PURINONE COMPOUNDS AS KINASE INHIBITORS
    111.
    发明申请
    PURINONE COMPOUNDS AS KINASE INHIBITORS 审中-公开
    嘌呤酮化合物作为激酶抑制剂

    公开(公告)号:WO2015002894A1

    公开(公告)日:2015-01-08

    申请号:PCT/US2014/044922

    申请日:2014-06-30

    CPC classification number: C07D473/34 A61K31/52

    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

    Abstract translation: 本文公开了与布鲁顿酪氨酸激酶(Btk)形成共价键的化合物。 也描述了Btk的不可逆抑制剂。 此外,还描述了Btk的可逆抑制剂。 还公开了包含化合物的药物组合物。 单独或与其它治疗剂组合使用Btk抑制剂的方法用于治疗自身免疫性疾病或病症,异种免疫疾病或病症,癌症,包括淋巴瘤和炎性疾病或病症。

    COMPANION DIAGNOSTICS FOR TEC FAMILY KINASE INHIBITOR THERAPY
    113.
    发明申请
    COMPANION DIAGNOSTICS FOR TEC FAMILY KINASE INHIBITOR THERAPY 审中-公开
    TEC家族激素抑制剂治疗的组合诊断

    公开(公告)号:WO2014059368A1

    公开(公告)日:2014-04-17

    申请号:PCT/US2013/064688

    申请日:2013-10-11

    Abstract: The invention provides methods, assays and systems for determining the efficacy of a TEC family kinase inhibitor on a target kinase. The methods, assays and systems relate to determining the occupancy of a target kinase by a TEC family kinase inhibitor (e.g., BTK inhibitors). Such quantitative measurements are used to inform therapeutic treatment and the over-all health care management of a subject. For example, diagnostic kits for diagnosing, prognosing, and monitoring a disease or indication benefitting from treatment with a TEC family kinase inhibitor are provided. In another example, diagnostic kits for identifying responders to TEC family kinase inhibitor therapy, determining therapeutic regimens, and detecting resistance to TEC family kinase inhibitor also are provided.

    Abstract translation: 本发明提供用于确定TEC家族激酶抑制剂对靶激酶的功效的方法,测定和系统。 方法,测定和系统涉及确定TEC家族激酶抑制剂(例如BTK抑制剂)对靶激酶的占据。 这种定量测量用于指导治疗和治疗受试者的全部保健管理。 例如,提供用于诊断,预测和监测受益于用TEC家族激酶抑制剂治疗的疾病或指征的诊断试剂盒。 在另一个实例中,提供用于鉴定TEC家族激酶抑制剂治疗的应答​​者,确定治疗方案和检测对TEC家族激酶抑制剂的抗性的诊断试剂盒。

    METHODS AND COMPOSITIONS FOR INHIBITION OF BONE RESORPTION
    116.
    发明申请
    METHODS AND COMPOSITIONS FOR INHIBITION OF BONE RESORPTION 审中-公开
    用于抑制骨恢复的方法和组合物

    公开(公告)号:WO2013003629A3

    公开(公告)日:2013-04-11

    申请号:PCT/US2012044708

    申请日:2012-06-28

    Abstract: Disclosed herein are methods and compounds for inhibiting bone and/or cartilage resorption in an individual. The methods comprise administering to the individual a composition comprising a therapeutically effective amount of a compound that is an irreversible inhibitor of a Bruton's tyrosine kinase (BTK), or a pharmaceutically acceptable salt thereof. Also described are irreversible inhibitors of Btk and methods for the preparation of the compounds. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the inhibition of cancer metastasis, and for inhibition of bone or cartilage resorption in cancer patients.

    Abstract translation: 本文公开了用于抑制个体中的骨和/或软骨再吸收的方法和化合物。 所述方法包括向个体施用包含治疗有效量的化合物或其药学上可接受的盐的组合物,所述化合物是布鲁顿氏酪氨酸激酶(BTK)的不可逆抑制剂。 还描述了Btk的不可逆抑制剂和制备该化合物的方法。 还公开了包含该化合物的药物组合物。 公开了单独或与其他治疗剂组合使用Btk抑制剂的方法,用于抑制癌症转移,以及抑制癌症患者中的骨或软骨再吸收。

    TREATMENT OF NON-LOCALIZED INFLAMMATION WITH PAN-HDAC INHIBITORS
    119.
    发明申请
    TREATMENT OF NON-LOCALIZED INFLAMMATION WITH PAN-HDAC INHIBITORS 审中-公开
    用PAN-HDAC抑制剂治疗非局部化的炎症

    公开(公告)号:WO2010123507A1

    公开(公告)日:2010-10-28

    申请号:PCT/US2009/041726

    申请日:2009-10-07

    Abstract: Described herein are compositions and methods for treating a subject suffering from a non-localized inflammatory condition (or any symptoms associated with such inflammation), including systemic inflammation, and inflammatory conditions affecting the large portions of or the whole body, or sepsis by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a compound that is a pan-HDAC inhibitor. Also described herein are methods for decreasing iNOS and cytokine expression by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a compound that is a pan-HDAC inhibitor.

    Abstract translation: 本文描述的是用于治疗患有非局部炎症状况(或与此类炎症相关的任何症状)的受试者(包括全身性炎症)和影响大部分或全身或炎症的受试者或败血症的组合物和方法, 该受试者包含治疗有效量的泛 - HDAC抑制剂的化合物的药物组合物。 本文还描述了通过向受试者施用包含治疗有效量的作为pan-HDAC抑制剂的化合物的药物组合物来降低iNOS和细胞因子表达的方法。

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