Compositions and methods for inhibiting proteases
    4.
    发明授权
    Compositions and methods for inhibiting proteases 有权
    抑制蛋白酶的组合物和方法

    公开(公告)号:US09409944B2

    公开(公告)日:2016-08-09

    申请号:US14131681

    申请日:2012-07-12

    摘要: In particular, in alternative embodiments, the invention provides pharmaceutical compounds and formulations comprising a family of epoxyketone compounds, which include racemic mixtures or racemates, isomers, stereoisomers, diastereoisomers, derivatives and analogs, and methods for making and using them. In alternative embodiments, pharmaceutical compositions and formulations of the invention are administered to an individual in need thereof in an amount sufficient to treat, prevent, reverse and/or ameliorate an infection, disease or condition that can be ameliorated, treated, prevented or reversed by partially or completely inhibiting a chymotrypsin-like protease or a proteasome activity, including e.g., a retroviral infection such as human immunodeficiency virus-1 (HIV-1) infection, an immune disorder, a neurodegenerative disease or condition, or a cancer such as a myeloma or multiple myeloma, an adenocarcinoma such as a lung adenocarcinoma, a pancreatic cancer, a B-cell related cancer, and lymphomas such as non-Hodgkin's lymphoma.

    摘要翻译: 特别地,在替代实施方案中,本发明提供包含一系列环氧酮化合物的药物化合物和制剂,其包括外消旋混合物或外消旋体,异构体,立体异构体,非对映异构体,衍生物和类似物,以及制备和使用它们的方法。 在替代实施方案中,将本发明的药物组合物和制剂以足以治疗,预防,逆转和/或改善可被改善,治疗,预防或逆转的感染,疾病或病症的量施用于有需要的个体 部分或完全抑制胰凝乳蛋白酶样蛋白酶或蛋白酶体活性,包括例如逆转录病毒感染如人免疫缺陷病毒-1(HIV-1)感染,免疫疾病,神经变性疾病或病症,或癌症如 骨髓瘤或多发性骨髓瘤,腺癌如肺腺癌,胰腺癌,B细胞相关癌症,淋巴瘤如非霍奇金淋巴瘤。

    COMPOSITIONS AND METHODS FOR INHIBITING PROTEASES
    6.
    发明申请
    COMPOSITIONS AND METHODS FOR INHIBITING PROTEASES 有权
    用于抑制蛋白质的组合物和方法

    公开(公告)号:US20140248333A1

    公开(公告)日:2014-09-04

    申请号:US14131681

    申请日:2012-07-12

    IPC分类号: C07K5/083

    摘要: In particular, in alternative embodiments, the invention provides pharmaceutical compounds and formulations comprising a family of epoxyketone compounds, which include racemic mixtures or racemates, isomers, stereoisomers, diastereoisomers, derivatives and analogs, and methods for making and using them. In alternative embodiments, pharmaceutical compositions and formulations of the invention are administered to an individual in need thereof in an amount sufficient to treat, prevent, reverse and/or ameliorate an infection, disease or condition that can be ameliorated, treated, prevented or reversed by partially or completely inhibiting a chymotrypsin-like protease or a proteasome activity, including e.g., a retroviral infection such as human immunodeficiency virus-1 (HIV-1) infection, an immune disorder, a neurodegenerative disease or condition, or a cancer such as a myeloma or multiple myeloma, an adenocarcinoma such as a lung adenocarcinoma, a pancreatic cancer, a B-cell related cancer, and lymphomas such as non-Hodgkin's lymphoma.

    摘要翻译: 特别地,在替代实施方案中,本发明提供包含一系列环氧酮化合物的药物化合物和制剂,其包括外消旋混合物或外消旋体,异构体,立体异构体,非对映异构体,衍生物和类似物,以及制备和使用它们的方法。 在替代实施方案中,将本发明的药物组合物和制剂以足以治疗,预防,逆转和/或改善可被改善,治疗,预防或逆转的感染,疾病或病症的量施用于有需要的个体 部分或完全抑制胰凝乳蛋白酶样蛋白酶或蛋白酶体活性,包括例如逆转录病毒感染如人免疫缺陷病毒-1(HIV-1)感染,免疫疾病,神经变性疾病或病症,或癌症如 骨髓瘤或多发性骨髓瘤,腺癌如肺腺癌,胰腺癌,B细胞相关癌症,淋巴瘤如非霍奇金淋巴瘤。

