The N-hetero Ring Is Part Of A Bicyclic Ring System Patents (Class 536/26.7)
  • Patent number: 9744183
    Abstract: Described herein are nucleic acid prodrugs and nucleic acid prodrugs comprising chiral phosphorous moieties. Also described herein are methods of making and using nucleic acid prodrugs and nucleic acid prodrugs comprising chiral phosphorous moieties.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: August 29, 2017
    Assignee: WAVE LIFE SCIENCES LTD.
    Inventors: Gregory L. Verdine, Meena ., Naoki Iwamoto
  • Patent number: 9475831
    Abstract: A compound has Formula I: A, B, C, D, W, X, Y, and Z are independently selected from hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 alkoxy, aryl, aldehyde, protected aldehyde, CH, N, O, S, null, and bond; Q is selected from aldehyde, protected aldehyde, and null, at least one of A, B, C, D, W, X, Y, Z, or Q is an aldehyde or protected aldehyde; the bonds between each of A-B, B-C, C-D, W-X, X-Y, and Y-Z are selected from single bond, double bond, triple bond, and no bond; L is a linker selected from a C1-C12 alkyl, aralkyl, and aryl, any of which is optionally substituted; one or more methylene unit (CH2) of the C1-C12 alkyl is optionally replaced by any combination of oxygen, carbonyl(C?O), and NH; and R1 and R2 are independently selected from —NR3R4, halogen, C1-C8 alkoxy, aralkoxy, alkenyloxy, alkynyloxy, and OCH2CH2CN; R3 and R4 are independently a C1-C4, straight chain or branched alkyl group.
    Type: Grant
    Filed: January 20, 2016
    Date of Patent: October 25, 2016
    Assignee: Illumina, Inc.
    Inventors: Ryan Christopher Smith, Randall Smith, Xiaodong Zhao
  • 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: 20150141490
    Abstract: The present invention relates to pyrazolotriazolyl nucleoside analogues, oligonucleotide comprising them, and uses thereof. Further the invention relates to a method for reducing gene expression in a cell comprising transfecting the cell with such an oligonucleotide. It has been found, in accordance with the present invention, that certain pyrazolotriazolyl-based nucleoside analogues such as 8-[3?-(2-cyanoethyl)-(N,Ndiisopropyl)]-phosphoramidite-(2?-deoxy-5?-dimethoxytrity 1-13-D-ribofuranozyl)-4-{N-benzoylamino)-pyrazolo[1,5a]-1,3,5-triazine, can be incorporated into oligonucleotides, substituting natural purine nucleosides and imparting acid stability and nuclease stability to the oligonucleotide. Furthermore, oligonucleotides comprising one or more such nucleoside analogues are capable of hybridizing with oligonucleotides having complementary sequences thereto in which no such analogues are incorporated.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 21, 2015
    Inventors: Jean-Christophe Truffert, Myriam Lefoix, Jean Hildesheim, Tirtsa Kleinman
  • Patent number: 9029335
    Abstract: Provided herein are novel bicyclic nucleosides, oligomeric compounds that include such bicyclic nucleosides and methods of using the oligomeric compounds. More particularly, the novel bicyclic nucleosides comprise a furanose ring system having a bridge comprising a 4?-methylene group attached to a 2?-sulfoxide or sulfone group and optionally including one or more substituent groups attached to the 4?-methylene and or the 5?-position. In certain embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 12, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Eric E. Swayze
  • Publication number: 20150111958
    Abstract: This invention relates to antisense oligonucleotides comprising at least one N3??P5? phosphorodiamidate linkage (NPN) in the backbone as well as methods for using the same. The antisense oligonucleotides can effectively prevent or decrease protein expression.
