Phosphorus Containing Patents (Class 514/51)
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Patent number: 7700576Abstract: Novel pharmaceutical compositions which contain one of the reverse transcriptase inhibitors, viz., Zidovudine, Lamivudine or Stavudine in clinically efficacious amount and Meldonium as well as pharmaceutically applicable excipients. It has been proved that inclusion of Meldonium in these pharmaceutical compositions essentially diminishes the cardio- and neuro-toxicity of the reverse transcriptase inhibitor.Type: GrantFiled: August 8, 2006Date of Patent: April 20, 2010Assignee: Latvian Institute of Organic SynthesisInventors: Vija Klusha, Sergejs Isajevs, Jolanta Pupure, Juris Rumaks, Valentina Gordjushina, Immanuels Taivans, Ivars Kalvinsh
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Publication number: 20100087388Abstract: The present invention includes the utility of anti-viral and/or antibacterial effective amounts of 6-substituted nucleoside derivatives of formula (I) (e.g. 6-iodouridine and 6-iodouridine monophosphate) in the treatment or prevention of viral infections (e.g. Flavivridae, Bunyaviridae, or Togaviridae, or viral infections of hepatitis C, hepatitis B, herpes, influenza, HIV, polio, Coxsackie A/B, rhino, small pox, Ebola, West Nile, or corona virus) and/or bacterial infections (e.g. H. pylori, S. Aureus, B. anthracis, Mycobacterial tuberculosis, M. leprae, M. avium, P. aueruginosa, Streptococcal species, and Pneumocystis carinii).Type: ApplicationFiled: October 3, 2006Publication date: April 8, 2010Inventors: Lakshmi P. Kotra, Emil F. Pai
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Patent number: 7691826Abstract: A polysialic acid compound is reacted with a hetero-bifunctional reagent to introduce a pendant functional group for site-specific conjugation to sulfhydryl groups, for instance side chains of cysteine units in drugs, drug delivery systems, proteins or peptides. The functional group is, for instance, an N-maleimide group.Type: GrantFiled: August 12, 2004Date of Patent: April 6, 2010Assignee: Lipoxen Technologies LimitedInventors: Dale Howard Hreczuk-Hirst, Sanjay Jain, Peter Laing, Gregory Gregoriadis, Ioannis Papaioannou
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Patent number: 7691890Abstract: The present invention relates to anti-viral uses of leflunomide product, alone or in combination with other anti-viral agents, or in combination with a pyrimidine such as uridine.Type: GrantFiled: March 11, 1999Date of Patent: April 6, 2010Inventors: James W. Williams, Anita Chong, W. James Waldman
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Publication number: 20100068179Abstract: The invention provides compounds comprising at least one phosphohalohydrin group of the formula: where X is a halogen selected from among I, Br, Cl, R1 is selected from among —CH3 and —CH2—CH3, Cat+ is an organic or inorganic cation, and n is an integer between 2 and 20, processes for the production thereof and uses theroef, in particular therapeutic uses and for activating primate T?9?2 lymphocytes.Type: ApplicationFiled: November 24, 2009Publication date: March 18, 2010Applicant: Institut National de la Sante et de la Recherche MedicaleInventors: Christian Belmant, Jean-Jacques Fournie, Marc Bonneville, Marie-Alix Peyrat
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Patent number: 7666856Abstract: 4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.Type: GrantFiled: October 10, 2007Date of Patent: February 23, 2010Assignee: Medivir ABInventors: Nils-Gunnar Johansson, Genadiy Kalyanov, Joseph Armstrong Martin, David Bernard Smith, Anna Winqvist
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Publication number: 20100041621Abstract: The invention provides methods and compositions for improving cognitive performance involving administration of a cytidine-containing or uridine-containing compound to a neuropsychologically healthy human.Type: ApplicationFiled: August 14, 2009Publication date: February 18, 2010Inventors: Perry Renshaw, Deborah Yurgelun-Todd
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Patent number: 7662798Abstract: 2? and 3?-Prodrugs of 1?, 2?, 3? or 4?-branched ?-D or ?-L nucleosides, or their pharmaceutically acceptable salts and derivatives are described, which are useful in the prevention and treatment of Flaviviridae infections and other related conditions. These modified nucleosides provide superior results against flaviviruses and pestiviruses, including hepatitis C virus and viruses generally that replicate through an RNA dependent RNA reverse transcriptase. Compounds, compositions, methods and uses are provided for the treatment of Flaviviridae infection, including HCV infection, that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.Type: GrantFiled: June 27, 2003Date of Patent: February 16, 2010Assignees: Idenix Pharmaceuticals, Inc., University of Cagliari, Centre National de la Recherche Scientifique, L'Universite Montpellier IIInventors: Paola LaColla, Jean-Pierre Sommadossi, Gilles Gosselin
