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    BTK INHIBITOR COMBINATIONS AND DOSING REGIMEN
    5.
    发明公开
    BTK INHIBITOR COMBINATIONS AND DOSING REGIMEN 审中-公开
    BTK抑制剂组合和给药方案

    公开(公告)号：EP3236968A1

    公开(公告)日：2017-11-01

    申请号：EP15874346.8

    申请日：2015-12-22

    申请人： Pharmacyclics LLC

    发明人： JAGLOWSKI, Samantha M.

    IPC分类号： A61K31/52

    CPC分类号： A61K31/52 ,  A61K31/167 ,  A61K31/196 ,  A61K31/495 ,  A61K31/519 ,  A61K31/675 ,  A61K39/39558 ,  A61K2039/505 ,  A61K2039/545 ,  C07K16/2887 ,  C07K2317/21 ,  A61K2300/00 ,  A61K31/454 ,  A61K31/606 ,  A61K31/704 ,  A61K31/7076

    摘要： Disclosed herein are methods and combination dosing regimen of administering a combination of a BTK inhibitor (e.g. ibrutinib) and an anti-CD20 therapeutic agent for the treatment of a hematologic malignancy. In one aspect is a combination dosing regimen for the treatment of a hematologic malignancy in a subject in need thereof comprising a first phase and a second phase, wherein the first phase is an administration of a BTK inhibitor as a single-agent treatment for a first extended period of time, and the second phase is an administration of a combination of the BTK inhibitor and an anti-CD20 therapeutic agent for a second extended period of time. In one embodiment, the first extended period of time is a period of up to 90 days.

    摘要翻译： 本文公开了施用BTK抑制剂（例如依鲁替尼）和抗CD20治疗剂的组合用于治疗血液恶性肿瘤的方法和组合给药方案。 一方面是用于治疗有需要的受试者中的血液恶性肿瘤的组合给药方案，其包含第一阶段和第二阶段，其中第一阶段是作为单一药剂治疗的BTK抑制剂的第一阶段治疗，用于第一阶段 延长的时间段，并且第二阶段是在第二延长的时间段内施用BTK抑制剂和抗CD20治疗剂的组合。 在一个实施例中，第一延长时间段是长达90天的时间段。

    INHIBITORS OF BRUTON'S TYROSINE KINASE
    9.
    发明公开
    INHIBITORS OF BRUTON'S TYROSINE KINASE 审中-公开
    酪氨酸激酶抑制剂

    公开(公告)号：EP3174539A1

    公开(公告)日：2017-06-07

    申请号：EP15827550.3

    申请日：2015-07-31

    申请人： Pharmacyclics, LLC

    发明人： CHEN, Wei ,  WANG, Longcheng ,  JIA, Zhaozhong J.

    IPC分类号： A61K31/519 ,  C07D487/00 ,  A61P35/00

    CPC分类号： C07D487/04 ,  A61K31/4162

    摘要： Disclosed herein are amido compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. 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.

    摘要翻译： 本文公开了与布鲁顿酪氨酸激酶（Btk）形成共价键的酰胺基化合物。 还描述了Btk的不可逆抑制剂。 还公开了包含该化合物的药物组合物。 单独或与其他治疗剂组合使用Btk抑制剂的方法用于治疗自身免疫疾病或病症，异质性免疫疾病或病症，癌症（包括淋巴瘤）和炎性疾病或病症。

    PURINONE COMPOUNDS AS KINASE INHIBITORS
    10.
    发明公开
    PURINONE COMPOUNDS AS KINASE INHIBITORS 审中-公开
    PURINONVERBINDUNGEN ALS KINASEHEMMER

    公开(公告)号：EP3147285A3

    公开(公告)日：2017-05-17

    申请号：EP16170469.7

    申请日：2013-01-30

    申请人： Pharmacyclics LLC

    发明人： YAN, Shunqi ,  WANG, Longcheng ,  FRYE, Leah, Lynn ,  CHEN, Wei ,  LOURY, David, J

    IPC分类号： C07D473/32 ,  A61K31/52 ,  A61P37/00 ,  A61P35/00

    CPC分类号： C07D473/34

    摘要： 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.

    摘要翻译： 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。