Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Application
Filed:
March 29, 2007
Publication date:
October 25, 2007
Applicants:
Myriad Genetics, Incorporated, Cytovia, Inc.
Inventors:
Sui Cai, Nilantha Sirisoma, Azra Pervin, John Drewe, Shailaja Kasibhatla, Songchun Jiang, Hong Zhang, Chris Pleiman, Vijay Baichwal, John Manfredi, Leena Bhoite
Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Inventors:
Sui Cai, Nilantha Sirisoma, Azra Pervin, John Drewe, Shailaja Kasibhatla, Songchun Jiang, Hong Zhang, Chris Pleiman, Vijay Baichwal, John Manfredi, Leena Bhoite
Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Application
Filed:
March 13, 2007
Publication date:
October 18, 2007
Applicants:
Myriad Genetics, Incorporated, Cytovia, Inc.
Inventors:
Sui Cai, Nilantha Sirisoma, Azra Pervin, John Drewe, Shailaja Kasibhatla, Songchun Jiang, Hong Zhang, Chris Pleiman, Vijay Baichwal, John Manfredi, Leena Bhoite
Abstract: The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, dipeptidyl peptidase IV, calpain, aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.
Type:
Grant
Filed:
April 22, 2004
Date of Patent:
September 18, 2007
Assignee:
Cytovia, Inc.
Inventors:
Eckard Weber, Sui Xiong Cai, John F. W. Keana, John A. Drewe, Han-Zhong Zhang
Abstract: Disclosed are N-alkyl-N-aryl-thienopyrimidin-4-amines and analogs thereof, represented by the Formulae I-II: wherein Ar, R1-R4 and R10 are defined herein. The present invention relates to the discovery that compounds having Formulae I-II are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Application
Filed:
November 2, 2006
Publication date:
September 13, 2007
Applicant:
Cytovia, Inc.
Inventors:
Sui Cai, William Kemnitzer, Nilantha Sirisoma
Abstract: The present invention is directed to multifluoro-substituted Chalcones and analogs thereof, represented by the general Formula I: wherein Ar and R6-R10 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
March 14, 2002
Date of Patent:
August 14, 2007
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, P. Sanjeeva Reddy, John A. Drewe, Bao Ngoc Nguyen, Shailaja Kasibhatla
Abstract: The present invention is directed to substituted coumarins and quinolines and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
November 16, 2004
Date of Patent:
June 26, 2007
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, Hong Zhang, William E. Kemnitzer, Songchun Jiang, John Drewe, Richard Storer
Abstract: The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: wherein A, Ar1, Ar2, R1 and R3 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
November 10, 2003
Date of Patent:
June 5, 2007
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, John A Drewe, P. Sanjeeva Reddy, Bao Nguyen, Azra Pervin
Abstract: Disclosed are 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, R2, A, B and D are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Application
Filed:
November 6, 2006
Publication date:
May 17, 2007
Applicant:
Cytovia, Inc.
Inventors:
Sui Cai, Han-Zhong Zhang, Jared Kuemmerle, Hong Zhang, William Kemnitzer
Abstract: Disclosed are N-arylalkyl-thienopyrimidin-4-amines and analogs thereof, represented by the Formula I: wherein Ar, R1, R3, R4, R10-R12 and n are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Application
Filed:
November 2, 2006
Publication date:
May 3, 2007
Applicant:
Cytovia, Inc.
Inventors:
Sui Cai, John Drewe, William Kemnitzer, Nilantha Sirisoma
Abstract: Disclosed are N-aryl-thienopyrimidin-4-amines and analogs thereof, represented by the Formulae I-II: wherein Ar and R1-R4 are defined herein. The present invention relates to the discovery that compounds having Formulae I-II are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Application
Filed:
November 2, 2006
Publication date:
May 3, 2007
Applicant:
Cytovia, Inc.
Inventors:
Sui Cai, William Kemnitzer, Nilantha Sirisoma, Han-Zhong Zhang
Abstract: The present invention is directed to derivatives of gambogic acid and analogs thereof. Exemplary gambogic acid derivatives of the present invention include, among others, derivatives substituted in the C10 and C28 positions of gambogic acid. The present invention also relates to the discovery that certain preferred compounds of the present invention are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
July 1, 2003
Date of Patent:
February 13, 2007
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, Shailaja Kasibhatla, Kristin P. Ollis, Han-Zhong Zhang, John A. Drewe, Ben Tseng, Nilantha Sudath Sirisoma
Abstract: Disclosed are 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, R2, A, B and D are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
December 18, 2003
Date of Patent:
December 5, 2006
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, Han-Zhong Zhang, Jared D Kuemmerle, Hong Zhang, William E Kemnitzer
Abstract: The present invention is directed to substituted 1-benzoyl-3-cyano-pyrrolo[1,2-?]quinolines and analogs thereof, represented by the general Formula I: wherein R1–R8, L, Q, dash line and Ar are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
December 12, 2003
Date of Patent:
November 14, 2006
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, John A Drewe, Sungchun Jiang, Shailaja Kasibhatla, Jared Daniel Kuemmerle, Nilantha Sudath Sirisoma, Han-Zhong Zhang
Abstract: The present invention is directed to substituted N?-(arylcarbonyl)-benzhydrazides, N?-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: wherein Ar1, Ar2, and R1–R2 are defined herein. The present invention also relates to the discovery that compounds having Formulae I and II are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
April 5, 2004
Date of Patent:
July 11, 2006
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, Shailaja Kasibhatla, John Drewe, P. Sanjeeva Reddy, Han-Zhong Zhang
Abstract: The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the general Formula I: wherein R1–R5, A, Y and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Abstract: The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the Formula (I): wherein R1, R3-R5, A, D, Y and Z are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Application
Filed:
May 16, 2003
Publication date:
May 18, 2006
Applicant:
Cytovia, Inc.
Inventors:
Sui Cai, Songchun Jiang, William Kemnitzer, Hong Zhang, Giorgio Attardo, Real Denis
Abstract: The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
June 10, 2002
Date of Patent:
May 9, 2006
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, Han-Zhong Zhang, John A. Drewe, P. Sanjeeva Reddy, Shailaja Kasibhatla, Jared Daniel Kuemmerle, Kristin P. Ollis
Abstract: The present invention is directed to substituted coumarins and quinolines and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
May 16, 2002
Date of Patent:
March 21, 2006
Assignees:
Cytovia, Inc., Shire BioChem Inc.
Inventors:
Sui Xiong Cai, Hong Zhang, William E. Kemnitzer, Songchun Jiang, John Drewe, Richard Storer
Abstract: The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the general Formula I: wherein R1-R5, A, Y and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
Type:
Application
Filed:
June 13, 2005
Publication date:
February 16, 2006
Applicant:
Cytovia, Inc.
Inventors:
Sui Cai, Hong Zhang, Songchun Jiang, Richard Storer