Abstract: The present invention concerns an oligonucleotide modified by substitution at the 3? or the 5? end by a moiety comprising at least one ketal functional group, wherein the ketal carbon of said ketal functional group bears two saturated or unsaturated, linear or branched, hydrocarbon chains comprising from 1 to 22 carbon atoms, and the use therefore as a medicament, in particular for use for treating cancer.
Type:
Grant
Filed:
June 5, 2014
Date of Patent:
July 11, 2017
Assignees:
INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), UNIVERSITE DE BORDEAUX, UNIVERSITE D 'AIX-MARSEILLE, INSTITUT JEAN PAOLI & IRENE CALMETTES, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
Inventors:
Philippe Barthelemy, Khalid Oumzil, Palma Rocchi, Julie Acunzo
Abstract: Provided herein are methods for the synthesis of oligomeric compounds wherein the standard coupling protocols are modified when coupling bicyclic nucleosides of Formula I. More particularly, the modified coupling protocols provide for a decrease in the ratio of phosphoramidite solution to activator solution in the coupling reagent with an increased contact time. The modified coupling protocols provide for oligomeric compounds having comparable yields to similar oligomeric compounds having modified nucleosides other than bicyclic nucleosides of Formula I.
Type:
Grant
Filed:
January 30, 2014
Date of Patent:
July 11, 2017
Assignee:
Ionis Pharmaceuticals, Inc.
Inventors:
Isaiah E. Cedillo, Michael T. Migawa, W. Brad Wan
Abstract: An object of the present invention is to provide a technique for preparing RNA ready for an enzymatic reaction more easily than conventional techniques. The present invention provides a reagent for RNA extraction from a biological sample which contains an alkali metal salt and a surfactant.
Type:
Grant
Filed:
October 25, 2013
Date of Patent:
July 4, 2017
Assignee:
KANEKA CORPORATION
Inventors:
Sotaro Sano, Shigehiko Miyamoto, Jun Tomono, Hajime Hiratsuka
Abstract: Provided herein are methods for treating subjects having a cancer, such as a relapsed or refractory solid tumor, wherein the method comprises administering to the subject a cytidine analog. In certain of the methods, the cytidine analog is administered alone or in combination with one or more anti-cancer agents. Also provided are methods for using a cytidine analog, to treat diseases and disorders including disorders related to abnormal cell proliferation, hematologic disorders, and immune disorders, among others. In certain of the methods, the cytidine analog is formulated in an oral dosage form and administered orally.
Type:
Grant
Filed:
April 16, 2015
Date of Patent:
July 4, 2017
Assignee:
Celgene Corporation
Inventors:
Kyle J. MacBeth, Aaron N. Nguyen, Jorge Dimartino
Abstract: A novel C1-phosphate log of uridine-5?-diphosphate (UDP)-GlcNAc as an effective OGT (O-linked N-acetylglucosamine (O-GlcNAc) transferase) inhibitor, and a preparation method for the same provides a compound having an OGT inhibitory effect that can be used as a useful tool in the studies on various vital phenomena in association with the protein modification by O-GlcNAc within cells and furthermore as a candidate substance in the treatment or research of diseases related to the protein modification by O-GlcNAc, such as cancers, diabetes, or degenerative neurological diseases.
Type:
Grant
Filed:
December 15, 2015
Date of Patent:
July 4, 2017
Assignee:
SOONCHUNHYANG UNIVERSITY INDUSTRY ACADEMY COOPERATION FOUNDATION
Abstract: The present invention is directed to a use of a heat shock protein inhibitor in preparing pharmaceutical composition for treating hepatitis by scavenging hepatitis B virus-infected cells. The heat shock protein inhibitor is selected from a group including VER-155008, Pifithrin-?, and pharmaceutical acceptable salts thereof. The present invention is also directed to a use of a heat shock protein inhibitor in preparing pharmaceutical composition for treating hepatoma.
Abstract: The present invention relates to substituted purine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
Abstract: 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 unsavory 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 unsavory nucleoside and/or nucleotide component, in particular comprising an uridine-containing nucleoside and/or a nucleotide in combination with an unsavory edible oil, such as a fish oil.
