Patents Examined by Brian E McDowell
  • Patent number: 10968188
    Abstract: The present disclosure provides a compound of general Formula (I) having c-abl kinase inhibitory activity or pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the compound, and a method useful to treat or prevent neurodegenerative diseases using the compound.
    Type: Grant
    Filed: May 14, 2020
    Date of Patent: April 6, 2021
    Assignee: 1st Biotherapeutics, Inc.
    Inventors: Jinhwa Lee, Suyeon Jo, A Yeong Park, Gwibin Lee, Jae Eun Kim, Misoon Kim, Gyooseung Jung, Seung Mook Lim, Keonseung Lim, Minwoo Lee, Heekyoung Yang, Hyonam Kim, Hyeongjun Kim, Wanjun Li, Mingzhu Fan
  • Patent number: 10968235
    Abstract: The present invention relates to compounds of formula I: in which p, q, Y1, Y2, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b, R7 and R8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.
    Type: Grant
    Filed: May 21, 2019
    Date of Patent: April 6, 2021
    Assignee: NOVARTIS AG
    Inventors: Christine Hiu-Tung Chen, Zhuoliang Chen, Michael Dore, Jorge Garcia Fortanet, John William Giraldes, Rajesh Karki, Mitsunori Kato, Matthew J. LaMarche, Lawrence Blas Perez, Martin Sendzik, Troy Douglas Smith, Bakary-Barry Toure, Sarah Williams
  • Patent number: 10968183
    Abstract: Novel compounds are disclosed along with methods of inhibiting the TGF? pathway and methods of treating Idiopathic Pulmonary Fibrosis (IPF) using such compounds.
    Type: Grant
    Filed: June 7, 2019
    Date of Patent: April 6, 2021
    Inventor: Beibei Chen
  • Patent number: 10968207
    Abstract: The invention provides improved methods of synthesizing oltipraz, which result in higher overall yield and better purity of the desired product.
    Type: Grant
    Filed: April 21, 2020
    Date of Patent: April 6, 2021
    Assignee: ST IP Holding AG
    Inventor: Bomi P. Framroze
  • Patent number: 10959989
    Abstract: Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as breast cancer.
    Type: Grant
    Filed: May 5, 2020
    Date of Patent: March 30, 2021
    Assignee: Recurium IP Holdings, LLC
    Inventors: Peter Qinhua Huang, Deborah Helen Slee, Sayee Gajanan Hegde, Chad Daniel Hopkins, Kevin Duane Bunker, Joseph Robert Pinchman, Rakesh Kumar Sit
  • Patent number: 10961266
    Abstract: A chemoselective and reactive Mn(CF3-PDP) catalyst system that enables for the first time the strategic advantages of late-stage aliphatic C—H hydroxylation to be leveraged in aromatic compounds. This discovery will benefit small molecule therapeutics by enabling the rapid diversification of aromatic drugs and natural products and identification of their metabolites.
    Type: Grant
    Filed: September 12, 2019
    Date of Patent: March 30, 2021
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: M. Christina White, Jinpeng Zhao
  • Patent number: 10961447
    Abstract: A method for manufacturing a light emitting material of the constitutional formula is provided. The structure is unitary, and the formula weight is determined, and the better solubility and film formation are provided, and the thin film status is stable; it possesses a very high decomposition temperature and a lower sublimation temperature, and is easy to sublime to be light emitting material of high purity, and can be applied for small molecule organic light emitting diode. In the method for manufacturing the light emitting material, p-bromothiophenol and 4-Bromo-2-fluorobenzonitrile are employed to be starting materials, and an intermediate of the light emitting material is obtained with a series of simple reactions, and finally, the light emitting material is obtained with Ullmann reaction or Suzuki reaction, and these steps are simple and the production is high.
    Type: Grant
    Filed: January 9, 2020
    Date of Patent: March 30, 2021
    Inventors: Xianjie Li, Yuanchun Wu, Shijian Su, Yunchuan Li
  • Patent number: 10954225
    Abstract: The present disclosure provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) compounds are ligands for NR2B N-Methyl-D-aspartate (NMDA) receptor and thereby making them useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: December 9, 2019
    Date of Patent: March 23, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Imadul Islam, Srinivasan Thangathirupathy, Jayakumar Sankara Warrier, Srinivas Cheruku, Poornima Shetty, John E. Macor
  • Patent number: 10954246
    Abstract: A crystalline form of Mod. I of Formula I: And, a process for the preparation of the crystalline form and a pharmaceutical use of the crystalline form.
    Type: Grant
    Filed: October 11, 2019
    Date of Patent: March 23, 2021
    Assignee: Taizhou EOC Pharma Co., Ltd.
    Inventors: Heting Li, Deqiang Wang, Wei Chang, Hongrui Yu, Xiaoming Zou
  • Patent number: 10954257
    Abstract: The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R1, R2, R2?, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.
    Type: Grant
    Filed: June 27, 2019
    Date of Patent: March 23, 2021
    Assignees: The Johns Hopkins University, Ústav organické chemie a biochemie AV {hacek over (C)}R, v.v.i.
    Inventors: Barbara Slusher, Rana Rais, Lukas Tenora, Pavel Majer, Andrej Jancarik
  • 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: 10947225
    Abstract: This disclosure relates to phosphoinositide 3-kinases (PI3Ks) inhibitors such as N-(5-(imidazo[1,2-a]pyridin-6-yl)pyridin-3-yl)sulfonamide derivatives and uses related thereto. In certain embodiments, the disclosure relates to methods of treating PI3K associated diseases or conditions comprising administering an effective amount of a compound disclosed herein to a subject in need thereof. In certain embodiments, the subject is at risk of, exhibiting symptoms of, suffering from, or diagnosed with cancer or a hematological malignancy.
    Type: Grant
    Filed: May 11, 2017
    Date of Patent: March 16, 2021
    Assignee: Emory University
    Inventors: Qi Shi, Thomas Kaiser, John DiRaddo, James Snyder, Dennis Liotta, Zackery Dentmon
  • Patent number: 10947224
    Abstract: The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
    Type: Grant
    Filed: April 27, 2018
    Date of Patent: March 16, 2021
    Assignees: Indiana University Research and Technology Corporation, Assembly Biosciences, Inc.
    Inventors: William W. Turner, Jr., Lee Daniel Arnold, Hans Maag, Adam Zlotnick
  • 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: 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: 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: 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