Abstract: The invention is directed to a process for the preparation of substituted threonolactone and substituted threose compounds which are intermediates in the synthesis of phosphonate nucleosides being useful antiviral agents.
Type:
Grant
Filed:
September 28, 2015
Date of Patent:
December 20, 2016
Assignee:
K.U. Leuven Research & Development
Inventors:
Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
Abstract: Described herein is a combination that includes compound (A) of the formula and compound (B) of the formula or a pharmaceutically acceptable salt(s) of the foregoing, for ameliorating and/or treating a hepatitis C viral infection.
Type:
Grant
Filed:
April 3, 2014
Date of Patent:
November 29, 2016
Assignee:
Alios BioPharma, Inc.
Inventors:
Julie Krop, Margaret James Koziel, Lawrence M. Blatt, John Fry, Sushmita Mukherjee Chanda
Abstract: Described herein are conjugated modified oligonucleotides that are complementary to a target RNA. The conjugate facilitates cellular uptake of the modified oligonucleotide, resulting improved potency.
Abstract: The present invention relates to a compound represented by Formulas 1, 2 or 3 as described herein, and a nucleic acid each of which contains a dye exhibiting an exciton effect, a method of producing such a nucleic acid by using the compound, and a kit for producing the nucleic acid.
Abstract: The present invention provides fluorinated 5-aza-2?-deoxycytidine compounds, such as 2?,2?-difluoro-5-aza-2?-deoxycytidine, compositions that include the compounds, methods for making the compounds, and methods for inhibiting DNA methyltransferase, treating solid tumors, and treating hematologic cancers by administering the compounds.
Abstract: The present invention relates to a pentosanpolysulfate (PPS) or a pharmaceutically acceptable salt thereof for use in the amelioration, treatment, or prevention of adverse neurological events caused by administering an antibody or fragment thereof comprising a CD3 binding domain, including a CD19 x CD3 bispecific single chain antibody, such as blinatumomab. PPS is a semi-synthetically produced heparin-like macromolecular carbohydrate derivative, which chemically and structurally resembles glycosaminoglycans. Kits comprising a PPS, an antibody or fragment thereof comprising a CD3 binding domain, and instructions for administration, which indicate that the PPS is to be employed for the amelioration, treatment or prevention of adverse neurological events caused by administering the antibody or fragment thereof comprising said CD3 binding domain, are also disclosed.
Type:
Grant
Filed:
February 8, 2014
Date of Patent:
November 8, 2016
Assignee:
AMGEN RESEARCH (MUNICH) GMBH
Inventors:
Peter Kufer, Dirk Nagorsen, Juergen Scheele, Gerhard Zugmaier, Matthias Klinger, Patrick Hoffmann, Virginie Naegele, Elaine-Pashupati Dopfer
Abstract: A method of isolating nucleic acid from a sample is provided that includes contacting a sample that includes nucleic acid with a solid support, wherein the surface of the solid support includes groups that can complex with the nucleic acid, in the presence of a solution that includes an oligoethylene glycol having 10 or fewer ethylene oxide-units and a salt comprising a monovalent or divalent metal ion, whereby soluble nucleic acid in said sample binds to the surface of the support; separating the solid support with bound nucleic acid from the sample; and eluting the bound nucleic acid from the solid support, thereby isolating nucleic acid from the sample. Also provided is a method of washing nucleic acids bound to a solid support that includes providing a solid support, wherein nucleic acid molecules are bound to the surface of the solid support; and washing the solid support with a solution that includes an oligoethylene glycol having 10 or fewer ethylene oxide units.
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:
January 22, 2015
Date of Patent:
September 27, 2016
Assignee:
ALNYLAM PHARMACEUTICALS, INC.
Inventors:
Muthiah Manoharan, Kallanthottathil G. Rajeev, Alexander V. Kelin, Sudhakar Rao Takkellapati, Shigeo Matsuda
Abstract: A deuterated nucleoside analog of the formula and the pharmaceutically acceptable salts thereof are provided by this disclosure. The disclosure also includes pharmaceutical compositions comprising a compound or salt of the formula and a carrier. Compounds and salts of this formula are useful for treating viral infections, including HCV infections. A method for treating a host afflicted with hepatitis C or other disorders is also presented that includes administering an effective treatment amount of a nucleoside or nucleotide that has deuterium with at least 50% enrichment at the 5?-position of the nucleoside or nucleotide.
