Phosphorus Containing Patents (Class 514/51)
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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: 20110135713Abstract: The present invention provides protonated compounds having antiviral and antimicrobial activity. The invention also provides antimicrobial compositions comprising protonated compounds of the invention. The protonated compounds of the invention provide efficacious antimicrobial activity against resistant strains of bacteria and opportunistic fungi. The invention also provides antiviral compositions comprising compounds of the invention. Viruses that may be treated by compositions of the invention include, but are not limited to, HIV, HSV, CMV, HBV, HCV and influenza virus.Type: ApplicationFiled: January 6, 2011Publication date: June 9, 2011Applicant: Lakewood-Amedex, Inc.Inventor: Roderic M.K. Dale
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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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Patent number: 7939510Abstract: 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: April 27, 2009Date of Patent: May 10, 2011Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Edward G. Brown
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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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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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Patent number: 7935681Abstract: 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: September 24, 2010Date of Patent: May 3, 2011Assignee: Medivir ABInventors: Nils-Gunnar Johansson, Genaidy Kalyanov, Joseph Armstrong Martin, David Bernard Smith, Anna Winqvist
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Publication number: 20110098238Abstract: A method, computer-readable medium, and system for identifying compounds from chemical libraries that can be used for the therapeutic treatment of a disease or used as lead compounds in a drug development program. In particular, information from homologous proteins is used to predict, for a target protein, molecular functions that can be used to screen libraries of compounds for individual compounds that are predicted to have high binding affinities for the target protein.Type: ApplicationFiled: December 22, 2008Publication date: April 28, 2011Applicant: GEORGIA TECH RESEARCH CORPORATIONInventors: Jeffrey Skolnick, Michal Brylinski
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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: 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: 7888330Abstract: 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: GrantFiled: November 9, 2006Date of Patent: February 15, 2011Assignee: Wayne State UniversityInventors: Anthony F. Shields, Jiri Zemlicka, Sridhar Nimmagadda
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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: 20110015149Abstract: The present application provides methods and compositions for improving the bioavailability of a lipid-containing antiviral compound, and in particular, an antiviral lipid-containing compound. In one embodiment, pharmaceutically acceptable compositions are provided that include an antiviral lipid-containing compound, or salt, ester, or prodrug thereof and one or more bioavailability enhancing compounds, such as inhibitors of cytochrome P450 enzymes.Type: ApplicationFiled: September 22, 2010Publication date: January 20, 2011Inventors: Merrick R. Almond, George R. Painter
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Publication number: 20110009356Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.Type: ApplicationFiled: September 24, 2010Publication date: January 13, 2011Applicant: Metabasis Therapeutics, Inc.Inventors: Mark D. ERION, K. Raja Reddy, Serge H. Boyer
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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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Patent number: 7863255Abstract: Antitumor treatment regimens comprising: administering, to a patient diagnosed with cancer, an antitumor agent comprising 4-amino-1-(2-cyano-2-deoxy-?-D-arabinofuranosyl)-2(1H)-pyrimidinone, or a salt thereof, by way of continuous intravenous infusion, in an amount of 2.0 to 4.0 mg per m2 total body surface area of the patient, of 4-amino-1-(2-cyano-2-deoxy-?-D-arabinofuranosyl)-2(1H)-pyrimidinone equivalent, per day, for a duration of 168 to 336 hours. Compositions for providing the methods are also disclosed.Type: GrantFiled: April 29, 2008Date of Patent: January 4, 2011Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Hiroyuki Okabe, Kazuhito Arakawa
