Phosphorus Containing Patents (Class 514/47)
  • Patent number: 11060715
    Abstract: The technology relates in part to methods and compositions for ex vivo proliferation and expansion of epithelial cells.
    Type: Grant
    Filed: July 30, 2019
    Date of Patent: July 13, 2021
    Assignee: PROPAGENIX INC.
    Inventor: Chengkang Zhang
  • Patent number: 10993947
    Abstract: The present invention is relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1, X2 and X3 are N; Y is N or CH; W is H or F; with the proviso that when W is F, then X1, X2 and X3 are N; R1 and R2 are independently of each other (i) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: May 4, 2021
    Assignee: TORQUR
    Inventors: Doriano Fabbro, Paul Hebeisen, Petra Hillmann-Wuellner, Anton Stuetz, John T. Seykora, Florent Beaufils
  • Patent number: 10987372
    Abstract: It is an object of the present invention to provide a novel therapeutic agent for hepatoma viruses. Specifically, the present invention relates to an anti-hepatoma virus agent, containing as an active ingredient a compound represented by the following Formula (I) or a pharmaceutically acceptable salt thereof: (wherein R1 is fluorine or hydrogen).
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: April 27, 2021
    Assignees: KAGOSHIMA UNIVERSITY, NATIONAL UNIVERSITY CORPORATION OKAYAMA UNIVERSITY, DAIKIN INDUSTRIES, LTD.
    Inventors: Masanori Ikeda, Midori Takeda, Masanori Baba, Nobuyuki Kato
  • Patent number: 10960006
    Abstract: A topical formulation comprising (a) a therapeutically effective amount of tofacitinib; (b) at least one solvent; and (c) optionally one or more other pharmaceutically acceptable excipients is provided. Also provided is a method for treating and/or preventing autoimmune diseases in a subject administering said topical formulation.
    Type: Grant
    Filed: January 22, 2019
    Date of Patent: March 30, 2021
    Assignee: TWi Pharmaceuticals, Inc.
    Inventors: Chih-Ming Chen, Guang-Wei Lu, Ling-Ying Liaw, Fan-Lun Liu, Shih-Fen Liao, Chou-Hsiung Chen, Yu-Han Kao, Yu-Yin Chen
  • Patent number: 10953030
    Abstract: Cytidine nucleoside analogues of Formula I, wherein the variables are as described herein, in combination with uridine nucleoside analogues of Formula II, wherein the variables are as described herein, produce a synergistic effect on the inhibition of HCV polymerase.
    Type: Grant
    Filed: August 5, 2019
    Date of Patent: March 23, 2021
    Assignee: Riboscience LLC
    Inventors: Mark Smith, Klaus G. Klumpp
  • Patent number: 10919922
    Abstract: Antiviral compounds comprising prodrugs with differing side chains derived from a tyrosine substance in the form of a tyrosine amide in which the amide substituent side chain is an alkyl ether, thioether, or alkene. Embodiments of the compounds have a range of effective lipophilicity values allowing variation in aqueous solubility, oral bioavailability, cell permeability and in vivo activation properties. The embodiments have promoieties derived from a single amino acid, which are expected to have low toxicity. The features described above also make possible a novel “precision medicine” approach to treatment of viral infections, whereby the prodrug variations can be exploited to match optimal activation of the prodrug to a given patient or strain of virus.
    Type: Grant
    Filed: October 31, 2017
    Date of Patent: February 16, 2021
    Assignee: University of Southern California
    Inventors: Charles E. McKenna, Boris A. Kashemirov, Jaijun Fan, Jinglei Lyu
  • Patent number: 10906929
    Abstract: This invention relates to derivatives of cladribine of Formula (I). The compounds are phosphoramidate derivatives in which the phosphoramidate moiety is situated on the 3?-hydroxyl group of cladribine. The invention also relates to pharmaceutical formulations of the cladribine derivatives and their use in methods of treatment. The compounds are useful in the treatment of cancer.
    Type: Grant
    Filed: May 31, 2017
    Date of Patent: February 2, 2021
    Assignee: NuCana plc
    Inventors: Hugh Griffith, Michaela Serpi, Magdalena Slusarczyk, Christopher McGuigan
  • Patent number: 10906928
    Abstract: A hemi-sulfate salt of the structure: to treat a host infected with hepatitis C, as well as pharmaceutical compositions and dosage forms, including solid dosage forms, thereof.
    Type: Grant
    Filed: November 18, 2019
    Date of Patent: February 2, 2021
    Assignee: Atea Pharmaceuticals, Inc.
