Abstract: Disclosed herein are carbonyl compounds of Formula I as described herein. Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.
Type:
Grant
Filed:
June 9, 2005
Date of Patent:
December 30, 2008
Assignee:
Kalypsys, Inc.
Inventors:
James William Malecha, Stewart Alwyn Noble, Christian Andreus Hassig, Paul L. Wash, Brandon M. Wiley, Charles Maxwell Lawrence, Timothy Z. Hoffman
Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
Type:
Application
Filed:
October 11, 2006
Publication date:
November 20, 2008
Applicant:
KALYPSYS, INC.
Inventors:
James W. Malecha, Andrew K. Lindstrom, Sergio G. Duron, Steven P. Govek
Abstract: A system for a droplet detection device to monitor the dispensing operation in an ultra high throughput (uHTS) system. The system includes a microtitre plate with a defined number of wells and well walls, a dispenser for dispensing fluids into the wells, an illuminating sensor to extract image features from the wells and well walls, and a controller for analyzing the extracted image features to determine the presence or absence of the dispensing fluid on the wells and well walls.
Abstract: Disclosed herein are compounds useful as modulators of TGR5 and methods for the treatment or prevention of metabolic, cardiovascular, and inflammatory diseases.
Type:
Application
Filed:
February 5, 2008
Publication date:
September 11, 2008
Applicant:
KALYPSYS, INC.
Inventors:
Anthony B. Pinkerton, Ayman Kabakibi, Mark R. Herbert, Dana Siegel
Abstract: A system for identifying biological activity of one or more samples using prolonged signaling. The system includes a sample plate, an assay in a permeable media, a test plate, an automated liquid handler and an electronic reader. The sample plate includes one or more individual wells which are used for storing one or more samples. A feature of the system uses an automated liquid handler to aspirate samples from the sample plate and to dispense each of these samples directly onto the assay in the permeable media. The automated liquid handler transfers the test plate in communicable range to an electronic reader for reporting transient biological events.
Abstract: Disclosed herein are carbonyl compounds of Formula: (I) as described herein. Compounds as modulators of his-tone deacetylase (HDAC), pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
Type:
Application
Filed:
December 9, 2005
Publication date:
August 14, 2008
Applicant:
Kalypsys, Inc.
Inventors:
James Malecha, Stewart Noble, Christian Hassig, Paul Wash, Brandon Wiley, Charles Lawrence, Timothy Hoffman, Celine Bonnefous, NIcholas Smith
Abstract: Disclosed herein are new methods of treatment of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and other fibrotic diseases of the liver in a subject by modulating PPAR? with sulfonyl-substituted bicyclic compounds and compositions as pharmaceuticals.
Abstract: The present invention relates to novel quinolones of Formula I that inhibit inducible NOS synthase together with methods of synthesizing and using the compounds including methods for inhibiting or modulating nitric oxide synthesis and/or lowering nitric oxide levels in a patient by administering the compounds for the treatment of disease.
Type:
Application
Filed:
February 23, 2007
Publication date:
June 12, 2008
Applicant:
KALYPSYS, INC.
Inventors:
Nicholas D. Smith, Jeffrey R. Roppe, Celine Bonnefous, Joseph E. Payne, Hui Zhuang, Xiaohong Chen, Andrew K. Lindstrom, Sergio G. Duron, Christian A. Hassig, Stewart A. Noble
Abstract: Disclosed herein are carbonyl compounds of having the structural formula: or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof, Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.
Type:
Grant
Filed:
June 9, 2005
Date of Patent:
June 3, 2008
Assignee:
Kalypsys, Inc.
Inventors:
James William Malecha, Stewart Alwyn Noble, Christian Andreus Hassig, Paul L. Wash, Brandon M. Wiley, Charles Maxwell Lawrence, Timothy Z. Hoffman
Abstract: The present invention discloses methods to reduce C-reactive protein (CRP) in patients in need thereof comprising the selective modulation of PPAR?.
Type:
Application
Filed:
June 26, 2007
Publication date:
January 3, 2008
Applicant:
KALYPSYS, INC.
Inventors:
Tadimeti S. Rao, John P. McKearn, Mausumee Guha
Abstract: The present invention relates to compounds and methods useful as inhibitors of PPAR, particularly PPAR?, and for the treatment or prevention of PPAR-mediated diseases, including metabolic diseases.
Type:
Application
Filed:
May 16, 2007
Publication date:
November 22, 2007
Applicant:
KALYPSYS, INC.
