Phosphorus Containing Patents (Class 514/51)
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Publication number: 20120270830Abstract: Nutritional compositions and methods of making and using the nutritional compositions are provided. In a general embodiment, the present disclosure provides a nutritional composition including theanine and one or more exogenous nucleotides. The nutritional compositions can be specifically used to treat functional bowel disorders, including inflammatory bowel syndrome.Type: ApplicationFiled: August 23, 2010Publication date: October 25, 2012Applicant: NESTEC S.A.Inventors: Norman Alan Greenberg, Peter Geoffrey McLean, Magali Faure
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Publication number: 20120263678Abstract: Provided are compounds of Formula I: nucleosides, nucleoside phosphates and prodrugs thereof, wherein R6 is CN, ethenyl, 2-haloethen-1-yl, or (C2-C8)-alkyn-1-yl. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.Type: ApplicationFiled: April 13, 2012Publication date: October 18, 2012Applicant: GILEAD SCIENCES, INC.Inventors: Aesop Cho, Choung U. Kim, Thorsten A. Kirschberg, Michael R. Mish, Neil Squires
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Publication number: 20120258928Abstract: Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:Type: ApplicationFiled: April 5, 2012Publication date: October 11, 2012Applicant: GILEAD PHARMASSET LLCInventors: JINFA DU, DHANAPALAN NAGARATHNAM, GANAPATI REDDY PAMULAPATI, BRUCE S. ROSS, MICHAEL JOSEPH SOFIA
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Patent number: 8283336Abstract: The invention pertains to a composition comprising (i) uridine in nucleobase, nucleoside and/or nucleotide form; (ii) docosahexaenoic acid (DHA) and/or eicosapentaenoic acid (EPA); and (iii) a tocopherol and/or an equivalent thereof, wherein said composition has: a) a weight of 200-3000 mg per unit dose; b) an energy content of less than 50 kcal per unit dose; and/or c) a volume between 0.1 and 10 ml per unit dose. The invention also pertains to the use of such composition in reducing abeta plaque burden and neurodegeneration, in the treatment of diseases related with imparted nerve functioning, in particular dementia, Alzheimer's disease and memory disorders.Type: GrantFiled: October 27, 2008Date of Patent: October 9, 2012Assignee: N. V. NutriciaInventors: Martine Groenendijk, Robert Johan Joseph Hageman, Patrick Joseph Gerardus Hendrikus Kamphuis, Erwin Peke Meijer
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Publication number: 20120237480Abstract: The present invention relates to 2?-allene-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.Type: ApplicationFiled: March 16, 2012Publication date: September 20, 2012Inventors: YAT SUN OR, Jun Ma, Guoqiang Wang, In Jong Kim, Jiang Long, Yao-Ling Qiu
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Publication number: 20120225839Abstract: Compounds of formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen, —C(?O)R6 or —C(?O)CHR7—NH2; R2 is hydrogen; or C1-C6alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C1-C6alkyl, C2-C6-alkenyl and C1-C6alkoxy, hydroxy or amino, or R2 is naphtyl; or R2 is indolyl, R3 is hydrogen, C1-C6alkyl, benzyl; R4 is hydrogen, C1-C6alkyl, benzyl; or R3 and R4 together with the carbon atom to which they are attached form C3-C7cycloalkyl; R5 is C1-C10alkyl, C3-C7-cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C1-C6alkoxy, amino, mono- and diC1-C6alkylamino; R6 is C1-C6 alkyl; R7 is C1-C6 alkyl; R8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.Type: ApplicationFiled: September 29, 2010Publication date: September 6, 2012Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Michael Pelcman, Bengt Christian Sund, Horst Jurgen Wahling, Pedro Manuel Passos Pinho, Anna Winqvist, Karl Magnus Nilsson
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Patent number: 8258116Abstract: The present invention relates to therapeutic combinations comprising a protease inhibitor and a polymerase inhibitor for the treatment of HCV. The present invention also relates to therapeutic combinations comprising VX-950 and a polymerase inhibitor. Also within the scope of the invention are methods using the therapeutic combinations of the present invention for treating HCV infection or alleviating one or more symptoms thereof in a patient. The present invention also provides kits comprising the combinations of the present invention.Type: GrantFiled: May 5, 2008Date of Patent: September 4, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ann Kwong, Nagraj Mani, Yi Zhou, Chao Lin
