Patents Assigned to Cytovia, Inc.
  • Fluorescence dyes and their applications for whole-cell fluorescence screening assays for caspases, peptidases, proteases and other enzymes and the use thereof
    Patent number: 6984718
    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: Grant
    Filed: May 6, 2002
    Date of Patent: January 10, 2006
    Assignee: Cytovia, Inc.
    Inventors: Han-Zhong Zhang, Sui Xiong Cai, John A. Drewe, Wu Yang
  • Dipeptide apoptosis inhibitors and the use thereof
    Patent number: 6949516
    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: May 5, 2003
    Date of Patent: September 27, 2005
    Assignee: Cytovia, Inc.
    Inventors: John F. W. Keana, Sui Xiong Cai, John Guastella, Wu Yang, John A. Drewe, Eckard Weber
  • Substituted 4H-chromene and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Publication number: 20050154015
    Abstract: The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, Z and R5 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: March 7, 2005
    Publication date: July 14, 2005
    Applicant: Cytovia, Inc.
    Inventors: John Drewe, Sui Cai, Yan Wang
  • Substituted 4H-chromene and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Patent number: 6906203
    Abstract: The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I: wherein A, B, X, Y, Z and R5 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 6, 2000
    Date of Patent: June 14, 2005
    Assignee: Cytovia, Inc.
    Inventors: John A. Drewe, Sui Xiong Cai, Yan Wang
  • Substituted coumarins and quinolines and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Patent number: 6900325
    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: May 31, 2005
    Assignees: Cytovia, Inc., Shire BioChem Inc.
    Inventors: Sui Xiong Cai, Hong Zhang, William E. Kemnitzer, Songchun Jiang, John Drewe, Richard Storer
  • Substituted coumarins and quinolines and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Publication number: 20050090526
    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: Application
    Filed: November 16, 2004
    Publication date: April 28, 2005
    Applicants: Cytovia, Inc., Shire BioChem, Inc.
    Inventors: Sui Cai, Hong Zhang, William Kemnitzer, Songchun Jiang, John Drewe, Richard Storer
  • Substituted 1, 4-thiazepine and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Patent number: 6861419
    Abstract: The present invention is directed to substituted 1,4-thiazepine and analogs thereof, represented by the general Formula I: wherein the dashed lines, A1, A2, A3, X1 and R1 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of capases 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: April 18, 2001
    Date of Patent: March 1, 2005
    Assignee: Cytovia, Inc.
    Inventors: John A. Drewe, Sui Xiong Cai, Emma Jane Shelton, Joane Litvak, David Sperandio, Jeffrey R. Spencer, Martin Sendzik
  • 7,8-fused 4H-chromene and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Patent number: 6858607
    Abstract: The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I: or pharmaceutically acceptable salts or prodrugs thereof, wherein: wherein A, R1, R2, R5, X, Y, and Z, are defined herein and B is a fused thiazole, oxazole, 2-imino-imidazole, 2,1,3-thiadiazo-2-one, thiazol-2-one, oxazol-2-one, imidazol-2-thione, thiazol-2-thione, oxazol-2-thione, imidazoline, oxazoline, thiazoline, triazole, oxazine, oxazine-2,3-dione, or piperazine ring. 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: February 22, 2005
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Lifen Xu, Richard Storer, Giorgio Attardo
  • Novel phenyl derivatives as inducers of apoptosis
    Publication number: 20050026929
    Abstract: The present invention related to certain phenyl derivatives that are activators of caspases and inducers of apoptosis, pharmaceutical composition comprising these compounds and method of treating cancer utilizing these compounds.
    Type: Application
    Filed: April 23, 2003
    Publication date: February 3, 2005
    Applicants: AXYS PHARMACEUTICALS, INC., CYTOVIA, INC.
    Inventors: Sui Cai, Ben Cebon, Joane Litvak, Keith Pararajasingham, Emma Shelton, Jeffrey Spencer, David Sperandio, Paul Sprengeler, Vincent Tai, Robert Yee
  • Method of identifying immunosuppressive agents
    Patent number: 6828091
    Abstract: A method for identifying therapeutically effective immunosuppressive agents by screening such agents for those which induce apoptosis in activated T cells is disclosed. T cells were isolated then activated and treating with various test compounds. A caspase substrate is added to detect caspase activation and apoptosis in the cells. Compounds which stimulate caspase activation and apoptosis are also tested against resting T cells to determine those agents which are more effective in activated T cells compared to resting T cells. Compounds with this selectivity are effective in treating immunopathological disorders such as arthritis, graft rejection, graft versus host disease, inflammatory bowel syndrome and the like.