    Inventors: Adel Moussa, Jean-Pierre Sommadossi
  • Patent number: 10744149
    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: March 18, 2019
    Date of Patent: August 18, 2020
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Lisa Ruderman Chen, Simona Skerjanec, Dawn Bell, Jayne Prats, Meredith Todd
  • Patent number: 10723753
    Abstract: Described herein are compounds of Formulae (I)-(II), and pharmaceutically acceptable salts, and pharmaceutical compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases such as cancers (e.g., lung cancer, large bowel cancer, pancreas cancer, biliary tract cancer, or endometrial cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases in a subject.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: July 28, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael Gray, Sang Min Lim, Hwan Geun Choi, Kenneth Dale Westover, Matthew Meyerson
  • Patent number: 10716766
    Abstract: A method of treating a disease state or condition in humans via topical brainstem afferent stimulation therapy via the administration of a cannabinoid drug(s) to the back of the neck of a human patient to provide regional neuro-affective therapy is disclosed. In certain preferred embodiments, the cannabinoid drug(s) are not psychoactive or substantially not psychoactive. In certain embodiments, the cannabinoid drug(s) are incorporated into a pharmaceutically acceptable topical carrier, e.g., a cream. In certain preferred embodiments, the cannabinoid drug(s) comprises cannabidiol.
    Type: Grant
    Filed: March 2, 2016
    Date of Patent: July 21, 2020
    Assignee: AfGin Pharma, LLC
    Inventor: Ronald Aung-Din
  • Patent number: 10702479
    Abstract: The invention relates to pharmaceutical formulation in form of a film-coating tablet comprising sembragiline or a salt thereof.
    Type: Grant
    Filed: September 26, 2017
    Date of Patent: July 7, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Zoltan Mathe, Lene Maurer, Valérie Verhoeven
  • Patent number: 10683321
    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 4?-OR nucleosides of Formula I: or a pharmaceutically acceptable salt thereof, wherein Base, PD, R, Z1, Z2, Z3, and Z4 are as defined herein.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: June 16, 2020
    Assignee: Idenix Pharmaceuticals LLC
    Inventors: David Dukhan, Cyril B. Dousson, Adel M. Moussa, Benjamin Alexander Mayes, Alistair James Stewart
  • Patent number: 10654883
    Abstract: The present invention relates to inorganic salts of nicotinic acid mononucleotides and compositions of Formula I, useful in the treatment of disorders and diseases associated with deficiencies in NAD+: wherein A, M1, M2, k, R1, R2, and R3 are as described herein.
    Type: Grant
    Filed: April 3, 2019
    Date of Patent: May 19, 2020
    Assignees: Jumpstart Fertility Pty Ltd, Life Biosciences, Inc.
    Inventors: Michel Wathier, Roland Dolle, Sebastian Mario Marcuccio, Rohan David Joyce, Simon Tucker
  • Patent number: 10654884
    Abstract: Provided are novel purine nucleoside/nucleotide analogues compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are inhibitors of CD73 and are useful in the treatment of cancer.
    Type: Grant
    Filed: April 23, 2015
    Date of Patent: May 19, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Salvacion Cacatian, David A. Claremon, Lanqi Jia, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Yajun Zheng
  • Patent number: 10596094
    Abstract: The present invention provides compositions and methods for reducing skin pigmentation. The invention comprises inhibitors of sialyltransferase, inhibitors of oligosaccharide formation or oligosaccharide activity, and methods of using such inhibitors. In certain embodiments, the invention comprises inhibiting the formation and/or activity of Neu5Ac(?2,6)Gal/GalNAc-containing oligosaccharides.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: March 24, 2020
    Assignee: YALE UNIVERSITY
    Inventor: John Mason Pawelek
  • Patent number: 10570167
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: February 25, 2020
    Assignee: Calithera Biosciences, Inc.
    Inventors: Roland J. Billedeau, Jim Li, Lijing Chen
  • Patent number: 10428105
    Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent, and methods of using the compounds and compositions for treatment of viral infections, especially HRV.