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Patent number: 8242087Abstract: This invention relates to novel phosphate-modified nucleosides, and methods for producing them, being useful for the prevention or treatment of a viral infection in a mammal, and for preparing oligonucleotides by DNA/RNA polymerase-dependent amplification, e.g. PCR.Type: GrantFiled: August 27, 2009Date of Patent: August 14, 2012Assignee: K.U.Leuven Research & DevelopmentInventors: Olga Adelfinskaya, Piet Herdewijn
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Publication number: 20120190620Abstract: The present invention discloses methods to identify targets, pathways and molecules regulating purinosomes and their uses for treating pathophysiological disorders associated with purinosomes. Disclosed are methods related to both label-free cellular assays and fluorescence imaging to confirm the regulatory roles of various targets and molecules in purinosome dynamics. Disclosed are methods to classify molecules and the uses of these molecules for different indications. Specifically, the purinosome-disrupting molecules can be used for improved prevention and treatment of cancer development.Type: ApplicationFiled: July 18, 2011Publication date: July 26, 2012Inventors: Stephen Benkovic, Ye Fang, Songon An, Florence Verrier
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Publication number: 20120189597Abstract: Nutritional compositions and methods of making and using the nutritional compositions are provided. In a general embodiment, the present disclosure provides a nutritional composition including one or more exogenous nucleotides.Type: ApplicationFiled: August 9, 2010Publication date: July 26, 2012Applicant: NESTEC S.A.Inventors: Norman Alan Greenberg, Douglas Richard Bolster
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Publication number: 20120184503Abstract: Disclosed are nutritional compositions including human milk oligosaccharides and nucleotides that can be administered to preterm infants, term infants, toddlers, and children for reducing inflammation and the incidence of inflammatory diseases.Type: ApplicationFiled: December 22, 2011Publication date: July 19, 2012Applicant: ABBOTT LABORATORIESInventors: Rachael Buck, Debra L. Thomas, Joseph P. Schaller
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Publication number: 20120165286Abstract: Disclosed herein are cyclic nucleotide analogs, methods of synthesizing cyclic nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with cyclic nucleotide analogs.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
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Patent number: 8207143Abstract: 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: January 11, 2011Date of Patent: June 26, 2012Assignee: Yale UniversityInventor: Yung-chi Cheng
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Patent number: 8193338Abstract: A di(pyrimidine nucleoside 5?-)polyphosphate is synthesized by converting a pyrimidine nucleoside 5?-triphosphate into a pyrimidine nucleoside 5?-cyclic triphosphate by use of a condensing agent, and subsequently reacting the pyrimidine nucleoside 5?-cyclic triphosphate with a pyrimidine nucleotide in the presence of a salt of a metal selected from among magnesium, manganese, and iron. Through the method of the invention, a di(pyrimidine nucleoside 5?-)polyphosphate can be synthesized from an unprotected pyrimidine nucleoside 5?-phosphate serving as a starting material at a synthesis yield of 50% or higher. Therefore, the method of the invention is suitable for large-scale synthesis of a di(pyrimidine nucleoside 5?-)polyphosphate.Type: GrantFiled: July 25, 2007Date of Patent: June 5, 2012Assignee: Yamasa CorporationInventors: Satoru Kogo, Kohei Yamada, Yuko Iwai, Kazuomi Osawa, Hiroyuki Hayakawa
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Patent number: 8193165Abstract: The present invention relates to novel compounds according to the general formulas I, II, III, IV or V: wherein B is nucleoside base according to the structure: and the remaining variables as defined in the specification, and pharmaceutical compositions comprising the compounds. The compounds are useful interalia as anti-viral agents in viral therapy.Type: GrantFiled: August 17, 2009Date of Patent: June 5, 2012Assignee: Yale UniversityInventors: Yung-chi Cheng, Hiromichi Tanaka, Masanori Baba