    Type: Application
    Filed: September 26, 2014
    Publication date: April 23, 2015
    Inventors: Krisztina PONGRACZ, Mahesh Ramaseshan
  • 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
  • Publication number: 20150080457
    Abstract: The present invention provides nucleosides and oligonucleotides comprising a 5? phosphate mimics of formula (IVc) or (Vc), One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such dinucleotide of formula (Ia). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Muthiah MANOHARAN, Kallanthottathil G. RAJEEV, Marija PRHAVC, Ivan ZLATEV
  • 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: 20150072345
    Abstract: Oligonucleotides with a novel sugar-phosphate backbone containing at least one 2?-arabino-fluoronucleoside and an internucleoside 3?-NH—P(—O)(OR)—O-5? linkage, where R is a positively charged counter ion or hydrogen, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive phosphoramidate 2?-arabino-fluorooligonucleotides have a high RNA binding affinity to complementary nucleic acids and are base and acid stable.
    Type: Application
    Filed: September 11, 2014
    Publication date: March 12, 2015
    Inventors: Sergei M. Gryaznov, Ronald G. Schultz
  • Patent number: 8975389
    Abstract: The present invention provides nucleosides of formula (1) and oligonucleotides comprising at least one nucleoside of formula (2): Another aspect of the invention relates to a method of inhibiting the expression of a gene in cell, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: March 10, 2015
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Alexander V. Kelin, Sudhakar Rao Takkellapati, Shigeo Matsuda
  • Patent number: 8957045
    Abstract: A nucleoside compound having activity against hepatitis C virus is disclosed.
    Type: Grant
    Filed: February 25, 2013
    Date of Patent: February 17, 2015
    Assignee: Gilead Pharmasset LLC
    Inventors: Michael Joseph Sofia, Jinfa Du, Peiyuan Wang, Dhanapalan Nagarathnam
  • Patent number: 8951986
    Abstract: The invention is related to salts of anti-viral compounds, compositions containing such salts, and therapeutic methods that include the administration of such salts, as well as to processes and intermediates useful for preparing such salts.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: February 10, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Benjamin R. Graetz, Richard Polniaszek
  • Publication number: 20150025220
    Abstract: The invention provides a compound of formula I: wherein R1-R6 and X have any of the values described herein, as well as pharmaceutical compostions comprising such compounds and therapeutic methods comprising the administration of such compounds.
    Type: Application
    Filed: July 21, 2014
    Publication date: January 22, 2015
    Inventor: Carston R. Wagner
  • Publication number: 20150018300
    Abstract: Disclosed herein are 2?-spiro-nucleosides and derivatives thereof useful for treating a subject infected by hepatitis C virus or dengue virus.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 15, 2015
    Applicant: GILEAD PHARMASSET LLC
    Inventors: Jinfa Du, Michael Joseph Sofia
  • Publication number: 20140350234
    Abstract: The present invention is directed to n-alkylated synthetic nucleosides of high regiospecific purity and oligonucleotides that can be utilized for studies on reversal of cytotoxic and mutagenic DNA damage, and as diagnostic tools.
    Type: Application
    Filed: February 20, 2014
    Publication date: November 27, 2014
    Applicant: ChemGenes Corporation
    Inventors: Satya P. Bajpai, Sant K. Srivastav, Suresh C. Srivastava
  • 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: 20140315850
    Abstract: The present invention is made to fulfill the foregoing need. Since most of antiHN nucleosides are 2?,3?-dideoxynucleosides that have been proved to be excellent substrates of kinases for the phosphorylations. 2?,3?-Dideoxy-2,-a-fluoro-2?-{3-C-methyl-nucleosides can be considered as one unique class of 2?,3?-dideoxynucleosides to be good substrate of kinases because fluorine mimics hydrogen. It also can be considered as ribo-nucleosides to incorporate into RNA of HCV because 2?-fluorine-a mimics 2?-a-OH group.
    Type: Application
    Filed: July 19, 2012
    Publication date: October 23, 2014
    Applicant: Nanjing Molecular Research, Inc.
    Inventors: Qiang Huang, Suping Zhou, Junbiao Chang
  • Publication number: 20140308343
    Abstract: The invention relates to a method for preparing nanoparticles based on functional amphiphilic molecules or macromolecules, optionally in the presence of at least one colipide, enabling the encapsulation of therapeutic agents, especially anti-tumoral agents, and the use thereof for the transport and vectorization of therapeutic agents, especially anti-tumoral agents.