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: December 7, 2004
    Assignee: Cytovia, Inc.
    Inventors: Shailaja Kasibhatla, Douglas R. Green, Ben Tseng
  • Substituted nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Publication number: 20040235846
    Abstract: The present invention is directed to substituted nicotinamides and analogs thereof, represented by Formula V: 1
    Type: Application
    Filed: June 28, 2004
    Publication date: November 25, 2004
    Applicant: Cytovia, Inc.
    Inventors: Sui Xiong Cai, John A. Drewe
  • Novel fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for caspases and other enzymes and the use thereof
    Publication number: 20040191844
    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: April 22, 2004
    Publication date: September 30, 2004
    Applicant: Cytovia, Inc.
    Inventors: Eckard Weber, Sui Xiong Cai, John F.W. Keana, John A. Drewe, Han-Zhong Zhang
  • Substituted nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Patent number: 6794397
    Abstract: The present invention is directed to substituted nicotinamides and analogs thereof, represented by Formula V: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Ar′ and Ar are independently optionally substituted aryl or optionally substituted heteroaryl, provided that the ring structure of said optionally substituted heteroaryl comprises not more than two nitrogen atoms; and R11 is hydrogen; or alkyl, cycloalkyl, aryl or heteroaryl, each of which is optionally substituted. The present invention also relates to the discovery that compounds having Formula V are activators of caspases and inducers of apoptosis. Therefore, 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: January 26, 2001
    Date of Patent: September 21, 2004
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, John A. Drewe
  • 4-substituted-1-(arylmethylidene)thiosemicarbazide, 4-substituted-1-(arylcarbonyl)thiosemicarbazide and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Patent number: 6794400
    Abstract: The present invention is directed to optionally substituted 4-substituted-1-(arylmethylidene)thiosemicarbazide, 4-substituted-1-(arylcarbonyl)thiosemicarbazide and analogs thereof, represented by the Formulae I and II: wherein A1, A2, Q and R1-R3 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: June 3, 2002
    Date of Patent: September 21, 2004
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Bao Ngoc Nguyen, John Drewe, P. Sanjeeva Reddy, Shailaja Kasibhatla, Azra Pervin
  • Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for caspases and other enzymes and the use thereof
    Patent number: 6759207
    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: September 7, 2001
    Date of Patent: July 6, 2004
    Assignee: Cytovia, Inc.
    Inventors: Eckard Weber, Sui Xiong Cai, John F. W. Keana, John A. Drewe, Han-Zhong Zhang
  • 3,5-Disubstituted-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Publication number: 20040127521
    Abstract: Disclosed are 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: 1
    Type: Application
    Filed: December 18, 2003
    Publication date: July 1, 2004
    Applicant: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Han-Zhong Zhang, Jared D. Kuemmerle, Hong Zhang, William E. Kemnitzer
  • Caspase inhibitors and the use thereof
    Publication number: 20040116355
    Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I: 1
    Type: Application
    Filed: November 26, 2003
    Publication date: June 17, 2004
    Applicant: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Eckard Weber, Yan Wang, Gordon B. Mills, Douglas R. Green
  • Substituted indole-2-carboxylic acid benzylidene-hydrazides and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Patent number: 6747052
    Abstract: The present invention is directed to substituted indole-2-carboxylic acid benzylidene-hydrazides and analogs thereof, represented by the general Formula I: wherein X, Ar1, R2-R6 and R12 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 19, 2002
    Date of Patent: June 8, 2004
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, John A. Drewe, Han-Zhong Zhang
  • Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Publication number: 20040097503
    Abstract: The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: 1
    Type: Application
    Filed: November 10, 2003
    Publication date: May 20, 2004
    Applicant: Cytovia, Inc.
    Inventors: Sui Xiong Cai, John A. Drewe, P. Sanjeeva Reddy, Bao Nguyen, Azra Pervin
  • Derivatives of gambogic acid and analogs as activators of caspases and inducers of apoptosis
    Publication number: 20040082066
    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: Application
    Filed: July 1, 2003
    Publication date: April 29, 2004
    Applicant: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Shailaja Kasibhatla, Kristin P. Ollis, Han-Zhong Zhang, John A. Drewe, Ben Tseng, Nilantha Sudath Sirisoma