    Type: Grant
    Filed: May 8, 2018
    Date of Patent: October 1, 2019
    Assignee: Novartis AG
    Inventors: Martijn Fenaux, Oliver Saunders, Fumiaki Yokokawa, Weidong Zhong
  • Patent number: 10385091
    Abstract: The invention relates to compositions, methods, kits, and assays related to the use and/or exploitation of isomers of cGAMP as well as the structure of the enzyme cGAS.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: August 20, 2019
    Assignees: Memorial Sloan Kettering Cancer Center, The Rockefeller University, Rutgers, The State University of New Jersey, University of Bonn
    Inventors: Dinshaw J. Patel, Thomas Tuschl, Manuel Ascano, Jr., Yang Wu, Yizhou Liu, Winfried Barchet, Gunther Hartmann, Thomas Zillinger, Roger Jones, Barbara L. Gaffney, Pu Gao
  • Patent number: 10335412
    Abstract: The present invention relates to adenine which is useful to activate AMP-activated protein kinase (AMPK) and the use of adenine in the prevention or treatment of conditions or disease and thereby prevent or treat conditions or diseases which can be ameliorated by AMPK in a mammal.
    Type: Grant
    Filed: April 10, 2013
    Date of Patent: July 2, 2019
    Assignee: ENERGENESIS BIOMEDICAL CO., LTD
    Inventors: Han-Min Chen, Cheng-Yi Kuo, Chun-Fang Huang, Jiun-Tsai Lin
  • Patent number: 10160779
    Abstract: A process for preparing a compound of formula (I) or a salt thereof, the process comprising providing a compound of formula (III) wherein PG is an inert electron withdrawing hydroxyl protecting group, reacting the compound of formula (III) with a fluorinating agent, obtaining a compound of formula (II) and deprotecting the compound of formula (II).
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: December 25, 2018
    Assignee: Sandoz AG
    Inventors: Olga Schöne, Thorsten Wilhelm
  • Patent number: 10143652
    Abstract: Provided herein are methods for preparing liposomes and uses thereof. In certain embodiments, liposomes are prepared without using heat, organic solvents, proteins, and/or inorganic salts in the process. In certain embodiments, the liposomal preparation contains one or more active agents. In certain embodiments, the liposomal preparations are used in the treatment of diseases or disorders.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: December 4, 2018
    Assignee: CuriRx Inc.
    Inventors: Indu Javeri, Kaliappanadar Nellaiappan
  • Patent number: 10111904
    Abstract: Sterile micron-sized gold particles contained in capped vials, a kit of part including the vial and a liquid capable of suspending the particles, as well as their preparation, medical devices or medicaments prepared by their preparation as well as uses thereof in treating inflammation. Also, gold coated implants preferably for use in combination with the medical devices.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: October 30, 2018
    Assignee: Berlock ApS
    Inventor: Gorm Danscher
  • Patent number: 10092590
    Abstract: The present invention provides a composition comprising HMB and ATP. Methods of administering HMB and ATP to an animal are also described. HMB and ATP are administered to increase power and strength. The combination of HMB and ATP together has a synergistic effect, which results in a surprising and unexpected level of improvement in power and strength. HMB and ATP are also administered to increase lean body mass and muscle hypertrophy and to prevent typical declines in performance that are characteristic of overreaching.
    Type: Grant
    Filed: September 10, 2013
    Date of Patent: October 9, 2018
    Assignee: Metabolic Technologies, Inc.
    Inventors: Shawn Baier, Larry Kolb, John Rathmacher
  • Patent number: 10092649
    Abstract: The application discloses nucleoside derivatives of Formula I as inhibitors of Influenza RNA replication. In particular, the application discloses the use of purine and pyrimidine nucleoside derivatives of Formula I as inhibitors of Influenza RNA replication and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: October 9, 2018
    Assignee: Riboscience LLC
    Inventors: Mark Smith, Klaus G. Klumpp
  • Patent number: 10086009
    Abstract: This invention provides methods of enhancing brain development; increasing or enhancing intelligence; increasing or enhancing synthesis and levels of phospholipids, synapses, synaptic proteins, and synaptic membranes by a neural cell or brain cell, comprising contacting a subject or a pregnant or nursing mother thereof with a composition comprising an omega-3 fatty acid, an omega-6 fatty acid, and/or uridine, a metabolic precursor thereof, or a combination thereof.