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Patent number: 7662361Abstract: The invention provides methods and compositions for modulating the activity of therapeutic agents for the treatment of a cancer by administering one or more agents that (either alone or in combination) induces telomere damage and inhibits telomerase activity in the cancer cell. The method initially uses, e.g., a telomere damage-inducing agent such as paclitaxel, and a telomerase inhibitory agent such as AZT. The invention also provides methods for identifying other agents with telomere damage-inducing activity and/or telomerase inhibitory activity (as well as and compositions having such activity), for use in the treatment of cancer.Type: GrantFiled: February 2, 2006Date of Patent: February 16, 2010Inventors: Jessie L.-S. Au, M. Guillaume Wientjes
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Publication number: 20100016251Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.Type: ApplicationFiled: March 21, 2008Publication date: January 21, 2010Applicant: PHARMASSET, INC.Inventors: MICHAEL JOSEPH SOFIA, JINFA DU, PEIYUAN WANG, DHANAPALAN NAGARATHNAM
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Patent number: 7635690Abstract: The present invention discloses a method for treating HIV that includes administering ?-D-D4FC 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 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using ?-D-D4FC as “salvage therapy” to patients which exhibit drug resistance to other anti-HIV agents. ?-D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.Type: GrantFiled: October 3, 2006Date of Patent: December 22, 2009Assignee: Emory UniversityInventors: Raymond F. Schinazi, Jennifer L. Hammond, John W. Mellors, Dennis C. Liotta
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Patent number: 7632821Abstract: The present invention provides ribonucleoside 2?,3?-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2?,3?-cyclic acetals alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection.Type: GrantFiled: August 4, 2006Date of Patent: December 15, 2009Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Kenneth Alan Koeplinger, Malcolm MacCoss, Daniel R. McMasters, David B. Olsen, Lihu Yang
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Publication number: 20090306009Abstract: The present invention relates to the field of regulating the activity of the purinergic receptors for the modulation of the vascular tone, particularly for the purpose of treatment of haemodynamic conditions by overriding of vasoconstriction activity, such as increases in sympathic vasoconstriction. Modulators, such as UTP analogues as described herein are preferably specific for P2Y2. Compounds capable of stimulating the P2Y2 receptor are suitable for the treatment or prevention wherein inhibition of vasoconstriction activity is desirable such as hypertension and hypertension relates disorders or diseases, whereas compound capable of counteracting the activity of the P2Y2 receptor are suitable for the treatment of or prevention wherein inhibition of vasodilatation is desirable.Type: ApplicationFiled: December 6, 2006Publication date: December 10, 2009Applicant: P2-SCIENCE APSInventor: Jaya Rosenmeier
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Publication number: 20090306010Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The present invention also provides a method of treating cystic fibrosis. The present invention also provides a method of treating sinusitis. The present invention further provides P1-(2?-deoxycytidine 5?-)P4-(uridine 5?-)tetraphosphate, tetra-(alkali metal) salts such as tetrasodium, tetralithium, tetrapotassium, and mixed (tetra-alkali metal) salts.Type: ApplicationFiled: May 6, 2009Publication date: December 10, 2009Inventors: Benjamin R. Yerxa, Ward M. Peterson, Janet L. Rideout, William Pendergast
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Patent number: 7615542Abstract: The present invention relates to the use of a dioxolane thymine compound according to the chemical structure of Formula (I): where R1 is H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group, for use in the treatment of HIV infections which exhibit resistance to 3TC and/or AZT. Preferably, compounds according to the present invention are combined with at least one anti-HIV agent which inhibits HIV by a mechanism other than through the inhibition of thymidine kinase (TK). These agents include those selected from among nuleocoside reverse transcriptase inhibitors (NRTI), non-nucloeoside reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, among others.Type: GrantFiled: December 8, 2003Date of Patent: November 10, 2009Assignees: University of Georgia Research Foundation, Inc., Emory UNiversityInventors: Chung K. Chu, Raymond F. Schinazi
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Patent number: 7612047Abstract: The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.Type: GrantFiled: September 10, 2008Date of Patent: November 3, 2009Assignee: Inspire Pharmaceuticals, Inc.Inventors: James G. Douglass, III, Benjamin R. Yerxa, Sammy R. Shaver, Ward M. Peterson, Edward G. Brown, Christopher S. Crean, José L. Boyer