    Type: Application
    Filed: March 13, 2014
    Publication date: October 16, 2014
    Applicants: UNIVERSITE VICTOR SEGALEN BORDEAUX 2, UNIVERSITE DE LA MEDITERRANEE, UNIVERSITE DE BOURGOGNE
    Inventors: Philippe BARTHELEMY, Michel CAMPLO, Nathalie CAMPINS, Bruno CHAUFFERT, Florence BOUYER
  • Publication number: 20140296177
    Abstract: A new class of biotin protein ligase (BPL) inhibitors that have antibacterial activity against multiple Staphylococcus aureus isolates, including clinically important methicillin-resistant S. aureus (MRSA) are disclosed that are non-toxic.
    Type: Application
    Filed: September 21, 2012
    Publication date: October 2, 2014
    Inventors: Andrew Abel, Steven Polyak, Grant Booker, John Wallace, Tatiana Soares Da Costa, Angie Jarrad, William Tieu, Kelly Lee Keeling, Daniel Sejer Pederson, Nicole Pendini, Matthew Wilce, Min Yin Yap
  • Publication number: 20140286903
    Abstract: This invention is directed to compounds of Formula (I) having the structure that are useful in the treatment of viral infections in mammals, particularly in humans, mediated, at least in part, by a virus in the Flaviviridae family of viruses.
    Type: Application
    Filed: November 8, 2012
    Publication date: September 25, 2014
    Applicants: INHIBITEX, INC., UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
    Inventors: Stanley Chamberlain, John Vernachio, Srinivas K. Battina, Changalvala V.S. Ramamurty, C. Srinivas Rao, Chris McGuigan, Andrea Brancale
  • Publication number: 20140288294
    Abstract: The invention is related to phosphorus substituted anti-viral inhibitory 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: Application
    Filed: February 11, 2014
    Publication date: September 25, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Constantine G. BOOJAMRA, Kuei-Ying LIN, Richard L. MACKMAN, David Y. MARKEVITCH, Oleg V. PETRAKOVSKY, Adrian S. RAY, Lijun ZHANG
  • Publication number: 20140248242
    Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, the compounds are according to Formula 2001: where PD, Base, RA and RB are as provided herein. 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: Application
    Filed: March 3, 2014
    Publication date: September 4, 2014
    Inventors: Cyril B. DOUSSON, Benjamin Alexander MAYES, David DUKHAN, Adel M. MOUSSA, Alistair James STEWART
  • Publication number: 20140248241
    Abstract: 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 3?-deoxy nucleoside compounds according to Formula 3001a or 3001b: or a pharmaceutically acceptable salts, solvates, stereoisomeric forms, tautomeric forms, or polymorphic forms thereof, wherein PD, Base1 and Base2 are as provided herein.
    Type: Application
    Filed: March 3, 2014
    Publication date: September 4, 2014
    Inventors: Alistair James STEWART, Adel M. MOUSSA, Benjamin Alexander MAYES, Francois-Rene ALEXANDRE, Dominique SURLERAUX, Christophe Claude PARSY, Claire PIERRA, David DUKHAN, Gilles GOSSELIN
  • Patent number: 8822671
    Abstract: A 2?-modified ribonucleoside having an alkoxymethyl protective group can be imparted with a high duplex-forming ability by introducing, as a substituent, a halogen atom into the protective group moiety. A modified form of RNA having a halogen-substituted alkoxymethyl protective group exhibits a high duplex-forming ability that is comparable to the duplex-forming ability of a 2?-O-methyl modified nucleic acid.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: September 2, 2014
    Assignees: The University of Tokyo, Chiralgen, Ltd.
    Inventors: Mamoru Shimizu, Takeshi Wada, Kouichiro Arai
  • Publication number: 20140235567
    Abstract: The present invention relates to 5?-Substituted Nucleoside Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein B, X, Y, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Derivative, and methods of using the 5?-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 10, 2012
    Publication date: August 21, 2014
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Vinay Girijavallabhan, Stephane L. Bogen, Qun Dang, David B. Olsen
  • Patent number: 8809520
    Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: August 19, 2014
    Assignee: K.U. Leuven Research & Development
    Inventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
  • Publication number: 20140227224
    Abstract: The invention is related to salts of anti-viral compounds, compositions containing such salts, and therapeutic methods that include the administration of such salts, as well as to processes and intermediates useful for preparing such salts.
