公开(公告)号：EP2543375A1

公开(公告)日：2013-01-09

申请号：EP12172840.6

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： A61K31/52 ,  A61P29/00 ,  A61P35/00 ,  A61K31/519 ,  C07D253/06 ,  C07D487/04 ,  C07D473/34 ,  C07D471/04

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。

公开(公告)号：EP2529621A1

公开(公告)日：2012-12-05

申请号：EP12166298.5

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.

公开(公告)号：EP2443929A1

公开(公告)日：2012-04-25

申请号：EP12151943.3

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： 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.

公开(公告)号：EP2548558A1

公开(公告)日：2013-01-23

申请号：EP12172841.4

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： A61K31/52 ,  A61P29/00 ,  A61P35/00 ,  A61K31/519 ,  C07D253/06 ,  C07D487/04 ,  C07D473/34 ,  C07D471/04

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 having the structure:

wherein:

is an active site binding moiety selected from


Y is a linker moiety and G is a Michael acceptor moiety; 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： 本文描述的是具有以下结构的不可逆激酶抑制剂化合物：其中：是选自Y的活性位点结合部分是连接体部分，G是迈克尔受体部分; 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。

公开(公告)号：EP2526933A2

公开(公告)日：2012-11-28

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。 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。 公开了使用Btk抑制剂的方法，单独或与其它治疗剂组合用于治疗B细胞增殖性疾病。

公开(公告)号：EP2526771A1

公开(公告)日：2012-11-28

申请号：EP12166300.9

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.