公开(公告)号：WO2015048689A1

公开(公告)日：2015-04-02

申请号：PCT/US2014/058132

申请日：2014-09-29

Applicant: PHARMACYCLICS, INC.

Inventor： WANG, Longcheng ,  CHEN, Wei ,  JIA, Zhaozahong, J. ,  LOURY, David, J.

IPC: C07D403/14 ,  C07D401/14 ,  A61K31/519 ,  A61P19/02 ,  A61P19/00

CPC classification number: C07D487/04

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. 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: 本文所公开的是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。 另外，还描述了Btk的可逆抑制剂。 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Btk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：WO2014130693A1

公开(公告)日：2014-08-28

申请号：PCT/US2014/017436

申请日：2014-02-20

Applicant: PHARMACYCLICS, INC. ,  CHEN, Wei ,  YAN, Shunqi ,  LOURY, David, J. ,  FRYE, Leah, Lynn ,  GREENWOOD, Jeremy, Robert ,  SHELLEY, Mee, Yoo ,  WANG, Longcheng

Inventor： CHEN, Wei ,  YAN, Shunqi ,  LOURY, David, J. ,  FRYE, Leah, Lynn ,  GREENWOOD, Jeremy, Robert ,  SHELLEY, Mee, Yoo ,  WANG, Longcheng

IPC: C07D473/02 ,  A61K31/22 ,  A61P37/00

CPC classification number: C07D473/32 ,  C07D487/04

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. 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。 此外，还描述了Btk的可逆抑制剂。 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：WO2014078578A1

公开(公告)日：2014-05-22

申请号：PCT/US2013/070164

申请日：2013-11-14

Applicant: PHARMACYCLICS, INC.

Inventor： CHEN, Wei ,  LOURY, David, J. ,  WANG, Longcheng

IPC: C07D487/04 ,  A61K31/519 ,  A61P37/00 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D487/04 ,  A61K31/519

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. 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。 此外，还描述了Btk的可逆抑制剂。 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：WO2013116382A1

公开(公告)日：2013-08-08

申请号：PCT/US2013/023918

申请日：2013-01-30

Applicant: PHARMACYCLICS, INC. ,  YAN, Shunqi ,  WANG, Longcheng ,  FRYE, Leah, Lynn

Inventor： YAN, Shunqi ,  WANG, Longcheng ,  FRYE, Leah, Lynn ,  CHEN, Wei ,  LOURY, David, J.

IPC: C07D473/32 ,  A61K31/52 ,  A61P37/00 ,  A61P35/00

CPC classification number: C07D473/34

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. 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。 此外，还描述了Btk的可逆抑制剂。 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：EP2920180A1

公开(公告)日：2015-09-23

申请号：EP13854424.2

申请日：2013-11-14

Applicant: Pharmacyclics, Inc.

Inventor： CHEN, Wei ,  LOURY, David, J. ,  WANG, Longcheng

IPC: C07D487/04 ,  A61K31/519 ,  A61P37/00 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D487/04 ,  A61K31/519

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. 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。 另外，还描述了Btk的可逆抑制剂。 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Btk抑制剂的方法用于治疗自身免疫疾病或病症，异质性免疫疾病或病症，癌症（包括淋巴瘤）和炎性疾病或病症。

公开(公告)号：EP2731612A2

公开(公告)日：2014-05-21

申请号：EP12811600.1

申请日：2012-07-13

Applicant: Pharmacyclics, Inc.

Inventor： CHEN, Wei ,  LOURY, David, J. ,  MODY, Tarak, D. ,  WANG, Longcheng

IPC: A61K31/52 ,  A61K31/433 ,  C07D473/34 ,  C07D473/32 ,  A61P17/00 ,  A61P29/00

CPC classification number: C07D487/04 ,  A61K31/52 ,  C07D473/34

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

公开(公告)号：EP2809672A1

公开(公告)日：2014-12-10

申请号：EP13743025.2

申请日：2013-01-30

Applicant: Pharmacyclics, Inc.

Inventor： YAN, Shunqi ,  WANG, Longcheng ,  FRYE, Leah, Lynn ,  CHEN, Wei ,  LOURY, David, J.

IPC: C07D473/32 ,  A61K31/52 ,  A61P37/00 ,  A61P35/00

CPC classification number: C07D473/34

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. 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：EP3147285A2

公开(公告)日：2017-03-29

申请号：EP16170469.7

申请日：2013-01-30

Applicant: Pharmacyclics, Inc.

Inventor： YAN, Shunqi ,  WANG, Longcheng ,  FRYE, Leah, Lynn ,  CHEN, Wei ,  LOURY, David, J

IPC: C07D473/32 ,  A61K31/52 ,  A61P37/00 ,  A61P35/00

CPC classification number: C07D473/34

Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. 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。 另外，还描述了Btk的可逆抑制剂。 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Btk抑制剂的方法用于治疗自身免疫疾病或病症，异质性免疫疾病或病症，癌症（包括淋巴瘤）和炎性疾病或病症。