    Type: Application
    Filed: January 8, 2014
    Publication date: August 14, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Benjamin R. GRAETZ, Richard POLNIASZEK
  • Publication number: 20140221304
    Abstract: The present invention relates to 5?-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Analog, and methods of using the 5?-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 10, 2012
    Publication date: August 7, 2014
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
  • Publication number: 20140212382
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing viral infections using nucleoside analog monophosphate prodrugs. More specifically, HCV, Norovirus, Saporovirus, Dengue virus, Chikungunya virus and Yellow fever in human patients or other animal hosts. The compounds are certain 2,6-diamino 2-C-methyl purine nucleoside monophosphate prodrugs and modified prodrug analogs, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HCV, Norovirus, Saporovirus, Dengue virus, Chikungunya virus and Yellow fever. This invention teaches how to modify the metabolic pathway of 2,6-diamino 2?-C-methyl purine and deliver nucleotide triphosphate(s) to polymerases at heretofore unobtainable therapeutically-relevant concentrations.
    Type: Application
    Filed: May 16, 2012
    Publication date: July 31, 2014
    Applicants: EMORY UNIVERSITY, RFS PHARMA, LLC
    Inventors: Raymond F. Schinazi, Jong Hyun Cho, Longhu Zhou, Hongwang Zhang, Ugo Pradere, Steven J. Coats
  • Publication number: 20140206640
    Abstract: The present invention relates to 2?-Azido 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?-Azido Substituted Nucleoside Derivative, and methods of using the 2?-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: April 11, 2012
    Publication date: July 24, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Frank Bennett, Vishal Verma, Ashok Arasappan, Kevin X. Chen, Ying Huang, Angela Kerekes, Latha Nair, Dimitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • Publication number: 20140206856
    Abstract: The invention provides a glucoside compound, which is capable of providing a phosphoramidite, which can be produced at low cost and can produce a nucleic acid in high yield and with high purity. The glycoside compound has the formula wherein B, R1, R2, and R3 are as described herein.
    Type: Application
    Filed: August 24, 2012
    Publication date: July 24, 2014
    Applicant: BONAC CORPORATION
    Inventors: Eriko Aoki, Hiroshi Suzuki, Akihiro Itoh
  • Publication number: 20140193339
    Abstract: A new family of analogues of NADP+ or NADPH, their preparation and their application in therapeutics.
    Type: Application
    Filed: June 19, 2012
    Publication date: July 10, 2014
    Inventors: Anny Slama-Schwok, Jean-Luc Boucher, Yun Xu-Li, Eric Deprez, Etienne Henry, Chantal Dessy, Olivier Feron, Bogdan Tarus
  • Patent number: 8765935
    Abstract: The invention provides a compound of formula (I), wherein R1-R6 and X have any of the values described, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: July 1, 2014
    Assignee: Regents of the University of Minnesota
    Inventor: Carston R. Wagner
  • Publication number: 20140179627
    Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 26, 2014
    Applicant: ALIOS BIOPHARMA, INC.
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith
  • Publication number: 20140178338
    Abstract: 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 according to Formula 1501: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, PD, RA, RB, RC, L, M and Z are as described herein.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 26, 2014
    Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART, Gilles GOSSELIN
  • Patent number: 8759316
    Abstract: A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure is described. The method of this invention can be used for patients in need of antiplatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding.
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: June 24, 2014
    Assignee: The Medicines Company
    Inventors: Lisa Ruderman Chen, Simona Skerjanec, Dawn Bell, Jayne Prats, Meredith Todd, Clive Arthur Arculus-Meanwell, Diane Mould
  • Patent number: 8759508
    Abstract: The compounds are of class of chromophoric 1,2,3-triazolyl equipped silyl linking groups that are useful in the chemical synthesis of RNA.
