2,4-diketone Pyrimidine Or Derivative (e.g., Uracil, Etc.) Patents (Class 514/50)
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Publication number: 20110201675Abstract: The invention includes compositions and methods of treatment of cancers susceptible to treatment with nucleotide analog chemotherapeutic agent, including cancers in which nucleotide analog resistant tumors have developed, including identifying a subject having cancer susceptible to treatment with a nucleotide analog chemotherapeutic agent and a mitotic disruptor/polo-like kinase (Plk) pathway inhibitor to a subject; and monitoring the subject for a reduction or stabilization of at least one sign or symptom of cancer.Type: ApplicationFiled: April 17, 2008Publication date: August 18, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Antonio Jimeno, Manuel Medina Hidalgo
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Publication number: 20110195922Abstract: 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-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2?-deoxy-?-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. The 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2?-deoxy-?-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.Type: ApplicationFiled: December 8, 2009Publication date: August 11, 2011Applicants: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, L'Universite Montpellier IIInventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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Patent number: 7994143Abstract: The present invention relates to phosphonate, nucleoside phosphonate or nucleoside phosphate compounds, compositions containing them, processes for obtaining them, and their use in treating a variety of medical disorders, in particular viral infections, cancers and the like.Type: GrantFiled: June 9, 2010Date of Patent: August 9, 2011Assignees: Chimerix, Inc., The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle, Jacqueline Ruiz, Merrick R. Almond, George R. Painter, Timothy A. Riley, Paula Francom
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Publication number: 20110182856Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof. These compounds inhibit serine protease, particularly the hepatitis C virus NS3-NS4A protease.Type: ApplicationFiled: March 29, 2011Publication date: July 28, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Amaud Le Tiran, Emanuele Perola
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Publication number: 20110182857Abstract: Liquid pharmaceutical compositions for administration to a mucosal surface, including a therapeutic agent and a pectin with a low degree of esterification are described. Such compositions gel, or can be adapted to gel, at the site of application in the absence of an extraneous source of divalent metal ions.Type: ApplicationFiled: April 1, 2011Publication date: July 28, 2011Applicant: ARCHIMEDES DEVELOPMENT LIMITEDInventors: Peter James WATTS, Lisbeth ILLUM
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Publication number: 20110183933Abstract: In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits.Type: ApplicationFiled: November 5, 2008Publication date: July 28, 2011Inventors: Timothy J. Guzi, David A. Parry, Marc A. Labroli, Michael P. Dwyer, Kamil Paruch
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Publication number: 20110183021Abstract: This invention encompasses methods of preserving protein function by contacting a protein with a composition comprising one or more purine nucleosides (such as e.g., adenosine or uridine) and an antioxidant (such as e.g., manganese). In addition, the invention encompasses methods of treating and/or preventing a side effect of radiation exposure and methods of preventing a side effect of radiotherapy comprising administration of a pharmaceutically effective amount of a composition comprising one or more purine nucleosides (such as e.g., adenosine or uridine) and an antioxidant (such as e.g., manganese) to a subject in need thereof. The compositions may comprise D. radiodurans extracts.Type: ApplicationFiled: August 18, 2008Publication date: July 28, 2011Inventors: Michael J. Daly, Elena K. Gaidamakova, Vera Y. Metrosova, Rodney L. Levine, Nancy B. Wehr
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Publication number: 20110172178Abstract: It has been discovered that ?-L-2?-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.Type: ApplicationFiled: March 21, 2011Publication date: July 14, 2011Applicant: NOVARTIS AGInventors: David Standring, Jean-Pierre Sommadossi, April L. Patty, Maria Seifer
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Publication number: 20110166096Abstract: Disclosed are uracil derivatives of the formula (I): wherein R1, R2, R3, and X are as defined herein, and use thereof as therapeutic agents. The uracil derivatives are used in particular together with a cytostatic agent for suppressing or reducing resistance building up on cytostatic treatment.Type: ApplicationFiled: June 25, 2009Publication date: July 7, 2011Applicant: RESPROTECT GMBHInventors: Rudolf Fahrig, Kurt Eger, Martin Führer, Nicole Heinze, Matthias Klemm, Jörg-Christian Heinrich
