成O- [5-(4-氨基 - 噻唑-2-基) - 吡啶-2-基甲基] - 羟胺的新方法,其是合成桥接的 红霉素衍生物及其各自的药学上可接受的盐在PCT申请WO 03/097659 A1中。 特别地,本发明涉及制备式(Ia)化合物的方法和中间体:

    Pyridazinonyl Macrocyclic Hepatitis C Serine Protease Inhibitors
    92.
    发明申请
    Pyridazinonyl Macrocyclic Hepatitis C Serine Protease Inhibitors 有权
    哒嗪基大环丙型肝炎丝氨酸蛋白酶抑制剂

    公开(公告)号:US20090035272A1

    公开(公告)日:2009-02-05

    申请号:US11832893

    申请日:2007-08-02

    摘要: The present invention relates to 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 a compound of the present invention.

    摘要翻译: 本发明涉及抑制丝氨酸蛋白酶活性,特别是丙型肝炎病毒(HCV)NS3-NS4A蛋白酶活性的式I化合物或其药学上可接受的盐,酯或前药。 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。

    PROCESSES FOR THE PREPARATION OF HYDROXYLAMINES
    93.
    发明申请
    PROCESSES FOR THE PREPARATION OF HYDROXYLAMINES 失效
    制备羟甲基胺的方法

    公开(公告)号:US20080242865A1

    公开(公告)日:2008-10-02

    申请号:US12135299

    申请日:2008-06-09

    IPC分类号: C07D401/04

    CPC分类号: C07D401/04 C07D401/14

    摘要: The present invention relates generally to novel methods for the synthesis of O-(6-pyrazol-1-yl-pyridin-3-ylmethyl)-hydroxylamine which is an essential reagent in the synthesis of one of the bridged erythromycin derivatives and their respective pharmaceutically acceptable salts in PCT Application WO 03/097659 A1. In particular, the present invention relates to processes and intermediates for the preparation of a compound of formula (Ia):

    摘要翻译: 本发明一般涉及合成O-(6-吡唑-1-基 - 吡啶-3-基甲基) - 羟胺的新方法,其是合成桥联红霉素衍生物之一及其各自药学上的必需试剂 PCT申请WO 03/097659 A1中的可接受的盐。 特别地,本发明涉及制备式(Ia)化合物的方法和中间体:

    Phosphorus-containing hepatitis C serine protease inhibitors
    94.
    发明授权
    Phosphorus-containing hepatitis C serine protease inhibitors 有权
    含磷的丙型肝炎丝氨酸蛋白酶抑制剂

    公开(公告)号:US07582605B2

    公开(公告)日:2009-09-01

    申请号:US11503407

    申请日:2006-08-11

    IPC分类号: A61K38/06 C07K5/08

    摘要: The present invention relates to phosphorus-derived compounds of Formula I or Formula II, or a pharmaceutically acceptable salt, ester, or prodrug, 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: 本发明涉及抑制丝氨酸蛋白酶活性,特别是丙型肝炎病毒(HCV)NS3-NS4A蛋白酶活性的式I或式II的磷衍生化合物或其药学上可接受的盐,酯或前药。 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。

    TRIAZOLYL ACYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS
    97.
    发明申请
    TRIAZOLYL ACYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS 审中-公开
    三唑乙酰胆碱酯酶蛋白酶抑制剂

    公开(公告)号:US20080038225A1

    公开(公告)日:2008-02-14

    申请号:US11835157

    申请日:2007-08-07

    摘要: The present invention relates to compounds of Formula I or II, 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 to the subject a pharmaceutical composition comprising a compound of the present invention.

    摘要翻译: 本发明涉及式I或II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。 本发明还涉及通过向受试者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。

    Triazolyl macrocyclic hepatitis C serine protease inhibitors
    98.
    发明授权
    Triazolyl macrocyclic hepatitis C serine protease inhibitors 失效
    三唑基大环丙型肝炎丝氨酸蛋白酶抑制剂

    公开(公告)号:US07662779B2

    公开(公告)日:2010-02-16

    申请号:US11835657

    申请日:2007-08-08

    IPC分类号: A61K38/12 C07K5/12

    摘要: The present invention relates to compounds of Formula I or II, 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 to the subject a pharmaceutical composition comprising a compound of the present invention.

    摘要翻译: 本发明涉及式I或II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。 本发明还涉及通过向受试者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。

    OXIMYL DIPEPTIDE HEPATITIS C PROTEASE INHIBITORS
    100.
    发明申请
    OXIMYL DIPEPTIDE HEPATITIS C PROTEASE INHIBITORS 审中-公开
    OXIMYL DIPEPTIDE HEPATITIS C蛋白酶抑制剂

    公开(公告)号:US20080292587A1

    公开(公告)日:2008-11-27

    申请号:US12108659

    申请日:2008-04-24

    摘要: The present invention discloses compounds of formulae 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,酯或前体药物: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。