Patents Examined by Brian E McDowell
  • Patent number: 10947203
    Abstract: In an aspect, the invention relates to 1,4,5-substituted 1,2,3-triazole and 1,2,4,5-substituted imidazoles having a structure represented by a formula: which are modulators the pregnane X receptor (“PXR”); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of modulating an adverse drug reaction in a mammal using the compounds and pharmaceutical compositions; methods of treatment of a disorder of uncontrolled cellular proliferation, such as a cancer, using the compounds and pharmaceutical compositions; methods of modulating pregnane X receptor activity in a mammal using the compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: November 8, 2019
    Date of Patent: March 16, 2021
    Inventors: Taosheng Chen, Wenwei Lin, Yueming Wang
  • Patent number: 10947214
    Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TLR7/8 antagonists.
    Type: Grant
    Filed: August 7, 2017
    Date of Patent: March 16, 2021
    Assignee: Merck Patent GmbH
    Inventors: Brian A. Sherer, Xiaoling Chen, Esther Cleary, Nadia Brugger
  • Patent number: 10941172
    Abstract: Described is heme iron having Chemical Formula 1 not derived from porcine blood and a method of preparing the same, and more particularly to a method of chemically preparing heme iron having Chemical Formula 1 not derived from porcine blood, a method of preparing a salt thereof, and an iron supplement containing the salt thus prepared as an active ingredient:
    Type: Grant
    Filed: December 6, 2017
    Date of Patent: March 9, 2021
    Inventors: Seong Jun Yoon, Jung In Pyo, Soon Hye Hwang, Soo Youn Jun, Sang Hyeon Kang
  • Patent number: 10919856
    Abstract: A cyclohexene compound and use thereof, which relates to the technical field of pharmaceutical chemistry is provided. The cyclohexene compound is the cyclohexene compound having a structural formula I or a pharmaceutically acceptable salt, an ester group prodrug or a stereoisomer thereof. It is verified by activity assay for influenza NA that the cyclohexene compound has a great inhibiting activity against both wild-typed and drug-resistant influenza viruses, and the inhibiting activity IC50 of some compounds against wild-typed and drug-resistant influenza viruses is lower than 5 nM, showing significant inhibiting effect on influenza viruses. This shows that the cyclohexene compound or a pharmaceutically acceptable salt or a stereoisomer thereof has superior application prospect on preparing anti-influenza drugs, thereby providing a new drug choice for treating influenza clinically.
    Type: Grant
    Filed: September 5, 2017
    Date of Patent: February 16, 2021
    Inventors: Jiancun Zhang, Kun Wang, Yan Liu, Deyao Li
  • Patent number: 10906906
    Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, the compounds of formula I: in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of central nervous system (CNS) diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the ?-opioid receptor.
    Type: Grant
    Filed: December 29, 2017
    Date of Patent: February 2, 2021
    Inventors: Peng Li, Robert Davis
  • Patent number: 10905780
    Abstract: Compounds, systems, and methods are provided for the design and assembly of a non-invasive, analyte sensing dressing. The dressing can be therapeutic. The dressing includes a sensor and a matrix. The sensor is capable of detecting analytes such as molecular oxygen, carbon dioxide, nitric oxides, dissolved analytes in plasma, and hydrogen ions. The matrix is at least partially permeable to the analyte. The device emits a detectable signal when the sensor is excited in the presence of the analyte. In one version of the dressing, the sensor includes a meso-unsubstituted metallated porphyrin that is sensitive towards oxygen. The metallated porphyrin can be excited when illuminated at a first wavelength, followed by emission of phosphorescence at a second wavelength whose intensity can be used as an indicator for oxygen concentration.
