Phosphorus Containing Patents (Class 514/51)
  • Patent number: 10278985
    Abstract: Provided is an aqueous ophthalmic solution comprising diquafosol or a salt thereof at a concentration of 0.1% to 10% (w/v) and a chlorhexidine at a concentration of 0.0001% to 0.1% (w/v).
    Type: Grant
    Filed: December 25, 2015
    Date of Patent: May 7, 2019
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Koji Inagaki, Naoki Matsumoto, Toshihiro Ogawa, Yukihisa Wakabayashi, Asuka Kamimura, Yoshihiro Oshita, Hitoshi Nakazawa, Isao Matsuoka
  • Patent number: 10071113
    Abstract: Regarding Diquafosol ophthalmic solution comprising a chelating agent at a concentration of 0.0001 to 1% (w/v), formation of insoluble precipitates found in Diquafosol ophthalmic solution during storage of the solution, as well as deterioration of the filtration performance in the course of production (course of filtration sterilization), have been inhibited. Further, in Diquafosol ophthalmic solution comprising a chelating agent, reduction of eye irritation and enhancement of the preservative effectiveness have been confirmed, in comparison to Diquafosol ophthalmic solution comprising no chelating agent. Accordingly, the present invention has been confirmed to provide physicochemical properties that are stable during the courses of production and distribution as well as the course of storage by a patient, and also reduce eye irritation and enhance preservative effectiveness.
    Type: Grant
    Filed: October 10, 2016
    Date of Patent: September 11, 2018
    Assignee: SANTEN PHARMACEUTICAL CO., LTD.
    Inventors: Akiko Sakatani, Tatsuo Ikei, Koji Inagaki, Masatsugu Nakamura, Kazuhiro Hosoi, Mikiko Saito, Masaki Sonoda, Yoko Fukui, Mitsuaki Kuwano
  • Patent number: 10039732
    Abstract: The present invention relates to food compositions comprising nutritional composition for use in the treatment or nutritional management of phenylketonuria or hyperphenylalaninemia or for preserving or improving brain function in PKU or hyperphenylalaninemia. The composition comprises a specific protein source, long chain polyunsaturated fatty acids and at least one of uridine or cytidine.
    Type: Grant
    Filed: April 17, 2014
    Date of Patent: August 7, 2018
    Assignee: N.V. NUTRICIA
    Inventors: Rogier Daniël Van Anholt, Amos Attali
  • Patent number: 10022390
    Abstract: Phosphoramidate derivates 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: Grant
    Filed: April 18, 2017
    Date of Patent: July 17, 2018
    Assignee: NuCana plc
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Patent number: 10005810
    Abstract: Provided are phosphoramidate nucleoside compounds of Formula (I), or pharmaceutically acceptable salts or esters or solvates thereof, useful in the treatment of cancer, viral infections and other diseases: Also provided is a process for the synthesis of the compounds of Formula (I) where a desired enantiomer, having regard to the asymmetric chiral center of the phosphorus atom P, is provided in an enriched amount. The process comprises admixing a nucleoside with a phosphorochloridate in the presence of a catalyst comprising a metal salt selected from the group consisting of salts of Cu, Fe, La and Yb.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: June 26, 2018
    Assignee: University College Cardiff Consultants Limited
    Inventors: Chirstopher McGuigan, Fabrizio Pertusati
  • Patent number: 9655915
    Abstract: 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: Grant
    Filed: November 17, 2015
    Date of Patent: May 23, 2017
    Assignee: NuCana BioMed Limited
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Patent number: 9572830
    Abstract: The present invention provides methods for increasing secretion of dopamine and other neurotransmitters and treating or reducing the incidence of diseases involving decreased secretion of dopamine and other neurotransmitters, e.g. Parkinson's disease, comprising administering to the subject a uridine or a source thereof, and compositions for treating or reducing an incidence of Parkinson's disease, comprising a uridine, a uridine monophosphate, or a source thereof.