    Type: Grant
    Filed: May 23, 2006
    Date of Patent: October 2, 2018
    Assignee: MASSACHUSETTS INSTITUTE OF TECHNOLOGIES
    Inventors: Richard J. Wurtman, Ingrid Richardson
  • Patent number: 10080784
    Abstract: The use of a purine nucleoside phosphorylase or nucleoside hydrolase or a vector encoding expression of one of these enzymes is detailed along with the use of a prodrug cleaved by the purine nucleoside phosphorylase or nucleoside hydrolase for the preparation of a direct injection inhibition of replicating or non-replicating targeted cells. The targeted cells do not normally express the introduced purine nucleoside phosphorylase or nucleoside hydrolase. The enzyme and prodrug are amenable to intermixing and injection as a single dose or as separate injection or administration to the targeted cells. The substance and prodrug efficacy are enhanced through exposure of the targeted cells to X-ray radiation. Administration of a prodrug regardless of administration route to the targeted cells is effective in combination with X-ray radiation therapy to kill or inhibit function of the targeted cells.
    Type: Grant
    Filed: February 20, 2012
    Date of Patent: September 25, 2018
    Assignees: SOUTHERN RESEARCH INSTITUTE, THE UAB RESEARCH FOUNDATION
    Inventors: William B. Parker, Eric J. Sorscher
  • Patent number: 10039780
    Abstract: The present invention relates to high purity cangrelor, pharmaceutical formulations comprising high purity cangrelor as an active ingredient, methods for preparing such compounds and formulations, and methods for using the pharmaceutical formulations in the inhibition of platelet activation and aggregation.
    Type: Grant
    Filed: July 7, 2017
    Date of Patent: August 7, 2018
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Panna Dutta, Adel Rafai Far, Min Ding, Rajeshwar Motheram
  • Patent number: 10028941
    Abstract: A pharmaceutical dosage system comprising (a) an effective amount of one or more of Doxylamine, an analog thereof, a derivative thereof, a prodrug thereof, a metabolite thereof and/or a salt thereof; (b) an effective amount of one or more of (i) Pyridoxine, (ii) an analog thereof, (iii) a derivative thereof, (iv) a prodrug thereof, (v) a metabolite thereof and (vi) a salt of any of (i)-(v); and (c) an effective amount of one or more compounds of formula (I) wherein R is H, PO3 or. The system exhibits an improved pharmacokinetic profile relative to the current Diclectin®/Diclegis® formulation and is useful for example for the alleviation of the symptoms of nausea and vomiting, for example in the case of nausea and vomiting of pregnancy (NVP).
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: July 24, 2018
    Assignee: DUCHESNAY INC.
    Inventors: Manon Vranderick, Jean-Luc St-Onge, Michele Gallo, Éric Gervais
  • Patent number: 9988416
    Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent, and methods of using the compounds and compositions for treatment of viral infections, especially HRV.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: June 5, 2018
    Assignee: Novartis AG
    Inventors: Martijn Fenaux, Oliver Saunders, Fumiaki Yokokawa, Weidong Zhong
  • Patent number: 9872875
    Abstract: A method for treating viral infection includes administering to a subject in need thereof a composition containing P2X receptor antagonists. The methods may achieve preventive or therapeutic effect on hand foot and mouth disease by inhibiting viruses. The P2X receptor antagonists can inhibit infection by a positive-sense single-stranded RNA picornavirus. The virus may be an enterovirus or a Coxsackie virus, such as human enterovirus 71. The P2X receptor antagonist may be PPADS, iso-PPADS, PPNDS, Suramin, NF023, TNP-ATP, NF279, NF157, Evans Blue, an analog thereof, a derivative thereof, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: January 23, 2018
    Assignee: Honz Pharmaceutical Co., Ltd.
    Inventors: Altmeyer Ralf, Peijun Ren
  • Patent number: 9700575
    Abstract: The present invention relates to high purity cangrelor, pharmaceutical formulations comprising high purity cangrelor as an active ingredient, methods for preparing such compounds and formulations, and methods for using the pharmaceutical formulations in the inhibition of platelet activation and aggregation.
    Type: Grant
    Filed: June 21, 2016
    Date of Patent: July 11, 2017
    Assignee: Chiesi Farmaceutici, S.P.A.
    Inventors: Panna Dutta, Adel Rafai Far, Min Ding, Rajeshwar Motheram
  • Patent number: 9644039
    Abstract: Compositions and methods of making a modified polyhydroxylated polymer comprising a polyhydroxylated polymer having reversibly modified hydroxyl groups, whereby the hydroxyl groups are modified by an acid-catalyzed reaction between a polydroxylated polymer and a reagent such as acetals, aldehydes, vinyl ethers and ketones such that the modified polyhydroxylated polymers become insoluble in water but freely soluble in common organic solvents allowing for the facile preparation of acid-sensitive materials. Materials made from these polymers can be made to degrade in a pH-dependent manner. Both hydrophobic and hydrophilic cargoes were successfully loaded into particles made from the present polymers using single and double emulsion techniques, respectively. Due to its ease of preparation, processability, pH-sensitivity, and biocompatibility, of the present modified polyhydroxylated polymers should find use in numerous drug delivery applications.