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Publication number: 20100330164Abstract: A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5?-triphosphate (UTP), dinucleotides, cytidine 5?-triphosphate (CTP), adenosine 5?-triphosphate (ATP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.Type: ApplicationFiled: June 28, 2010Publication date: December 30, 2010Inventors: Benjamin R. Yerxa, Karla M. Jacobus, William Pendergast, Janet L. Rideout
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Publication number: 20100331258Abstract: The invention thus pertains to the use of a composition comprising: (a) uridine or uridine phosphate; and (b) docosahexaenoic acid and/or eicosapentaenoic acid, for improving memory and/or the treatment or prevention of impaired memory function, in a subject with a mini-mental state examination of 24-26, wherein said composition is enterally administered to the subject. In the MMSE test, any score of 27 or higher (out of 30) is effectively normal. In the patients with dementia, 20-26 indicates mild dementia, 10-19 moderate dementia, and below 10 severe dementia. It was the present inventors' belief that within the group of 20-26, the memory impairment in the sub-group of 24-26 may even be reversible, as the pathological pathways have just started to develop. In this group of subjects the pathological pathways have just started to develop. Clinical studies show excellent results for this subgroup.Type: ApplicationFiled: June 20, 2008Publication date: December 30, 2010Inventors: Patrick Joseph Gerardus Hendrikus Kamphuis, Martine Groenendijk, Anke Bongers
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Patent number: 7858594Abstract: 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: July 20, 2009Date of Patent: December 28, 2010Assignee: Novartis Pharma AGInventors: David Jonaitis, Richard Storer
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Publication number: 20100323982Abstract: A composition comprising (a) one or more ?-3 fatty acids selected from DHA, DPA and EPA, (b) uridine or its equivalent, and (c) a methyl donor, useful in the treatment of a person having characteristics of a prodromal dementia patient. The characteristics include e.g. a level of more than 350 ng Total-tau per litre cerebrospinal fluid (CSF), and a weight ratio of abeta-42/Phospho-tau-181 of less than 6.5 in CSF.Type: ApplicationFiled: June 20, 2008Publication date: December 23, 2010Inventors: Robert Johan Joseph Hageman, Patrick Joseph Gerardus Hendrikus Kamphuis, Ladislaus Maria Broersen
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Publication number: 20100316594Abstract: 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: ApplicationFiled: June 2, 2008Publication date: December 16, 2010Inventors: Jean-Pierre Sommadossi, Paolo LaColla, Richard Storer, Gilles Gosselin
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Patent number: 7851456Abstract: This invention is directed to a method of enhancing or facilitating the clearance of the lung mucus secretions in a subject. This invention is also directed to a method of facilitating the hydration of the lung mucus secretions in a subject. This invention is further directed to a method of preventing or treating diseases or conditions associated with impaired lung or airway function in a human or other mammal. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y6 receptor agonist compound, wherein said amount is effective to activate the P2Y6 receptors on the luminal surface of lung epithelia. The P2Y6 receptor agonist compounds useful for this invention include mononucleoside 5?-diphosphates, dinucleoside monophosphate, dinucleoside diphosphates, or dinucleoside triphosphates of general Formula I, or salts, solvates, hydrates thereof.Type: GrantFiled: June 28, 2006Date of Patent: December 14, 2010Assignee: Inspire Pharmaceuticals, Inc.Inventors: José L. Boyer, Sammy R. Shaver, James G. Douglass, III, Catherine C. Redick
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Patent number: 7851479Abstract: A pyrimidinedione derivative of formula (I) or a pharmaceutically acceptable salt thereof exhibits excellent inhibitory activity against hepatitis C virus.Type: GrantFiled: February 8, 2007Date of Patent: December 14, 2010Assignee: Samjin Pharm. Co., Ltd.Inventors: Ho-Seok Kwon, Jae-Woong Lee, Sun-Hwan Lee, Young-Hee Lee, Jeong-Ho Joo, Sun-Gan Chung, Hyun-Tae Kim, Eui-Hwan Cho, Hyun-Nam Myung
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Publication number: 20100305060Abstract: This application provides compositions or compounds as disclosed herein that are suitable for treating hepatic viral diseases, such as hepatitis C(HCV).Type: ApplicationFiled: November 26, 2008Publication date: December 2, 2010Applicant: Ligand Pharmaceuticals IncorporatedInventors: Scott J. Hecker, K. Raja Reddy
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Patent number: 7842672Abstract: A compound of Formula I, Formula II, Formula III, or Formula IV: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, therapeutic compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: July 6, 2007Date of Patent: November 30, 2010Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, James M. Chen, Alan X. Huang, Choung U. Kim, Kuei-Ying Lin, Richard L. Mackman, David A. Oare, Jason K. Perry, Oliver L. Saunders, Sundaramoorthi Swaminathan, Lijun Zhang
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Publication number: 20100298257Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.Type: ApplicationFiled: May 20, 2010Publication date: November 25, 2010Applicant: PHARMASSET, INC.Inventors: BRUCE ROSS, MICHAEL JOSEPH SOFIA, GANAPATI REDDY PAMULAPATI, SUGUNA RACHAKONDA, HAI-REN ZHANG, BYOUNG-KWON CHUN, PEIYUAN WANG
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Publication number: 20100292135Abstract: Compounds for modulating RecA protein activity are provided. In some embodiments, the compounds modulate RecA activity by interfering with assembly of monomeric RecA protein subunits into a nucleoprotein filament. In some embodiments, the compounds modulate RecA activity by interfering with adenosine triphosphate hydrolysis by the RecA protein. Methods of screening for and methods of using the compounds are also provided.Type: ApplicationFiled: May 28, 2010Publication date: November 18, 2010Inventor: SCOTT FAIN SINGLETON
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Publication number: 20100286083Abstract: A purified compound having activity against hepatitis C virus is disclosed.Type: ApplicationFiled: December 23, 2009Publication date: November 11, 2010Applicant: PHARMASSET, INC.Inventors: DONGHUI BAO, Wonsuk Chang, Dhanapalan Nagarathnam, Michael Joseph Sofia
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Patent number: 7829548Abstract: There is provided inter alia use of 2?,3?-dideoxy-3?-hydroxymethylcytidine or a prodrug or salt thereof in the manufacture of a medicament for the treatment of HIV infection wherein the reverse transcriptase of the HIV bears at least one mutation that allows an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.Type: GrantFiled: December 28, 2005Date of Patent: November 9, 2010Assignee: Medivir ABInventors: Xiao-Xiong Zhou, Hong Zhang
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Publication number: 20100272791Abstract: Provided is a composition comprising, as an active ingredient, at least one material selected from the group consisting of uridine and derivatives thereof which promote synthesis of hyaluronic acid in animal and human cell and body, and a pharmaceutical preparation containing the same. The composition and pharmaceutical preparation of the present invention is effective in the treatment and prevention of dry eye syndrome.Type: ApplicationFiled: July 8, 2010Publication date: October 28, 2010Applicant: MD BIOALPHA CO., LTD.Inventors: Myung-Gyu PARK, Min-Kyung KUON
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Patent number: 7807654Abstract: Compounds, compositions, and methods are provided for treatment of disorders related to mitochondrial dysfunction. The methods comprise administering to a mammal a composition containing pyrimidine nucleotide precursors in amounts sufficient to treat symptoms resulting from mitochondrial respiratory chain deficiencies.Type: GrantFiled: August 16, 2001Date of Patent: October 5, 2010Assignee: Wellstat Therapeutics CorporationInventors: Reid W. Von Borstel, Joel A. Saydoff
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Patent number: 7807655Abstract: The invention relates to the use of a pyrimidine nucleotide for treating affections of the peripheral nervous system, particularly polyneuropathies, neuritides, and myopathies, and the use thereof for stimulating the regeneration of nerves.Type: GrantFiled: April 10, 2003Date of Patent: October 5, 2010Assignee: Trommsdorff GmbH & Co. KG ArzneimittelInventor: Monika Hedding-Eckerich
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Publication number: 20100249056Abstract: 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: ApplicationFiled: June 9, 2010Publication date: September 30, 2010Applicants: CHIMERIX, INC., THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Karl Y. Hostetler, James R. Beadle, Jacqueline Ruiz, Merrick R. Almond, George R. Painter, Tim Riley, Paula Francom
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Publication number: 20100240604Abstract: Disclosed herein are nucleotide analogs with protected phosphates, methods of synthesizing nucleotide analogs with protected phosphates and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with protected phosphates.Type: ApplicationFiled: March 19, 2010Publication date: September 23, 2010Applicant: Alios BioPharma, Inc.Inventors: Leonid Beigelman, Lawrence Blatt, Harri Lonnberg
