Phosphorus Containing Patents (Class 514/51)
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Publication number: 20140161770Abstract: The present invention relates to 2?-Cyano Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Cyano Substituted Nucleoside Derivative, and methods of using the 2?-Cyano Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.Type: ApplicationFiled: April 11, 2012Publication date: June 12, 2014Applicant: MERCK SHARP & DOHME CORP.Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Angela Kerekes, Frank Bennett, Ying Huang, Latha Nair, Dmitri Pissarnitski, Vishal Verma, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
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Publication number: 20140162972Abstract: This disclosure relates to prodrugs of uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those prodrugs of the UDP derivatives and methods of using those prodrugs or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma, and inflammatory conditions.Type: ApplicationFiled: September 27, 2013Publication date: June 12, 2014Applicant: Tufts UniversityInventors: Philip G. Haydon, Jinbo Lee
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Publication number: 20140162973Abstract: The present invention relates to the use of a taste masking agent selected from the group of starch; cellulose; 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 nucleoside and/or a nucleotide. It also relates to a nutritional composition comprising an unsavoury nucleoside and/or nucleotide component, having improved sensory characteristics such as improved mouth feel, taste, aftertaste and smell. In particular, it relates to a composition comprising said unsavoury nucleoside and/or nucleotide component, in particular comprising an uridine-containing nucleoside and/or a nucleotide in combination with an unsavoury edible oil, such as a fish oil.Type: ApplicationFiled: December 3, 2013Publication date: June 12, 2014Applicant: N.V. NutriciaInventors: Esther Jacqueline DE KORT, Martine GROENENDIJK, Patrick Joseph Gerardus Hendrikus KAMPHUIS
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Publication number: 20140155345Abstract: The invention provides new biotinylated compounds and methods for their use.Type: ApplicationFiled: December 4, 2013Publication date: June 5, 2014Applicant: Rutgers, the State University of New JerseyInventors: Roger A. Jones, Barbara L. Gaffney
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Publication number: 20140154210Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.Type: ApplicationFiled: March 11, 2013Publication date: June 5, 2014Inventors: Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent
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Patent number: 8735372Abstract: 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: October 18, 2013Date of Patent: May 27, 2014Assignee: Gilead Pharmasset LLCInventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
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Publication number: 20140140951Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, provided herein is an isolated compound according to Formula Ia: or a pharmaceutically acceptable salt or solvate thereof.Type: ApplicationFiled: November 13, 2013Publication date: May 22, 2014Inventors: Adel M. MOUSSA, Benjamin Alexander MAYES, Cyril B. DOUSSON, David DUKHAN
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Publication number: 20140140952Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, provided herein is an isolated compound according to Formula Ib: or a pharmaceutically acceptable salt or solvate thereof.Type: ApplicationFiled: November 13, 2013Publication date: May 22, 2014Inventors: Adel M. MOUSSA, Benjamin Alexander MAYES, Cyril B. DOUSSON, David DUKHAN
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Publication number: 20140128339Abstract: The present invention relates to 2?-Methyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3, are as defined herein. The present invention also relates to compositions comprising at least one 2?-Methyl Substituted Nucleoside Derivative, and methods of using the 2?-Methyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.Type: ApplicationFiled: October 15, 2013Publication date: May 8, 2014Inventors: Vinay Girijavallabhan, Stephane Bogen, Quang T. Truong, Ping Chen, Angela Kerekes, Frank Bennett, Sara Esposite, Qingmei Hong, Ian Davies
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Publication number: 20140112887Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2?,4?-bridged nucleosides which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the 2?,4?-bridged nucleosides are of Formula 3001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, where PD, B, W, X, RA, RB, RC and RD are as described herein.Type: ApplicationFiled: October 21, 2013Publication date: April 24, 2014Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART
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Publication number: 20140107060Abstract: 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 16, 2013Publication date: April 17, 2014Applicant: University of North Carolina at WilmingtonInventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Publication number: 20140107016Abstract: The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to a subject an effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), and an inhibitor of cytochrome P450 (e.g., ritonavir).Type: ApplicationFiled: December 23, 2013Publication date: April 17, 2014Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Thomas J. Podsadecki
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Publication number: 20140107017Abstract: The present invention features interferon-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to the subject effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), an inhibitor of cytochrome P450 (e.g., ritonavir), and ribavirin.Type: ApplicationFiled: December 23, 2013Publication date: April 17, 2014Applicant: AbbVie Inc.Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Thomas J. Podsadecki
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Publication number: 20140099283Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2?-chloro nucleosides according to Formula 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.Type: ApplicationFiled: October 7, 2013Publication date: April 10, 2014Inventors: Gilles GOSSELIN, Christophe Claude PARSY, Francois-Rene ALEXANDRE, Houcine RAHALI, Jean-Francois GRIFFON, Julien MILHAU, Dominique SURLERAUX, Cyril B. DOUSSON, Claire PIERRA, Adel M. MOUSSA, Benjamin Alexander MAYES
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Patent number: 8680048Abstract: The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to a subject an effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), and an inhibitor of cytochrome P450 (e.g., ritonavir).Type: GrantFiled: October 19, 2012Date of Patent: March 25, 2014Assignee: AbbVie Inc.Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Thomas J. Podsadecki, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein
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Publication number: 20140066397Abstract: The invention relates to a composition comprising: i) one or more of uridine and cytidine, or salts, phosphates, acyl derivatives or esters thereof; ii) a lipid fraction comprising at least one of docosahexaenoic acid (22:6; DHA), eicosapentaenoic acid (20:5; EPA) and docosapentaenoic acid (22:5; DPA), or esters thereof, in which the lipid fraction comprises less than 2 weight % of ?-linolenic acid (ALA), calculated on the weight of all fatty acids; iii) choline, or salts or esters thereof; for use in the prevention or treatment of neurotrauma, traumatic brain injury, cerebral palsy and spinal cord injury.Type: ApplicationFiled: March 14, 2012Publication date: March 6, 2014Inventors: Mattheus Cornelis De Wilde, Johannes Wilhelmus Christina Suben, Patrick Joseph Gerardus Hendrikus Kamphuis, Robert Johan Joseph Hageman
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Publication number: 20140065101Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is defined herein, which is a 2?-branched nucleoside useful for the treatment or prevention of viral infections, particularly dengue virus, yellow fever virus, West Nile virus, Japanese encephalitis virus, tick-borne encephalitis virus, Kunjin virus, Murray Valley encephalitis, St Louis encephalitis, Omsk hemorrhagic fever virus, bovine viral diarrhea virus, Zika virus and Hepatitis C virus.Type: ApplicationFiled: August 27, 2013Publication date: March 6, 2014Applicant: Novartis AGInventor: Fumiaki Yokokawa
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Publication number: 20140066398Abstract: The invention provides compounds of the formula: which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.Type: ApplicationFiled: October 10, 2013Publication date: March 6, 2014Applicant: Medivir, ABInventors: Anders ENEROTH, Bjorn Klasson, Magnus Nilsson, Pedro Pinho, Bertil Samuelsson, Christian Sund
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Patent number: 8664195Abstract: 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: GrantFiled: December 19, 2011Date of Patent: March 4, 2014Assignee: Metabasis Therapeutics, Inc.Inventors: Mark D. Erion, K. Raja Reddy, Serge H. Boyer