    Type: Grant
    Filed: January 10, 2011
    Date of Patent: May 9, 2017
    Assignee: The Regents of the University of California
    Inventors: Jean M. J. Frechet, Eric M. Bachelder, Tristan T. Beaudette, Kyle E. Broaders
  • Patent number: 9605018
    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: Grant
    Filed: January 29, 2015
    Date of Patent: March 28, 2017
    Assignee: Alios BioPharma, Inc.
    Inventors: Guangyi Wang, Leonid Beigelman
  • Patent number: 9579333
    Abstract: A process is provided for protecting a primate host from a self-replicating infection by an immunodeficiency retrovirus. Protection is achieved by administering to the primate host a combination of a pharmaceutically effective amount of a nucleoside reverse transcriptase inhibitor and a pharmaceutically effective amount of a nucleotide reverse transcriptase inhibitor prior to exposure to the immunodeficiency retrovirus. The administration is effective if provided in a single dose within 24 hours of the exposure. A regime of regular daily doses is also effective in providing protection against an immunodeficiency retrovirus becoming self-replicating after infecting a primate host.
    Type: Grant
    Filed: April 6, 2015
    Date of Patent: February 28, 2017
    Assignee: THE UNITED STATES OF AMERICA, as represented by the Secretary, Department of Health and Human Services
    Inventors: Walid Heneine, Thomas M. Folks, Robert Janssen, Ronald A. Otten, Jose Gerardo Garcia Lerma
  • Patent number: 9579332
    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: Grant
    Filed: October 17, 2012
    Date of Patent: February 28, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Constantine G. Boojamra, Kuei-Ying Lin, Richard L. Mackman, David Y. Markevitch, Oleg V. Petrakovsky, Adrian S. Ray, Lijun Zhang
  • Patent number: 9512154
    Abstract: The present invention discloses 18FDG conjugated positron emission tomography (PET) imaging agents. In particular, the present invention discloses a cancer specific 18FDG multimeric PET imaging agents.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: December 6, 2016
    Inventors: Kumar Ranjan Bhushan, Preeti Misra
  • Patent number: 9493502
    Abstract: The present invention relates to the compounds of the formulae (I) and (I-1) and the process for preparing the same, uses of the compounds for the treatment of diseases associated with platelet aggregation and in the manufacture of a medicament for the treatment of diseases associated with platelet aggregation, and relates to a pharmaceutical composition and a pharmaceutical formulation containing the compounds, wherein the definitions of R1, R2, R3 and R2a in the formulae are the same as those in the description.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: November 15, 2016
    Assignee: Beijing KBD Pharmaceuticals Co., Ltd.
    Inventors: Hongguang Du, Guocheng Liu, Zhongren Ding, Shuming Wang
  • Patent number: 9447132
    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
  • Patent number: 9439921
    Abstract: The present invention relates to high purity cangrelor, pharmaceutical formulations comprising high purity cangrelor as an active ingredient, methods for preparing such compounds and formulations, and methods for using the pharmaceutical formulations in the inhibition of platelet activation and aggregation.
    Type: Grant
    Filed: February 22, 2016
    Date of Patent: September 13, 2016
    Assignee: THE MEDICINES COMPANY
    Inventors: Panna Dutta, Adel Rafai Far, Min Ding, Rajeshwar Motheram
  • Patent number: 9428829
    Abstract: A method of forming a high-quality graphene layer including forming a board layer; forming a stress reduction layer on the board layer; forming a metal catalyst layer on the stress reduction layer, the metal catalyst layer functioning as a catalyst for forming the graphene layer; and growing a graphene layer on the metal catalyst layer. The stress reduction layer reduces the stress of the metal thin film, thus, improving crystallinity and surface roughness of the metal thin film, and thereby effectively forming a high-quality graphene layer.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: August 30, 2016
    Assignee: Korea Advanced Institute of Science and Technology
    Inventors: Byung Jin Cho, Jeong Hun Mun
  • Patent number: 9381206
    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 process and intermediates useful for preparing such salts.