    Type: Grant
    Filed: May 11, 2005
    Date of Patent: February 21, 2017
    Assignee: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventor: Richard J. Wurtman
  • Patent number: 9284342
    Abstract: 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: Grant
    Filed: June 24, 2013
    Date of Patent: March 15, 2016
    Assignee: Gilead Pharmasset LLC
    Inventors: Bruce S. Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Suguna Rachakonda, Hai-Ren Zhang, Byoung-Kwon Chun, Peiyuan Wang
  • Patent number: 9227993
    Abstract: 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: Grant
    Filed: July 3, 2014
    Date of Patent: January 5, 2016
    Assignee: TUFTS UNIVERSITY
    Inventors: Philip G. Haydon, Jinbo Lee, Jinghui Dong, Stephen Moss, Raquel Revilla-Sanchez
  • Patent number: 9221866
    Abstract: 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: Grant
    Filed: December 4, 2014
    Date of Patent: December 29, 2015
    Assignee: NuCana Biomed Limited
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Patent number: 9206412
    Abstract: The invention provides methods to inhibit the replication of a flavivirus, methods of inhibiting the guanosine triphosphate (GTP)-binding and guanylyltransferase activity of a flavivirus RNA capping enzyme, and methods of treating a subject infected with a flavivirus. The methods can include contacting a flavivirus with an effective amount of a thioxothiazolidine compound described herein, or a derivative thereof, such as a compound of Formula (I).
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: December 8, 2015
    Assignee: Colorado State University Research Foundation
    Inventors: Brian J. Geiss, Susan M. Keenan, Hillary Jo Beek
  • Patent number: 9108999
    Abstract: The present disclosure relates to compounds of Formula (I): Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of using the compounds of Formula (I) and/or compositions comprising the compounds of Formula (I) for the treatment of HCV.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: August 18, 2015
    Assignee: Riboscience LLC
    Inventors: Jing Zhang, Zhuming Zhang
  • Publication number: 20150141363
    Abstract: 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: Application
    Filed: January 29, 2015
    Publication date: May 21, 2015
    Inventors: Guangyi Wang, Leonid Beigelman
  • Publication number: 20150141365
    Abstract: The present invention relates to compounds of the formula I: including any possible stereoisomers thereof, wherein R9 has the meaning as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Application
    Filed: May 24, 2013
    Publication date: May 21, 2015
    Applicant: Janssen R&D Ireland
    Inventors: Ioannis Nicolaos Houpis, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri
  • Patent number: 9029346
    Abstract: Methods and compounds are disclosed for irreversibly inhibiting a DNA repair enzyme that possesses lyase activity.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: May 12, 2015
    Assignee: The Johns Hopkins University
    Inventors: Marc M. Greenberg, Dumitru Arian, Theodore L. Deweese, Mohammad Hedayati
  • Publication number: 20150110871
    Abstract: The present invention relates to a gastric retentive tablet composition comprising: (1) coated particles essentially consisting of a drug and an amino methacrylate copolymer, (2) a methacrylic acid copolymer and (3) an excipient, wherein items 1, 2, and 3 are blended together, and then compressed into a gastric retentive tablet. Thus, the coated particles (item 1), a methacrylic acid copolymer and the excipient are evenly distributed in the tablet. The excipient is selected from a group consisting of a retarding agent, a binder, a filler, a chelating agent, a diluent, a disintegrant, a lubricant, a colorant, a solubilizing agent, or a mixture thereof. The coated particles (item 1) do not contain methacrylic acid polymer.
    Type: Application
    Filed: January 3, 2015
    Publication date: April 23, 2015
    Inventor: David Wong
  • Patent number: 9012428
    Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate useful in the treatment of patients infected with the hepatitis C virus (HCV).
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: April 21, 2015
    Assignees: Janssen Products, LP, Medivir AB
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
  • Patent number: 9012427
    Abstract: 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: Grant
    Filed: March 12, 2013
    Date of Patent: April 21, 2015
    Assignee: 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
  • Publication number: 20150105341
    Abstract: Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus and/or Flaviviridae infection with one or more nucleosides, nucleotides and nucleotide analogs.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 16, 2015
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith, Marija Prhavc, Christian Andreas Jekle, Jerome Deval
  • Patent number: 9006209
    Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate which inhibits the hepatitis C virus (HCV).
