Abstract: Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders, for example, by modulating the activity of KSP, are disclosed.
Type:
Grant
Filed:
July 23, 2003
Date of Patent:
May 1, 2007
Assignee:
Cytokinetics, Incorporated
Inventors:
Gustave Bergnes, Whitney W. Smith, Bing Yao, David J. Morgans, Jr., Andrew MacDonald
Abstract: Described herein are methods which identify candidate agents as binding to a protein or as a modulator of the binding characteristics or biological activity of a protein. Generally, the methods involve the use of ADP or phosphate. The assays can be used in a high throughput system to obviate the cumbersome steps of using gels or radioactive materials.
Type:
Grant
Filed:
November 8, 2005
Date of Patent:
April 10, 2007
Assignee:
Cytokinetics, Inc.
Inventors:
Jeffrey T. Finer, Fady Malik, Roman Sakowicz, Christopher Shumate, Kenneth Wood
Abstract: The present invention provides novel quinazolinone compositions of matter comprising enantiomerically pure compound represented by Formula I: or a pharmaceutically acceptable salt thereof, having a detectable amount of one or more starting material and/or reagent used in the synthesis thereof.
Abstract: According to the present invention, computer based techniques for using information technology in therapeutics or drug discovery. In an exemplary embodiment, computer based techniques for determining information about the properties of substances based upon information about structure of living or non-living cells exposed to substances are provided. Computer software according to the present invention enables researchers and/or scientists to identify promising candidates in the search for new and better medicines or treatments using, for example, a cellular informatics database.
Type:
Application
Filed:
May 19, 2006
Publication date:
January 4, 2007
Applicant:
Cytokinetics, Inc.
Inventors:
Eugeni Vaisberg, Cynthia Adams, James Sabry, Anne Crompton
Abstract: Methods, code and apparatus analyze cell images to automatically identify and characterize the Golgi complex in individual cells. This is accomplished by first locating the cells in the image and defining boundaries of those cells that subsume some or all of the Golgi complex of those cells. The Golgi complex in the images typically have intensity values corresponding to the concentration of a Golgi component in the cell (e.g. a polysaccharide associated with the Golgi complex). The method/system then analyzes the Golgi components of the image (typically on a pixel-by-pixel basis) to mathematically characterize the Golgi complex of individual cells. This mathematical characterization represents phenotypic information about the cells' Golgi complex and can be used to classify cells. From this information, mechanism of action and other important biological information can be deduced.
Type:
Grant
Filed:
February 20, 2001
Date of Patent:
December 19, 2006
Assignee:
Cytokinetics, Inc.
Inventors:
Eugeni A. Vaisberg, Ge Cong, Hsien-Hsun Wu
Abstract: Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders, for example, by modulating the activity of KSP, are disclosed.
Abstract: The present invention provides assays for detecting ADP, GDP and inorganic phosphate. These assays can be used directly to detect the presence of ADP, GDP and inorganic phosphate or can be used as part of a number of methods for identifying candidate agents that bind to a target protein or serve as modulators of the biological activity of a target protein.
Type:
Application
Filed:
December 6, 2005
Publication date:
November 16, 2006
Applicant:
Cytokinetics, Inc.
Inventors:
Ramesh Baliga, Donglin Guo, Daniel Pierce, Jeffrey Finer
Abstract: According to the present invention, computer based techniques for using information technology in therapeutics or drug discovery. In an exemplary embodiment, computer based techniques for determining information about the properties of substances based upon information about structure of living or non-living cells exposed to substances are provided. Computer software according to the present invention enables researchers and/or scientists to identify promising candidates in the search for new and better medicines or treatments using, for example, a cellular informatics database.
Type:
Application
Filed:
March 13, 2006
Publication date:
October 12, 2006
Applicant:
Cytokinetics, Inc.
Inventors:
Eugeni Vaisberg, Cynthia Adams, James Sabry, Anne Crompton
Abstract: Phenothiazine derivatives of formula (I) are disclosed. The compounds are inhibitors of the mitotic kinesin KSP and are useful in the treatment of cellular proliferative diseases, such as cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.
Abstract: Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity.
Type:
Grant
Filed:
November 28, 2000
Date of Patent:
September 12, 2006
Assignee:
Cytokinetics, Inc.
Inventors:
Gustave Bergnes, Whitney W. Smith, John C. Chabala
Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
Type:
Application
Filed:
February 14, 2006
Publication date:
August 3, 2006
Applicant:
Cytokinetics, Inc.
Inventors:
Fady Malik, Adam Tomasi, Bainian Feng, Erica Kraynack, Kathleen Elias, Pu-Ping Lu, Whitney Smith, Xiangping Qian, David Morgans
Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
Type:
Grant
Filed:
January 20, 2005
Date of Patent:
May 30, 2006
Assignee:
Cytokinetics, Inc.
Inventors:
Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
Abstract: The present invention relates to protein modulators, especially modulators of kinesin bioactivities. The present invention provides methods for screening protein modulators, e.g., kinesin modulators that bind to a region of a kinesin and/or that modulate kinesin bioactivities. The present invention also provide methods and compositions for treatment of disorders mediated by abnormal cellular proliferation activities.
Abstract: Provided herein are certain compounds of Formula I: that can be used to treat diseases of proliferating cells. The compounds are KSP kinesin inhibitors, particularly inhibitors of human KSP.
Abstract: A method for generating stimulus response curves (e.g., dose response curves) shows how the phenotype of one or more cells change in response to varying levels of the stimulus. Each “point” on the curve represents quantitative phenotype for cell(s) at a particular level of stimulus (e.g., dose of a therapeutic). The quantitative phenotypes are multivariate phenotypic representations of the cell(s). They include various features of the cell(s) obtained by image analysis. Such features often include basic parameters obtained from images (e.g., cell shape, nucleus area, Golgi texture) and/or biological characterizations derived from the basic parameters (e.g., cell cycle state, mitotic index, etc.). The stimulus response curves may be compared to allow classification of stimuli and identify subtle differences in related stimuli. To facilitate the comparison, it may be desirable to present the response curves in a principal component space.
Type:
Grant
Filed:
February 20, 2001
Date of Patent:
March 21, 2006
Assignee:
Cytokinetics, Inc.
Inventors:
Eugeni A. Vaisberg, Donald R. Oestreicher, Cynthia L. Adams
Abstract: The present invention is directed to methods for the preparation of enantiomerically pure quinazolinones, intermediates in such methods, and compositions comprising such quinazolinones.