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    SOLVATED FORMS OF A BRUTON'S TYROSINE KINASE INHIBITOR
    61.
    发明申请
    SOLVATED FORMS OF A BRUTON'S TYROSINE KINASE INHIBITOR 审中-公开
    BRUTON的酪氨酸激酶抑制剂的溶解形式

    公开(公告)号：WO2016160598A1

    公开(公告)日：2016-10-06

    申请号：PCT/US2016/024305

    申请日：2016-03-25

    Applicant: PHARMACYCLICS LLC

    Inventor： GOLDMAN, Erick ,  SMYTH, Mark, Stephen ,  BONNAUD, Thierry ,  MUNOZ GARCIA, Alberto ,  WORRALL, Christopher, Peter

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

    CPC classification number: C07D487/04 ,  A61K31/519 ,  G01N23/20075

    Abstract: Described herein are solvates of the Bruton's tyrosine kinase (Btk) inhibitor l-((R)-3-(4-amino- 3 -(4-phenoxyphenyl)- lH-pyrazolo[3,4-d]pyrimidin- 1 -yl)piperidin- 1 -yl)prop-2-en- 1 -one, including crystalline forms, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the solvates, as well as methods of using the solvates, 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: 本文描述了Bruton的酪氨酸激酶（Btk）抑制剂1 - （（R）-3-（4-氨基-3-（4-苯氧基苯基）-1H-吡唑并[3,4-d]嘧啶-1-基 ）哌啶-1-基）丙-2-烯-1-酮，包括结晶形式及其药学上可接受的盐。 还公开了包括溶剂化物的药物组合物，以及使用溶剂合物单独或与其它治疗剂组合用于治疗自身免疫疾病或病症，异种免疫疾病或病症，癌症，包括淋巴瘤和炎性疾病的方法 或条件。

    PHARMACEUTICAL FORMULATIONS OF BRUTON'S TYROSINE KINASE INHIBTOR
    62.
    发明申请
    PHARMACEUTICAL FORMULATIONS OF BRUTON'S TYROSINE KINASE INHIBTOR 审中-公开
    BRUTON的酪氨酸激酶抑制剂的药物制剂

    公开(公告)号：WO2016141068A1

    公开(公告)日：2016-09-09

    申请号：PCT/US2016/020467

    申请日：2016-03-02

    Applicant: PHARMACYCLICS LLC

    Inventor： ATLURI, Harisha ,  CHONG, Ching, Wah ,  KUEHL, Robert ,  TAN, Heow

    IPC: A61K31/436 ,  A61K31/519

    CPC classification number: A61K9/2054 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2095 ,  A61K31/519

    Abstract: Described herein are pharmaceutical formulations of Bruton's tyrosine kinase (Btk) inhibitor 1- ((R)-3-(4-amino-3-(4-phenoxyphenyl)-lH-pyrazolo[3,4-d]pyrimidin-l-yl)piperidin-l-yl)prop-2- en-l-one. Also disclosed are methods of using the Btk inhibitor, 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: 本文描述的是布鲁顿酪氨酸激酶（Btk）抑制剂1-（（R）-3-（4-氨基-3-（4-苯氧基苯基）-1H-吡唑并[3,4-d]嘧啶-1-基 ）哌啶-1-基）丙-2-烯-1-酮。 还公开了使用Btk抑制剂单独或与其它治疗剂组合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的方法。

    METHODS FOR TREATING EGFR MUTANT DISORDERS
    65.
    发明申请
    METHODS FOR TREATING EGFR MUTANT DISORDERS 审中-公开
    治疗EGFR突变性疾病的方法

    公开(公告)号：WO2016029175A1

    公开(公告)日：2016-02-25

    申请号：PCT/US2015/046401

    申请日：2015-08-21

    Applicant: PHARMACYCLICS LLC

    Inventor： CHANG, Betty ,  KINOSHITA, Taisei

    IPC: A61K31/00

    CPC classification number: A61K31/519 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/5377 ,  A61K45/06 ,  A61K2300/00

    Abstract: Disclosed herein are methods, systems, and kits for patient stratification based on the presence or absence of at least one of a modification at amino acid position 858 in EGFR and a deletion from amino acid position 746 to amino acid position 750 in EGFR. Further described are methods of monitoring a therapeutic regimen, and optimizing a therapeutic regimen. Additional modifications in EGFR include modification at amino acid position 790, modifications in KRAS, and expression level of PTEN.

    Abstract translation: 本文公开了基于在EGFR中氨基酸位置858处的修饰和EGFR中氨基酸位置746至氨基酸位置750的缺失中至少一种的存在或不存在的用于患者分层的方法，系统和试剂盒。 进一步描述了监测治疗方案并优化治疗方案的方法。 EGFR的其他修饰包括在氨基酸位置790的修饰，KRAS的修饰和PTEN的表达水平。

    INHIBITORS OF BRUTON'S TYROSINE KINASE
    66.
    发明申请
    INHIBITORS OF BRUTON'S TYROSINE KINASE 审中-公开

    公开(公告)号：WO2016019237A3

    公开(公告)日：2016-02-04

    申请号：PCT/US2015/043102

    申请日：2015-07-31

    Applicant: PHARMACYCLICS LLC

    Inventor： CHEN, Wei ,  WANG, Longcheng ,  JIA, Zhaozhong, J. ,  PALMER, James, T.

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

    Abstract: Described herein are cyano containing bicyciic heteroaryl compounds that are irreversible inhibitors of Bruton's tyrosine kinase (BTK) activity and pharmaceutical compositions containing the same for the teatment of BTK mediated disorders in a subject. Methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases such as cancer, mastocytosis, B-cell lymphoma, lupus and osteoporosis are also described.

    INHIBITORS OF BRUTON'S TYROSINE KINASE
    68.
    发明申请
    INHIBITORS OF BRUTON'S TYROSINE KINASE 审中-公开
    BRUTON的酪氨酸激酶抑制剂

    公开(公告)号：WO2016004280A2

    公开(公告)日：2016-01-07

    申请号：PCT/US2015038947

    申请日：2015-07-02

    Applicant: PHARMACYCLICS LLC

    Inventor： CHEN WEI ,  JIA ZHAOZHONG J

    IPC: F24J2/04

    CPC classification number: 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.

    Abstract translation: 本文描述的是作为激酶抑制剂的杂芳基化合物。 还描述了合成这种抑制剂的方法，以及在治疗疾病中使用这些抑制剂的方法。

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