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Publication number: 20120122810Abstract: 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: January 23, 2012Publication date: May 17, 2012Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Patent number: 8173620Abstract: The disclosure encompasses caged compounds such as caged nucleoside phosphoesters (caged nucleotides). In an embodiment, the caged nucleotides include compounds corresponding to those described by formula (I) that may be activated by two-photon excitation, and methods of synthesis of such compounds. 8-Bromo-7-hydroxyquinoline-caged ATP was synthesized and examined for its photochemistry as a biologically useful, temporally and spatially controlled ATP-releasing reagent. The combination of two-photon excitation hydrolysis and activation of caged ATP enables methods for finely focusing ATP activation at the sub-cellular level or to a greater depth of activation, thereby providing improved resolution of ATP-dependent processes at the cellular level.Type: GrantFiled: August 20, 2009Date of Patent: May 8, 2012Assignee: University of Georgia Research Foundation, Inc.Inventors: Timothy M. Dore, Yue Zhu, Khalilah G. Reddie, James D. Lauderdale
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Publication number: 20120108531Abstract: Disclosed herein are novel phosphonate nucleosides and thiophosphonate nucleosides comprising a phosphonalkoxy-substituted or phosphonothioalkyl-substituted five-membered, saturated or unsaturated, oxygen-containing or sulfur-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections.Type: ApplicationFiled: November 8, 2011Publication date: May 3, 2012Applicant: K.U.LEUVEN RESEARCH & DEVELOPMENTInventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De clercq
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Patent number: 8168597Abstract: 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: GrantFiled: October 21, 2009Date of Patent: May 1, 2012Assignee: Inspire Pharmaceuticals, Inc.Inventors: Donald J. Kellerman, Ramesh Krishnamoorthy, José L. Boyer, Amy E. Schaberg
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Publication number: 20120093729Abstract: 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: December 19, 2011Publication date: April 19, 2012Applicant: METABASIS THERAPEUTICS, INC.Inventors: Mark D. ERION, K. Raja REDDY, Serge H. BOYER
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Patent number: 8158606Abstract: 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: March 21, 2011Date of Patent: April 17, 2012Assignee: Novartis, AGInventors: David Standring, Jean-Pierre Sommadossi, April Patty, Maria Seifer
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Patent number: 8148349Abstract: The present invention provides nucleoside cyclic phosphoramidates of formula (I), pharmaceutical compositions comprising the compounds of formula (I) and methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection using the compounds of formula (I).Type: GrantFiled: December 14, 2007Date of Patent: April 3, 2012Assignees: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.P.A., Merck Sharp & Dohme Corp.Inventors: Malte Meppen, Frank Narjes, Barbara Pacini, Cristina Gardelli, Philippe L. Durette
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Patent number: 8143234Abstract: The present invention provides methods of improving a cognitive function or a neurological function, treating or ameliorating a decline in a cognitive function or a neurological function, increasing cytidine levels, or treating a neurological disorder in a subject, comprising administering a uridine, a uridine precursor, or a derivative or metabolite thereof to the subject. The invention also provides methods of improving neural function, comprising contacting the neuron with a uridine, a uridine precursor, or a derivative or metabolite thereof.Type: GrantFiled: September 20, 2004Date of Patent: March 27, 2012Assignee: Massachusetts Institute of TechnologyInventors: Richard J. Wurtman, Carol Watkins
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Publication number: 20120070415Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.Type: ApplicationFiled: September 19, 2011Publication date: March 22, 2012Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
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Publication number: 20120071434Abstract: Disclosed herein are phosphorothioate nucleotide analogs, methods of synthesizing phosphorothioate nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the phosphorothioate nucleotide analogs.Type: ApplicationFiled: September 19, 2011Publication date: March 22, 2012Applicant: ALIOS BIOPHARMA, INC.Inventors: David Bernard Smith, Jerome Deval, Natalia Dyatkina, Leonid Beigelman, Guangyi Wang
