Patents Examined by Traviss C. McIntosh, III
  • Process for making 3-substituted 5-amino-6H-thiazolo[4,5-d]pyrimidine-2, 7-dione compounds useful for the treatment of virus infection
    Patent number: 11180525
    Abstract: The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: April 13, 2020
    Date of Patent: November 23, 2021
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Dongdong Chen, Song Feng, Lu Gao, Chao Li, Baoxia Wang, Lisha Wang, Hongying Yun, Xiufang Zheng
  • DNMT inhibitor as solid tumor therapeutic drug
    Patent number: 11173174
    Abstract: [Problem] To provide, in place of injected agents (such as Vidaza® and Dacogen®) clinically used as therapeutic drugs for high-risk myelodysplastic syndromes, a medicine as a therapeutic drug or a prophylactic drug for various advanced solid tumors, said medicine having high stability with respect to cytidine deaminase which is a hydrolytic metabolic enzyme, being absorbed into the body even by oral administration, and having an effect of being integrated into a nucleic acid biosynthetic route and inhibiting DNA methyltransferases, i.e., DNMTs. [Solution] The aforementioned problem is solved by a novel compound represented by formula (I). (In the formula, R is a hydroxyl group or a hydrogen atom, and R1 and R2 are each a benzyl group that may have a substituent.
    Type: Grant
    Filed: April 24, 2018
    Date of Patent: November 16, 2021
    Assignee: Ohara Pharmaceutical Co., Ltd.
    Inventors: Sako Magoichi, Toshikazu Ushijima, Naoko Hattori
  • Method for synthesizing ribonucleic acid H-phosphonate monomer, and oligonucleotide synthesis in which said monomer is used
    Patent number: 11174279
    Abstract: The present invention pertains to a method for synthesizing a ribonucleic acid H-phosphonate monomer, and a method for performing oligonucleotide synthesis in which said monomer is used. The present invention pertains to a method for manufacturing an inexpensively manufacturable H-phosphonate nucleoside derivative in which selective protection is provided to position 2? of a ribonucleoside monomer required in RNA oligonucleotide synthesis. The present invention is characterized in that: hydroxyl groups in position 2? and position 3?, which have slightly different reactivity, are caused to react with an aromatic acyl halide at low temperature to selectively esterify position 2?; and subsequently the hydroxyl group at position 3? in one pot is captured by a phosphityl group to prevent position 2? and position 3? transfer of the acyl group.
    Type: Grant
    Filed: June 20, 2017
    Date of Patent: November 16, 2021
    Assignees: NATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGY, GeneDesign, Inc.
    Inventors: Satoshi Inoue, Kohei Himeno, Hirokazu Nankai, Mutsuo Tanaka, Teiichi Murakami
  • Thermally-cleavable protecting and linker groups
    Patent number: 11161869
    Abstract: The present invention relates to chemical linkers and protecting groups, compounds and compositions containing the chemical linkers or protecting groups, and intermediates and processes that can be used to prepare them. The chemical linkers and protecting groups are based on pyrrolidine and piperidine activating groups, which undergo intramolecular cyclisation upon heating with release of carbon dioxide, thereby releasing the organic compound from a substrate. In particular, those chemical linkers and protecting groups are useful in the solid phase synthesis of oligonucleotides according to the following representative schemes.
    Type: Grant
    Filed: April 12, 2018
    Date of Patent: November 2, 2021
    Assignee: Evonetix Ltd.
    Inventors: Stuart Richard Crosby, Mathew Jennison, Joseph Brennan
  • 2?3?-cyclic dinucleotides
    Patent number: 11149052
    Abstract: The present disclosure relates to 2?3?-cyclic dinucleotides modified with a 2?- or 3?-phosphonoalkyl bond and derivatives thereof, that can modulate the activity of the STING adaptor protein.
    Type: Grant
    Filed: April 4, 2019
    Date of Patent: October 19, 2021
    Assignee: INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.
    Inventors: Gabriel Birkus, Ondrej Pav, Ivan Rosenberg, Ondrej Simak
  • Substituted nucleosides, nucleotides and analogs thereof
    Patent number: 11149049
    Abstract: Disclosed herein are compounds of the Formula (I) and pharmaceutically acceptable salts thereof: (I) where the variables in Formula (I) are described herein. Methods of synthesizing such compounds and methods of using them to treat diseases and/or conditions such as a Picornaviridae, Flaviviridae, Filoviridae, Pneumoviridae and/or Coronaviridae viral infections are also disclosed.