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: April 14, 2015
    Assignees: Janssen Products, LP, Medivir AB
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
  • Patent number: 9006208
    Abstract: An agent for treatment of dry eye comprising a combination of a P2Y2 receptor agonist at a therapeutically effective concentration and hyaluronic acid or a salt thereof at a therapeutically effective concentration, which agent has a dosage form of an ophthalmic agent, can promote the secretion of tear remarkably and can improve corneal epithelial disorders remarkably, and is therefore expected to be a novel agent for treatment of dry eye.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: April 14, 2015
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Yuko Shichijo, Atsuyoshi Dota, Takashi Nagano, Masatsugu Nakamura, Asuka Sakamoto
  • Patent number: 8980865
    Abstract: Disclosed herein are phosphorothioate nucleotide analogs, such as thiophosphoroamidate prodrugs and thiophosphates (including ?-thiomonophosphates, ?-thiodiphosphates, and ?-thiotriphosphates), methods of synthesizing phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates and methods of treating viral infections, such as HCV, cancer, and/or parasitic diseases with the phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: March 17, 2015
    Assignee: Alios BioPharma, Inc.
    Inventors: Guangyi Wang, Leonid Beigelman
  • Publication number: 20150072951
    Abstract: Regarding Diquafosol ophthalmic solution comprising a chelating agent at a concentration of 0.0001 to 1% (w/v), formation of insoluble precipitates found in Diquafosol ophthalmic solution during storage of the solution, as well as deterioration of the filtration performance in the course of production (course of filtration sterilization), have been inhibited. Further, in Diquafosol ophthalmic solution comprising a chelating agent, reduction of eye irritation and enhancement of the preservative effectiveness have been confirmed, in comparison to Diquafosol ophthalmic solution comprising no chelating agent. Accordingly, the present invention has been confirmed to provide physicochemical properties that are stable during the courses of production and distribution as well as the course of storage by a patient, and also reduce eye irritation and enhance preservative effectiveness.
    Type: Application
    Filed: March 25, 2013
    Publication date: March 12, 2015
    Inventors: Akiko Sakatani, Tatsuo Ikei, Koji Inagaki, Masatsugu Nakamura, Kazuhiro Hosoi, Mikiko Saito, Masaki Sonoda, Yoko Fukui, Mitsuaki Kuwano
  • Patent number: 8975299
    Abstract: The subject invention thus provides a composition comprising at least one triglyceride, at least one phospholipid and at least one poly-unsaturated fatty acids (LC-PUFA); wherein at least about 1% of the LC-PUFA in the composition is conjugated to said at least one phospholipid and uses thereof.
    Type: Grant
    Filed: November 2, 2008
    Date of Patent: March 10, 2015
    Assignee: Enzymotec Ltd.
    Inventors: Fabiana Bar Yosef, Dori Pollod, Ariel Katz
  • Publication number: 20150064253
    Abstract: Disclosed are pharmaceutical compositions comprising Compound I, having the formula: and an effective amount of sofosbuvir wherein the sofosbuvir is substantially crystalline. Also disclosed are methods of use for the pharmaceutical composition.
    Type: Application
    Filed: January 30, 2014
    Publication date: March 5, 2015
    Inventors: Eric Gorman, Erik Mogalian, Reza Oliyai, Dimitrios Stefanidis, Lauren Wiser, Vahid Zia
  • Patent number: 8957046
    Abstract: 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: Grant
    Filed: April 16, 2014
    Date of Patent: February 17, 2015
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
  • Publication number: 20150044138
    Abstract: The invention relates to a composition comprising: (i) one or more of uridine and cytidine, or salts, phosphates, acyl derivatives or esters thereof; and (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, for use in preserving or improving functional synaptic connectivity and/or preserving brain network organization in a subject in need thereof.
    Type: Application
    Filed: March 4, 2013
    Publication date: February 12, 2015
    Applicant: N.V. Nutricia
    Inventors: Marieke Lansbergen, Martine Groenendijk, Patrick Joseph Gerardus Hendrikus Kamphuis, Mattheus Cornelis De Wilde
  • Publication number: 20150045319
    Abstract: 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: Application
    Filed: July 3, 2014
    Publication date: February 12, 2015
    Inventors: Philip G. Haydon, Jinbo Lee, Jinghui Dong, Stephen Moss, Raquel Revilla-Sanchez
  • Patent number: 8951985
    Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: February 10, 2015
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Dominique Surleraux, Cyril B. Dousson, David Dukhan, Claire Pierra
  • Publication number: 20150038451
    Abstract: 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: Application
    Filed: October 21, 2014
    Publication date: February 5, 2015
    Inventors: David Bernard Smith, Jerome Deval, Natalia Dyatkina, Leonid Beigelman, Guangyi Wang
  • Publication number: 20150037282
    Abstract: Provided herein are compounds, compositions, and methods for the treatment of viral infections, for example, 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 D-amino acid phosphoramidate halogeno pyrimidine nucleoside analog compounds which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the compounds are of Formula I: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein: PD, X, R1, R2, RA, and RB are as described herein.