    Type: Grant
    Filed: May 16, 2008
    Date of Patent: June 24, 2014
    Assignee: GE Healthcare Dharmacon, Inc.
    Inventor: Michael Oren Delaney
  • Patent number: 8759502
    Abstract: A protecting group for 1-nitrogen atom of an indole group including a sulfonylethyl carbamate group, wherein the protecting group is represented by the following General Formula (I) and capable of being removed from the 1-nitrogen atom of the indole group in an aprotic solvent: where R represents an alkyl group, a derivative of the alkyl group, a phenyl group or a derivative of the phenyl group.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: June 24, 2014
    Assignee: Apta Biosciences Ltd.
    Inventor: Tsuyoshi Fujihara
  • Patent number: 8759510
    Abstract: 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: Grant
    Filed: April 5, 2012
    Date of Patent: June 24, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Ganapati Reddy Pamulapati, Bruce S. Ross, Michael Joseph Sofia
  • Publication number: 20140163216
    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: Application
    Filed: February 14, 2014
    Publication date: June 12, 2014
    Applicants: Centre National de la Recherche Scientifique, Idenix Pharmaceuticals, Inc.
    Inventors: Dominique SURLERAUX, Gilles GOSSELIN
  • Publication number: 20140161770
    Abstract: 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: Application
    Filed: April 11, 2012
    Publication date: June 12, 2014
    Applicant: 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
  • Publication number: 20140154211
    Abstract: The present invention relates to 2?-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Substituted Nucleoside Derivative, and methods of using the 2?-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: April 11, 2012
    Publication date: June 5, 2014
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Vishal Verma, Frank Bennett, Angela Kereles, Ashok Arasappan, Dmitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • Publication number: 20140140955
    Abstract: This invention is directed to novel compounds of formula (I) having the structure (I) wherein U, V, W, Z, R1, X1, X2, and Y are defined herein. The compounds of formula (I) and pharmaceutical compositions containing these compounds are useful in the treatment of viral infections in mammals mediated, at least in part, by a virus in the Flaviviridae family of viruses, in particular hepatitis C virus (HCV).
    Type: Application
    Filed: December 29, 2011
    Publication date: May 22, 2014
    Applicants: UNIVERSITY COLLEGE OF CARDIFF CONSULTANTS LIMITED, INHIBITEX, INC.
    Inventors: Chris McGuigan, Karolina Madela, Claire Bourdin, John Vernachio, Stanley Chamberlain
  • Patent number: 8716262
    Abstract: A nucleoside compound having activity against hepatitis C virus is disclosed.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: May 6, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Michael Joseph Sofia, Jinfa Du, Peiyuan Wang, Dhanapalan Nagarathnam
  • Patent number: 8716263
    Abstract: A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: May 6, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Byoung-Kwon Chun, Jinfa Du, Suguna Rachakonda, Bruce Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Wonsuk Chang, Hai-Ren Zhang, Dhanapalan Nagarathnam
  • Publication number: 20140123342
    Abstract: The role of extracellular nucleotides and apyrase enzymes in the guard cells that border stomata in regulating stomatal aperture and the plant's resistance to drought and pathogens is disclosed herein. Expression of apyrases APY1 and APY2, in guard cell protoplasts is strongly correlated with cell growth, cell secretory activity and with conditions that favor stomatal opening. Both short-term inhibition of ectoapyrase activity and long-term suppression of APY1 and APY2 transcript levels significantly disrupt normal stomatal behavior in light. Furthermore, two punnoceptor inhibitors in mammals, pyridoxalphosphate-6-azo-phenyl-2?,4?-disulphonic acid (PPADS) and Reactive Blue 2, block ATPS- and ADP?S-induced opening and closing, and also partially block the ability of abscisic acid (ABA) to induce stomatal closure, and light-induced stomatal opening.
    Type: Application
    Filed: June 1, 2012
    Publication date: May 1, 2014
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Stanley J. Roux, Iris Steinebrunner, Gregory B. Clark
  • Publication number: 20140112887
    Abstract: 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: Application
    Filed: October 21, 2013
    Publication date: April 24, 2014
    Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART