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    METHODS AND ASSAYS FOR QUANTIFICATION AND NORMALIZATION OF KINASE AND LIGAND BINDING
    41.
    发明申请
    METHODS AND ASSAYS FOR QUANTIFICATION AND NORMALIZATION OF KINASE AND LIGAND BINDING 审中-公开
    激酶和配体结​​合的定量和正常化的方法和测定

    公开(公告)号：WO2016100593A1

    公开(公告)日：2016-06-23

    申请号：PCT/US2015/066244

    申请日：2015-12-17

    Applicant: PHARMACYCLICS LLC

    Inventor： CHANG, Stella ,  GURURAJA, Tarikere, L. ,  CHANG, Betty, Y.

    IPC: C12Q1/48

    CPC classification number: G01N33/573 ,  G01N2333/9121

    Abstract: The invention provides methods and assay systems for both quantitative determination of a target, particularly a kinase, including a Tec family kinase, particularly BTK, and target occupancy, including the relative amount of available target associated with a target inhibitor or ligand, particularly wherein the target inhibitor or ligand is a covalent or irreversible kinase inhibitor, particularly including irreversible BTK inhibitor. The invention also relates to assays for determining target occupancy, normalized to total quantified target in a biological system or clinical sample, wherein target is quantified, normalized and occupancy determined using the same or a common assay format. In an aspect of the invention, biotinylated anti-BTK antibody and biotinylated BTK inhibitor probe are utilized in the assay format, on samples split for simultaneous or commensurate analysis.

    Abstract translation: 本发明提供了用于定量测定靶标，特别是激酶（包括Tec家族激酶，特别是BTK）和靶标占有率的方法和测定系统，包括与靶标抑制剂或配体相关的可用靶标的相对量，特别是其中 靶抑制剂或配体是共价或不可逆激酶抑制剂，特别是包括不可逆的BTK抑制剂。 本发明还涉及用于确定在生物系统或临床样品中归一化到总量化靶的靶占据率的测定法，其中使用相同或常见的测定形式确定靶标定量，归一化和占有。 在本发明的一个方面，生物素化的抗BTK抗体和生物素化的BTK抑制剂探针以测定形式用于分离用于同时或相称分析的样品。

    DENDRITIC CELL BASED VACCINE WITH BRUTON'S TYROSINE KINASE INHIBITOR
    42.
    发明申请
    DENDRITIC CELL BASED VACCINE WITH BRUTON'S TYROSINE KINASE INHIBITOR 审中-公开
    具有BRUTON'S酪氨酸激酶抑制剂的基于DENDRITIC细胞的疫苗

    公开(公告)号：WO2016044774A1

    公开(公告)日：2016-03-24

    申请号：PCT/US2015/051034

    申请日：2015-09-18

    Applicant: PHARMACYCLICS LLC

    Inventor： NATARAJAN, Gayathri ,  SATOSKAR, Abhay R. ,  TERRAZAS, Cesar

    IPC: A61K31/519

    CPC classification number: A61K31/519

    Abstract: Disclosed herein are methods, compounds, and kits comprising a BTK inhibitor for promoting dendritic cell maturation in a subject having cancer. Disclosed herein, in certain embodiments, is a pharmaceutical composition comprising an effective amount of a BTK inhibitor for promoting Th17 cell differentiation in a subject having cancer. In some embodiments, the Th17 cell differentiation leads to secretion of Th17 associated cytokines. In some embodiments, the Th17 associated cytokines include IL17A, IL17F, IL21, and IL22.

    Abstract translation: 本文公开了包含用于在具有癌症的受试者中促进树突状细胞成熟的BTK抑制剂的方法，化合物和试剂盒。 在某些实施方案中，本文公开了包含有效量的用于在具有癌症的受试者中Th17细胞分化的BTK抑制剂的药物组合物。 在一些实施方案中，Th17细胞分化导致Th17相关细胞因子的分泌。 在一些实施方案中，Th17相关细胞因子包括IL17A，IL17F，IL21和IL22。

    INHIBITORS OF BRUTON'S TYROSINE KINASE
    44.
    发明申请
    INHIBITORS OF BRUTON'S TYROSINE KINASE 审中-公开

    公开(公告)号：WO2016004280A3

    公开(公告)日：2016-01-07

    申请号：PCT/US2015/038947

    申请日：2015-07-02

    Applicant: PHARMACYCLICS LLC

    Inventor： CHEN, Wei ,  JIA, Zhaozhong, J.

    IPC: A61K31/4166

    Abstract: Described herein are heteroaryl compounds as kinase inhibitors. Methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases are also described. Described herein are inhibitors of Bruton's tyrosine kinase (Btk). Also described herein are irreversible inhibitors of Btk. Also described herein are reversible inhibitors of Btk. Further described are irreversible inhibitors ofBtk that form a covalent bond with a cysteine residue on Btk. Further described herein are irreversible inhibitors of other tyrosine kinases, wherein the other tyrosine kinases share homology with Btk by having a cysteine residue (including a Cys 481 residue) that can form a covalent bond with the irreversible inhibitor (such tyrosine kinases, are referred herein as "Btk tyrosine kinase cysteine homologs").

    BTK INHIBITOR COMBINATIONS AND DOSING REGIMEN
    45.
    发明申请
    BTK INHIBITOR COMBINATIONS AND DOSING REGIMEN 审中-公开
    BTK抑制剂组合和剂量方案

    公开(公告)号：WO2016106381A1

    公开(公告)日：2016-06-30

    申请号：PCT/US2015/067504

    申请日：2015-12-22

    Applicant: PHARMACYCLICS LLC

    Inventor： JAGLOWSKI, Samantha M.

    IPC: A61K31/52

    CPC classification number: 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

    Abstract: 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.

    Abstract translation: 本文公开了施用BTK抑制剂（例如伊布他坦）和用于治疗血液恶性肿瘤的抗CD20治疗剂的组合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的血液恶性肿瘤的组合给药方案，其包括第一阶段和第二阶段，其中第一阶段是施用BTK抑制剂作为第一阶段的单一药剂治疗 延长的时间段，第二阶段是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，第一延长的时间段是长达90天的时间段。

    BET INHIBITOR AND BRUTON'S TYROSINE KINASE INHIBITOR COMBINATIONS
    47.
    发明申请
    BET INHIBITOR AND BRUTON'S TYROSINE KINASE INHIBITOR COMBINATIONS 审中-公开
    BET抑制剂和BRUTON的酪氨酸激酶抑制剂组合

    公开(公告)号：WO2016014859A1

    公开(公告)日：2016-01-28

    申请号：PCT/US2015/041841

    申请日：2015-07-23

    Applicant: PHARMACYCLICS LLC

    Inventor： KUO, Hsu-Ping ,  HSIEH, Hsin-Kang ,  CHANG, Betty

    IPC: A61P35/00 ,  A61P35/02 ,  A61K31/519 ,  C07D401/04

    CPC classification number: A61K31/519 ,  A61K31/4745 ,  A61K31/4747 ,  A61K31/551 ,  A61K45/06 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158 ,  G01N33/57407 ,  G01N33/57426 ,  G01N2333/4704 ,  G01N2800/52 ,  A61K2300/00

    Abstract: Disclosed herein are methods, compositions, and kits for treating a B-cell malignancy comprising administering a combination of a BTK inhibitor (e.g., ibrutinib) and a BET inhibitor. Also disclosed herein are methods, compositions, and kits for treating a BTK-resistant B cell malignancy, or a MYC-driven B cell malignancy comprising administering a combination of a BTK inhibitor (e.g., ibrutinib) and a BET inhibitor. Further disclosed herein are methods of evaluating a patient having a B-cell malignancy for treatment with a combination of a BTK inhibitor (e.g., ibrutinib) and a BET inhibitor based on the MYC expression level of the patient.