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Publication number: 20110165120Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease.Type: ApplicationFiled: February 28, 2011Publication date: July 7, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola
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Publication number: 20110160158Abstract: A method of treating an individual diagnosed with bipolar disorder, comprises determining the number of manic episodes and/or depressive episodes experienced by an individual exhibiting one or more symptoms of bipolar disorder (e.g., bipolar disorder I); and if the number of manic episodes and/or the number of depressive episodes is each 2 or greater (e.g., 3 or greater, 4 or greater, 5 or greater, 6 or greater, 10 or greater, or 15 or greater), administering to the individual an effective amount of a uridine composition.Type: ApplicationFiled: June 12, 2009Publication date: June 30, 2011Applicant: REPLIGEN CORPORATIONInventor: David R. Jacoby
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Publication number: 20110159111Abstract: The invention provides combinations of an ancillary compound of the formula (0): and a compound of the formula (I?): Also provided are crystalline forms of the constituent compounds, methods for making them and their uses in treating cancers.Type: ApplicationFiled: June 29, 2007Publication date: June 30, 2011Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Jayne Elizabeth Curry, Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson
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Publication number: 20110158935Abstract: Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.Type: ApplicationFiled: December 29, 2009Publication date: June 30, 2011Inventor: Kelly Sullivan Kraft
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Publication number: 20110150961Abstract: Anti-infective catheters are provided. Such catheters comprise a composition that comprises a pyrimidine analog, polyurethane, and cellulose or a cellulose-derived polymer, for example, in form of a coating. In addition, anti-infective compositions and methods of making and using anti-infective catheters are provided.Type: ApplicationFiled: February 18, 2009Publication date: June 23, 2011Applicant: Angiotech International AGInventors: Joy Erann Perry, Alexandra M. Chamberlain, Scott F. Rosebrough
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Publication number: 20110150829Abstract: Compounds having the formula I wherein R1, R2 and R3 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: January 26, 2011Publication date: June 23, 2011Applicant: F. Hoffmann-La Roche AGInventors: Han Ma, Keshab Sarma, David Bernard Smith
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Publication number: 20110150836Abstract: This application relates to a purine derivative and pharmaceutical compositions which are useful for treating a hepatitis B viral infection or a hepatitis C viral infection.Type: ApplicationFiled: December 16, 2010Publication date: June 23, 2011Applicant: Gilead Sciences, Inc.Inventors: Randall L. HALCOMB, Sundaramoorthi Swaminathan, Daniel B. Tumas
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Patent number: 7964580Abstract: 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: GrantFiled: March 21, 2008Date of Patent: June 21, 2011Assignee: Pharmasset, Inc.Inventors: Michael Joseph Sofia, Jinfa Du, Peiyuan Wang
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Publication number: 20110144051Abstract: Compounds, compositions, and methods are provided for treatment of disorders related to mitochondrial dysfunction. The methods comprise administering to a mammal a composition containing pyrimidien nucleotide precursors in amounts sufficient to treat symptoms resulting from mitochondrial respiratory chain deficiencies.Type: ApplicationFiled: February 16, 2011Publication date: June 16, 2011Applicant: Wellstat Therapeutics CorporationInventor: Reld W. Von Borstel
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Publication number: 20110142794Abstract: A method for determining a therapeutically effective amount of suramin for administering to a patient, who is to receive a cytotoxic agent, which comprises the steps of determining the circulating suramin concentration in the patient; administering suramin, if required, to establish a low circulating concentration of suramin in the patient of below about 200 ?M; and administering the chemotherapeutic agent to the patient when the low circulating concentration of suramin is present in the patient. Conveniently a nomogram can be constructed for use in clinical settings with the suramin.Type: ApplicationFiled: February 21, 2011Publication date: June 16, 2011Inventors: Jessie L.-S. Au, M. Guillaume Wientjes
