Abstract: Compounds and pharmaceutical compositions active against hepatitis B virus are provided, as is a method for the treatment of hepatitis B virus infection in humans and other host animals is provided comprising administering an effective amount of a &bgr;-L-(2′or 3′-azido)-2′,3′-dideoxy-5-fluorocytosine of the formula
wherein R is H, acyl, monophosphate, diphosphate, or triphosphate, or a stabilized phosphate derivative (to form a stabilized nucleotide prodrug), and R′is H, acyl, or alkyl.
Type:
Grant
Filed:
November 5, 1999
Date of Patent:
October 1, 2002
Assignees:
Emory University, Centre National de la Recherche Scientifique, UAB Research Foundation
Inventors:
Gilles Gosselin, Jean-Louis Imbach, Jean-Pierre Sommadossi, Raymond F. Schinazi
Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside has the formula:
wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted.
Type:
Grant
Filed:
December 10, 1999
Date of Patent:
September 3, 2002
Assignees:
Novirio Pharmaceuticals Limited, Centre National da la Recherche Scientifique
Inventors:
Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
Abstract: Methods and compositions for directing adipose-derived stromal cells cultivated in vitro to differentiate into cells of the chondrocyte lineage are disclosed. The invention further provides a variety of chondroinductive agents which can be used singly or in combination with other nutrient components to induce chondrogenesis in adipose-derived stromal cells either in cultivating monolayers or in a biocompatible lattice or matrix in a three-dimensional configuration. Use of the differentiated chondrocytes for the therapeutic treatment of a number of human conditions and diseases including repair of cartilage in vivo is disclosed.
Type:
Grant
Filed:
May 17, 2000
Date of Patent:
August 6, 2002
Assignee:
Artecel Science, Inc.
Inventors:
Yuan-Di C. Halvorsen, William O. Wilkison, Jeffrey Martin Gimble
Abstract: The present invention is a method and composition to increase bone strength in a manner that decreases fracture incidence, which may or may not include increasing bone mineral density (“BMD”). The invention includes administering an effective amount of a bisphosphonate to a host in need thereof to increase bone strength, which inhibits the apoptosis of osteoblasts and osteocytes, without a significant effect on osteoclasts. In one embodiment, the bisphosphonate is not 1-amino-3-(N,N-dimethylamino)-propyliden-1,1-bisphosphonic acid or its pharmaceutically acceptable salt. An increase in osteoblast life span can lead to an increase in bone mass, i.e., an anabolic effect. Preservation of osteocyte life span can increase bone strength, which may be disproportional to the increase in bone mass.
Type:
Grant
Filed:
November 19, 1999
Date of Patent:
July 9, 2002
Assignee:
Board of Trustees of the University of Arkansas
Abstract: Compounds and pharmaceutical compositions active against HIV are provided, as is a method for the treatment of HIV infection in humans and other host animals is provided comprising administering an effective amount of a &bgr;-L-(2′ or 3′-azido)-2′,3′-dideoxy-5-fluorocytosine of the formula
wherein R is H, acyl, monophosphate, diphosphate, or triphosphate, or a stabilized phosphate derivative (to form a stabilized nucleotide prodrug), and R′ is H, acyl, or alkyl.
Type:
Grant
Filed:
November 5, 1999
Date of Patent:
June 18, 2002
Assignees:
Emory University, Centre National de la Recherche Scientifique, The UAB Research Foundation
Inventors:
Gilles Gosselin, Jean-Louis Imbach, Jean-Pierre Sommadossi, Raymond F. Schinazi
Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside has the formula:
wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted.
Type:
Grant
Filed:
August 10, 1999
Date of Patent:
May 28, 2002
Assignees:
Novirio Pharmaceuticals Limited, Centre National da la Recherche Scientifique
Inventors:
Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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 N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.