    Abstract translation: 本文公开了用于治疗B细胞恶性肿瘤的方法，组合物和试剂盒，其包括施用BTK抑制剂（例如伊布他坦）和BET抑制剂的组合。 本文还公开了用于治疗BTK抗性B细胞恶性肿瘤或MYC驱动的B细胞恶性肿瘤的方法，组合物和试剂盒，其包括施用BTK抑制剂（例如伊布他坦）和BET抑制剂的组合。 本文进一步公开的是基于患者的MYC表达水平评估具有B细胞恶性肿瘤以治疗BTK抑制剂（例如伊布他他布）和BET抑制剂的组合的患者的方法。

    INHIBITORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE
    49.
    发明申请
    INHIBITORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 审中-公开
    白细胞介素-1受体相关激酶的抑制剂

    公开(公告)号：WO2017205766A1

    公开(公告)日：2017-11-30

    申请号：PCT/US2017/034721

    申请日：2017-05-26

    Applicant: PHARMACYCLICS LLC

    Inventor： CHEN, Wei ,  JIA, Zhaozhong, J. ,  THOMAS, William, D. ,  WONE, David

    IPC: C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  A61K31/519 ,  A61P35/00

    Abstract: Disclosed herein are inhibitors of IRAK protein kinase of formula (I). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the IRAK inhibitors are described, 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: 本文公开了式（I）的IRAK蛋白激酶的抑制剂。 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IRAK抑制剂的方法用于治疗自身免疫性疾病或病症，异质性免疫性疾病或病症，癌症（包括淋巴瘤和炎症性疾病或病症）。

    METHOD OF TREATMENT OF FOLLICULAR LYMPHOMA WITH A BTK INHIBITOR
    50.
    发明申请
    METHOD OF TREATMENT OF FOLLICULAR LYMPHOMA WITH A BTK INHIBITOR 审中-公开
    用BTK抑制剂治疗卵巢淋巴瘤的方法

    公开(公告)号：WO2017087947A3

    公开(公告)日：2017-05-26

    申请号：PCT/US2016/063085

    申请日：2016-11-21

    Applicant: PHARMACYCLICS LLC ,  WANG, Zhengyuang

    Inventor： WANG, Zhengyuang ,  CHANG, Betty ,  CHEUNG, Leo ,  ECKERT, Karl ,  SCHWEIGHOFER, Karl ,  WU, Shiquan

    IPC: C12Q1/68 ,  A61P35/00 ,  A61K31/519

    Abstract: Disclosed herein are methods of treating follicular lymphoma in an individual in need thereof wherein the individual has an overexpression of one or more genes selected from CALB2, P2RY11 (PPAN-P2RY11), DNAJC8, TTC19, VCAMl, CSAG3, GP1BA, RPA1, RSC1A1, STS-1 (UBASH3B), ADPRM (C170RF48) and FILIPl, or a normal expression or underexpression of one or more genes selected from CERCAM, POM121C (LOC100131972), PPP1R3D, PLOD2, SDHA (SDHAP3), OSBPL2, HCFC1R1, and DHRS7, which method comprises administering or continuing to administer to the individual a therapeutically effective amount of ibrutinib or a pharmaceutically acceptable salt or solvate thereof.

    Abstract translation: 本文公开了治疗有需要的个体中的滤泡性淋巴瘤的方法，其中所述个体具有选自CALB2，P2RY11（PPAN-P2RY11），DNAJC8，TTC19，VCAM1，或其组合的一种或多种基因的过表达， （LOC100131972），PPP1R3D，PLOD2，SDHA（SDHAP3）中的一种或多种基因的正常表达或表达不足，或选自CERCAM，POM121C（LOC100131972），PPP1R3D，PLOD2，SDHA ，OSBPL2，HCFC1R1和DHRS7，所述方法包括给予或继续给予个体治疗有效量的依鲁替尼或其药学上可接受的盐或溶剂化物。

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