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Publication number: 20110129463Abstract: Provided are quinazolin-4(3A)-one derivatives, which are inhibitors of the ubiquitin ligase activity of a human polypeptide, particularly to POSH inhibitors, and to compositions and methods for the treatment RING E3 ubiquitin ligase related diseases.Type: ApplicationFiled: November 26, 2010Publication date: June 2, 2011Applicant: Proteologics, Ltd.Inventors: Omri EREZ, Philippe NAKACHE
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Publication number: 20110129440Abstract: The present invention relates to novel Heterocyclic Urea and Thiourea Derivatives of formula (I), compositions comprising the Heterocyclic Urea and Thiourea Derivatives, and methods for using the Heterocyclic Urea and Thiourea Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 27, 2008Publication date: June 2, 2011Inventors: Praveen K. Tadikonda, David F. Cauble, Timothy J. Guzi, M. Arshad Siddiqui
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Patent number: 7951789Abstract: 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: GrantFiled: December 27, 2007Date of Patent: May 31, 2011Assignees: Idenix Pharmaceuticals, Inc., L'Université Montpellier IIInventors: Jean-Pierre Sommadossi, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
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Patent number: 7947661Abstract: 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: GrantFiled: August 10, 2005Date of Patent: May 24, 2011Assignee: The McLean Hospital CorporationInventors: Scott E. Lukas, Perry F. Renshaw
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Publication number: 20110117193Abstract: The present disclosure provides fast disintegrating formulations for the treatment of human immunodeficiency virus (HIV) and acquired immune deficiency syndrome (AIDS) in patients such as neonatal, perinatal and pediatric children. Neonatal and perinatal formulations provide for the prevention or reduction of incidence of mother to child transmission of HIV. Also provided are formulations and methods for treating pediatric children having HIV/AIDS. The orally administered fast disintegrating formulations are in granule and tablet form and are specially formulation for children to increase adherence to treatment protocols.Type: ApplicationFiled: January 16, 2009Publication date: May 19, 2011Applicant: Duquesne University of the Holy SpiritInventors: Moji C. Adeyeye, Fredrick Esseku, Anajali Joshi
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Publication number: 20110110890Abstract: The embodiments provide compounds of the general Formula I and compound 105S, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: November 8, 2010Publication date: May 12, 2011Applicant: INTERMUNE, INC.Inventors: Leonid Beigelman, Guangyi Wang, Brad Buckman, Antitsa Dimitrova Stoycheva
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Publication number: 20110104267Abstract: The present invention relates to the stable pharmaceutical dosage forms of combination of antiretroviral agents. More particularly, the present invention relates to stable pharmaceutical dosage forms of Lamivudine, Zidovudine and Nevirapine, prepared by granulation technology.Type: ApplicationFiled: April 24, 2006Publication date: May 5, 2011Applicant: AUROBINDO PHARMA LIMITEDInventor: Umesh Mutt Hanjagi
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Publication number: 20110104108Abstract: The present invention relates to the use of the compound according to formula (I), below for the treatment of tumors, cancer and hyperproliferative diseases, among other conditions or disease states: Where X is H or F; R1 and R2 are independently H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or a phosphodiester group, a (A) or (B) group; Where Nu is a radical of a biologically active compound such as an anticancer, antiviral or antihyperproliferative compound such that an amino group or hydroxyl group from said biologically active agent forms a phosphate, phosphoramidate, carbonate or urethane group with the adjacent moiety; each R8 is independently H, or a C1-C20 alkyl or ether group, preferably a C1-C12 alkyl group; k is 0-12, preferably, 0-2; and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: January 11, 2011Publication date: May 5, 2011Applicant: YALE UNIVERSITYInventor: Yung-Chi CHENG
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Publication number: 20110105594Abstract: The present invention relates to the use of a taste masking agent selected from the group of cellulose; starch; xanthan gum; gellan gum; alginate; galactomannans such as fenugreek, guar gum, tara gum, locust bean gum, and cassia gum; gum karaya; gum tragacanth; carrageenan; and mixture thereof, for improving one or more of mouth feel, taste, aftertaste and smell of a liquid aqueous nutritional composition comprising a nucleotide and/or a nucleoside. It also relates to a nutritional composition comprising an unsavoury nucleotide and/or a nucleoside component, having improved sensory characteristics such as improved mouth feel, taste, aftertaste and smell. In particular, it relates to a composition comprising said un-savoury nucleotide and/or a nucleoside component, in particular comprising an uridine-containing nucleotide and/or a nucleoside in combination with an unsavoury edible oil, such as a fish oil.Type: ApplicationFiled: December 22, 2008Publication date: May 5, 2011Inventors: Esther Jacqueline De Kort, Martin Groenendijk, Patrick Joseph Gerardus Hendrikus Kamphuis
