公开(公告)号：EP2650294A1

公开(公告)日：2013-10-16

申请号：EP13166272.8

申请日：2010-10-12

申请人： Pharmacyclics, Inc.

发明人： Chen, Wei ,  Loury, David J. ,  Mody, Tarak D. ,  Verner, Erik ,  Smyth, Mark Stephen ,  Luo, Wenchen

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P19/02 ,  A61P19/10

CPC分类号： C07D487/04 ,  C07D519/00

摘要： Described herein are kinase inhibitor compounds of formula (II), methods for synthesizing such inhibitors, and their use in the treatment of diseases.

Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.

摘要翻译： 本文描述了式（II）的激酶抑制剂化合物，合成这种抑制剂的方法，以及它们在治疗疾病中的用途。 本文进一步描述了用于确定蛋白质（包括激酶）的适当抑制剂的方法，测定和系统。

公开(公告)号：EP2201840A1

公开(公告)日：2010-06-30

申请号：EP10155834.4

申请日：2006-12-28

申请人： Pharmacyclics, Inc.

发明人： Honigberg, Lee ,  Verner, Erik ,  Pan, Zhengying

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/04 ,  A61P35/00

CPC分类号： A61K31/52 ,  A61K9/4825 ,  A61K31/00 ,  A61K31/519 ,  A61K39/3955 ,  A61K45/06 ,  A61K2300/00 ,  C07D487/04 ,  C07K16/2887 ,  C07K2317/24

摘要： Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described arc irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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.

公开(公告)号：EP2526933B1

公开(公告)日：2015-02-25

申请号：EP12166301.7

申请日：2006-12-28

申请人： Pharmacyclics, Inc.

发明人： Honigberg, Lee ,  Verner, Erik ,  Pan, Zhengying ,  Mody, Tarak

IPC分类号： A61K31/00 ,  A61K31/519 ,  A61P35/00 ,  A61P35/02 ,  C07D487/04

CPC分类号： A61K31/52 ,  A61K9/4825 ,  A61K31/00 ,  A61K31/519 ,  A61K39/3955 ,  A61K45/06 ,  A61K2300/00 ,  C07D487/04 ,  C07K16/2887 ,  C07K2317/24

摘要： Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described arc irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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。 还描述了Btk的电弧不可逆抑制剂。 公开了制备化合物的方法。 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。

公开(公告)号：EP2201840B1

公开(公告)日：2011-11-02

申请号：EP10155834.4

申请日：2006-12-28

申请人： Pharmacyclics, Inc.

发明人： Honigberg, Lee ,  Verner, Erik ,  Pan, Zhengying

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/04 ,  A61P35/00

CPC分类号： A61K31/52 ,  A61K9/4825 ,  A61K31/00 ,  A61K31/519 ,  A61K39/3955 ,  A61K45/06 ,  A61K2300/00 ,  C07D487/04 ,  C07K16/2887 ,  C07K2317/24

摘要： Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described arc irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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.

公开(公告)号：EP2954900A1

公开(公告)日：2015-12-16

申请号：EP15170739.5

申请日：2008-03-27

申请人： Pharmacyclics, Inc.

发明人： Honigberg, Lee ,  Verner, Erik ,  Buggy, Joseph, J ,  Loury, David ,  Chen, Wei

IPC分类号： A61K31/52 ,  A61P29/00 ,  A61P35/00 ,  A61K31/519

CPC分类号： C07D487/04 ,  A61K31/52 ,  C07D471/04 ,  C12Q1/485 ,  G01N33/57426 ,  G01N2440/14 ,  G01N2500/00

摘要： (R)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one for use in treating a B-cell proliferative cancer.

摘要翻译： （R）-1-（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-one用于治疗B细胞增殖性癌症。

公开(公告)号：EP2561875A2

公开(公告)日：2013-02-27

申请号：EP12172842.2

申请日：2008-03-27

申请人： Pharmacyclics, Inc.

发明人： Honigberg, Lee ,  Verner, Erik ,  Buggy, Joseph, J. ,  Loury, David ,  Chen, Wei ,  Mody, Tarak

IPC分类号： A61K31/519 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/52 ,  C07D471/04 ,  C12Q1/485 ,  G01N33/57426 ,  G01N2440/14 ,  G01N2500/00

摘要： Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.

摘要翻译： 本文描述的是不可逆的激酶抑制剂化合物，合成这种不可逆抑制剂的方法，以及使用这种不可逆抑制剂治疗疾病的方法。 本文进一步描述了用于确定蛋白质（包括激酶）的适当不可逆抑制剂的方法，测定和系统。

公开(公告)号：EP2529622A1

公开(公告)日：2012-12-05

申请号：EP12166302.5

申请日：2006-12-28

申请人： Pharmacyclics, Inc.

发明人： Honigberg, Lee ,  Verner, Erik ,  Pan, Zhengying

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/04 ,  A61P35/00

CPC分类号： A61K31/52 ,  A61K9/4825 ,  A61K31/00 ,  A61K31/519 ,  A61K39/3955 ,  A61K45/06 ,  A61K2300/00 ,  C07D487/04 ,  C07K16/2887 ,  C07K2317/24

摘要： Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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。 公开了制备化合物的方法。 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。

公开(公告)号：EP2526933A3

公开(公告)日：2012-12-05

申请号：EP12166301.7

申请日：2006-12-28

申请人： Pharmacyclics, Inc.

发明人： Honigberg, Lee ,  Verner, Erik ,  Pan, Zhengying ,  Mody, Tarak

IPC分类号： A61K31/00 ,  A61K31/519 ,  A61P35/00 ,  A61P35/02 ,  C07D487/04

CPC分类号： A61K31/52 ,  A61K9/4825 ,  A61K31/00 ,  A61K31/519 ,  A61K39/3955 ,  A61K45/06 ,  A61K2300/00 ,  C07D487/04 ,  C07K16/2887 ,  C07K2317/24

摘要： Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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 B-cell proliferative disorders.

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。 还描述了Btk的不可逆抑制剂。 公开了制备这些化合物的方法。 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联合使用Btk抑制剂的方法，用于治疗B细胞增殖性疾病。

公开(公告)号：EP2561875A3

公开(公告)日：2013-06-12

申请号：EP12172842.2

申请日：2008-03-27

申请人： Pharmacyclics, Inc.

发明人： Honigberg, Lee ,  Verner, Erik ,  Buggy, Joseph, J. ,  Loury, David ,  Chen, Wei ,  Mody, Tarak

IPC分类号： A61K31/519 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/52 ,  C07D471/04 ,  C12Q1/485 ,  G01N33/57426 ,  G01N2440/14 ,  G01N2500/00

摘要： Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.

公开(公告)号：EP2560007A1

公开(公告)日：2013-02-20

申请号：EP12172843.0

申请日：2008-03-27

申请人： Pharmacyclics, Inc.

发明人： Honigberger, Lee ,  Verner, Erik ,  Buggy, Joseph J. ,  Loury, David ,  Chen, Wei

IPC分类号： G01N33/68

CPC分类号： C07D487/04 ,  A61K31/52 ,  C07D471/04 ,  C12Q1/485 ,  G01N33/57426 ,  G01N2440/14 ,  G01N2500/00

摘要： Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.

摘要翻译： 本文描述的是不可逆激酶抑制剂化合物，用于合成这种不可逆抑制剂的方法，以及使用这种不可逆抑制剂治疗疾病的方法。 本文进一步描述了用于测定蛋白质（包括激酶）的合适的不可逆抑制剂的方法，测定和系统。