公开(公告)号：US20140336206A1

公开(公告)日：2014-11-13

申请号：US14340483

申请日：2014-07-24

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 pyrazolo[3,4-d]pyrimidines 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: 本文公开了与布鲁特酪氨酸激酶（Btk）形成共价键的吡唑并[3,4-d]嘧啶。 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：US20150306103A1

公开(公告)日：2015-10-29

申请号：US14613309

申请日：2015-02-03

Applicant: Pharmacyclics, Inc.

Inventor： Lee HONIGBERG ,  Erik VERNER ,  Zhengying PAN

IPC: A61K31/519 ,  A61K45/06

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.

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：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：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：US20140080844A1

公开(公告)日：2014-03-20

申请号：US14085722

申请日：2013-11-20

Applicant: Pharmacyclics, Inc.

Inventor： Wei CHEN ,  David J. LOURY ,  Tarak D. MODY ,  Erik VERNER ,  Mark Stephen SMYTH ,  Wenchen LUO

IPC: C07D487/04

CPC classification number: C07D487/04 ,  C07D519/00

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.

Abstract translation: 本文描述的是激酶抑制剂化合物，用于合成这种抑制剂的方法，以及在治疗疾病中使用这些抑制剂的方法。 本文进一步描述了用于测定包括激酶在内的蛋白质的适当抑制剂的方法，测定和系统。

公开(公告)号：US20150320758A1

公开(公告)日：2015-11-12

申请号：US14521377

申请日：2014-10-22

Applicant: Pharmacyclics, Inc.

Inventor： Erik VERNER ,  Sriram BALASUBRAMANIAN ,  Joseph J. BUGGY

IPC: A61K31/5377 ,  A61K45/06 ,  A61K31/4439 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/401

CPC classification number: A61K45/06 ,  A61K31/40 ,  A61K31/401 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/5377 ,  C07D207/337 ,  C07D209/08 ,  C07D209/12 ,  C07D209/14 ,  C07D235/06 ,  C07D307/79 ,  C07D307/80 ,  C07D333/54 ,  C07D333/56 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D409/06 ,  C07D471/04 ,  Y02A50/40

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

Abstract translation: 本文描述了含有这种化合物的化合物和药物组合物，其抑制组蛋白脱乙酰酶8（HDAC8）的活性。 本文还描述了将这样的HDAC8抑制剂单独使用并与其它化合物联合用于治疗将受益于抑制HDAC8活性的疾病或病症的方法。

公开(公告)号：US20150152115A1

公开(公告)日：2015-06-04

申请号：US14613313

申请日：2015-02-03

Applicant: Pharmacyclics, Inc.

Inventor： Lee HONIGBERG ,  Erik VERNER ,  Joseph J. BUGGY ,  David LOURY ,  Wei CHEN

IPC: C07D487/04 ,  G01N33/573

CPC classification number: C07D487/04 ,  G01N33/573 ,  G01N2500/04

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.

公开(公告)号：US20140171453A1

公开(公告)日：2014-06-19

申请号：US14080640

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：US20140004174A1

公开(公告)日：2014-01-02

申请号：US13897582

申请日：2013-05-20

Applicant: Pharmacyclics, Inc.

Inventor： Erik VERNER ,  Sriram BALASUBRAMANIAN ,  Joseph J. BUGGY

IPC: C07D401/06 ,  A61K31/40 ,  C07D209/14 ,  A61K45/06 ,  A61K31/4439 ,  C07D209/12 ,  A61K31/5377 ,  C07D207/337 ,  A61K31/404

CPC classification number: A61K45/06 ,  A61K31/40 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/5377 ,  C07D207/337 ,  C07D209/08 ,  C07D209/12 ,  C07D209/14 ,  C07D235/06 ,  C07D307/79 ,  C07D307/80 ,  C07D333/54 ,  C07D333/56 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D409/06 ,  C07D471/04 ,  Y02A50/40

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

Abstract translation: 本文描述了含有这种化合物的化合物和药物组合物，其抑制组蛋白脱乙酰酶8（HDAC8）的活性。 本文还描述了将这样的HDAC8抑制剂单独使用并与其它化合物联合用于治疗将受益于抑制HDAC8活性的疾病或病症的方法。

公开(公告)号：US20150307500A1

公开(公告)日：2015-10-29

申请号：US14703750

申请日：2015-05-04

Applicant: Pharmacyclics, Inc.

Inventor： Lee HONIGBERG ,  Erik VERNER ,  Joseph J. BUGGY ,  David LOURY ,  Wei CHEN

IPC: C07D487/04 ,  A61K45/06 ,  A61K31/519

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.