    Compositions for ameliorating cell proliferative disorders and methods of making and using them
    8.
    发明授权
    Compositions for ameliorating cell proliferative disorders and methods of making and using them 有权
    用于改善细胞增殖性疾病的组合物及其制备和使用方法

    公开(公告)号:US08598313B2

    公开(公告)日:2013-12-03

    申请号:US13581288

    申请日:2011-03-11

    IPC分类号: A61K38/12

    CPC分类号: C07D513/18 C07D513/08

    摘要: In alternative embodiments, the invention provides apratoxin F and apratoxin G compounds, which include apratoxin F and apratoxin G stereoisomers, derivatives and analogs compositions and methods. In alternative embodiments, the invention provides pharmaceutical compositions and formulations comprising apratoxin F (compound 6 of FIG. 1) and apratoxin G (compound 7 of FIG. 1) and their stereoisomers, derivatives and analogs. In alternative embodiments, pharmaceutical compositions and formulations of the invention are administered in an amount sufficient to treat, prevent and/or ameliorate a disease or condition that can be ameliorated by decreasing or inhibiting cell growth, e.g., pathological, uncontrolled or unwanted cell growth, e.g., a cancer or a metastases, or any disease or condition (e.g., allergy) or infection having a hyperproliferative cell growth component.

    摘要翻译: 在替代实施方案中,本发明提供了包括阿曲毒素F和阿曲毒素G立体异构体,衍生物和类似物组合物和方法的阿曲毒素F和阿曲毒素G化合物。 在替代实施方案中,本发明提供包含阿曲毒素F(图1的化合物6)和阿曲毒素G(图1的化合物7)及其立体异构体,衍生物和类似物的药物组合物和制剂。 在替代实施方案中,本发明的药物组合物和制剂以足以治疗,预防和/或改善可以通过减少或抑制细胞生长(例如病理,不受控制或不期望的细胞生长)而改善的疾病或病症的量施用, 例如癌症或转移瘤,或任何疾病或病症(例如过敏)或具有过度增殖细胞生长成分的感染。

    COMPOSITIONS FOR AMELIORATING CELL PROLIFERATIVE DISORDERS AND METHODS OF MAKING AND USING THEM
    9.
    发明申请
    COMPOSITIONS FOR AMELIORATING CELL PROLIFERATIVE DISORDERS AND METHODS OF MAKING AND USING THEM 有权
    用于改善细胞增殖性疾病的组合物及其制备和使用它们的方法

    公开(公告)号:US20130045925A1

    公开(公告)日:2013-02-21

    申请号:US13581288

    申请日:2011-03-11

    CPC分类号: C07D513/18 C07D513/08

    摘要: In alternative embodiments, the invention provides apratoxin F and apratoxin G compounds, which include apratoxin F and apratoxin G stereoisomers, derivatives and analogs compositions and methods. In alternative embodiments, the invention provides pharmaceutical compositions and formulations comprising apratoxin F (compound 6 of FIG. 1) and apratoxin G (compound 7 of FIG. 1) and their stereoisomers, derivatives and analogs. In alternative embodiments, pharmaceutical compositions and formulations of the invention are administered in an amount sufficient to treat, prevent and/or ameliorate a disease or condition that can be ameliorated by decreasing or inhibiting cell growth, e.g., pathological, uncontrolled or unwanted cell growth, e.g., a cancer or a metastases, or any disease or condition (e.g., allergy) or infection having a hyperproliferative cell growth component.

    摘要翻译: 在替代实施方案中,本发明提供了包括阿曲毒素F和阿曲毒素G立体异构体,衍生物和类似物组合物和方法的阿曲毒素F和阿曲毒素G化合物。 在替代实施方案中,本发明提供包含阿曲毒素F(图1的化合物6)和阿曲毒素G(图1的化合物7)及其立体异构体,衍生物和类似物的药物组合物和制剂。 在替代实施方案中,本发明的药物组合物和制剂以足以治疗,预防和/或改善可以通过减少或抑制细胞生长(例如病理,不受控制或不期望的细胞生长)而改善的疾病或病症的量施用, 例如癌症或转移瘤,或任何疾病或病症(例如过敏)或具有过度增殖细胞生长成分的感染。