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Patent number: 7932235Abstract: This invention relates to novel triazolyl tropane derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by blocking or reducing the binding ability of the CCR5 receptor.Type: GrantFiled: November 16, 2007Date of Patent: April 26, 2011Assignee: Concert Pharmaceuticals, Inc.Inventor: Roger Tung
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Publication number: 20110091418Abstract: Methods for treating viral infections using polyamine analogs, including mitoguazone (MGBG), are provided. In these methods, polyamine analogs destroy macrophages that act as viral reservoirs, facilitating the destruction of the viruses that dwell within the macrophages. Examples of viral infections that may be treated with the present methods include, but are not limited to, infections from human immunodeficiency viruses. These methods differ from previous methods of treatment using polyamine analogs, wherein the polyamine analogs were administered only as anti-tumor agents.Type: ApplicationFiled: December 21, 2010Publication date: April 21, 2011Applicant: Pathlogica, LLCInventors: Michael S. McGrath, Kenneth G. Hadlock
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Publication number: 20110092453Abstract: The present invention relates to the prevention or treatment of hydrocephalus. In one embodiment, the invention includes the use of one or more bioavailable folate derivatives, or salts thereof, for the prevention or treatment of hydrocephalus. Examples of more bioavailable folate derivatives that may be used include any combination of: folinic acid, tetrahydrofolate, thymidine, 10-formyltetrahydrofolate or methyltetrahydrofolate, or salts thereof. The invention also relates to a composition comprising two or more bioavailable folate derivative(s); for example, folinic acid and tetrahydrofolate.Type: ApplicationFiled: August 7, 2008Publication date: April 21, 2011Applicant: THE UNIVERSITY OF MANCHESTERInventors: Jaleel Ahmed Miyan, Penelope Jane Owen-Lynch
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Patent number: 7928086Abstract: It has been discovered that ?-L-2?-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.Type: GrantFiled: January 9, 2007Date of Patent: April 19, 2011Assignee: Novartis AGInventors: David Standring, Jean-Pierre Sommadossi, April L. Patty, Maria Seifer
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Patent number: 7923448Abstract: The present invention is directed to a method of treating a subject with acute spinal cord injury by administering a purine receptor antagonist to the subject under conditions effective to treat spinal cord injury. The purine receptor antagonist inhibits P2X purine receptor activation. The inhibition of P2X purine receptor activation can also be used in conjunction with methods of treating a subject with spinal cord ischemia resulting from stroke or vascular insult, interruption, or mechanical injury, treating a subject with ischemic or traumatic insults of brain tissue in regions expressing P2X receptors, and for inhibiting ATP-triggered brain or spinal cord cell death.Type: GrantFiled: November 2, 2004Date of Patent: April 12, 2011Assignees: Cornell Research Foundation, Inc., New York Medical CollegeInventors: Maiken Nedergaard, Steven A. Goldman
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Publication number: 20110076276Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: June 26, 2008Publication date: March 31, 2011Applicants: Gilead Sciences, Inc., Korean Research Institute of Chemical TechnologyInventors: Hongyan Guo, Choung U. Kim, Ill Y. Lee, Michael L. Mitchell, Gerry Rhodes, Jong C. Son, Lianhong Xu
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Patent number: 7915233Abstract: Compounds, compositions, and methods are provided for treatment of disorders related to mitochondrial dysfunction. The methods comprise administering to a mammal a composition containing pyrimidien nucleotide precursors in amounts sufficient to treat symptoms resulting from mitochondrial respiratory chain deficiencies.Type: GrantFiled: August 31, 1999Date of Patent: March 29, 2011Assignee: Wellstat Therapeutics CorporationInventor: Reld W. Von Borstel