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Publication number: 20140057835Abstract: The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to a subject an effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), and an inhibitor of cytochrome P450 (e.g., ritonavir).Type: ApplicationFiled: July 5, 2013Publication date: February 27, 2014Applicant: AbbVie Inc.Inventors: Barry M. BERNSTEIN, Rajeev M. MENON, Amit KHATRI, Sven MENSING, Sandeep DUTTA, Daniel E. COHEN, Scott C. BRUN, Walid M. AWNI, Emily O. DUMAS, Cheri E. KLEIN, Thomas J. PODSADECKI
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Publication number: 20140057864Abstract: The invention provides methods, compositions, and kits featuring a ribonucleoside chain terminator for use in preventing or inhibiting a retrovirus infection.Type: ApplicationFiled: October 4, 2011Publication date: February 27, 2014Applicant: University of RochesterInventor: Baek Kim
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Publication number: 20140057866Abstract: Phosphoramidate derivatives of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.Type: ApplicationFiled: September 7, 2012Publication date: February 27, 2014Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
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Patent number: 8658619Abstract: 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: GrantFiled: January 18, 2011Date of Patent: February 25, 2014Inventor: Robert K. Ilowite
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Publication number: 20140045783Abstract: 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: October 18, 2013Publication date: February 13, 2014Applicant: GILEAD PHARMASSET LLCInventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
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Publication number: 20140038916Abstract: This application discloses novel phosphoramidate and phosphonoamidate prodrugs of nucleosides, nucleotides, C-nucleosides, C-nucleotides, phosphonates, and other alcohol-containing drugs; use of these prodrugs for treatment of infectious diseases and cancers, in particular, liver infections and cancers; and methods of preparing these novel phosphoramidate and phosphonoamidate prodrugs.Type: ApplicationFiled: December 30, 2011Publication date: February 6, 2014Applicant: Nanjing Molecular Research, Inc.Inventors: Zheng Wang, Suping Zhou
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Patent number: 8633309Abstract: 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: GrantFiled: January 10, 2013Date of Patent: January 21, 2014Assignee: Gilead Pharmasset LLCInventors: Bruce Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Suguna Rachakonda, Hai-Ren Zhang, Byoung-Kwon Chun, Peiyuan Wang
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Patent number: 8618074Abstract: 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: GrantFiled: March 17, 2008Date of Patent: December 31, 2013Assignee: Board of Regents of the University of Texas SystemInventor: James D. Lechleiter
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Patent number: 8618077Abstract: Compositions and methods of treatment or prophylaxis of fragile-X associated disorders are provided, as well as methods of screening compounds and kits to screen a library of compounds.Type: GrantFiled: April 27, 2012Date of Patent: December 31, 2013Assignee: Emory UniversityInventors: Peng Jin, Abrar Qurashi
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Patent number: 8618076Abstract: 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: GrantFiled: March 31, 2011Date of Patent: December 31, 2013Assignee: Gilead Pharmasset LLCInventors: 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: 20130337055Abstract: The present invention is directed to pharmaceutical compositions and methods of treatment that relate to the inhibition, resolution and/or prevention of an array of the manifestations of metabolic syndromes, including Type 2 diabetes, hyperlipidemia, weight gain, obesity, insulin resistance, hypertension, atherosclerosis, fatty liver diseases and certain chronic inflammatory states that lead to these manifestations, among others. In additional aspects, the present invention relates to compositions and methods which may be used to treat, inhibit or reduce the likelihood of hepatitis viral infections, including Hepatitis B and Hepatitis C viral infections, as well as the secondary disease states and/or conditions which are often associated with such viral infections, including hepatic steatosis (steatohepatitis), cirrhosis, fatty liver and hepatocellular cancer, among other disease states or conditions.Type: ApplicationFiled: February 24, 2012Publication date: December 19, 2013Inventors: Jerome Schentag, Joseph M. Fayad
