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: 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.
Type:
Application
Filed:
November 20, 2013
Publication date:
March 20, 2014
Applicant:
Pharmacyclics, Inc.
Inventors:
Wei CHEN, David J. LOURY, Tarak D. MODY, Erik VERNER, Mark Stephen SMYTH, Wenchen LUO
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.
Type:
Application
Filed:
September 20, 2012
Publication date:
March 20, 2014
Applicant:
PHARMACYCLICS, INC.
Inventors:
Daniel A. Dickman, Dange Vijay Kumar, Colin O'Bryan, Roopa Rai, William Dvorak Shrader
Abstract: Disclosed herein are compounds, including compounds having the structure of Formula (A), (B), (C), and (D), as described in further detail herein, 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.
Type:
Grant
Filed:
May 15, 2012
Date of Patent:
March 4, 2014
Assignee:
Pharmacyclics, Inc.
Inventors:
Lee Honigberg, Erik Verner, Zhengying Pan
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.
Type:
Application
Filed:
October 31, 2013
Publication date:
February 27, 2014
Applicant:
PHARMACYCLICS, INC.
Inventors:
Lee HONIGBERG, Erik Verner, Joseph J. Buggy, David Loury, Wei Chen
Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.
Type:
Application
Filed:
October 31, 2013
Publication date:
February 27, 2014
Applicant:
Pharmacyclics, Inc.
Inventors:
David J. LOURY, Joseph J. BUGGY, Tarak D. MODY, Erik J. VERNER, Norbert PURRO, Sriram Balasubramanian
Abstract: Disclosed herein are compounds, including compounds having the structure of Formula (A), (B), (C), and (D), as described in further detail herein, 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.
Type:
Grant
Filed:
January 30, 2012
Date of Patent:
February 25, 2014
Assignee:
Pharmacyclics, Inc.
Inventors:
Lee Honigberg, Erik Verner, Zhengying Pan
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.
Type:
Application
Filed:
July 26, 2013
Publication date:
February 6, 2014
Applicant:
Pharmacyclics, Inc.
Inventors:
Lee Honigberg, Erik Verner, Zhengying Pan
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.
Type:
Application
Filed:
May 20, 2013
Publication date:
January 2, 2014
Applicant:
Pharmacyclics, Inc.
Inventors:
Erik VERNER, Sriram BALASUBRAMANIAN, Joseph J. BUGGY
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.
Type:
Application
Filed:
June 3, 2013
Publication date:
December 19, 2013
Applicant:
Pharmacyclics, Inc.
Inventors:
Mark Smyth, Erick Goldman, David D. Wirth, Norbert Purro
Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.
Type:
Grant
Filed:
April 16, 2010
Date of Patent:
December 10, 2013
Assignee:
Pharmacyclics, Inc.
Inventors:
David J. Loury, Joseph J. Buggy, Tarak D. Mody, Erik J. Verner, Norbert Purro, Sriram Balasubramanian
Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
Type:
Application
Filed:
April 24, 2013
Publication date:
November 21, 2013
Applicant:
PHARMACYCLICS, INC.
Inventors:
Joseph J. Buggy, Laurence Elias, Gwen Fyfe, Eric Hedrick, David J. Loury, Tarak D. Mody
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.
Type:
Grant
Filed:
January 30, 2012
Date of Patent:
October 22, 2013
Assignee:
Pharmacyclics, Inc.
Inventors:
Lee Honigberg, Erik Verner, Zhengying Pan
Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
Type:
Application
Filed:
January 22, 2013
Publication date:
October 17, 2013
Applicant:
Pharmacyclics, Inc.
Inventors:
Joseph J. Buggy, Laurence Elias, Gwen Fyfe, Eric Hedrick, David J. Loury, Tarak D. Mody
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.
Type:
Grant
Filed:
June 18, 2012
Date of Patent:
October 8, 2013
Assignee:
Pharmacyclics, Inc.
Inventors:
Lee Honigberg, Erik Verner, Zhengying Pan
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: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
Type:
Application
Filed:
January 8, 2013
Publication date:
August 8, 2013
Applicant:
Pharmacyclics, Inc.
Inventors:
Joseph J. Buggy, Laurence Elias, Gwen Fyfe, Eric Hedrick, David J. Loury, Tarak D. Mody
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.