    Type: Grant
    Filed: September 18, 2018
    Date of Patent: October 19, 2021
    Assignee: JANSSEN BIOPHARMA, INC.
    Inventors: Leonid Beigelman, Jerome Deval, Marija Prhavc
  • N4-hydroxycytidine and derivatives and anti-viral uses related thereto
    Patent number: 11147826
    Abstract: This disclosure relates to certain N4-hydroxycytidine derivatives, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to the treatment or prophylaxis of viral infections, such as Eastern, Western, and Venezuelan Equine Encephalitis (EEE, WEE and VEE, respectively), Chikungunya fever (CHIK), Ebola, Influenza, RSV, and Zika virus infection with the disclosed compounds.
    Type: Grant
    Filed: December 7, 2018
    Date of Patent: October 19, 2021
    Assignee: Emory University
    Inventors: George R. Painter, Gregory R. Bluemling, Michael G. Natchus, David Guthrie
  • Lipophosphonoxins of second generation, and their use
    Patent number: 11135237
    Abstract: Lipophosphonoxins of general Formula I are described, in which R1 is C8-C22, preferably C10-C18 and more preferably C12-C16 alkyl, or hexadecyloxypropyl, tetradecyloxypropyl, tetradecyloxyethyl or hexadecyloxyethyl, R2 is uracil, thymine, or cytosine, and R3 is selected from a group which contains compounds of general formulas II and III.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: October 5, 2021
    Assignees: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., TRIOS, SPOL. S R.O.
    Inventors: Dominik Rejman, Radek Pohl, Eva Zbornikova, Libor Krasny, Tomas Latal, Milan Kolar
  • Uridine nucleoside derivatives, compositions and methods of use
    Patent number: 11124536
    Abstract: This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside 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, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.
    Type: Grant
    Filed: January 27, 2020
    Date of Patent: September 21, 2021
    Assignee: Tufts University
    Inventors: Philip G. Haydon, Jinbo Lee
  • Lincosamide antibiotics and uses thereof
    Patent number: 11124534
    Abstract: Provided are lincosamide compounds for the treatment of infectious diseases. The lincosamides described herein are modified at the amino acid (southern) region. The lincosamides may have further modification at the C-1 and C-7 positions of the aminooctose (northern) region, thus distinguishing them from lincomycin and clindamycin. Also provided are methods for preparing the lincosamide compounds, pharmaceutical compositions comprising the lincosamide compounds, and methods of treating infectious diseases using the disclosed lincosamide compounds.
    Type: Grant
    Filed: August 10, 2018
    Date of Patent: September 21, 2021
    Assignee: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, Matthew James Mitcheltree, Katherine J. Silvestre
  • Antibacterial aminoglycoside analogs
    Patent number: 11117915
    Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R8 and R9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: November 8, 2019
    Date of Patent: September 14, 2021
    Assignee: CIPLA USA, INC.
    Inventors: James Bradley Aggen, Adam Aaron Goldblum, Martin Sheringham Linsell, Paola Dozzo, Heinz Ernst Moser, Darin James Hildebrandt, Micah James Gliedt
  • Carbohydrate-based surfactants
    Patent number: 11117914
    Abstract: The present invention provides carbohydrate-based surfactants and methods for producing the same. Methods for producing carbohydrate-based surfactants include using a glycosylation promoter to link a carbohydrate or its derivative to a hydrophobic compound.
    Type: Grant
    Filed: November 22, 2016
    Date of Patent: September 14, 2021
    Assignee: Arizona Board of Regents on behalf of the University of Arizona
    Inventors: Jeanne E. Pemberton, Robin L. Polt, Raina M. Maier, Ricardo Palos Pacheco
  • Methods for modulating corticosterone levels in psychologically stressed individuals
    Patent number: 11116779
    Abstract: Disclosed are methods of modulating and/or decreasing serum corticosterone levels in an individual affected by stress. Further disclosed are methods of modulating the hypothalamic pituitary adrenal response in an individual. The methods include administration of 2-fucosyl-lactose to an individual.
    Type: Grant
    Filed: August 30, 2019
    Date of Patent: September 14, 2021
    Assignee: ABBOTT LABORATORIES
    Inventors: Enrique Vazquez Hernandez, Ricardo Rueda Cabrera, Rachael Buck, Maria Ramirez Gonzalez
  • Catecholamine prodrugs for use in the treatment of Parkinson's disease
    Patent number: 11110110
    Abstract: The present invention provides compounds of formula (I) that are prodrugs of catecholamine for use in treatment of neurodegenerative diseases and disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating neurodegenerative or neuropsychiatric diseases and disorders using the compounds of the invention, in particular Parkinson's disease.