Inventors:
James W. Malecha, Stewart A. Noble, Sergio G. Duron, Andrew Lindstrom, Andrew Shiau, Steven Govek
Abstract: The present invention is directed to novel compositions and their application as pharmaceuticals for the treatment of disease. Methods of upregulation of GLUT4 via activation of peroxisome proliferator activated receptor delta activity in the adipose tissue of a human or animal subject are also provided, for the treatment of conditions such as diabetes, obesity, insulin resistance, metabolic syndrome, and others in which a reduction in insulin resistance, an increase in glucose utilization, a reduction in visceral fat, a reduction in triglyceride (TG) levels, or an increase in levels of high-density lipoprotein (HDL), is beneficial.
Abstract: The present invention relates to novel alkylamine-substituted bicyclic aryl compounds, pharmaceutical compositions comprising the same, useful as modulators of PPAR, and methods for the treatment or prevention of disease.
Abstract: Disclosed herein are carbonyl compounds of Formula I, II, or III, and others as described herein. Also disclosed are methods of treating disease, such as cancer, neurological disorders, including polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, autoimmune diseases and cardiovascular conditions, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.
Type:
Grant
Filed:
June 10, 2004
Date of Patent:
September 18, 2007
Assignee:
Kalypsys, Inc.
Inventors:
Paul L. Wash, Brandon M. Wiley, Christian Hassig, James W. Malecha, Stewart A. Noble
Abstract: The present invention relates to compounds and methods useful as modulators of Peroxisome Proliferator-Activated Receptors (PPARs) for treatment or prevention of disease.
Type:
Application
Filed:
February 14, 2007
Publication date:
August 16, 2007
Applicant:
KALYPSYS, INC.
Inventors:
Dennis Bennett, Daniel Severance, J. Semple
Abstract: The present invention relates to methods of selective modulation of peroxisome proliferator activated receptors (PPARs) over G-protein coupled receptor 40 (GPR40), and the use of therapeutically effective amounts of compounds and pharmaceutical compositions which selectively modulate PPAR over GPR40 for the treatment of diseases in patients in need thereof. The methods disclosed herein are exceptionally useful in treating metabolic diseases whilst avoiding certain side effects common to modulators of PPAR previously disclosed in the art.
Type:
Application
Filed:
March 19, 2007
Publication date:
August 16, 2007
Applicant:
KALYPSYS, INC.
Inventors:
Andrew Shiau, Mark Massari, Guy Oshiro, Ayman Kabakibi, James Malecha, Stewart Noble
Abstract: The present invention relates to compounds and methods useful as inhibitors of protein kinases, including B-Raf and several receptor tyrosine and cytoplasmic tyrosine kinases. The present invention is directed to new substituted pyrimidinyloxy urea compounds of Formulas II, III and IV and compositions and their application as pharmaceuticals for the treatment of disease. Methods of modulating of protein kinase activity in a human or animal subject are also provided for the treatment diseases such as cancers.
Type:
Application
Filed:
December 22, 2006
Publication date:
July 5, 2007
Applicant:
KALYPSYS, INC.
Inventors:
Hengyuan Lang, Timothy Gahman, Mark Herbert, Paul Wash, Cunxiang Zhao, Robert Davis
Abstract: The present invention relates to compounds and methods useful as inhibitors of protein kinases, including B-Raf and several receptor tyrosine and cytoplasmic tyrosine kinases. The present invention is directed to new substituted pyrimidinyloxy urea compounds of Formulas II, III and IV and compositions and their application as pharmaceuticals for the treatment of disease. Methods of modulating of protein kinase activity in a human or animal subject are also provided for the treatment diseases such as cancers.
Type:
Application
Filed:
December 22, 2006
Publication date:
July 5, 2007
Applicant:
KALYPSYS, INC.
Inventors:
Hengyuan Lang, Timothy Gahman, Mark Herbert, Paul Wash, Cunxiang Zhao, Robert Davis
Abstract: Disclosed herein are carbonyl compounds of having the structural formula: or a salt, ester, or prodrug thereof, Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.
Type:
Application
Filed:
December 8, 2006
Publication date:
June 14, 2007
Applicant:
KALYPSYS, INC
Inventors:
Nicholas Smith, Celine Bonnefous, Joseph Payne, Timothy Hoffman, Paul Wash, Christian Hassig, Shawn Scranton