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Patent number: 7915234Abstract: The present invention relates to novel uridine esters of the general formula wherein R represents a carboxylic acid residue, preferably a fatty acid residue and R? represents hydrogen or a hydroxy group, their use as pharmaceutically active agents against a variety of diseases, methods for the preparation of said uridine esters and pharmaceutical compositions containing at least one uridine ester as active ingredient. The present invention relates also to a drug combination comprising free fatty acids and/or fatty acid esters and uridine, deoxyuridine, uridine monophosphate and/or deoxyuridine monophosphate, and to the use of such a drug combination.Type: GrantFiled: September 29, 2004Date of Patent: March 29, 2011Assignee: Trommsdorff Gmbh & Co. KG ArzneimittelInventor: Rudy Susilo
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Publication number: 20110070192Abstract: Processes for the preparation of racemic and optically active nucleoside analogs of formula (A) are described. These compounds are useful as anti-infective agents, antisense therapeutic agents and hybridization assay probes.Type: ApplicationFiled: November 8, 2004Publication date: March 24, 2011Inventors: Bruno Tse, Borcherng Hong, Wei-Hung Chen, Yea-Fen Jiang, Shuo-Cang Zhang, Subramanian Marappan, Sepehr Sarshar
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Publication number: 20110065631Abstract: A process for the synthesis of bisfuran intermediates of formula (0) useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed. Furthermore disclosed is a HIV protease inhibitor of formula (IV) as well as various intermediates thereof.Type: ApplicationFiled: March 29, 2007Publication date: March 17, 2011Applicant: Gilead Sciences, IncInventors: Kenneth R. Crawford, Eric D. Dowdy, Arnold Gutierrez, Richard Polniaszek, Richard H. Yu
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Publication number: 20110065663Abstract: The present invention relates to a combination of therapeutic agents comprising: (a) a cytosine-based anti-cancer drug and/or a purine-based anticancer drug and (b) a therapeutic agent selected from the group consisting of thymidine phosphorylase inhibitors, and antibiotics against Mollicutes bacteria. The present invention also relates to the simultaneous, separate or sequential use of said combination for the treatment of cancer in mammals, especially in humans. The present invention also relates to methods of treatment of cancer, preferably in mammals infected with Mollicutes bacteria.Type: ApplicationFiled: May 15, 2009Publication date: March 17, 2011Inventors: Jan Balzarini, Sandra Liekens
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Publication number: 20110053884Abstract: Combinations of antiretroviral nucleoside reverse transcriptase inhibitors, and methods for their use in treating retroviral infections, are provided. In one embodiment, the combinations include non-thymidine nucleoside antiretroviral agents, such as tenofovir-DF, abacavir, APD and DAPD, that select for the K65R mutation and relatively low doses of zidovudine (AZT) or other thymidine nucleoside antiretroviral agents. The thymidine nucleoside antiretroviral agents retard development of the K65R mutation, and at the low doses, are less likely to produce side effects. In another embodiment, the combinations include DAPD and AZT. DAPD retards the development of TAMs, and AZT retards the development of the K65R mutation. In a third embodiment, the combinations include adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog.Type: ApplicationFiled: September 29, 2008Publication date: March 3, 2011Inventor: Raymond F. Schinazi
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Publication number: 20110039798Abstract: The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/AIDS.Type: ApplicationFiled: July 9, 2008Publication date: February 17, 2011Applicant: EASTERN VIRGINIA MEDICAL SCHOOLInventors: Gustavo F. Doncel, Keykavous Parang, Hitesh Kumar Agarwal
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Publication number: 20110039800Abstract: The present invention concerns a prolonged release bioadhesive mucosal therapeutic system containing at least one active principle, with an active principle dissolution test of more than 70% over 8 hours and to a method for its preparation. Said bioadhesive therapeutic system comprises quantities of natural proteins representing at least 50% by weight of active principle and at least 20% by weight of said tablet, between 10% and 20% of a hydrophilic polymer, and compression excipients, and comprising between 4% and 10% of an alkali metal alkylsulphate to reinforce the local availability of active principle and between 0.1% and 1% of a monohydrate sugar.Type: ApplicationFiled: July 2, 2010Publication date: February 17, 2011Inventors: Jean-Marc AIACHE, Dominique Costantini, Christine Chaumont
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Patent number: 7888391Abstract: 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: GrantFiled: March 10, 2008Date of Patent: February 15, 2011Assignee: N.V. NutriciaInventors: Amanda Johanne Kiliaan, Robert Johan Joseph Hageman