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Publication number: 20120070411Abstract: Disclosed herein are phosphoroamidate nucleotide analogs, methods of synthesizing phosphoroamidate nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the phosphoroamidate nucleotide analogs.Type: ApplicationFiled: September 19, 2011Publication date: March 22, 2012Applicant: Alios BioPharma, Inc.Inventors: Leonid Beigelman, Lawrence Blatt, Guangyi Wang, Vivek Kumar Rajwanshi, Natalia Dyatkina, David Bernard Smith
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Publication number: 20120064127Abstract: It has now been found that after administration to a diseased person or person that is at risk for developing such disease of a neutraceutical or pharmaceutical composition that comprises a) a lipid fraction comprising at least one of docosahexaenoic acid (DHA), docosapentaenoic acid (DPA) and eicosapentaenoic acid (EPA); b) a protein fraction comprising proteinaceous material from non-human origin which provide at least cysteine and/or taurine; and c) a mineral fraction comprising at least one of manganese and molybdenum, the health of these persons improves. Membrane function of several types of mammalian cells improves, which allows efficient treatment of immune related disorders, such as allergy, autoimmune diseases, cancer, cognitive dysfunction and other diseases of the nervous system, neuropathies, such as diabetic neuropathies and neuropathic pains, neuronal damage during insulin resistance, and gut diseases and support of the development of gut and lung function during growth or recovery.Type: ApplicationFiled: November 11, 2011Publication date: March 15, 2012Applicant: N.V.NUTRICIAInventor: Robert J.J. Hageman
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Publication number: 20120065156Abstract: Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8? are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8? form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.Type: ApplicationFiled: May 11, 2010Publication date: March 15, 2012Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Raboisson, Koen Vandyck, Steven Maurice Van Hoof, Lili Hu, Abdellah Tahri
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Publication number: 20120035115Abstract: The invention features compounds of formula I or II: In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.Type: ApplicationFiled: September 23, 2009Publication date: February 9, 2012Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Takeshi Yamada, David Butler, K. Narayanannair Jayaprakash, Muthusamy Jayraman, Shigeo Matsuda, Rajendra K. Pandey, Chang Geng Peng
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Publication number: 20120022014Abstract: The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, novel tetrahydropyran nucleoside analogs are provided having at least one chiral substituent that are expected to be useful for enhancing one or more properties of oligomeric compounds such as nuclease resistance and/or binding affinity. In certain embodiments, the oligomeric compounds are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: ApplicationFiled: February 1, 2010Publication date: January 26, 2012Inventors: Thazha P. Prakash, Eric E. Swayze
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Patent number: 8097711Abstract: Embodiments of the invention include nucleotide and nucleoside monomers protected at the 5?- or 3?-hydroxyls with thioether substituted aryl carbonate protecting groups. In certain cases, the carbonate protecting groups include an aryl moiety, e.g., a phenyl group, attached to the carbonate, where the aryl moiety further includes a thioether group, e.g., an alkyl or aryl thioether group, bound directly to the aryl ring. Aspects of the invention further include methods of synthesizing nucleic acids, e.g., oligonucleotides, using such protected nucleoside monomer monomers, as well as nucleic acids produced using methods of the invention and compositions thereof.Type: GrantFiled: August 31, 2007Date of Patent: January 17, 2012Assignee: Agilent Technologies, Inc.Inventors: Zoltan Timar, Zoltan Kupihar, Douglas J. Dellinger, Marvin H. Caruthers
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Patent number: 8097600Abstract: 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 28, 2010Date of Patent: January 17, 2012Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Karla M. Jacobus, William Pendergast, Janet L. Rideout