    Type: Grant
    Filed: August 3, 2018
    Date of Patent: February 2, 2021
    Assignee: The General Hospital Corporation
    Inventors: Conor L. Evans, Gabriela Apiou, Alexander J. Nichols, Emmanouil Rousakis, Zongxi Li
  • Patent number: 10906879
    Abstract: A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}acetic acid (hereinafter referred to as “Compound B”). A form-I crystal of Compound B, which shows peaks at diffraction angles (2?) of 6.4°, 8.1°, 9.5°, 10.9°, 13.2°, 15.7°, 17.0°, 19.5°, 20.3°, 21.0°, and 22.8° in a powder X-ray diffraction spectrum obtained using a Cu-K? radiation (?=1.54 ?). A form-III crystal of Compound B, which shows peaks at diffraction angles (2?) of 9.6°, 11.4°, 11.7°, 16.3°, 17.5°, 18.5°, 18.7°, 19.9°, 20.1°, 21.0°, and 24.6° in a powder X-ray diffraction spectrum obtained using a Cu-K? radiation (?=1.54 ?).
    Type: Grant
    Filed: September 27, 2018
    Date of Patent: February 2, 2021
    Inventor: Toshio Fujiwara
  • Patent number: 10889560
    Abstract: The present invention concerns 4-amino-2-pyrido-bicyclic pyrimidines of Formula (I) that function as type II topoisomerase inhibitors and their use thereof as medicaments especially in the treatment of cancer. The invention also provides a method for the manufacture of 4-amino-2-pyrido bicyclic pyrimidines of Formula (I).
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: January 12, 2021
    Inventors: Marco De Vivo, Jose Antonio Ortega Martinez, Jose Manuel Arencibia Jimenez, Anna Minarini, Claudia Sissi
  • Patent number: 10882869
    Abstract: A condensed heterocyclic compound represented by the following formula or its salt or an N-oxide thereof: wherein G1 is C(Y1); G2 is C(Y2); G3 is C(Y3); G4 is C(Y4); A4 is a nitrogen atom or C(R4); A5 is a nitrogen atom or C(R5); and n is an integer of 0, 1 or 2.
    Type: Grant
    Filed: August 20, 2019
    Date of Patent: January 5, 2021
    Inventors: Takao Kudo, Yukihiro Maizuru, Ayano Tanaka, Kenkichi Noto, Hiroto Matsui, Masaki Kobayashi
  • Patent number: 10875861
    Abstract: The invention provides a compound of formula I: or a salt thereof, wherein R2-R4 and p have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as anti-cancer agents.
    Type: Grant
    Filed: August 27, 2019
    Date of Patent: December 29, 2020
    Assignee: Rutgers, the State University of New Jersey
    Inventors: David J. Augeri, Hatem E. Sabaawy
  • Patent number: 10875863
    Abstract: The invention is a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Values for the variables are provided herein. Also included is a pharmaceutical composition comprising the compound represented by Structural Formula (I) and a pharmaceutically acceptable carrier or diluent and methods of treating a subject with cancer with the compound of Structural Formula (I).
    Type: Grant
    Filed: January 28, 2019
    Date of Patent: December 29, 2020
    Inventors: Radoslaw Laufer, Grace Ng, Richard Brokx, Heinz W. Pauls, Sze-Wan Li, Jacqueline M. Mason, Mark R. Bray
  • Patent number: 10870624
    Abstract: The present invention is a compound of the formula or a pharmaceutically acceptable salt thereof. The compounds are useful as HDAC inhibitors.
    Type: Grant
    Filed: August 2, 2017
    Date of Patent: December 22, 2020
    Assignee: Karus Therapeutics Limited
    Inventors: Stephen J. Shuttleworth, Cyrille D. Tomassi, Alexander R. L. Cecil, Somhairle MacCormick, William J. Nodes, Franck A. Silva
  • Patent number: 10865194
    Abstract: Pharmaceutical compounds are disclosed having a bicyclic-sulphonamide structure of Formula 1: wherein R1 represents an unsubstituted or a substituted heteroaryl ring; R2, R3, R4, and R5 are independently selected from hydrogen, alkyl, hydroxyalkyl, and alkyl-O-alkyl, provided that either R2 and R3, or R4 and R5 are linked or taken together to form a bridge between the carbon atoms to which R2 and R3, or R4 and R5 respectively are directly linked, whereby the N-containing ring in Formula 1 is an azabicyclo moiety. The compounds and compositions including the compounds may be used in therapy as brain-cell-death protectants, for example, in the treatment of chronic neurodegenerative diseases. The compounds are active as inhibitors of N-acylethanolamine-hydrolysing acid amidase (NAAA) and may be used for the therapeutic treatment and prevention of pain and inflammatory disorders and other disorders which benefit from the modulation of fatty acid ethanolamides, particularly palmitoylethanolamide (PEA).