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Publication number: 20100227834Abstract: The invention relates to special nucleosides, for example, a nucleoside of the formula I, wherein R1-R5 are as described herein, and also to drugs which contain these nucleosides. Furthermore, the invention relates to the use of such nucleosides in a method for suppressing or reducing the formation of resistance in the case of cytostatic treatment of a cancer patient.Type: ApplicationFiled: August 13, 2007Publication date: September 9, 2010Applicant: RESprotech GmbHInventors: Rudolf Fahrig, Dieter Lohmann, Andreas Rolfs, Henrik Dieks, Janek Teubner, Jörg-Christian Heinrich
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Publication number: 20100227801Abstract: This invention relates to combinations comprising 3-[(R)-2-(N,N-dimethylamino)ethylthio-Sar]-4-(gammahydroxymethylleucine)cyclosporine, or a pharmaceutically acceptable salt, solvate or hydrate thereof; and certain nucleoside analogues, and their use in the treatment of hepatitis C virus.Type: ApplicationFiled: January 7, 2010Publication date: September 9, 2010Applicant: Scynexis, Inc.Inventor: Samuel Earl HOPKINS
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Publication number: 20100216735Abstract: Disclosed are methods of preventing or treating neuronal damage associated with oxidative stress and/or neuronal injury. The method comprises administering to a patient a pharmaceutical composition comprising a purinergic P2Y receptor ligand, in an amount effective to increase the extracellular concentration of said agonist in the brain of the subject such that at least a portion of cell surface P2Y receptors expressed by astrocytes are activated to mount a neuroprotective response. The pharmaceutical composition may be administered orally or parenterally. The pharmaceutical composition with typically be administered to an individual within at least one hour of the event that caused oxidative stress in the subject.Type: ApplicationFiled: March 17, 2008Publication date: August 26, 2010Inventor: James D. Lechleiter
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Publication number: 20100209354Abstract: The invention relates to nanoparticles made from organometallic hybrid materials made from iron carboxylates, used for example as contrast agents. The particles can also be used for the encapsulation and vectoring of molecules of interest such as active3 pharmaceutical agents, cosmetically interesting compounds and markers. Apart from the intrinsic properties thereof for imaging, said nanoparticles give good results in terms of capacity for loading with medicaments and in biocompatibility.Type: ApplicationFiled: October 1, 2008Publication date: August 19, 2010Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS, UNIVERSITE DE VERSAILLES - SAINT-QUENTIN- EN-YVELINESInventors: Patricia Horcajada-Cortes, Gérard Ferey, Christian Serre, Ruxandra Gref, Patrick Couvreur
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Publication number: 20100204162Abstract: The present invention provides a compound which is an inhibitor of sphingolipid biosynthesis for use in the treatment of a disease which has a secondary Niemann-Pick type C disease like cellular phenotype.Type: ApplicationFiled: June 26, 2008Publication date: August 12, 2010Inventors: Mary Frances Platt, Emyr Lloyd-Evans, Forbes Dennison Porter
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Patent number: 7772208Abstract: A method for the treatment or prevention of Flaviviridae infections, in particular, hepatitis C virus infection, in a host, and in particular, a human, is provided that includes administering an effective amount of a ?-L- or ?-D-2?,3?-dideoxynucleoside or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable diluent or excipient.Type: GrantFiled: January 8, 2008Date of Patent: August 10, 2010Assignees: Pharmasset, Inc., Leland Stanford Junior University, Emory UniversityInventors: Raymond Schinazi, Robert Striker, Junxing Shi
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Publication number: 20100184718Abstract: The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell.Type: ApplicationFiled: December 2, 2009Publication date: July 22, 2010Inventors: Louis S. KUCERA, Ronald A. Fleming, Khalid S. Ishaq, Gregory L. Kucera, Susan L. Morris-Natschke
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Patent number: 7759322Abstract: A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5?-triphosphate (UTP), dinucleotides, cytidine 5?-triphosphate (CTP), adenosine 5?-triphosphate (ATP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.Type: GrantFiled: June 20, 2007Date of Patent: July 20, 2010Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Karla M. Jacobus, William Pendergast, Janet L. Rideout
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ETHYNYLATED HETERODINUCLEOSIDE PHOSPHATE ANALOGS, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF
Publication number: 20100151001Abstract: The invention relates to novel ethynylated heterodinucleoside phosphate analogs, the production thereof, substances containing at least one of said compounds, and the use thereof for the treatment of cancer and infectious diseases.Type: ApplicationFiled: April 10, 2008Publication date: June 17, 2010Applicant: Eberhard Karls Universitat TubingenInventors: Herbert Schott, Peter Ludwig -
Publication number: 20100130438Abstract: A method for increasing oxytocin release through direct action on the epidermal keratinocytes is provided. The method for increasing oxytocin release in the epidermis includes increasing the calcium ion concentration in the epidermal cells. In the method of the present invention, the increase of the calcium ion concentration in the epidermal cells may be achieved by physically stimulating the skin. The physical stimulation may be achieved by applying a heat stimulus and/or a massage. The increase of the calcium ion concentration in the epidermal cells may be achieved by stimulating the epidermal cells by at least one agent selected from the group consisting of ATP, UTP, 4 alpha-phorbol 12,13-didecanoate, and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: November 12, 2009Publication date: May 27, 2010Applicant: SHISEIDO COMPANY, LTD.Inventors: Sumiko Denda, Mitsuhiro Denda, Kazuyuki Ikeyama
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Patent number: 7713948Abstract: The invention relates to the use of at least one overexpression inhibitor of DNA repair genes and oncogenes for producing a drug to increase the apoptotic effect of cytostatics after chemotherapy.Type: GrantFiled: November 20, 2003Date of Patent: May 11, 2010Assignee: Resprotect GmbHInventors: Rudolf Fahrig, Joerg-Christian Heinrich, Georg Krupitza
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Patent number: 7709449Abstract: The invention provides compounds capable of treating against hepatitis infections, particularly hepatitis B viral infections. Compounds of the invention are nucleic acid-based and preferably comprise 2, 3, 4, 5 or 6 nucleoside units.Type: GrantFiled: July 10, 2007Date of Patent: May 4, 2010Assignee: Migenix, Inc.Inventors: Radhakrishnan P. Iyer, Yi Jin, Arlene Roland, Wenqiang Zhou
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Publication number: 20100104532Abstract: The invention provides unsaturated phosphonates of Formula I or a tautomer or pharmaceutically accepatble salt thereof, as described herein, as well as pharmaceutical compositions comprising the compounds, and therapeutic methods comprising administering the compounds. The compounds have anti-viral properties and are useful for treating viral infections (e.g. HCV) in animals (e.g. humans).Type: ApplicationFiled: February 8, 2008Publication date: April 29, 2010Applicant: GILEAD SCIENCES, INC.Inventors: James M. Chen, Alan X. Huang, Richard L. Mackman, Jay Parrish, Jason K. Perry, Oliver L. Saunders, David Sperandio
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Publication number: 20100099643Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.Type: ApplicationFiled: December 22, 2009Publication date: April 22, 2010Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Publication number: 20100099645Abstract: This invention provides methods of increasing or enhancing the synthesis and levels of phospholipids, synapses, synaptic proteins, and synaptic membranes by a neural cell or brain cell; methods of treating a subject with a memory disorder, memory impairment, neurological disorder, or brain disease or disorder, comprising administering to the subject a composition comprising an omega-3 fatty acid, an omega-6 fatty acid, uridine, a metabolic precursor thereof, or a combination thereof.Type: ApplicationFiled: May 23, 2006Publication date: April 22, 2010Inventors: Richard J. Wurtman, Ingrid Richardson
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Publication number: 20100099635Abstract: The present invention is directed to a method for treating cystic fibrosis. The method comprises the steps of: identifying a patient suffering from cystic fibrosis, and administering to the patient an effective amount of denufosol or a pharmaceutically acceptable salt thereof and an effective amount of a macrolide. In one method, denufosol and the macrolide are administered by inhalation, preferably in a single formulation. In another method, denufosol is administered by inhalation and the macrolide is administered orally. The present invention is also directed to a pharmaceutical formulation comprising denufosol or a pharmaceutically acceptable salt thereof, a macrolide, and a pharmaceutically acceptable carrier. Preferred denufosol is denufosol tetrasodium and preferred macrolide is azithromycin. The pharmaceutical formulation preferably is in a form of an inhalable dry powder or in a liquid form.Type: ApplicationFiled: October 21, 2009Publication date: April 22, 2010Inventors: Donald J. Kellerman, Ramesh Krishnamoorthy, José L. Boyer, Amy E. Schaberg