    Type: Grant
    Filed: December 29, 2014
    Date of Patent: July 5, 2016
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Benjamin R. Graetz, Richard Polniaszek
  • Patent number: 9370569
    Abstract: The application discloses nucleoside derivatives of Formula I as inhibitors of Influenza RNA replication. In particular, the application discloses the use of purine and pyrimidine nucleoside derivatives of Formula I as inhibitors of Influenza RNA replication and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: June 21, 2016
    Assignee: Riboscience LLC
    Inventors: Mark Smith, Klaus G. Klumpp
  • Patent number: 9295687
    Abstract: The present invention relates to high purity cangrelor, pharmaceutical formulations comprising high purity cangrelor as an active ingredient, methods for preparing such compounds and formulations, and methods for using the pharmaceutical formulations in the inhibition of platelet activation and aggregation.
    Type: Grant
    Filed: July 10, 2015
    Date of Patent: March 29, 2016
    Assignee: THE MEDICINES COMPANY
    Inventors: Panna Dutta, Adel Rafai Far, Min Ding, Rajeshwar Motheram
  • Patent number: 9278990
    Abstract: Disclosed herein are phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs and thiohosphates (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, with the phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs and thiophosphates.
    Type: Grant
    Filed: October 21, 2014
    Date of Patent: March 8, 2016
    Assignee: Alios BioPharma, Inc.
    Inventors: David Bernard Smith, Jerome Deval, Natalia Dyatkina, Leonid Beigelman, Guangyi Wang
  • Patent number: 9221868
    Abstract: The disclosure provides particular uridine di- and tri-phosphate compounds of Formula I, and pharmaceutical compositions thereof. The definitions of variables such as R, Y, B, m, Z1, Z2, and Z3 are as provided in the disclosure. 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: Grant
    Filed: December 1, 2011
    Date of Patent: December 29, 2015
    Assignees: BAR-ILAN UNIVERSITY, UNIVERSIDAD COMPLUTENSE DE MADRID
    Inventors: Bilha Fischer, Jesus Jeronimo Pintor, Shay Elyahu, Tamar Ginsburg-Shmuel
  • Patent number: 9125928
    Abstract: An object of the present invention is to provide an agent for suppressing the formation of skin cells induced by exposure to light such as ultraviolet light. The object is achieved by using a purine nucleic acid for suppressing the formation of abnormal skin cells caused by exposure to light.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: September 8, 2015
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Mitsuaki Kawamura, Shigeo Shinohara, Fumiki Harano, Akihiro Aoki, Eri Ueno
  • Patent number: 9120820
    Abstract: Assay methods may generally comprise forming homogeneous assay mixtures comprising target SAM-utilizing protein, fluorescent detection analyte, and test compound, incubating, and measuring FP or TR-FRET signal emitted in order to determine a measure of test compound-SAM -utilizing protein binding. Assay mixtures comprise a SAM-utilizing protein, and a fluorescent detection analyte that binds with the SAM-utilizing protein in the absence of test compound. Assay mixtures may further comprise a test compound. Assay mixture embodiments may generate FP or TR-FRET signal properties that are a function of the inherent binding interactions of both the test compound and the detection analyte with the SAM-utilizing protein. Fluorescent detection analytes comprise a fluorophore moiety, a covalent linker moiety, and a SAM-utilizing protein ligand moiety and could be utilized in FP or TR-FRET assays to measure test compound binding.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: September 1, 2015
    Assignees: CAYMAN CHEMICAL COMPANY, INCORPORATED, THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Stephen Douglas Barrett, Daniel Austin Bochar, Levi Lynn Blazer, Fred Lawrence Ciske, Gregory William Endres, Jeffrey Keith Johnson, Gregory Scott Keyes, Ranjinder Singh Sidhu, Raymond C. Trievel, Margaret Lynn Collins
  • Publication number: 20150147306
    Abstract: The invention relates to a composition comprising NADH and D-galactose for treating a circadian rhythm disorder, in particular further comprising vitamins and/or coenzymes and/or minerals.
    Type: Application
    Filed: May 22, 2013
    Publication date: May 28, 2015
    Inventor: Jürgen Ruhlmann
  • Publication number: 20150119352
    Abstract: The invention provides a dinucleoside polyphosphate analogue, or a pharmaceutically acceptable salt thereof, for use in the inhibition (or down-regulation) of a pain, via a transducing ATP-gated P2X3 receptor, often by means of high-affinity desensitisation (HAD) mechanism.
    Type: Application
    Filed: May 24, 2013
    Publication date: April 30, 2015
    Applicant: GlobalAcornLtd.
    Inventors: Andrew David Miller, Natalya Lozovaya, Nail Burnashev, Rashid Giniatullin