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Patent number: 7608599Abstract: The invention provides novel nucleoside compounds of formula I wherein R1, R2a, R2b, R3, R4, R5 R6, R8a, R9 and R10 are as defined herein which are useful for the treatment of Hepatitis C Virus (HCV) mediated diseases.Type: GrantFiled: August 11, 2006Date of Patent: October 27, 2009Assignee: Roche Palo Alto LLCInventors: Klaus Klumpp, Joseph Armstrong Martin, Christopher McGuigan, David Bernard Smith
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Patent number: 7608600Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branched nucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.Type: GrantFiled: June 27, 2003Date of Patent: October 27, 2009Assignees: Idenix Pharmaceuticals, Inc., University of Cagliari, Centre National de la Recherche Scientifique, L'Universite Montfellier IIInventors: Richard Storer, Gilles Gosselin, Jean-Pierre Sommadossi, Paola LaColla
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Patent number: 7608597Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: GrantFiled: June 20, 2003Date of Patent: October 27, 2009Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi Di CagliariInventors: Jean-Pierre Sommadossi, Paulo LaColla
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Patent number: 7608602Abstract: The present invention provides gemcitabine prodrugs, methods of making gemcitabine prodrugs, pharmaceutical compositions of gemcitabine prodrugs and methods of using gemcitabine prodrugs and pharmaceutical compositions of using gemcitabine prodrugs to treat or prevent diseases or disorders such as cancer or viral infections.Type: GrantFiled: August 24, 2007Date of Patent: October 27, 2009Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Ge Peng, Thomas F. Woiwode, Kenneth C. Cundy
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Patent number: 7605144Abstract: This invention provides novel compounds selected from the group consisting of a 1,5-substituted pyrimidine derivative or analog and substituted furano-pyrimidone analogs. The compounds are useful to treat or prevent diseases such as cancer.Type: GrantFiled: October 7, 2003Date of Patent: October 20, 2009Assignee: Celmed Oncology (USA), Inc.Inventors: H. Michael Shepard, Ming Fai Chan, Michael P. Groziak
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Patent number: 7601703Abstract: This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expression as a result of selection by biologic or chemotherapy. This invention also provides methods and examples of molecules for selectively killing a pathological cell by contacting the cell with a prodrug that is a selective substrate for an endogenous, intracellular enzyme. The prodrug is subsequently converted to a cellular toxin. Further provided by this invention is a method for treating a pathology characterized by pathological, hyperproliferative cells in a subject by administering to the subject a prodrug that is a selective substrate for an endogenous, overexpressed, intracellular enzyme, and converted by the enzyme to a cellular toxin in the hyperproliferative cell.Type: GrantFiled: February 12, 2001Date of Patent: October 13, 2009Assignee: Celmed Oncology (USA), Inc.Inventors: H. Michael Shepard, Michael P. Groziak
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Patent number: 7598230Abstract: The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or base-modifications. The nucleotide mimics of the present invention, in a form of a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug, or a pharmaceutical formulation, are useful as antiviral, antimicrobial, and anticancer agents. The present invention provides a method for the treatment of viral infections, microbial infections, and proliferative disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of the present invention optionally in combination with other pharmaceutically active agents.Type: GrantFiled: June 14, 2007Date of Patent: October 6, 2009Assignee: Biota Scientific Management Pty LtdInventors: Phillip D. Cook, Guangyi Wang, Thomas W. Bruice, Nicholas A. Boyle, Janet M. Leeds, Jennifer L. Brooks, Marija Prhavc, Maria Eugenia Ariza, Patrick C. Fagan, Yi Jin, Vivek K. Rajwanshi, Kathleen D. Tucker
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Patent number: 7592446Abstract: The present invention provides selenium derivatives of nucleosides, nucleoside phosphoramidites, nucleotides, nucleotide triphosphates, oligonucleotides, polynucleotides, and larger nucleic acids and methods for their synthesis. Selenium derivatives of both ribonucleic acids and deoxyribonulcleic acids, as well as methods for their synthesis, crystallization and uses in structural determinations, particularly by X-ray crystallographic techniques are disclosed. The selenium derivatives of the present invention are also useful as food supplements.Type: GrantFiled: March 22, 2002Date of Patent: September 22, 2009Assignee: Georgia State University Research Foundation, Inc.Inventor: Zhen Huang
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Patent number: 7589078Abstract: The present invention relates to compounds according to the general formula: wherein B is or and the remaining variables are defined in the specification, and compositions comprising the compounds. The compounds are useful as anti-viral agents in viral therapy.Type: GrantFiled: February 18, 2004Date of Patent: September 15, 2009Assignee: Yale UniversityInventors: Yung-chi Cheng, Hiromichi Tanaka, Masanori Baba
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Patent number: 7589079Abstract: Physical forms of beta-L-2?-deoxythymidine are disclosed that can be characterized by physical appearance, purity levels, Infra-Red and Raman spectroscopy, X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These forms of beta-L-2?-deoxythymidine can be used in the manufacture of other forms of beta-L-2?-deoxythymidine, or in pharmaceutical compositions. Particularly preferred uses are in the treatment of hepatitis B.Type: GrantFiled: May 25, 2007Date of Patent: September 15, 2009Assignee: Novartis AGInventors: David Jonaitis, Richard Storer
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Patent number: 7585851Abstract: The present invention relates to compounds, compositions and methods for the treatment of a host infected with a hepatitis B virus. Specifically, compound and compositions of 3?-esters of 2?-deoxy-?-L-pyrimidine nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents. Compound and compositions of 3?,5?-diesters of 2?-deoxy-?-L-pyrimidine nucleosides are also disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents.Type: GrantFiled: October 25, 2004Date of Patent: September 8, 2009Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, L'Universite Montpellier IIInventors: Martin L. Bryant, Gilles Gosselin, Jean-Louis Imbach
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Publication number: 20090221524Abstract: The present invention includes methods of treating or preventing malaria by administering an anti-malarial effective amount of 6-substituted uridine derivatives to a subject need thereof. The invention also includes new 6-substituted uridine derivatives for use as therapeutics, in particular to treat malaria.Type: ApplicationFiled: October 3, 2006Publication date: September 3, 2009Inventors: Lakshmi P. Kotra, Emil F. Pai, Angelica M. Bello, Masahiro Fujihashi
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Publication number: 20090209481Abstract: Compounds having the formula I or II wherein R1, R2, B, and V are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: November 26, 2008Publication date: August 20, 2009Inventors: Scott J. Hecker, K. Raja Reddy, Zhili Sun, Brett C. Bookser, David Bernard Smith
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Publication number: 20090197825Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: November 26, 2008Publication date: August 6, 2009Applicant: ARDEA BIOSCIENCES, INC.Inventors: Barry D. QUART, Jean-Luc GIRARDET, Esmir GUNIC, Li-Tain YEH
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Publication number: 20090176732Abstract: Disclosed herein are nucleotide analogs with one or more protecting groups, methods of synthesizing nucleotide analogs with one or more protecting groups and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with one or more protecting groups.Type: ApplicationFiled: December 19, 2008Publication date: July 9, 2009Applicant: Alios BioPharma Inc.Inventors: Leonid Beigelman, Lawrence Blatt, Harri Lonnberg
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Patent number: 7557093Abstract: The invention provides a composition for promoting collagen production, and more specifically, provides a composition capable of promoting collagen production in human dermis. Further, the invention provides a method for promoting collagen production. The invention provides a composition for promoting collagen production containing a purine nucleic acid-related substance as an active ingredient as well as a composition for promoting collagen production containing a purine nucleic acid-related substance and a pyrimidine nucleic acid-related substance. The method for promoting collagen production of the invention comprises applying a purine nucleic acid-related substance alone or in combination with a pyrimidine nucleic acid-related substance to the skin.Type: GrantFiled: October 8, 2004Date of Patent: July 7, 2009Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Shigeo Shinohara, Mitsuaki Kawamura
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Publication number: 20090170806Abstract: Co-administration of alovudine and zidovudine at ratios considerably in excess of the prior art completely or substantially abolishes the mitochondrial toxicity of alovudine in mitochondrial DNA depletion experiments. The invention thus provides pharmaceutical compositions comprising alovudine and zidovudine in a molar ratio in the range 1:100 to 1:350 and methods for the treatment or prophylaxis of multiply resistant HIV comprising the simultaneous or consequential administration of alovudine and zidovudine in the characteristic molar ratio.Type: ApplicationFiled: May 4, 2007Publication date: July 2, 2009Inventors: Hong Zhang, Bo Oberg
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Publication number: 20090169504Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.Type: ApplicationFiled: April 25, 2008Publication date: July 2, 2009Inventors: Jean-Pierre Sommadossi, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
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Patent number: 7531525Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The present invention also provides a method of treating cystic fibrosis. The present invention further provides P1-(2?-deoxycytidine 5?-)P4-(uridine 5?-) tetraphosphate, tetra-(alkali metal) salts such as tetrasodium, tetralithium, tetrapotassium, and mixed (tetra-alkali metal) salts. The present further provides a pharmaceutical formulation comprising a P1-(2?-deoxycytidine 5?-)P4-(uridine 5?-) tetraphosphate, tetra-(alkali metal) salt, in a pharmaceutically acceptable carrier.Type: GrantFiled: March 23, 2007Date of Patent: May 12, 2009Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Ward M. Peterson, Janet L. Rideout, William Pendergast
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Patent number: 7528119Abstract: The present invention are directed to P1,P4-di(uridine 5?-)tetraphosphate, tetra-alkali metal salts such as tetrasodium, tetralithium, tetrapotassium, and mixed tetra-alkali metal cations thereof. The tetra alkali metal salts of P1,P4-di(uridine 5?-)tetraphosphate are water-soluble, nontoxic, and easy to handle during manufacture. These tetra-monovalent alkali metal salts are more resistant to hydrolysis than the mono-, di-, or tri-acid salts, therefore, they provide an improved stability and a longer shelf life for storage. The present invention also provides methods for the synthesis of P1,P4-di(uridine 5?-)tetraphosphate, and its pharmaceutically acceptably acceptable salts thereof, and demonstrates the applicability to the production of large quantities. The methods substantially reduce the time required to synthesize diuridine tetraphosphate, for example, to three days or less.Type: GrantFiled: July 14, 2006Date of Patent: May 5, 2009Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Edward G. Brown
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Publication number: 20090105189Abstract: The present invention is directed to methods and compositions for treating and ameliorating AAMI, hippocampal dysfunction, memory disorders, and brain damage, comprising a composition comprising uridine, an acyl derivative thereof, or a uridine phosphate.Type: ApplicationFiled: January 30, 2007Publication date: April 23, 2009Inventors: Dick Wurtman, Lisa A. Teather
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Publication number: 20090069268Abstract: This invention provides compounds, compositions and methods for treating cancer, infectious disease, an autoimmune disorder or an inflammatory condition.Type: ApplicationFiled: September 23, 2008Publication date: March 12, 2009Inventors: H. MICHAEL SHEPARD, ANDREW REIN VAINO, DANIELLE M. LEHSTEN
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Publication number: 20090054370Abstract: The invention is based on the discovery that specific dosages of pyrimidine compositions, such as uridine compositions, can be used to treat patients diagnosed with bipolar disorder.Type: ApplicationFiled: June 10, 2005Publication date: February 26, 2009Applicant: MCLEAN HOSPITAL CORPORATIONInventor: Perry Renshaw
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Publication number: 20090010932Abstract: GB virus C (GBV-C or hepatitis G virus) is a flavivirus that frequently leads to chronic viremia in humans. The invention provides compositions and methods involving an anti-GBV-C antibody or other GBV-C binding agent, or a GBV-C antigen, for inhibiting and treating HIV infections.Type: ApplicationFiled: July 24, 2008Publication date: January 8, 2009Inventors: JACK T. STAPLETON, Jinhua Xiang, Donna Klinzman, James H. McLinden
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Patent number: 7462605Abstract: This invention provides compounds, compositions and methods for treating cancer, infectious disease, an autoimmune disorder or an inflammatory condition. Therapeutic compounds useful in the methods of this invention are 5?-phosphoramidatyl, 1,5-substituted pyrimidine compounds, derivatives, analogs and pharmaceutically acceptable salts thereof.Type: GrantFiled: April 9, 2002Date of Patent: December 9, 2008Assignee: Celmed Oncology (USA), Inc.Inventors: H. Michael Shepard, Andrew Rein Vaino, Danielle M. Lehsten
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Publication number: 20080300215Abstract: Herein described are prodrugs activated by RNA-dependent DNA-polymerases, such as telomerase and retroviral reverse transcriptases, their use for the treatment of haematological tumours and of blood and blood derivatives from patients affected by retroviral infections, and their use for the preparation of pharmaceutical compositions, to be used for the treatment of solid tumours, of precancerous states and of diseases caused by infection with retroviruses.Type: ApplicationFiled: August 2, 2005Publication date: December 4, 2008Applicant: PROTERA S.R.L.Inventors: Ivano Bertini, Claudio Luchinat, Alessandro Quattrone, Massimo Calamante, Alessandro Mordini
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Publication number: 20080300214Abstract: The invention provides methods for treating or suppressing marihuana usage, withdrawal, or dependence involving administration of a therapeutically-effective amount of a cytosine-containing or cytidine-containing compound, uridine-containing compound, creatine-containing compound, adenosine-containing, or adenosine-elevating compound to a mammal.Type: ApplicationFiled: August 10, 2005Publication date: December 4, 2008Inventors: Scott E. Lukas, Perry F. Renshaw
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Publication number: 20080292553Abstract: The present invention provides phosphoramidate derivatives of a furanosyluracil analog, FAU, that can effectively deliver FAU monophosphate, or a derivative thereof, intracellularly. FAU-Phosphoramidate diesters can bypass the first step of phosphorylation and be activated intracellularly so as to be converted to nucleoside monophosphates. This results in improved formation of nucleoside triphosphates, and higher incorporation into DNA. The compounds of the invention can be used to treat cancer.Type: ApplicationFiled: November 9, 2006Publication date: November 27, 2008Inventors: Anthony F. Shields, Jiri Zemlicka, Sridhar Nimmagadda
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Patent number: 7432252Abstract: The present invention provides a method of stimulating cervical and vaginal secretions in a mammal by treatment with P2Y2 and/or P2Y4 purinergic receptor agonists. Treatment of vaginal dryness associated with menopause, chemotherapy, and various disease states as well as the treatment of vulvar pain is discussed. Suitable agonists such as UTP, CTP, ATP, dinucleotides and analogs thereof are disclosed.Type: GrantFiled: March 20, 2000Date of Patent: October 7, 2008Assignee: Inspire Pharmaceuticals, Inc.Inventors: William Pendergast, Sammy Ray Shaver, David J. Drutz, Janet L. Rideout, Benjamin R. Yerxa
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Patent number: 7429572Abstract: The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2?R)-2?-deoxy-2?-fluoro-2?-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.Type: GrantFiled: April 21, 2004Date of Patent: September 30, 2008Assignee: Pharmasset, Inc.Inventor: Jeremy Clark
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Patent number: 7419968Abstract: This invention provides methods for using novel substituted pyrimidine compounds, derivatives and analogs thereof to treat diseases such as cancer. Examples of compounds and derivatives for use in the methods are (E)-5-(2-bromovinyl)-2?-deoxy-5?-uridyl phenyl L-alaninylphosphoramidate and (E)-5-(2-bromovinyl)-2?-deoxy-5?-uridyl phenyl L-alaninyl monophosphate.Type: GrantFiled: July 21, 2000Date of Patent: September 2, 2008Assignee: Celmed Oncology (USA), Inc.Inventor: H. Michael Shepard
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Patent number: 7419966Abstract: 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.Type: GrantFiled: January 16, 2004Date of Patent: September 2, 2008Assignee: Emory UniversityInventors: Raymond F. Schinazi, Dennis C. Liotta
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Publication number: 20080188439Abstract: Disclosed are compositions and methods of treatment with uridine-based and phosphoadenosine-based cofactors for the prevention and treatment of toxicity associated with compounds such as acetaminophen, which undergo Phase II glucuronidation and sulfonation in the liver. Uridine diphosphoglucose, phosphoadenosine-phosphosulfate, and their derivatives can be administered exogenously either to prevent their depletion in the liver during treatment with acetaminophen, or to replace depleted substrates of UDPGA-transferase or PAPS-transferase in order to treat an individual after a toxic dose of acetaminophen has been ingested.Type: ApplicationFiled: October 26, 2007Publication date: August 7, 2008Inventors: Steven D. Salhanick, Hilton A. Salhanick
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Publication number: 20080152726Abstract: The present invention relates to the use of polyunsaturated fatty acids and one or more components which have a beneficial effect on total methionine metabolism selected from the group consisting of vitamin B12 and precursors thereof, vitamin B6 and derivatives thereof, folic acid, zinc and magnesium, in the manufacture of a preparation for improving the action of receptors. This preparation is advantageously applied in patients suffering from Parkinson's disease, Huntington's chorea, epilepsy, schizophrenia, paranoia, depression, sleep disorders, impaired memory function, psychoses, dementia and ADHD.Type: ApplicationFiled: March 10, 2008Publication date: June 26, 2008Applicant: N.V. NUTRICIAInventors: Amanda Johanne Kiliaan, Robert Johan Joseph Hageman