    Type: Grant
    Filed: May 12, 2020
    Date of Patent: September 7, 2021
    Assignee: H. Lundbeck A/S
    Inventors: Klaus Gjervig Jensen, Lisbet Kværnø, Morten Jørgensen, Martin Juhl
  • Process for the manufacture of (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4AR,10AR)-7-hydroxy-1- propyl-1,2,3,4,4A,5,10,10A-octahydrobenzo[g]quinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid
    Patent number: 11104697
    Abstract: The present invention relates to a process for manufacturing (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4aR,10aR)-7-hydroxy-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]guinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid with the formula (Id) below and pharmaceutically acceptable salts thereof The compound of formula (Id) is a prodrug of a catecholamine for use in treatment of neurodegenerative diseases and disorders such as Parkinson's Disease. The invention also relates to a new intermediate of said process.
    Type: Grant
    Filed: May 18, 2020
    Date of Patent: August 31, 2021
    Assignee: H. Lundbeck A/S
    Inventors: Martin Juhl, Lisbet Kværnø, Mikkel Fog Jacobsen
  • Syntheses, activities, and methods of use of dihydronicotinamide riboside derivatives
    Patent number: 11098076
    Abstract: Disclosed is a compound of formula (I): wherein R1, R2, R3, and are as defined herein. Also disclosed are methods for increasing mammalian cell NAD+ production and improving mitochondrial cell densities comprising administering to a cell the compound or a salt thereof.
    Type: Grant
    Filed: August 26, 2019
    Date of Patent: August 24, 2021
    Assignee: Cornell University
    Inventors: Anthony Sauve, Farheen Sultana Mohammed, Yue Yang
  • HPPK inhibitors useful as antibacterial agents
    Patent number: 11091509
    Abstract: The disclosure provides linked purine pterin compounds of Formula I that are novel inhibitors of HPPK, a kinase responsible for an essential step in the biosynthesis of folic acid. (Formula I) The variables, e.g., A1-A3, R1-R4, B1-B2, and L1 are defined in the disclosure. These linked purine pterin inhibitors bind to HPPK with high affinity and specificity. Pharmaceutical compositions containing the HPPK inhibitors and methods of treating a bacterial infection in a patient with one or more of the HPPK inhibitors of the disclosure are also provided.
    Type: Grant
    Filed: October 11, 2017
    Date of Patent: August 17, 2021
    Assignee: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Xinhua Ji, Genbin Shi, Gary X. Shaw
  • Pharmaceutical composition, methods for treating and uses thereof
    Patent number: 11090323
    Abstract: The present invention relates to certain SGLT-2 inhibitors for treating and/or preventing metabolic disorders, such as type 1 or type 2 diabetes mellitus or pre-diabetes, in patients with renal impairment or chronic kidney disease (CKD).
    Type: Grant
    Filed: February 28, 2019
    Date of Patent: August 17, 2021
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Uli Christian Broedl, Sreeraj Macha, Maximilian von Eynatten, Hans-Juergen Woerle
  • Glucopyranosyl derivative and use thereof
    Patent number: 11084842
    Abstract: A glucopyranosyl derivative as a sodium-dependent glucose transporters inhibitor, especially as a SGLT1 inhibitor, a pharmaceutically acceptable salt or a stereoisomer thereof, a pharmaceutical composition thereof, and the uses of the compound and pharmaceutical composition thereof in the preparation of drugs for the treatment of diabetes and diabetes-related diseases.
    Type: Grant
    Filed: January 22, 2019
    Date of Patent: August 10, 2021
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Zheng Gu, Wuyong Wu, Tong Qu, Panpan Kang, Zongyuan Zhang, Weiming Huang, Jianyu Liu, Yingjun Zhang
  • Selective inhibitors of Alpha2-containing isoforms of Na,K-ATPase and use thereof for reduction of intraocular pressure
    Patent number: 11077128
    Abstract: Provided herein are alpha2-selective Na,K-ATPase inhibitors and prodrugs thereof, characterized by having a cyclic moiety attached to a digoxin or digitoxin derivative, as well as uses thereof in lowering intraocular pressure and in treating glaucoma and heart conditions.
    Type: Grant
    Filed: April 14, 2020
    Date of Patent: August 3, 2021
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: Steven J. D. Karlish, Adriana Katz, Daniel M. Tal, Arie Marcovich