    Type: Application
    Filed: July 31, 2014
    Publication date: February 5, 2015
    Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Cyril B. DOUSSON, Gilles GOSSELIN, Claire PIERRA, David DUKHAN
  • Publication number: 20150032045
    Abstract: The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In some embodiments, the Photolabile Compounds comprise a light antenna, such as a labeling molecule or an active derivative thereof. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect. In another embodiment, the photoreleasable ligand can be a labeling molecule, such as a fluorescent molecule.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 29, 2015
    Inventors: Rafael Yuste, Roberto Etchenique, Luis Baraldo
  • Patent number: 8933052
    Abstract: 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: Grant
    Filed: March 15, 2013
    Date of Patent: January 13, 2015
    Assignees: Janssen Products, LP, Medivir, AB
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
  • Patent number: 8933053
    Abstract: 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: Grant
    Filed: February 29, 2012
    Date of Patent: January 13, 2015
    Assignee: NuCana BioMed Limited
    Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
  • Publication number: 20150011497
    Abstract: 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 norovirus, with a nucleoside, a nucleotide and an analog thereof.
    Type: Application
    Filed: June 24, 2014
    Publication date: January 8, 2015
    Inventors: Leonid Beigelman, Jerome Deval, Zhinan Jin
  • Publication number: 20150004135
    Abstract: The present disclosure relates to compounds of Formula (I): Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of using the compounds of Formula (I) and/or compositions comprising the compounds of Formula (I) for the treatment of HCV.
    Type: Application
    Filed: December 17, 2012
    Publication date: January 1, 2015
    Applicants: HOFFMAN-LA ROCHE INC., RIBOSCIENCE LLC
    Inventors: Jing Zhang, Zhuming Zhang
  • Patent number: 8916538
    Abstract: 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: Grant
    Filed: March 11, 2013
    Date of Patent: December 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent
  • Publication number: 20140369959
    Abstract: The present invention relates to the use of nucleoside derivatives of formula (I) wherein the symbols are as the specification, and of pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: December 17, 2012
    Publication date: December 18, 2014
    Inventors: Mark Smith, Francisco Xavier Talamas, Jing Zhang, Zhuming Zhang
  • Patent number: 8906880
    Abstract: 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: Grant
    Filed: April 17, 2014
    Date of Patent: December 9, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
  • Publication number: 20140356325
    Abstract: Compositions and methods relating to 2?-C-methyl nucleoside 5?-monophosphate derivative compounds are provided. In some embodiments, the novel compounds are useful to treat viral infections. In particular, 2?-C-methyl nucleoside 5?-monophosphate derivative compounds, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of viral infection are described.
    Type: Application
    Filed: January 8, 2013
    Publication date: December 4, 2014
    Applicant: Ligand Pharmaceuticals Incorporated
    Inventors: Lin Zhi, K. Raja Reddy, Mark David Erion, Scott Hecker
  • Publication number: 20140357595
    Abstract: This application describes methods of preventing, treating or reducing the risk of recurrence of a hepatitis C virus infection in a subject after the subject has received a liver transplant. Disclosed herein are methods of preventing or reducing the risk of recurrence of a hepatitis C virus infection in a subject after the subject has received a liver transplant, the methods comprising administering to the subject an effective amount of Compound 1. Also disclosed are methods of reducing HCV RNA levels to about 25 IU/mL or lower in a subject having received a liver transplant comprising administering to the subject an effective amount of Compound 1.