Type:
Grant
Filed:
August 31, 2015
Date of Patent:
June 27, 2017
Assignee:
N.V. Nutricia
Inventors:
Esther Jacqueline Petra De Kort, Martine Groenendijk, Patrick Joseph Gerardus Hendrikus Kamphuis
Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
Type:
Grant
Filed:
August 28, 2015
Date of Patent:
June 20, 2017
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Adam D. Hughes, Erik Fenster, Melissa Fleury, Roland Gendron, Edmund J. Moran
Abstract: The present invention discloses compounds of formula (I), or a pharmaceutically acceptable salt thereof: which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Grant
Filed:
August 26, 2015
Date of Patent:
June 13, 2017
Assignee:
ENANTA PHARMACEUTICALS, INC.
Inventors:
Yao-Ling Qiu, Xiaowen Peng, Xuri Gao, Hui Cao, Yat Sun Or
Abstract: The invention relates to oligonucleotide-oligocation molecules AiBjH that can be synthetized via automated phosphoramidite chemistry having oligonucleotides moieties Ai and oligocations moieties Bj, wherein .Ai is an i-mer oligonucleotide residue, with i=5 to 50, where nucleotide A is an oligomer with naturally or non naturally occurring nucleobases and/or pentafuranosyl groups and/or native phosphodiester bonds, for example selected from the group comprising deoxyribo, ribo, locked (LNA) nucleotides as well as their chemical modifications or substitutions such as phosphorothioate, 2?-fluoro, 2?-O-alkyl, or a marker group such as a fluorescent agent, .Bj is a j-mer organic oligocation moiety, with j=1 to 50, where B is selected from the group comprising .—HPO3—R1—(X—R2n)n1—X—R3—O—, where R1, R2n and R3, identical or different, are lower alkylene, X is NH or NC(NH2)2, n varies from 1 to 5 and n1=2 to 20, .
Type:
Grant
Filed:
June 22, 2015
Date of Patent:
June 13, 2017
Assignees:
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE STRASBOURG, POLYPLUS TRANSFECTION
Abstract: Provided is a process for making (2-nitro)alkyl (meth)acrylate compounds of formula I: wherein n, R, R1, R2, R3, R4, R6, R7, and n are as defined herein, by a transesterification reaction between a nitroalcohol compound and a (meth)acrylate compound in the presence of a transesterification catalyst and a free radical inhibitor.
Type:
Grant
Filed:
February 18, 2014
Date of Patent:
June 6, 2017
Assignee:
ANGUS CHEMICAL COMPANY
Inventors:
Muhunthan Sathiosatham, Robert Wilczynski
Abstract: Disclosed are compositions and formulations comprising glucosamine or a pharmaceutically acceptable salt thereof for use in the treatment of joint conditions and adapted for use in a bath or soak or bath beads, powders, salts, and oils, kits, and methods of treatment using the same. Also disclosed are lozenges, suppositories, patches, and topical creams comprising glucosamine or a pharmaceutically acceptable salt thereof for use in the treatment of joint conditions and methods of treatment using the same. In some embodiments the joint conditions include osteoarthritis.
Type:
Grant
Filed:
March 18, 2015
Date of Patent:
June 6, 2017
Assignee:
Vital Medicine, LLC
Inventors:
Anjan Chatterji, Grant Cooper, David Schwartz
Abstract: The subject invention relates to improved tocopheryl quinone derivatives and tocopherol derivatives having improved pharmacokinetics in vivo that can, in some embodiments, be useful in the treatment of Lysosomal Storage Disorders, restoration of normal mitochondrial ATP production, modulation of intracellular calcium ion concentration and other treatments or therapies. The tocopheryl quinone derivatives and tocopherol derivatives have side chains that have terminally halogenated carbon atoms.
Type:
Grant
Filed:
November 14, 2013
Date of Patent:
May 30, 2017
Assignee:
The United States of America, As Presented by The Scretary, Department of Health and Human Services
Inventors:
Juan Jose Marugan, Wei Zheng, Jingbo Xiao, John McKew
Abstract: Contemplated compositions and methods employ betalains for treatment of various conditions, and especially osteoarthritis, sinusitis, contact dermatitis, acne, an allergic condition, reduced mental alertness, reduced physical strength, reduced physical endurance, and/or impaired mood.
Abstract: The invention provides a novel polymorph of Regadenoson. More particularly, the invention provides propylene glycol solvate of Regadenoson. The invention also provides a process for the preparation of propylene glycol solvate of Regadenoson.
Type:
Grant
Filed:
May 28, 2014
Date of Patent:
April 18, 2017
Assignee:
Biophore India Pharmaceuticals PVT. Ltd.