Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I:
where R1-R3, X and Y are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
Type:
Grant
Filed:
November 14, 2001
Date of Patent:
April 6, 2004
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, Eckard Weber, Yan Wang, Gordon B Mills, Douglas R Green
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:
May 10, 2002
Date of Patent:
April 6, 2004
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, John Drewe, Han-Zhong Zhang
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:
December 12, 2001
Date of Patent:
April 6, 2004
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, John A. Drewe, Bao Nguyen, Azra Pervin
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, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.
Type:
Application
Filed:
May 6, 2002
Publication date:
November 6, 2003
Applicant:
Cytovia, Inc.
Inventors:
Han-Zhong Zhang, Sui Xiong Cai, John A. Drewe, Wu Yang
Abstract: The present invention is directed to novel 2-aminobenzamide thereof, represented by the general Formula I:
where R1-R3, X, and A—D are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III:
wherein R1-R5 are defined in the specification.
Type:
Grant
Filed:
February 6, 2002
Date of Patent:
September 2, 2003
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, Han-Zhong Zhang, Shailaja Kasibhatla, Federico C. Gaeta
Abstract: The present invention is directed to novel dipeptides thereof, represented by the general Formula I:
where R1-R3 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
Type:
Grant
Filed:
August 31, 2000
Date of Patent:
July 22, 2003
Assignee:
Cytovia, Inc.
Inventors:
John F. W. Keana, Sui Xiong Cai, John Guastella, Wu Yang, John A. Drewe, Eckard Weber
Abstract: The present invention is directed to substituted indole-2-carboxylic acid benzylidene-hydrazides and analogs thereof, represented by the general Formula I: 1
Type:
Application
Filed:
November 19, 2002
Publication date:
June 5, 2003
Applicant:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, John A. Drewe, Han-Zhong Zhang
Abstract: The use of caspase inhibitors for treating, ameliorating, and preventing non-cancer cell death during chemotherapy and radiation therapy and for treating and ameliorating the side effects of chemotherapy and radiation therapy of cancer is disclosed.
Type:
Grant
Filed:
October 11, 2000
Date of Patent:
May 20, 2003
Assignee:
Cytovia, Inc.
Inventors:
Eckard Weber, Gordon B. Mills, Douglas R. Green
Abstract: Disclosed are methods for identifying potential therapeutically effective anti-cancer agents. In particular, the invention relates to the use of biochemical and cell based screening assays to identify compounds that directly or indirectly activate the apoptosis cascade and further a method for identifying those apoptosis inducers that are selective and effective apoptosis agents for use in treating cancer and other therapeutic indications characterized by a lack of appropriate apoptosis. Also disclosed is a method of identifying selective caspase inducers using a cell-line specific primary screen.
Type:
Application
Filed:
January 16, 2002
Publication date:
February 6, 2003
Applicant:
Cytovia, Inc.
Inventors:
Shailaja Kasibhatla, P. Sanjeeva Reddy, John A. Drewe
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: 1
Type:
Application
Filed:
May 10, 2002
Publication date:
January 16, 2003
Applicant:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, Shailaja Kasibhatla, John Drewe, P. Sanjeeva Reddy, Han-Zhong Zhang
Abstract: The present invention is directed to novel substituted &agr;-hydroxy acid thereof, represented by the general Formula I:
where R1-R5, X and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
Type:
Grant
Filed:
August 28, 2000
Date of Patent:
December 17, 2002
Assignee:
Cytovia, Inc.
Inventors:
Yan Wang, Sui Xiong Cai, Eckard Weber, Gordon B. Mills, Douglas R. Green, Lufeng Guan
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:
Application
Filed:
September 7, 2001
Publication date:
October 17, 2002
Applicant:
Cytovia, Inc.
Inventors:
Eckard Weber, Sui Xiong Cai, John F.W. Keana, John A. Drewe, Han-Zhong Zhang
Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III:
wherein R1-R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I-III 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 cell growth and spread of abnormal cells occurs.
Type:
Grant
Filed:
February 1, 2000
Date of Patent:
October 8, 2002
Assignee:
Cytovia, Inc.
Inventors:
Sui Xiong Cai, Han-Zhong Zhang, Yan Wang, Ben Tseng, Shailaja Kasibhatla, John A. Drewe