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:
July 7, 2009
Date of Patent:
August 6, 2013
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. 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: 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:
August 1, 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:
December 6, 2011
Date of Patent:
July 30, 2013
Assignee:
Pharmacyclics, Inc.
Inventors:
Lee Honigberg, Erik Verner, Zhengying Pan
Abstract: Disclosed herein are methods and compounds for inhibiting bone and/or cartilage resorption in an individual. The methods comprise administering to the individual a composition comprising a therapeutically effective amount of a compound that is an irreversible inhibitor of a Bruton's tyrosine kinase (BTK), or a pharmaceutically acceptable salt thereof. Also described are irreversible inhibitors of Btk and methods for the preparation of the compounds. 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 inhibition of cancer metastasis, and for inhibition of bone or cartilage resorption in cancer patients.
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: Disclosed herein are compounds, including compounds having the Formula (A) where A, R1, R2, R3, and R4 are as defined in the specification, 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:
December 16, 2011
Date of Patent:
July 2, 2013
Assignee:
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.
Abstract: Disclosed herein are the methods and compositions for the improved synthesis of texaphyrin metal complexes. The improved synthesis results in high-purity compositions of texaphyrin metal complexes in which more than about 98% of the texaphyrin metal complexes in the composition have the same structure and/or the same molecular weight. Further described herein are pharmaceutical compositions comprising such high-purity compositions, and the use of such high-purity compositions in the treatment of cancer and cardiovascular diseases and disorders.
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 7, 2012
Publication date:
June 20, 2013
Applicant:
Pharmacyclics, Inc.
Inventors:
Aleksandr Kolesnikov, Roopa Rai, William Dvorak Shrader, Steven M. Torkelson, Kieron E. Wesson, Wendy B. Young
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:
Grant
Filed:
April 15, 2009
Date of Patent:
June 18, 2013
Assignee:
Pharmacyclics, Inc.
Inventors:
Erik Verner, Sriram Balasubramanian, Joseph J. Buggy
Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
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:
Grant
Filed:
May 3, 2011
Date of Patent:
April 9, 2013
Assignee:
Pharmacyclics, Inc
Inventors:
Daniel A. Dickman, Dange Vijay Kumar, Colin O'Bryan, Roopa Rai, William Dvorak Shrader, Kieron Wesson
Abstract: Disclosed herein are the methods and compositions for the improved synthesis of texaphyrin metal complexes. The improved synthesis results in high-purity compositions of texaphyrin metal complexes in which more than about 98% of the texaphyrin metal complexes in the composition have the same structure and/or the same molecular weight. Further described herein are pharmaceutical compositions comprising such high-purity compositions, and the use of such high-purity compositions in the treatment of cancer and cardiovascular diseases and disorders.
Abstract: Described herein are methods for treating a subject suffering from an inflammatory, autoimmune, or heteroimmune condition by administering to the subject a pharmaceutical composition containing a therapeutically effective amount of a compound that is a selective inhibitor of histone deacetylase 8. Also described herein are methods for decreasing secretion of pro-inflammatory cytokines by administering an HDAC8-selective inhibitor compound. Further described herein are methods for predicting responsiveness to treatments for inflammatory conditions. Methods for predicting efficacy of treatments for inflammatory conditions are also described.
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.
Type:
Grant
Filed:
January 30, 2012
Date of Patent:
March 19, 2013
Assignee:
Pharmacyclics, Inc.
Inventors:
Lee Honigberg, Erik Verner, Zhengying Pan
Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
Type:
Grant
Filed:
August 12, 2011
Date of Patent:
March 5, 2013
Assignee:
Pharmacyclics, Inc.
Inventors:
Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
Abstract: Disclosed herein are compounds of Formula (II) 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: 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:
September 7, 2012
Publication date:
February 7, 2013
Applicant:
Pharmacyclics, Inc.
Inventors:
Lee HONIGBERG, Erik J. Verner, Joseph J. Buggy, David J. Loury, Wei Chen