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53 条记录 (耗时 0.038 秒)

    PARP inhibitor compounds, compositions and methods of use
    2.
    发明授权
    PARP inhibitor compounds, compositions and methods of use 有权
    PARP抑制剂化合物，组合物和使用方法

    公开(公告)号：US08894989B2

    公开(公告)日：2014-11-25

    申请号：US13527158

    申请日：2012-06-19

    申请人： Weizheng Xu ,  Greg Delahanty ,  Ling Wei ,  Jie Zhang

    发明人： Weizheng Xu ,  Greg Delahanty ,  Ling Wei ,  Jie Zhang

    IPC分类号： A61K45/00 ,  A01N43/58 ,  C07D491/00

    CPC分类号： A61K31/519 ,  A61K31/53 ,  C07D487/06 ,  C07D519/00

    摘要： The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly(ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.

    摘要翻译： 本发明涉及抑制聚（ADP-核糖）聚合酶（PARP）并可用于癌症治疗剂的化学敏化的四氮芥苯并三氮唑-3-酮化合物。 周围神经病变的诱导是许多常规和较新的化学疗法的常见副作用。 本发明还提供了可靠地预防或治愈化疗诱发的神经病变的方法。 本发明还涉及所公开的PARP抑制剂化合物在增强化疗剂如替莫唑胺的功效中的用途。 本发明还涉及所公开的PARP抑制剂化合物对肿瘤细胞对电离辐射进行放射增敏的用途。 本发明还涉及所公开的PARP抑制剂化合物用于治疗具有DNA修复缺陷的癌症的用途。

    Diazabenzo[de] anthracen-3-one compounds and methods for inhibiting PARP
    3.
    发明授权
    Diazabenzo[de] anthracen-3-one compounds and methods for inhibiting PARP 有权
    二氮杂苯并[de]蒽-3-酮化合物和抑制PARP的方法

    公开(公告)号：US08883787B2

    公开(公告)日：2014-11-11

    申请号：US13914067

    申请日：2013-06-10

    申请人： Eisai Inc.

    发明人： Weizheng Xu ,  Greg Delahanty ,  Jie Zhang

    IPC分类号： A61K31/5025

    CPC分类号： C07D491/06 ,  A61K31/495 ,  A61K31/5025

    摘要： The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.

    摘要翻译： 本发明涉及抑制聚（ADP-核糖）聚合酶（“PARP”）的二氮杂苯并[de]蒽-3-酮化合物，含有这些化合物的组合物和使用这些PARP抑制剂治疗，预防和/或改善 本文所述条件的效果。

    Thiolactones
    5.
    发明授权
    Thiolactones 失效
    硫内酯

    公开(公告)号：US07968593B2

    公开(公告)日：2011-06-28

    申请号：US12472251

    申请日：2009-05-26

    申请人： Barbara S. Slusher ,  Takashi Tsukamoto

    发明人： Barbara S. Slusher ,  Takashi Tsukamoto

    IPC分类号： A61K31/382 ,  A61K31/381 ,  C07D335/06 ,  C07D335/04

    CPC分类号： C07D335/02 ,  C07D335/06

    摘要： This invention provides new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, inhibiting angiogenesis, effecting a TGF-β activity or a neuronal activity, and treating a glutamate abnormality, a compulsive disorder, neuropathy, pain, a prostate disease, cancer, Huntington's disease, diabetes, a retinal disorder or glaucoma.

    摘要翻译： 本发明提供新的化合物，药物组合物和包含这些化合物的诊断试剂，以及使用这些化合物抑制NAALADase酶活性的方法，检测NAALADase水平被改变的疾病，抑制血管发生，影响TGF- 活动或神经元活动，以及治疗谷氨酸异常，强迫症，神经病，疼痛，前列腺疾病，癌症，亨廷顿氏病，糖尿病，视网膜病症或青光眼。

    Compounds having selective activity for retinoid X receptors, and means for modulation of processes mediated by retinoid X receptors
    9.
    发明授权
    Compounds having selective activity for retinoid X receptors, and means for modulation of processes mediated by retinoid X receptors 失效
    对类视黄醇X受体具有选择性活性的化合物，以及调节由类视黄醇X受体介导的过程的方法

    公开(公告)号：US07655699B1

    公开(公告)日：2010-02-02

    申请号：US08141246

    申请日：1993-10-22

    申请人： Marcus F. Boehm ,  Richard A. Heyman

    发明人： Marcus F. Boehm ,  Richard A. Heyman

    IPC分类号： C07D63/36 ,  A01N37/10 ,  A61K31/19

    CPC分类号： A61K31/192 ,  A61K9/0019 ,  A61K9/0031 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/4825 ,  A61K9/4866

    摘要： Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, pyrrole, and polyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

    摘要翻译： 调节视网膜X受体介导的方法的化合物，组合物和方法，使用对类维生素A受体（RXR）亚类的成员具有选择性的类视黄醇样化合物，优于视黄酸受体（RAR）亚类的成员， 。 这些化合物的实例是二环苄基，吡啶基，噻吩，呋喃基，吡咯和多烯酸衍生物，包括碳环多烯酸。 所公开的方法使用化合物调节由视黄醇X受体选择性介导的过程。

    Monoclonal antibodies that specifically block biological activity of a tumor antigen
    10.
    发明授权
    Monoclonal antibodies that specifically block biological activity of a tumor antigen 有权

    公开(公告)号：US10509037B2

    公开(公告)日：2019-12-17

    申请号：US15454412

    申请日：2017-03-09

    申请人： Eisai, Inc.

    发明人： Luigi Grasso ,  Nicholas C. Nicolaides ,  Philip M. Sass

    IPC分类号： G01N33/574 ,  C07K16/28 ,  C07K16/30 ,  A61K49/00 ,  A61K39/00

    摘要： This invention relates to novel monoclonal antibodies that specifically bind to the alpha-folate receptor. In some embodiments, the antibodies inhibit a biological activity of folate receptor-α (FR-α). The antibodies are useful in the treatment of certain cancers, particularly cancers that have increased cell surface expression of the alpha-folate receptor (“FR-α”), such as ovarian, breast, renal, colorectal, lung, endometrial, or brain cancer. The invention also relates to cells expressing the monoclonal antibodies, antibody derivatives, such as chimeric and humanized monoclonal antibodies, antibody fragments, and methods of detecting and treating cancer using the antibodies, derivatives, and fragments.