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: December 15, 2020
    Inventors: Fabio Bertozzi, Tiziano Bandiera, Silvia Pontis, Angelo Reggiani, Francesca Giacomina, Paolo Di Fruscia
  • Patent number: 10857153
    Abstract: The present disclosure relates to a class of pyrimidine derivatives having immunomodulating properties that act via TLR7 which are useful in the treatment of lung cancer and other respiratory conditions. The present disclosure specifically discloses compounds having the structuree of Formula (I), and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 3, 2019
    Date of Patent: December 8, 2020
    Inventors: Tom Yao-Hsiang Wu, Andrew T. Miller
  • Patent number: 10857140
    Abstract: Provided herein, inter alia, are methods and compounds of formula (I) for inhibiting K-Ras and for treating cancer.
    Type: Grant
    Filed: May 6, 2016
    Date of Patent: December 8, 2020
    Assignees: The Regents of the University of California, Leidos Biomedical Research, Inc.
    Inventors: Frank McCormick, Adam R. Renslo, David Turner, Stephan Gysin, Anna E. Maciag, Oleg Chertov
  • Patent number: 10851112
    Abstract: Disclosed are a class of fused cyclic compounds against the HCMV virus, and use thereof in the preparation of a drugs for treating diseases associated with the HCMV virus. In particular, disclosed is the compound shown in formula (II) and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 8, 2017
    Date of Patent: December 1, 2020
    Inventors: Jian Xiong, Jingjing Wang, Wentao Wu, Haizhong Tan, Xuanjia Peng, Yang Zhang, Kevin X. Chen, Jian Li, Shuhui Chen
  • Patent number: 10854835
    Abstract: An iridium complex which has a phenylpyridine bidentate ligand containing a group represented by the following general formula (A): wherein X represents a cyano group or a halogenated alkyl group; L represents a single bond or a divalent linking group; R represents a substituent; n represents an integer of 0 to 4; * represents a binding site to a phenylpyridine bidentate ligand.
    Type: Grant
    Filed: July 1, 2019
    Date of Patent: December 1, 2020
    Inventors: Kousuke Watanabe, Yuichirou Itai
  • Patent number: 10836774
    Abstract: Described herein are bacteriochlorins comprising an annulated isocyclic ring such as a compound Formula I: or a metal conjugate thereof, wherein: R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, and Z are each as defined herein. Also described are methods and intermediates for the synthesis of bacteriochlorins comprising an annulated isocyclic ring, and methods of using such bacteriochlorins for, among other things, diagnostic and therapeutic purposes such as, e.g., luminescent compounds in flow cytometry, and/or as active agents in photodynamic therapy (PDT).
    Type: Grant
    Filed: November 27, 2017
    Date of Patent: November 17, 2020
    Assignee: North Carolina State University
    Inventors: Jonathan S. Lindsey, Shaofei Zhang
  • Patent number: 10829489
    Abstract: Compounds of the formula Ia or of the formula Ib in which X, Y, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases such as cancer.
    Type: Grant
    Filed: October 29, 2019
    Date of Patent: November 10, 2020
    Assignee: Merck Patent GmbH
    Inventor: Hans-Peter Buchstaller
  • Patent number: 10822345
    Abstract: Compounds of formula (II) or a pharmaceutically acceptable salt or solvate thereof, the medical uses thereof for diseases or medical conditions where the inhibition of the voltage-gated potassium channel Kv1.3 is beneficial, and methods for their preparation.
    Type: Grant
    Filed: March 14, 2016
    Date of Patent: November 3, 2020
    Assignee: 4SC AG
    Inventors: Stefan Tasler, Ilga Krimmelbein, Juergen Kraus, Mirko Zaja