    Type: Application
    Filed: June 2, 2014
    Publication date: December 4, 2014
    Applicant: Gilead Pharmasset LLC
    Inventors: Jill M. Denning, John George McHutchison, G. Mani Subramanian, William Thomas Symonds, III
  • Patent number: 8895531
    Abstract: The present invention includes compounds and compositions of ®-2?-fluoronucleoside phosphonates, as well as methods to treat HIV, HBV, HCV or abnormal cellular proliferation comprising administering said compounds or compositions.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: November 25, 2014
    Assignee: RFS Pharma LLC
    Inventor: Junxing Shi
  • Patent number: 8895516
    Abstract: Saccharide-protein conjugates having a new type of linker are described. The conjugates comprising the new linker are prepared from modified saccharides comprising a moiety of the formula (I): -A-N(R1)-L-M wherein: A is a bond, —C(O)— or —OC(O)—; R1 is selected from H or C1-C6 alkyl; L is a C1-C12 alkylene group; and M is a masked aldehyde group. The new linker is especially useful for preparing conjugates of Neisseria meningitidis serogroup A saccharide. Conjugates having this new linker have improved immunogenicity compared to other types of conjugates.
    Type: Grant
    Filed: September 1, 2003
    Date of Patent: November 25, 2014
    Assignee: Novartis AG
    Inventors: Aldo Giannozzi, Giovanni Averani, Francesco Norelli, Paolo Costantino
  • Publication number: 20140343008
    Abstract: Disclosed are methods for treating hepatitis C in a human patient in need thereof that entails administering to the patient of about 350 mg of sofosbuvir and another anti-HCV compound.
    Type: Application
    Filed: January 30, 2014
    Publication date: November 20, 2014
    Inventor: Cheng Yong Yang
  • Publication number: 20140341847
    Abstract: The present disclosure relates to the compound of Formula I: Also disclosed are pharmaceutical compositions comprising the compound of Formula I, methods of using the compound of Formula I and/or compositions comprising the compound of Formula I for the treatment of HCV.
    Type: Application
    Filed: May 15, 2014
    Publication date: November 20, 2014
    Applicant: Riboscience LLC
    Inventors: Mark Smith, Klaus G. Klumpp
  • Patent number: 8877731
    Abstract: 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: Grant
    Filed: September 19, 2011
    Date of Patent: November 4, 2014
    Assignee: Alios Biopharma, Inc.
    Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
  • Patent number: 8871737
    Abstract: Disclosed herein are phosphorothioate nucleotide analogs, such as thiophosphoroamidate prodrugs and thiophosphates (including ?-thiomonophosphates, ?-thiodiphosphates, and ?-thiotriphosphates), methods of synthesizing phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates and methods of treating viral infections, such as HCV, cancer, and/or parasitic diseases with the phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: October 28, 2014
    Assignee: Alios BioPharma, Inc.
    Inventors: David Bernard Smith, Jerome Deval, Natalia Dyatkina, Leonid Beigelman, Guangyi Wang
  • Publication number: 20140315852
    Abstract: 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: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Applicant: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
  • Publication number: 20140309164
    Abstract: Deuterated nucleoside analogs of Formula (I) and the pharmaceutically acceptable salts thereof are provided by this disclosure The variables, e.g., B1, Y, R1, R2, R3, R3?, R4, R5, R6, R7, R8, and R9 carry definitions set forth in the disclosure. Compounds of Formula (I) are deuterated at one or more positions and the deuterium enrichment at each deuterated positions is at least 50%. Compounds and salts of Formula (I) are useful for treating viral infections, including HCV infections.
    Type: Application
    Filed: April 14, 2014
    Publication date: October 16, 2014
    Applicant: Achillion Pharmaceuticals, Inc.
    Inventors: Milind Deshpande, Jason Allan Wiles, Akihiro Hashimoto, Avinash Phadke
  • Publication number: 20140308342
    Abstract: The present invention relates to chimeric (preferably, bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic cancer where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells. The compounds preferably covalently bind to the urokinase receptor and recruit native antibodies of the patient or subject where the antibodies can selectively degrade and/or deactivate targeted cancer cells through antibody-dependent cellular phagocytosis and/or antibody-dependent cellular cytotoxicity (ADCC) against a large number and variety of cancers, thus providing cancer cell death and/or an inhibition of growth, elaboration and/or metastasis of the cancer, including remission and cure of the patient's cancer.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 16, 2014
    Inventors: David A. Spiegel, Charles E. Jakobsche