POLYMORPHIC FORMS OF 6-11 BICYCLIC KETOLIDE DERIVATIVES
    71.
    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

    CPC classification number: C07H17/08

    Abstract: 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.

    Abstract translation: 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。

    ACYCLIC OXIMYL HEPATITIS C PROTEASE INHIBITORS

    公开(公告)号:US20080187516A1

    公开(公告)日:2008-08-07

    申请号:US12016631

    申请日:2008-01-18

    Abstract: 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.

    3,6-bridged 9,12-oxolides
    73.
    发明授权
    3,6-bridged 9,12-oxolides 失效
    3,6-桥联的9,12-草甘膦

    公开(公告)号:US07407942B2

    公开(公告)日:2008-08-05

    申请号:US11435401

    申请日:2006-05-16

    CPC classification number: C07H17/08

    Abstract: 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.

    Abstract translation: 本发明公开了具有抗菌性质的式(I)化合物或其药学上可接受的盐,酯或前药。 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。

    MACROCYLIC OXIMYL HEPATITIS C PROTEASE INHIBITORS
    74.
    发明申请
    MACROCYLIC OXIMYL HEPATITIS C PROTEASE INHIBITORS 失效
    大环氧合酶抑制剂C蛋白酶抑制剂

    公开(公告)号:US20080181868A1

    公开(公告)日:2008-07-31

    申请号:US12016643

    申请日:2008-01-18

    CPC classification number: C07K5/0804 C07K5/0812 C07K7/06

    Abstract: 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.

    Abstract translation: 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。

    Polymorphic forms of 6-11 bicyclic ketolide derivatives
    75.
    发明授权
    Polymorphic forms of 6-11 bicyclic ketolide derivatives 有权
    6-11双环酮内酯衍生物的多形态

    公开(公告)号:US07384921B2

    公开(公告)日:2008-06-10

    申请号:US11057476

    申请日:2005-02-14

    CPC classification number: C07H17/08

    Abstract: 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.

    Abstract translation: 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。

    Quinoxalinyl tripeptide hepatitis C virus inhibitors
    76.
    发明申请
    Quinoxalinyl tripeptide hepatitis C virus inhibitors 有权
    喹喔啉三肽丙型肝炎病毒抑制剂

    公开(公告)号:US20080032936A1

    公开(公告)日:2008-02-07

    申请号:US11499917

    申请日:2006-08-04

    CPC classification number: C07K5/0808 A61K38/00

    Abstract: The present invention relates to compounds of Formula I, 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.

    Abstract translation: 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。

    MACROCYCLIC HEPATITIS C VIRUS SERINE PROTEASE INHIBITORS
    77.
    发明申请
    MACROCYCLIC HEPATITIS C VIRUS SERINE PROTEASE INHIBITORS 有权
    大肠杆菌C型病毒丝氨酸蛋白酶抑制剂

    公开(公告)号:US20080008681A1

    公开(公告)日:2008-01-10

    申请号:US11768712

    申请日:2007-06-26

    Abstract: The present invention relates to compounds, including compounds of Formula I, 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.

    Abstract translation: 本发明涉及包括式I化合物或其药学上可接受的盐,酯或前药的化合物,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。

    9N-substituted 6-11 bicyclic erythromycin derivatives
    78.
    发明授权
    9N-substituted 6-11 bicyclic erythromycin derivatives 失效
    9N-取代的6-11双环红霉素衍生物

    公开(公告)号:US07265094B2

    公开(公告)日:2007-09-04

    申请号:US11031465

    申请日:2005-01-07

    CPC classification number: C07H17/08

    Abstract: The present invention discloses compounds of formula I, II, III, or IV, or a racemate, enantiomer, regioisomer, salt, ester or prodrug 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.

    Abstract translation: 本发明公开了式I,II,III或IV的化合物或其外消旋物,对映异构体,区域异构体,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。

    Aza-peptide macrocyclic hepatitis c serine protease inhibitors
    79.
    发明申请
    Aza-peptide macrocyclic hepatitis c serine protease inhibitors 审中-公开
    氮杂大肽丙型肝炎丝氨酸蛋白酶抑制剂

    公开(公告)号:US20070021330A1

    公开(公告)日:2007-01-25

    申请号:US10561718

    申请日:2004-05-19

    CPC classification number: C07K5/06139 A61K38/00 C07K5/06165

    Abstract: The present invention relates to compounds of Formula (I), 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.

    Abstract translation: 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。

    Spirocyclic bicyclolides
    80.
    发明申请

    公开(公告)号:US20060252713A1

    公开(公告)日:2006-11-09

    申请号:US11416739

    申请日:2006-05-03

    CPC classification number: C07H17/08

    Abstract: 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.

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