公开(公告)号：US09844552B2

公开(公告)日：2017-12-19

申请号：US14957294

申请日：2015-12-02

Applicant: Pharmacyclics LLC

Inventor： Toni Jauset Gonzá#lez ,  Daniel Massó-Vallés ,  Laura Soucek

IPC: A61K31/519 ,  C09B31/147 ,  A61K31/7068

CPC classification number: A61K31/519 ,  A61K31/7068 ,  C09B31/147 ,  A61K2300/00

Abstract: Disclosed are methods of treating fibrosis in a patient, comprising administering to a patient in need thereof a therapeutically effective amount of an ACK inhibitor (e.g., a BTK inhibitor, such as for example an irreversible BTK inhibitor, such as for example, ibrutinib).

公开(公告)号：US09828383B1

公开(公告)日：2017-11-28

申请号：US15670614

申请日：2017-08-07

Applicant: Pharmacyclics LLC

Inventor： Norbert Purro ,  Mark Stephen Smyth ,  Erick Goldman ,  David D. Wirth

IPC: A61K31/505 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61J1/035 ,  A61K9/0053 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4825 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/519 ,  A61K45/06 ,  B65D75/36 ,  C07B2200/13 ,  A61K2300/00

Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, 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：US09795604B2

公开(公告)日：2017-10-24

申请号：US14523650

申请日：2014-10-24

Applicant: Pharmacyclics LLC

Inventor： John C. Byrd ,  Jason A. Dubovsky ,  Natarajan Muthusamy ,  Amy Jo Johnson ,  David Miklos

IPC: A61K31/519 ,  A61K38/13 ,  A61K35/17 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/56 ,  A61K35/28

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/56 ,  A61K35/17 ,  A61K35/28 ,  A61K38/13 ,  A61K45/06 ,  A61K2300/00

Abstract: Described herein are methods for treating and preventing graft versus host disease using ACK inhibitors. The methods include administering to an individual in need thereof an ACK inhibitor such as ibrutinib for treating and preventing graft versus host disease.

公开(公告)号：US20170266186A1

公开(公告)日：2017-09-21

申请号：US15393821

申请日：2016-12-29

Applicant: Pharmacyclics LLC

Inventor： Joseph J. Buggy ,  Laurence Elias ,  Gwen Fyfe ,  Eric Hedrick ,  David J. Loury ,  Tarak D. Mody

IPC: A61K31/519 ,  A61K45/06 ,  A61K31/337 ,  A61K31/4184 ,  A61K31/454 ,  C12Q1/68 ,  A61K31/4965 ,  A61K31/5383 ,  A61K31/704 ,  A61K31/7076 ,  A61K31/52 ,  G01N33/574 ,  A61K31/475

Abstract: Methods are provided for treating a hematologic cancer comprising administering an anticancer agent to a subject identified as having an increased mobilization of a subpopulation of lymphocytes from a malignancy following administration of an irreversible Btk inhibitor. Methods also are provided for identification of subjects for treatment and the analysis of cells mobilized from a hematologic malignancy following administration of an irreversible Btk inhibitor.

公开(公告)号：US20170258729A1

公开(公告)日：2017-09-14

申请号：US15467414

申请日：2017-03-23

Applicant: Pharmacyclics LLC

Inventor： Ching W. Chong ,  Robert Kuehl ,  Heow Tan ,  Harisha Atluri

IPC: A61K9/20 ,  A61K31/519

CPC classification number: A61K9/2054 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2095 ,  A61K31/519

Abstract: Described herein are pharmaceutical formulations of Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one. Also disclosed are methods of using the Btk inhibitor, 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：US09717731B2

公开(公告)日：2017-08-01

申请号：US14070420

申请日：2013-11-01

Applicant: Pharmacyclics LLC

Inventor： Joseph J. Buggy ,  Tarak D. Mody ,  John C. Byrd ,  Betty Y. Chang ,  Jason A. Dubovsky ,  Natarajan Muthusamy ,  Amy Jo Johnson

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：US09624224B2

公开(公告)日：2017-04-18

申请号：US14500897

申请日：2014-09-29

Applicant: Pharmacyclics LLC

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

IPC: C07D487/04 ,  A61K31/519 ,  A61P19/02 ,  A61P35/04 ,  A61P35/00 ,  A61P29/00 ,  A61P19/10

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.

公开(公告)号：US20170079981A1

公开(公告)日：2017-03-23

申请号：US15370535

申请日：2016-12-06

Applicant: Pharmacyclics LLC

Inventor： Harisha Atluri ,  Ching Wah Chong ,  Robert Kuehl ,  Cassandra Shu ,  Pearl Shwe-Cho Tay ,  James F. Hulvat ,  Alexander J. McVey ,  Ryan M. Minikis

IPC: A61K31/519 ,  A61K9/10 ,  A61K47/26 ,  A61K47/38 ,  A61K47/02 ,  A61K47/12

CPC classification number: A61K31/519 ,  A61K9/10 ,  A61K9/146 ,  A61K9/1652 ,  A61K9/2054 ,  A61K9/2077 ,  A61K47/02 ,  A61K47/12 ,  A61K47/26 ,  A61K47/38

Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including novel pharmaceutical formulations thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, 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：US09556182B2

公开(公告)日：2017-01-31

申请号：US14794685

申请日：2015-07-08

Applicant: Pharmacyclics LLC

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

IPC: A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/519 ,  A61K45/06

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.

Abstract translation: 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确定包括激酶在内的蛋白质的合适的不可逆抑制剂的方法，测定和系统。

公开(公告)号：US09546172B2

公开(公告)日：2017-01-17

申请号：US14369998

申请日：2012-12-28

Applicant: Pharmacyclics LLC

Inventor： Wei Chen ,  David J. Loury

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

CPC classification number: C07D487/04

Abstract: Disclosed herein are compounds such as those of Formula (I) 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。