Abstract: The invention provides a composition of an isolated human adipose tissue-derived stromal cell that has been differentiated to exhibit at least one characteristic of a non-adipocyte cell lineage wherein the non-adipocyte cell lineage is osteoblastic. The adipose-derived cell possessing an osteoblastic characteristic can be genetically modified or combined with a matrix. The compositions of the invention can be used in vivo to repair bone and treat bone diseases.
Abstract: A class of 2′-fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer.
Type:
Grant
Filed:
February 25, 1999
Date of Patent:
February 19, 2002
Assignees:
Emory University, University of Georgia Research Foundation, Inc.
Inventors:
Raymond F. Schinazi, Dennis C. Liotta, Chung K. Chu, J. Jeffrey McAtee, Junxing Shi, Yongseok Choi, Kyeong Lee, Joon H. Hong
Abstract: Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biolologically active compounds, and the compounds which may be synthesized from such intermediates.
Type:
Grant
Filed:
October 10, 1997
Date of Patent:
December 4, 2001
Assignee:
Pharmasset, Ltd.
Inventors:
Krzysztof W. Pankiewicz, Krystyna Lesiak, Kyoichi A. Watanabe
Abstract: A method for the treatment of a host, and in particular, a human, infected with hepatitis B virus (HBV) is provided that includes administering an effective amount of a nucleotide prodrug of &bgr;- L-2′, 3′-dideoxyadenosine, wherein the prodrug component of the nucleotide provides controlled delivery of the active species.
Type:
Grant
Filed:
July 9, 1998
Date of Patent:
June 12, 2001
Assignee:
Emory University
Inventors:
Raymond F. Schinazi, Jean-Pierre Sommadossi, Gilles Gosselin, Jean-Louis Imbach
Abstract: The invention provides methods for identifying compounds and compositions useful in the regulation of weight, the treatment of obesity, diabetes and other insulin resistance-related disorders hypertension, cardiovascular disease and the like. The methods comprise the use of adipocytes and predipocytes in assays and screens for compounds or compositions of interest. The present invention recognizes the presence of the sulfonylurea receptor in adipocytes and its utility in identifying compounds and in treating obesity and other insulin resistance-related disorders. In addition to assaying for agonists and antagonists of the sulfonylurea receptor, the methods of the invention also provide for identifying novel calcium channels or other calcium regulatory channels that are selectively expressed in human adipocytes as compared to human preadipocytes and for screening adipocytes for compounds that selectively antagonize calcium.
Type:
Grant
Filed:
June 12, 2000
Date of Patent:
June 5, 2001
Assignees:
Zen Bio, Inc., The University of Tennessee Research Corporation
Inventors:
William O. Wilkison, Michael B. Zemel, Naima Moustaid-Mousse
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 N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.
Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.
Type:
Grant
Filed:
August 12, 1999
Date of Patent:
April 10, 2001
Assignees:
Emory University, Triangle Pharmaceuticals, Inc.
Inventors:
George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
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 3, 2000
Date of Patent:
March 6, 2001
Assignees:
Emory University, The University of Georgia Research Foundation, Inc.
Inventors:
Raymond F. Schinazi, Chung K. Chu, Jinfa Du
Abstract: It has been discovered that 3′-azido-2′,3′-dideoxyuridine (CS-87) induces a transient mutation in HIV-1 at the 70th codon (K to R, i.e., lysine to arginine) of the reverse transcriptase region of the virus. Based on this discovery, a method and composition for treating HIV is provided that includes administering CS-87 or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70th codon of the reverse transcriptase region. This invention can be practiced by referring to the published mutation patterns for known anti-HIV drugs, or by determining the mutation pattern for a new drug.
Abstract: Carboranyl-containing nucleosides and oligonucleotides are provided for use in boron neutron capture therapy (BNCT) and for other therapeutic and diagnostic purposes.
Type:
Grant
Filed:
December 2, 1993
Date of Patent:
January 30, 2001
Inventors:
Raymond F. Schinazi, Geraldin{acute over (e)} Fulcrand-El Kattan, Zbigniew Jan Lesnikowski
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.