公开(公告)号：US09107924B2

公开(公告)日：2015-08-18

申请号：US13965135

申请日：2013-08-12

Applicant: Pharmacyclics, Inc.

Inventor： Joseph J. Buggy ,  Laurence Elias

IPC: A61K31/519 ,  A61P35/00 ,  A61P29/00 ,  A61P35/02 ,  C07D487/04 ,  A61K45/06 ,  A61K39/395 ,  A61K31/337 ,  A61K31/675 ,  A61K31/704 ,  A61K33/24

CPC classification number: A61K31/519 ,  A61K31/00 ,  A61K31/337 ,  A61K31/52 ,  A61K31/675 ,  A61K31/704 ,  A61K33/24 ,  A61K39/3955 ,  A61K39/39558 ,  A61K45/06 ,  A61K2300/00 ,  A61K31/19

Abstract: Described herein are irreversible Btk inhibitor compounds, and methods for using such irreversible inhibitors in the treatment of diseases and disorders characterized by the presence or development of solid tumors.

Abstract translation: 本文描述的是不可逆的Btk抑制剂化合物，以及使用这种不可逆抑制剂治疗以固体肿瘤的存在或发展为特征的疾病和病症的方法。

公开(公告)号：US09096604B2

公开(公告)日：2015-08-04

申请号：US14081053

申请日：2013-11-15

Applicant: Pharmacyclics, Inc.

Inventor： Wei Chen ,  David J. Loury ,  Longcheng Wang

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61K31/519

Abstract: Disclosed herein are compounds exemplified by the following structure Formula (I) that form covalent bonds with Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds of Formula (I). Methods of using the Btk inhibitors exemplified by the structure of Formula (I) 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: 本文公开了通过与布鲁特酪氨酸激酶（Btk）形成共价键的以下结构式（I）示例的化合物。 还公开了包含式（I）化合物的药物组合物。 公开了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，异种免疫性疾病或病症，包括淋巴瘤和炎性疾病在内的癌症的公式（I）结构所使用的Btk抑制剂的方法或 条件。

公开(公告)号：US20140275125A1

公开(公告)日：2014-09-18

申请号：US13849399

申请日：2013-03-22

Applicant: PHARMACYCLICS, INC.

Inventor： Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

IPC: 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：US20140243355A1

公开(公告)日：2014-08-28

申请号：US14079508

申请日：2013-11-13

Applicant: Pharmacyclics, Inc.

Inventor： Lee HONIGBERG ,  Erik Verner ,  Zhengying Pan

IPC: 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：US20140221667A1

公开(公告)日：2014-08-07

申请号：US14250936

申请日：2014-04-11

Applicant: Pharmacyclics, Inc.

Inventor： Daniel A. DICKMAN ,  Dange Vijay KUMAR ,  Colin O'BRYAN ,  Roopa RAI ,  William Dvorak SHRADER

IPC: C07D235/18 ,  C07F5/02

CPC classification number: C07F5/025 ,  C07D235/18

Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.

公开(公告)号：US20140187565A1

公开(公告)日：2014-07-03

申请号：US14080649

申请日：2013-11-14

Applicant: Pharmacyclics, Inc.

Inventor： Lee HONIGBERG ,  Erik Verner ,  Zhengying Pan

IPC: 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：US08759516B2

公开(公告)日：2014-06-24

申请号：US13952531

申请日：2013-07-26

Applicant: Pharmacyclics, Inc.

Inventor： Lee Honigberg ,  Erik Verner ,  Zhengying Pan

IPC: C07D487/00

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：US20140142123A1

公开(公告)日：2014-05-22

申请号：US14073594

申请日：2013-11-06

Applicant: Pharmacyclics, Inc.

Inventor： Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

IPC: 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：US20140134265A1

公开(公告)日：2014-05-15

申请号：US14070420

申请日：2013-11-01

Applicant: Pharmacyclics, Inc.

Inventor： Joseph J. BUGGY ,  Tarak MODY ,  Richard B. LOVE ,  John C. BYRD ,  Betty CHANG

IPC: A61K31/519 ,  A61N5/10 ,  A61K45/06

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

Abstract: Described herein are methods and compositions comprising a covalent TEC family kinase inhibitor for use in adjuvant therapy, including adjuvant cancer therapy, vaccination and treatment of immune disorders and pathogenic infections.

公开(公告)号：US20140080879A1

公开(公告)日：2014-03-20

申请号：US13623578

申请日：2012-09-20

Applicant: PHARMACYCLICS, INC.

Inventor： Daniel A. Dickman ,  Dange Vijay Kumar ,  Colin O'Bryan ,  Roopa Rai ,  William Dvorak Shrader

IPC: A61K31/4184 ,  A61P7/02 ,  C07D235/18

CPC classification number: C07F5/025 ,  C07D235/18

Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.

Abstract translation: 本发明涉及因子VIIa，IXa，Xa，XIa，特别是因子VIIa的新型抑制剂，包含这些抑制剂的药物组合物，以及使用这些抑制剂治疗或预防血栓栓塞性疾病，癌症或类风湿性关节炎的方法。 还公开了制备这些抑制剂的方法。