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Publication number: 20110312880Abstract: The present invention relates to compounds, in particular, dual antagonists comprising a nucleoside reverse transcriptase inhibitor (NRTI) or a nucleoside competititive reverse transcriptase inhibitor and a non-nucleoside reverse transcriptase inhibitor (NNRTI), linked together using a chemical linker, which may be used to inhibit HIV (HIV-1) reverse transcriptase and in the treatment of HIV infections, more severe cases of HIV infections, including ARC and AIDS, including reducing the likelihood of these infections and disease states.Type: ApplicationFiled: April 9, 2009Publication date: December 22, 2011Inventors: Karen S. Anderson, Roger Hunter
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Patent number: 8076310Abstract: Disclosed herein are novel phosphonate nucleosides and thiophosphonate nucleosides comprising a phosphonalkoxy-substituted or phosphonothioalkyl-substituted five-membered, saturated or unsaturated, oxygen-containing or sulfur-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections.Type: GrantFiled: March 4, 2005Date of Patent: December 13, 2011Assignee: K.U.Leuven Research & DevelopmentInventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clerq
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Publication number: 20110301115Abstract: Provided are methods of treating subclinical sun damage and of inducing a chemocytotoxic response in skin. Methods of treating subclinical sun damage include the steps of: topically administering to skin of a patient a composition comprising a chemocytotoxic agent in an amount effective to induce erythema, scaling, crusting, or combinations thereof and resolve at least a portion of the subclinical sun damage, where the skin has a condition of no clinical sign of sun damage and the patient was not previously treated for actinic keratosis or nonmelanoma skin cancer. The chemocytotoxic agent can comprise a fluorinated pyrimidine antimetabolite such as 5-fluorouracil (FU), 5-fluorouridine (FUR), 5-fluorouridine-5?-monophosphate (FUMP), 5-fluorodeoxyuridine (FUdR), 5-fluorodeoxyuridine-5?-monophosphate (FdUMP), or combinations thereof.Type: ApplicationFiled: January 18, 2011Publication date: December 8, 2011Inventor: Robert K. Ilowite
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Patent number: 8071567Abstract: The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing such compounds.Type: GrantFiled: September 16, 2009Date of Patent: December 6, 2011Assignee: Roche Palo Alto LLCInventors: Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
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Patent number: 8071568Abstract: The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to 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 to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention.Type: GrantFiled: December 28, 2007Date of Patent: December 6, 2011Assignees: Merck Sharp & Dohme Corp., Instituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.Inventors: Frank Narjes, Cristina Gardelli, Monica Donghi, Barbara Attenni, Philippe L. Durette
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Patent number: 8067392Abstract: 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: February 16, 2011Date of Patent: November 29, 2011Assignee: Wellstat Therapeutics CorporationInventor: Reid W. Von Borstel
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Patent number: 8067391Abstract: 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: GrantFiled: October 3, 2006Date of Patent: November 29, 2011Assignee: University Health NetworkInventors: Lakshmi P. Korta, Emil F. Pai, Angelica M. Bello, Masahiro Fujihashi
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Publication number: 20110286962Abstract: 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: May 26, 2011Publication date: November 24, 2011Inventors: Jean-Pierre SOMMADOSSI, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
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Patent number: 8063025Abstract: 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: GrantFiled: November 26, 2008Date of Patent: November 22, 2011Assignee: Metabasis Therapeutics, Inc.Inventors: Scott J. Hecker, K. Raja Reddy, Zhili Sun, Brett C. Bookser, David Bernard Smith
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Publication number: 20110268801Abstract: 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: June 30, 2011Publication date: November 3, 2011Applicant: Ardea Biosciences, Inc.Inventors: Barry D. Quart, Jean-Luc Girardet, Esmir Gunic, Li-Tain Yeh