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Patent number: 8609066Abstract: The present invention relates to methods for determining whether blood flow is restricted in a blood vessel of an individual suspected of compromised blood flow in the vessel, the method comprising the steps of delivering UTP, a derivative thereof, or a salt thereof to the vessel, assessing blood flow quantitatively in the vessel by obtaining a value that correlates to blood flow in said vessel, comparing the obtained value with a reference value, and determining whether the individual has compromised blood flow based on the results of the comparison. The invention also provides for methods of diagnosing atherosclerotic and ischemic heart diseases using UTP, a derivative thereof, or a salt thereof, as well as methods for inducing maximal hyperemia for diagnostic purposes.Type: GrantFiled: December 27, 2012Date of Patent: December 17, 2013Inventor: Jaya Brigitte Rosenmeier
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Publication number: 20130331352Abstract: Composition comprising at least two components, more preferably at least three components, more preferably at least four components, selected from the group of (i) a nucleoside equivalent, (ii) an ?-3 polyunsaturated fatty acid selected from the group of DHA, DPA and EPA, (iii) a vitamin B, (iv) a phospholipid, (v) an antioxidant and (vi) a choline, with the proviso that at least component (i) or (iii) is present, for use in the prevention or treatment of frailty in a mammal, wherein frailty is determined by compliance with at least 2 criterions, preferably 3 criterions, selected from the group of muscle weakness, excessive feelings of exhaustion or fatigue, abnormally low physical activity, slow or unsteady gait, weight loss, and neurological dysfunction.Type: ApplicationFiled: December 28, 2011Publication date: December 12, 2013Applicant: N.V. NUTRICIAInventors: Robert Johan Joseph Hageman, Mattheus Cornelis De Wilde, Martine Groenendijk, Patrick Joseph Gerardus Hendrikus Kamphuis
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Publication number: 20130330424Abstract: Non-medical use of at least two components selected from the group of: (i) nucleoside equivalents, (ii) n-3 polyunsaturated fatty acids selected from the group of DHA, DPA and EPA, (iii) vitamins B, (iv) phospholipids, (v) antioxidants and (vi) cholines—with the proviso that at least one (i) nucleoside or at least one (iii) vitamin B is present—for increasing or maintaining the body weight, for improving the ability to perform an activity of daily living of a mammal, for maintaining the ability to perform an activity of daily living of a mammal, or for reducing a deterioration in the ability to perform an activity of daily living of a mammal.Type: ApplicationFiled: August 11, 2011Publication date: December 12, 2013Applicant: N.V. NutriciaInventors: Martine Groenendijk, Patrick Joseph Gerardus Hendrikus Kamphuis, Mattheus Cornelis De Wilde, Robert Johan Joseph Hageman
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Patent number: 8604000Abstract: 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 unsavory 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-savory nucleotide and/or a nucleoside component, in particular comprising an uridine-containing nucleotide and/or a nucleoside in combination with an unsavory edible oil, such as a fish oil.Type: GrantFiled: December 22, 2008Date of Patent: December 10, 2013Assignee: N.V. NutriciaInventors: Esther Jacqueline de Kort, Martine Groenendijk, Patrick Joseph Gerardus Hendrikus Kamphuis
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Publication number: 20130324495Abstract: The invention provides particular uridine di- and tri-phosphate derivatives, and pharmaceutical compositions thereof. These compounds are useful for treatment of diseases, disorders and conditions modulated by P2Y6 receptors, and particularly for lowering intraocular pressure and thereby treating ocular hypertension and/or glaucoma.Type: ApplicationFiled: December 1, 2011Publication date: December 5, 2013Applicants: UNIVERSIDAD COMPLUTENSE DE MADRID, BAR-ILAN UNIVERSITYInventors: Bilha fischer, Jesus Jeronimo Pintor, Shay Elyahu, Tamar Ginsburg-Shmuel
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Patent number: 8598141Abstract: This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.Type: GrantFiled: March 8, 2013Date of Patent: December 3, 2013Assignee: Tufts UniversityInventors: Philip Haydon, Jinbo Lee, Jinghui Dong, Stephen Moss, Raquel Revilla-Sanchez
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Publication number: 20130316970Abstract: The object of the invention are nucleotide analogues, antiviral pro-nucleotides, a use of nucleotide analogues and pharmaceutical composition, a phosphorylating agent for synthesis of nucleotide analogue, and a method of synthesis of nucleotide analogue. More precisely, the invention applies to the new group of nucleotide analogues and their use in partial or complete inhibition of human immunodeficiency virus (HIV).Type: ApplicationFiled: October 13, 2011Publication date: November 28, 2013Applicants: NARODOWY INSTYTUT LEKOW, INSTYTUT CHEMII BIOORGANICZNEJ PANInventors: Adam Kraszewski, Joanna Romanowska, Michal Sobkowski, Agnieszka Szymanska-Michalak, Jacek Stawinski, Jerzy Boryski, Andrzej Lipniacki, Andrzej Piasek
