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:
September 21, 2010
Publication date:
January 13, 2011
Applicant:
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:
August 31, 2010
Publication date:
December 30, 2010
Applicant:
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:
March 19, 2010
Publication date:
December 23, 2010
Applicant:
Pharmacyclics, Inc. A Delaware corporation
Inventors:
Lee HONIGBERG, Erik Verner, Zhengying Pan
Abstract: Described herein are methods and compositions for determining whether a particular cancer is resistant to or susceptible to a histone deacetylase inhibitor or to histone deacetylase inhibitors. The methods include analysis of the expression levels of at least four biomarker genes associated with response to a histone deacetylase inhibitor. Also described herein are methods and compositions for increasing the likelihood of a therapeutically effective treatment in a patient, comprising an analysis of the expression levels of at least four biomarker genes associated with response to a histone deacetylase inhibitor. Also described herein are isolated populations of nucleic acids derived from a cancer sensitive to or resistant to a histone deacetylase inhibitor. Further described are kits and indications that are optionally used in conjunction with the aforementioned methods and compositions.
Type:
Grant
Filed:
January 30, 2008
Date of Patent:
November 23, 2010
Assignee:
Pharmacyclics, Inc.
Inventors:
Joseph J. Buggy, Sriram Balasubramanian
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: Described herein are methods for using calcium flux as a biomarker to select and predict patients likely to respond to an apoptotic agent as therapy. Further described herein is a method of using calcium flux as a clinical biomarker to determine whether a tumor is sensitive to an HDAC inhibitor.
Type:
Application
Filed:
April 11, 2008
Publication date:
November 11, 2010
Applicant:
PHARMACYCLICS, INC.
Inventors:
Sriram Balasubramanian, Joseph J. Buggy, Jason Ramos, Mint Sirisawad
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 26, 2007
Date of Patent:
November 2, 2010
Assignee:
Pharmacyclics, Inc.
Inventors:
Lee Honigberg, Erik Verner, Zhengying Pan
Abstract: Described herein are methods for treating a subject suffering from a T-cell lymphoma by administering to the subject a pharmaceutical composition containing a therapeutically effective amount of a selective inhibitor of histone deacetylase 8. Also described herein are methods for treating a subject suffering from a T-cell lymphoma by administering to the subject a population of autologous T-cells that have been exposed to a selective HDAC8 inhibitor composition ex vivo.
Type:
Grant
Filed:
July 18, 2007
Date of Patent:
October 26, 2010
Assignee:
Pharmacyclics Inc.
Inventors:
Joseph J. Buggy, Sriram Balasubramanian
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:
Grant
Filed:
October 16, 2009
Date of Patent:
June 22, 2010
Assignee:
Pharmacyclics, Inc.
Inventors:
Wei Chen, David J. Loury, Tarak D. Mody
Abstract: Disclosed herein are imidazo[1,5-f][1,2,4]triazine compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). The imidazo[1,5-f][1,2,4]triazine compounds described are irreversible inhibitors of Btk. Methods for the preparation of the imidazo[1,5-f][1,2,4]triazine compounds are disclosed. Also disclosed are pharmaceutical compositions that include the imidazo[1,5-f][1,2,4]triazine compounds. Methods of using the imidazo[1,5-f][1,2,4]triazine 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 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:
Grant
Filed:
October 16, 2009
Date of Patent:
May 18, 2010
Assignee:
Pharmacyclics, Inc.
Inventors:
Wei Chen, David J. Loury, Tarak D. Mody
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: 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 7, 2009
Publication date:
February 18, 2010
Applicant:
PHARMACYCLICS, INC.
Inventors:
Lee HONIGBERG, Erik VERNER, Zhengying PAN
Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.
Type:
Application
Filed:
October 7, 2009
Publication date:
February 11, 2010
Applicant:
Pharmacyclics, Inc.
Inventors:
Orion D. JANKOWSKI, James T. Palmer, Lee Honigberg
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 7, 2009
Publication date:
January 28, 2010
Applicant:
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 7, 2009
Publication date:
January 7, 2010
Applicant:
Pharmacyclics, Inc.
Inventors:
Lee HONIGBERG, Erik VERNER, Zhengying PAN
Abstract: Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided.
Type:
Grant
Filed:
December 28, 2006
Date of Patent:
December 1, 2009
Assignee:
Pharmacyclics, Inc.
Inventors:
Orion D. Jankowski, James T. Palmer, Lee Honigberg
Abstract: Described herein are compositions and methods for treating a subject suffering from a non-localized inflammatory condition (or any symptoms associated with such inflammation), including systemic inflammation, and inflammatory conditions affecting the large portions of or the whole body, or sepsis by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a compound that is a pan-HDAC inhibitor. Also described herein are methods for decreasing iNOS and cytokine expression by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of a compound that is a pan-HDAC inhibitor.
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.