公开(公告)号：US20100041677A1

公开(公告)日：2010-02-18

申请号：US12499002

申请日：2009-07-07

Applicant: Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

Inventor： Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

IPC: A61K31/519 ,  A61P37/06

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

Abstract: 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：US20080139582A1

公开(公告)日：2008-06-12

申请号：US11964285

申请日：2007-12-26

Applicant: Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

Inventor： Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

IPC: C07D487/04 ,  A61K31/519 ,  C12N9/99 ,  A61P35/00 ,  A61P37/00

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

Abstract: 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：US20120283276A1

公开(公告)日：2012-11-08

申请号：US13526161

申请日：2012-06-18

Applicant: Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

Inventor： Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

IPC: C07D487/04 ,  C12N9/96 ,  A61P35/00 ,  A61P35/02 ,  A61K31/519 ,  A61P29/00

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

Abstract: 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：US20100324050A1

公开(公告)日：2010-12-23

申请号：US12727703

申请日：2010-03-19

Applicant: Lee HONIGBERG ,  Erik Verner ,  Zhengying Pan

Inventor： Lee HONIGBERG ,  Erik Verner ,  Zhengying Pan

IPC: A61K31/4985 ,  C07D487/04 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P19/02 ,  A61P1/00 ,  A61P25/00

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

Abstract: 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：US20080214501A1

公开(公告)日：2008-09-04

申请号：US11935277

申请日：2007-11-05

Applicant: Zhengying PAN ,  Shyr Jiann Li ,  Heleen SCHEERENS ,  Lee HONIGBERG ,  Erik VERNER

Inventor： Zhengying PAN ,  Shyr Jiann Li ,  Heleen SCHEERENS ,  Lee HONIGBERG ,  Erik VERNER

IPC: A61K31/69 ,  C07F5/02 ,  C12N9/12

CPC classification number: C07D487/04 ,  G01N33/573 ,  G01N2333/9121 ,  G01N2500/00

Abstract: Described herein are probes for Bruton's tyrosine kinase (Btk). Such probes are used to characterize and develop Btk-selective inhibitors intended for therapeutic use.

Abstract translation: 本文描述的是布鲁顿酪氨酸激酶（Btk）的探针。 这种探针用于表征和开发用于治疗用途的Btk选择性抑制剂。

公开(公告)号：US20120277254A1

公开(公告)日：2012-11-01

申请号：US13542440

申请日：2012-07-05

Applicant: Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

Inventor： Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

IPC: A61K31/519 ,  A61P35/02 ,  A61P29/00 ,  A61P35/00 ,  C12N9/99 ,  C07D487/04

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

Abstract: 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：US20100022561A1

公开(公告)日：2010-01-28

申请号：US12499008

申请日：2009-07-07

Applicant: Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

Inventor： Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

IPC: A61K31/519 ,  A61P29/00

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

Abstract: 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：US20100004270A1

公开(公告)日：2010-01-07

申请号：US12499005

申请日：2009-07-07

Applicant: Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

Inventor： Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

IPC: A61K31/519 ,  A61P37/00

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

Abstract: 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.

Abstract translation: 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：US20130035334A1

公开(公告)日：2013-02-07

申请号：US13606949

申请日：2012-09-07

Applicant: Lee HONIGBERG ,  Erik J. Verner ,  Joseph J. Buggy ,  David J. Loury ,  Wei Chen

Inventor： Lee HONIGBERG ,  Erik J. Verner ,  Joseph J. Buggy ,  David J. Loury ,  Wei Chen

IPC: A61K31/519 ,  A61K31/5377 ,  A61P37/00 ,  A61P19/02 ,  A61P35/00 ,  C12Q1/02 ,  A61P19/10 ,  A61P29/00 ,  C12Q1/48 ,  G01N27/62 ,  G01N21/64 ,  C07D487/04 ,  A61P35/02

CPC classification number: C07D487/04 ,  A61K31/4985 ,  A61K31/519 ,  A61K45/06

Abstract: 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.