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Publication number: 20130315868Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disease and conditions, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.Type: ApplicationFiled: May 21, 2013Publication date: November 28, 2013Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART
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Publication number: 20130315863Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: ApplicationFiled: July 31, 2013Publication date: November 28, 2013Applicants: Universita' degli Studi di Cagliari, Idenix Pharmaceuticals, Inc.Inventors: Jean-Pierre SOMMADOSSI, Paolo LaColla
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Publication number: 20130316969Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: March 21, 2013Publication date: November 28, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130315864Abstract: The present invention provides nucleoside phosphoramidate compounds of Formula I, where R1, R2a, R2b, R3, R4, R5a, R5b, R6, R7, R8a, R8b, M and W are as defined herein. The invention further includes pharmaceutical compositions comprising a compound of Formula I, methods of use of these compounds for treating a viral infection, and methods of producing these compounds.Type: ApplicationFiled: May 17, 2013Publication date: November 28, 2013Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yat Sun Or, Jun Ma, Guoqiang Wang
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Publication number: 20130309195Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: March 14, 2013Publication date: November 21, 2013Inventors: John O. Link, Jeromy J. Cottell, Teresa Alejandra Trejo Martin
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Publication number: 20130309196Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: March 14, 2013Publication date: November 21, 2013Inventors: John O. Link, Jeromy J. Cottell, Teresa Alejandra Trejo Martin
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Publication number: 20130310336Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: ApplicationFiled: November 13, 2012Publication date: November 21, 2013Applicants: UNIVERSITA DEGLI STUDI DI CAGLIARI, IDENIX PHARMACEUTICALS, INC.Inventors: Jean-Pierre SOMMADOSSI, Paolo LACOLLA
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Patent number: 8580765Abstract: 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: September 11, 2012Date of Patent: November 12, 2013Assignee: Gilead Pharmasset LLCInventors: Michael Joseph Sofia, Jinfa Du, Peiyuan Wang, Dhanapalan Nagarathnam
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Publication number: 20130288997Abstract: 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: June 24, 2013Publication date: October 31, 2013Inventors: 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: 20130266538Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.Type: ApplicationFiled: March 11, 2013Publication date: October 10, 2013Inventors: Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent
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Patent number: 8551973Abstract: A purified compound having activity against hepatitis C virus is disclosed.Type: GrantFiled: December 23, 2009Date of Patent: October 8, 2013Assignee: Gilead Pharmasset LLCInventors: Donghui Bao, Wonsuk Chang, Dhanapalan Nagarathnam, Michael Joseph Sofia
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Publication number: 20130252920Abstract: Disclosed herein are pharmaceutical compositions that can include a thionucleotide analog for use in combination therapy with other agents. Also disclosed herein are methods of treating diseases and/or conditions with a pharmaceutical composition that can include a thionucleotide analog in combination therapy with other agents.Type: ApplicationFiled: March 12, 2013Publication date: September 26, 2013Applicants: VERTEX PHARMACEUTICALS INC., ALIOS BIOPHARMA, INC.Inventors: Lawrence M. Blatt, Leonid Beigelman, Hua Tan, Julian Alexander Symons, David Bernard Smith, Min Jiang, Tara Lynn Kieffer, Cornelis Arie Rijnbrand
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Publication number: 20130252919Abstract: This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.Type: ApplicationFiled: March 8, 2013Publication date: September 26, 2013Applicant: TUFTS UNIVERSITYInventors: Philip Haydon, Jinbo Lee, Jinghui Dong, Stephen Moss, Raquel Revilla-Sanchez