Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.
Abstract: This invention is a method and composition for the inhibition of VCAM-1, and in particular for the treatment of cardiovascular or inflammatory disease, including atherosclerosis, that includes the administration of an effective amount of an ester of probucol.
Abstract: A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5' or N.sup.4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
September 5, 2000
Assignee:
Emory University
Inventors:
Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
Abstract: A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
March 19, 1998
Date of Patent:
June 6, 2000
Assignees:
Emory University, The University of Georgia Research Foundation, Inc.
Inventors:
Raymond F. Schinazi, Chung K. Chu, Jinfa Du
Abstract: A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (-)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
May 30, 2000
Assignee:
Emory University
Inventors:
Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
Abstract: Respiratory viral infections may be effectively prevented or treated by administering an aerosol spray comprising a polyoxometalate to the lungs.
Abstract: A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)amino(alkyl or substituted alkyl) methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.
Type:
Grant
Filed:
December 24, 1996
Date of Patent:
November 23, 1999
Assignee:
Emory University
Inventors:
Dennis C. Liotta, Bharat Ramkrishna Lagu
Abstract: A method and composition for the treatment of humans infected with HIV that includes the administration of an HIV treatment amount of an enantiomerically pure .beta.-D-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.
Abstract: A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5' or N.sup.4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
June 22, 1999
Assignee:
Emory University
Inventors:
Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
Abstract: The present invention relates to a method of preparing BCH-189 and various analogs of BCH-189 from inexpensive precursors with the option of introducing functionality as needed. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds, .beta.-BCH-189 and related compounds. Furthermore, the steochemistry at the nucleoside 4' position can be controlled to produce enantiomerically-enriched .beta.-BCH-189 and its analogs.
Abstract: A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a ?5-carboxamido or 5-fluoro!-2',3'-dideoxy-2',3'-didehydro-pyrimidine nucleoside or a ?5-carboxamido or 5-fluoro!-3'-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5' or N.sup.4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.
Abstract: A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that referentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (-)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.
Type:
Grant
Filed:
July 14, 1998
Date of Patent:
April 6, 1999
Assignee:
Emory University
Inventors:
Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.
Type:
Grant
Filed:
October 17, 1996
Date of Patent:
March 2, 1999
Assignee:
Emory University
Inventors:
Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander
Abstract: Methods and compositions for treating urogenital tumors, and in particular, cancer of the prostate, bladder, and kidney, with BCNT, are disclosed. Any boron-containing compound that is sufficiently lipophilic to pass through the appropriate urogenital membranes in a quantity high enough to achieve therapy on irradiation with low-energy neutrons can be used. Carboranyl-containing nucleosides and oligonucleotides are particularly suited for use in BNCT of urogenital tumors. Preferred compounds include 5-carboranyl-2'-deoxyuridine (CDU) and 5-o-carboranyl-1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)uracil (CFAU). Nucleosides and oligonucleotides bearing an -O-?(carboran-1-yl)alkyl!phosphate, S-?(carboran-1-yl)alkyl!phosphorothioate, or Se-?(carboran-1-yl)alkyl!phosphoroselenoate in place of the (carboran-1-yl)phosphonate moiety can be used.
Type:
Grant
Filed:
February 3, 1997
Date of Patent:
February 16, 1999
Assignee:
Emory University
Inventors:
Raymond F. Schinazi, Thomas E. Keane, Dennis C. Liotta
Abstract: This invention includes the compounds 2'-deoxy-5-fluoro-3'-oxacytidine, (-)-2'-deoxy-5-fluoro-3'-oxacytidine, and (+)-2'-deoxy-5-fluoro-3+-oxacytidine, and pharmaceutically acceptable salts thereof for use in medical therapy, for example for the treatment or prophylaxis of an HIV infection.
Type:
Grant
Filed:
November 9, 1993
Date of Patent:
December 22, 1998
Assignee:
Emory University
Inventors:
Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 8, 1998
Assignee:
Emory University
Inventors:
Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
Abstract: A method and composition for the treatment of humans infected with HBV that includes the administration of an HBV treatment amount of a .beta.-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.
Abstract: A method and composition for the treatment of humans infected with HBV that includes the administration of an HBV treatment amount of a .beta.-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.
Abstract: A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (-)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner. In particular, deaminase, PPL, PLE and subtilisn are used to resolve 1,3-oxathiolane nucleoside enantiomers.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
October 27, 1998
Assignees:
Emory University, Yale University
Inventors:
Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi, Yung-Chi Cheng