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Publication number: 20110257109Abstract: The present invention encompasses compositions and methods that activate P2Y receptors for the increased production of new synapses in the central nervous system. The formulations of the invention may be administered to a healthy subject or to a subject in need thereof to restore synapses.Type: ApplicationFiled: April 19, 2011Publication date: October 20, 2011Inventor: Richard WURTMAN
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Publication number: 20110257122Abstract: 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: May 3, 2011Publication date: October 20, 2011Applicant: Pharmasset, Inc.Inventors: Michael Joseph Sofia, Jinfa Du, Peiyuan Wang
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Publication number: 20110251152Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 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: March 31, 2011Publication date: October 13, 2011Applicant: PHARMASSET, INC.Inventors: Bruce S. Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Suguna Rachakonda, Hai-Ren Zhang, Byoung-Kwon Chun, Peiyuan Wang
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Publication number: 20110230436Abstract: Compounds of the formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen or halo; R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is a group of formula R7 is optionally substituted phenyl; naphthyl; indolyl or N—C1-C6alkyloxycarbonylindolyl; R8 is hydrogen, C1-C6alkyl, benzyl; R8? is hydrogen, C1-C6alkyl, benzyl; or R8 and R8? together with the carbon atom to which they are attached form C3-C7cycloalkyl; R9 is C1-C10alkyl, benzyl, or optionally substituted phenyl; or a pharmaceutically acceptable salt or solvate thereof. pharmaceutical formulations and the use of compounds I as HCV inhibitors.Type: ApplicationFiled: December 8, 2009Publication date: September 22, 2011Applicants: CENTOCOR ORTHO BIOTECH PRODUCTS L.P., MEDIVIR ABInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Steven Maurice Paula Van Hoof, Leen Anna Maria Vandekerckhove, Koen Vandyck
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Patent number: 8017594Abstract: To provide a novel anti-psychosocial stress agent which is highly safety and can be continuously taken, more particularly, a novel anti-psychosocial stress agent which prevents or alleviates psychosocial stress. The invention provides an anti-psychosocial stress agent containing, as an active ingredient, uridylic acid, uridine, or uracil. Since uridylic acid, uridine, or uracil, which is an active ingredient of the anti-psychosocial stress agent of the present invention, is inexpensively available and is a biological component, the agent exhibits high safety and can be continuously taken. Therefore, the anti-psychosocial stress agent of the present invention is effective for mitigating, alleviating, or relieving psychosocial stress, which is an issue in modern society. When the anti-psychosocial stress agent is taken before development of symptoms associated with psychosocial stress, the symptoms can be prevented.Type: GrantFiled: June 26, 2007Date of Patent: September 13, 2011Assignee: Yamasa CorporationInventors: Kazuki Endo, Noriyuki Ashida
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Patent number: 8008274Abstract: 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: GrantFiled: May 6, 2009Date of Patent: August 30, 2011Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Ward M. Peterson, Janet L. Rideout, William Pendergast
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Patent number: 7999099Abstract: The invention relates to the field of molecular biology, virology and medicine and, more specifically, to novel derivatives of 3?-azido-3?-deoxythymidine phosphonates with the following general formula where R=alkyl groups, including those containing halogen atoms, carboxy-, hydroxy-, alkoxy- and acyloxy- groups as well as substituted aminocarbonyl groups. The compounds can be used as antiviral agents as they have low toxicity and can effectively inhibit replication of type 1 immunodeficiency virus in MT-4 cell culture and generate AZT in mammalians ensuring a gradual increase of its concentration in the blood.Type: GrantFiled: May 6, 2005Date of Patent: August 16, 2011Inventors: Marina Konstantinovna Kukhanova, Khandazhinskaya Anastasiya Lvovna, Maxim Vladimirovich Yasko, Elena Anatolievna Shirokova, Alexander Valerievich Shipitsyn, Andrey Georgievich Pokrovsky
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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