Abstract: It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post-angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.
Type:
Grant
Filed:
June 20, 2001
Date of Patent:
August 19, 2003
Assignee:
Atherogenics, Inc.
Inventors:
Liming Ni, Lee K. Hoong, James A. Sikorski, Charles Q. Meng
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.
Type:
Grant
Filed:
February 26, 2001
Date of Patent:
August 5, 2003
Assignees:
Emory University, Idenix Pharmaceuticals, Inc.
Inventors:
Raymond F. Schinazi, Martin L. Bryant, Maureen W. Myers
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: A method and composition for treating a host infected with hepatitis D comprising administering an effective hepatitis D treatment amount of a described 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof.
Type:
Grant
Filed:
May 29, 2001
Date of Patent:
July 22, 2003
Assignee:
Idenix Pharmaceuticals Inc.
Inventors:
Jean-Pierre Sommadossi, Martin L. Bryant
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 5, 2001
Date of Patent:
July 8, 2003
Assignees:
Emory University, The University of Georgia Research Foundation, Inc.
Inventors:
Raymond F. Schinazi, Chung K. Chu, Jinfa Du
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:
January 30, 2001
Date of Patent:
June 24, 2003
Assignee:
Emory University
Inventors:
Raymond F. Schinazi, Geraldiné Fulcrand-El Kattan, Zbigniew Jan Lesnikowski
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:
September 26, 2000
Date of Patent:
June 10, 2003
Assignee:
Triangle Pharmaceuticals, Inc.
Inventors:
George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
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:
May 27, 2003
Assignee:
Artecel Science, Inc.
Inventors:
William O. Wilkison, Michael B. Zemel, Naima Moustaid-Moussa
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 14, 2001
Date of Patent:
May 27, 2003
Assignee:
Idenix Pharmaceuticals Inc.
Inventors:
Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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-pentoftiranonucleoside 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 14, 2001
Date of Patent:
May 20, 2003
Assignee:
Idenix Pharmaceuticals, Inc.
Inventors:
Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
Abstract: The invention relates to methods and compositions for the differentiation of stromal cells from adipose tissue into hematopoietic supporting stromal cells and myocytes of both the skeletal and smooth muscle type. The cells produced by the methods are useful in providing a source of fully differentiated and functional cells for research, transplantation and development of tissue engineering products for the treatment of human diseases and traumatic tissue injury repair.
Type:
Grant
Filed:
August 14, 2000
Date of Patent:
April 29, 2003
Assignee:
Artecel Sciences, Inc.
Inventors:
Jeffrey Martin Gimble, Juan-Di Chang Halvorsen, William O. Wilkison
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: A method for inhibiting sexual transmission of HIV comprising topically applying to the skin or epithelial tissue of a human a composition comprising a non-nucleoside reverse transcriptase inhibitor (“NNRTI”) that is able to inhibit viral replication for periods exceeding 12, 24, or even 36 days, at concentrations below even 10 &mgr;M. In one embodiment the NNRTI is a dihydro-alkyloxy-benzyl-oxopyrimidine (DABO).
Type:
Grant
Filed:
November 19, 2001
Date of Patent:
April 8, 2003
Assignees:
Idenix (Cayman) Limited, Universita Degli Studi di Cagliari
Inventors:
Jean-Pierre Sommadossi, Martin L. Bryant, Marino Artico, Paolo La Colla
Abstract: The present invention is directed to a method for treating hepatitis B virus infection in humans comprising administering a synergistically effective amount of agents having known anti-hepatitis B virus activity in combination or alternation. Specifically, the invention is directed to a method for treating hepatitis B virus infection comprising administering FTC in combination or alternation with penciclovir, famciclovir or Bis-POM-PMEA. Additionally, the invention is directed to a method for treating hepatitis B virus infection comprising administering L-FMAU in combination or alternation with DAPD, penciclovir or Bis-POM-PMEA. The invention is further directed to a method for treating hepatitis B virus infection comprising administering DAPD in combination or alternation with Bis-POM-PMEA.
Type:
Grant
Filed:
November 2, 1999
Date of Patent:
March 4, 2003
Assignee:
Triangle Pharmaceuticals, Inc.
Inventors:
Phillip A. Furman, George R. Painter, III, David W. Barry, Franck Rousseau
Abstract: A phacoemulsification and aspiration device comprising: (a) a substantially hollow housing comprising a first end and a second end; (b) an electrical resistance heating element disposed at the first end of the housing and configured to thermally irradiate a space proximal to the first end and exterior to the housing; (c) a source of electricity in electrical contact with the heating element; and (d) a vacuum source disposed at and integrally connected to the second end of the housing; and a method for treating cataracts in vivo by liquefying a cataractous lens nucleus and aspirating the same from within a surrounding lens capsule comprising the steps of: (a) thermally irradiating and liquefying a lens; and (b) aspirating the lens.
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:
May 15, 2000
Date of Patent:
February 11, 2003
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: The present invention relates to a novel and improved process for preparing 2′-fluoro-5-methyl-&bgr;-L-arabinofuranosyluridine represented by formula (I) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus and Epstein-Barr virus:
Type:
Grant
Filed:
July 23, 1998
Date of Patent:
January 28, 2003
Assignee:
The University of Georgia Research Foundation
Abstract: Antisense oligonucleotides that hybridize to segments of the pres1, S, C, and &egr; regions of the hepatitis B virus (HBV) RNA pregenome inhibit replication of the virus. Pharmaceutical compositions which contain these oligonucleotides as the active ingredients are effective against HBV infection.
Abstract: The invention provides methods for determining the ability of compounds to regulate lipogenesis and lipolysis by acting as a sulfonylurea-1 (SUR 1) potassium channel activator, an adipocyte potassium channel activator, an SUR 1 antagonist, and an adipocyte specific SUR 1 antagonist. The present invention recognizes the presence of the sulfonylurea receptor in adipocytes and its utility in identifying compounds and in regulating lipogenesis and lipolysis.
Type:
Grant
Filed:
June 12, 2000
Date of Patent:
December 10, 2002
Assignee:
Artecel Sciences, Inc.
Inventors:
William O. Wilkison, Michael B. Zemel, Naima Moustaid-Moussa