Type:
Grant
Filed:
April 14, 2014
Date of Patent:
September 20, 2016
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Milind Deshpande, Jason Allan Wiles, Akihiro Hashimoto, Avinash Phadke
Abstract: This invention relates to a 2?-modified RNA agent comprising at least one RNA strand containing a 2?-O substituent having an alkyne functional group attaching to the O atom at the 2?-position on one or more ribose rings, wherein the 2?-O substituent is located at one or more of positions 2, 3, 4, 7, 8, 9, 10, 11, 13, 14, and 16, from 5?-end of the RNA strand. This invention also relates to a 2?-modified RNA agent comprising at least one RNA strand containing a 2?-O substituent having a triazole functional group attaching to the O atom at the 2?-position on one or more ribose rings, wherein the 2?-O substituent is located at one or more of positions 2, 3, 4, 7, 8, 9, 10, 11, 13, 14, and 16, from 5?-end of the RNA strand.
Abstract: The invention relates to a compound which is, 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine, which is a selective A2A adenosine receptor agonist in myocardial imaging. The new polymorph of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine (designated as polymorph E) is characterized by an X-ray diffraction pattern of X-RPD showing the following reflections at 2 Theta=5.8°, 12.3°, 15.9°, 17.3°, 20.5°, 22.6°, 23.6°, 27.7°, and 29.2°; and further characterized by a DSC scan showing marked endotherm in the range of 258 to 264° C.; and further characterized by a specific IR spectra.
Type:
Grant
Filed:
June 27, 2013
Date of Patent:
September 13, 2016
Assignee:
Farmak, a.s.
Inventors:
Lubomir Kvapil, Pavel Hradil, Martin Grepl, Petr Slezar, Barbora Dvorakova
Abstract: The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: Also disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.
Type:
Grant
Filed:
September 2, 2011
Date of Patent:
August 23, 2016
Assignees:
High & New Technology Research Center, Henan Academy of Sciences, Zhengzhou Granlen Pharmatech Ltd., Zhengzhou University
Inventors:
Junbiao Chang, Haoyun An, Xuejun Yu, Xiaohe Guo
Abstract: Compositions and techniques for the extraction, enrichment and isolation of nucleic acids from fresh, fixed or fixed and embedded cells, tissues, biological materials and cellular source material using amine monomers are disclosed herein.
Abstract: The present invention relates to 5?-Substituted Nucleoside Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2 and R3 are as defined herein and B is a 7-deaza-9-purinyl moiety. 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:
Grant
Filed:
July 10, 2012
Date of Patent:
August 16, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Vinay Girijavallabhan, Stephane L. Bogen, Qun Dang, David B. Olsen
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:
Grant
Filed:
July 10, 2012
Date of Patent:
August 9, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
Abstract: The present invention concerns an improved method for the isolation of nucleic acids such as DNA and RNA from bacterial, plant, animal or human cells as well as from cell cultures and virus cultures, wherein the nucleic acid is immobilised on a matrix having a silicon-oxygen compound in the presence of a chaotropic agent and an alkanol, carried out in a temperature range of 36° to 75° C.
Type:
Grant
Filed:
February 13, 2006
Date of Patent:
August 9, 2016
Assignee:
QIAGEN GMBH
Inventors:
Markus Sprenger-Haus-sels, Gaby Schulte, Thomas Deutschmann, Sibylle Felker
Abstract: Compositions and techniques for the extraction, enrichment and isolation of nucleic acids from fresh, fixed or fixed and embedded cells, tissues, biological materials and cellular source material using amine monomers are disclosed herein.
Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorders, 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 are compounds according to Formula I: or a pharmaceutically acceptable salt, solvate, tautomeric or polymorphic form thereof.
Type:
Grant
Filed:
September 11, 2012
Date of Patent:
August 2, 2016
Assignee:
IDENIX PHARMACEUTICALS LLC
Inventors:
Dominique Surleraux, Cyril B. Dousson, Gilles Gosselin, David Dukhan, Claire Pierra, Jerome Peyronnet