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Publication number: 20110033461Abstract: Compositions which act synergistically to inhibit the growth of cancer cells and methods of use thereof are disclosed.Type: ApplicationFiled: March 12, 2009Publication date: February 10, 2011Inventors: Vladimir Ratushny, Erica Golemis, Igor Astsaturov, Iiya G. Serebriiskii, Louis M. Weiner
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Patent number: 7879816Abstract: The present invention relates to the use of the compound according to formula (I), below for the treatment of tumors, cancer and hyperproliferative diseases, among other conditions or disease states: Where X is H or F; R1 and R2 are independently H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or a phosphodiester group, a (A) or (B) group; Where Nu is a radical of a biologically active compound such as an anticancer, antiviral or antihyperproliferative compound such that an amino group or hydroxyl group from said biologically active agent forms a phosphate, phosphoramidate, carbonate or urethane group with the adjacent moiety; each R8 is independently H, or a C1-C20 alkyl or ether group, preferably a C1-C12 alkyl group; k is 0-12, preferably, 0-2; and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 5, 2006Date of Patent: February 1, 2011Assignee: Yale UniversityInventor: Yung-chi Cheng
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Publication number: 20110014204Abstract: The present invention relates to targets of loss of imprinting (LOI) affected IGF2 gene products in pre-malignant tissues, where methods of inhibiting those targets, including IGFR1, are disclosed to prevent tumor development in subjects at risk for developing colorectal cancer (CRC). The present invention also relates to methods of identifying increased risk in developing CRC in a subject, including methods of assessing the efficacy of a chemotherapeutic regimen. Further, the present invention relates to methods for identifying anti-neoplastic agents.Type: ApplicationFiled: December 7, 2007Publication date: January 20, 2011Inventors: Andrew P. Feinberg, Andre Levchenko, Dan L. Longo, Minoru S.H. Ko
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Publication number: 20110014165Abstract: The invention relates to a composition comprising a stably integrating delivery vector; and a modified mammalian thymidylate kinase (tmpk) wherein the modified mammalian tmpk increases phosphorylation of a prodrug relative to phosphorylation of the prodrug by wild-type human tmpk. The invention also relates to use of these compositions in methods of treatment of diseases such as graft versus host disease and cancer.Type: ApplicationFiled: July 26, 2010Publication date: January 20, 2011Inventors: Jeffrey A. Medin, Arnon Lavie, Daniel H. Fowler
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Publication number: 20110009357Abstract: The invention pertains to the use of a lipid fraction for the support of brain function. The lipid fraction comprises the medium-chain fatty acids at least 4 g hexanoic acid and/or at least 5 g octanoic acid, at least 1 g eicosapentaenoic acid, and in addition more than 0.4 g ?-linolenic acid per 100 g fatty acids of the lipid fraction.Type: ApplicationFiled: June 20, 2008Publication date: January 13, 2011Inventors: Robert Johan Joseph Hageman, Eline Marleen Van Der Beek, Martine Groenendijk, Patrick Joseph Gerardus Hendrikus Kamphuis
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Publication number: 20110009351Abstract: The present invention relates to a novel assay or screen for identifying compounds with potential therapeutic value for the treatment of protein trafficking diseases such as Cystic Fibrosis (CF) and nephrogenic diabetes insipidus (NDI). The usual approach involves expressing the mutant form of the gene in cells and assaying function in a multiwell format when cells are exposed to libraries of compounds. Although such functional assays are useful, they do not directly test the ability of a compound to correct defective trafficking of the protein. To address this a novel corrector screening assay for CF has been developed in which the appearance of the mutant protein at the cell surface is measured as the assay output. This assay was used to screen more than 3100 compounds. This novel screening approach to protein trafficking diseases is robust and general, and may enable the selection of molecules that can be translated rapidly to a clinical setting.Type: ApplicationFiled: May 9, 2008Publication date: January 13, 2011Inventors: David Y. Thomas, John Hanrahan, Graeme Carlile, Renaud Robert
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Publication number: 20110002982Abstract: Liposomes that contain at least 10 mol % of a negatively charged lipid coupled to a non-zwitterionic moiety are stable in the blood. Liposomes containing at least 1 mol % of such lipids may be frozen safely.Type: ApplicationFiled: September 16, 2010Publication date: January 6, 2011Inventors: Paul TARDI, Murray Webb, Lawrence D. Mayer, Ludger M. Ickenstein