Patents Examined by Laura L. Stockton
  • 1 H-pyrazol-1-yl-thiazoles as inhibitors of lactate dehydrogenase and methods of use thereof
    Patent number: 10954228
    Abstract: The disclosure provides a compound of the formula (II) and pharmaceutically acceptable salts thereof. The variables, e.g. n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful for treating cancer and fibrosis. The compounds may be particularly useful for treating forms of cancer in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred. The disclosure also provides pharmaceutical compositions containing a compound of this formula and method for treating patients having cancer, fibrosis, or other conditions in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: March 23, 2021
    Assignees: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA, THE UAB RESEARCH FOUNDATION, VANDERBILT UNIVERSITY, NATIONAL INSTITUTES OF HEALTH, UNITED STATES DEPT. OF HEALTH AND HUMAN SERVICES
    Inventors: David J. Maloney, Alex Gregory Waterson, Ganesha Rai Bantukallu, Kyle Ryan Brimacombe, Plamen Christov, Chi V. Dang, Victor M. Darley-Usmar, Matthew Hall, Xin Hu, Ajit Jadhav, Somnath Jana, Kwangho Kim, William J. Moore, Bryan T. Mott, Leonard M. Neckers, Anton Simeonov, Gary Allen Sulikowski, Daniel Jason Urban, Shyh Ming Yang
  • Anti-angiogenesis compound
    Patent number: 10954200
    Abstract: An anti-angiogenic compound includes 4-Benzyl-N?-(2-(o-tolyloxy) acetyl) morpholine-2-carbohydrazide (BAMC), having the following structural formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 24, 2019
    Date of Patent: March 23, 2021
    Assignee: KING SAUD UNIVERSITY
    Inventors: Yasser Hussein Issa Mohammed, Nabil Ahmed Qassim Al-Zeqri, Ali Mohammed Alsalme, Fahed Ahmed Ali Alharthi, Ismail Khalil Warad, Anas Khaled Alali, Abdelkader M. Zarrouk
  • Cationic lipid
    Patent number: 10947193
    Abstract: The present invention provides a cationic lipid which is able to be used for nucleic acid delivery to the cytoplasm. A cationic lipid according to the present invention is, for example, a compound represented by formula (1) or a pharmaceutically acceptable salt thereof, wherein L1 and L2 independently represent an alkylene group having 3 to 10 carbon atoms; R1 and R2 independently represent an alkyl group having 4 to 24 carbon atoms or an alkenyl group having 4 to 24 carbon atoms; R3 represents an alkyl group having 1 to 3 carbon atoms; and X1 represents a single bond or CO—O—.
    Type: Grant
    Filed: June 10, 2020
    Date of Patent: March 16, 2021
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yuta Suzuki, Yoshinori Takahashi
  • TLR7/8 antagonists and uses thereof
    Patent number: 10947213
    Abstract: Compounds of Formula 1 and pharmaceutically acceptable compositions thereof are useful as TLR7/8 antagonists.
    Type: Grant
    Filed: April 28, 2020
    Date of Patent: March 16, 2021
    Assignee: Merck Patent GmbH
    Inventors: Brian A. Sherer, Nadia Brugger
  • Crystalline and salt forms of PPAR agonist compounds
    Patent number: 10927094
    Abstract: This disclosure relates to salt forms of compounds capable of activating PPAR? for use in drug substance and drug product development, and related compositions and methods.
    Type: Grant
    Filed: October 5, 2017
    Date of Patent: February 23, 2021
    Assignee: Mitobridge, Inc.
    Inventors: Bharat Lagu, Scott Trzaska
  • HSP90B N-terminal isoform-selective inhibitors
    Patent number: 10927076
    Abstract: The present technology provides compounds according to Formula (I) as well as compositions including such compounds useful for the treatment of cancers such as non-small cell lung cancer, bladder cancer, or colon cancer.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: February 23, 2021
    Assignee: University of Kansas
    Inventors: Brian S. J. Blagg, Caitlin Nicole Kent, Anuj Khandelwal, Sanket Jaiprakash Mishra
  • MCT4 inhibitors and uses thereof
    Patent number: 10919878
    Abstract: Presented herein are MCT4 inhibitors and uses thereof for treating cancer.
    Type: Grant
    Filed: April 25, 2019
    Date of Patent: February 16, 2021
    Assignee: CHARLES R. DREW UNIVERSITY OF MEDICINE AND SCIENCE
    Inventors: Yong Wu, Jay Vadgama, Zhimin Huang, Ke Wu
  • Hydroxycinnamic derivatives, methods and uses thereof
    Patent number: 10913757
    Abstract: The present disclosure relates to the design and development of new hydroxycinnamic derivatives that operate as mitochondriotropic antioxidants. Furthermore, this disclosure is also related to the methods and uses of the hydroxycinnamic derivatives, for example, in the field of human and animal diseases, for instance to treat mitochondrial dysfunction or mitochondrial deficiencies, and cosmetics, for instance to prevent or delay skin aging.
    Type: Grant
    Filed: October 16, 2017
    Date of Patent: February 9, 2021
    Assignees: UNIVERSIDADE DO PORTO, CENTRO DE NEUROCIÊNCIAS E BIOLOGIA CELULAR
    Inventors: Maria Fernanda Martins Borges, Paulo Jorge Gouveia Simões Da Silva Oliveira, JoséCarlos Santos Teixeira, Fernando Cagide Fagin, Ester Sofia Teixeira Benfeito
  • Benzoimidazol-1,2-yl amides as Kv7 channel activators
    Patent number: 10906877
    Abstract: Optionally substituted benzoimidazol-1,2-yl amides, such as compounds of Formula 1 or Formula 2, can be used to treat disorders associated with a Kv7 potassium channel activator. Compositions, medicaments, and dosage forms related to the treatment are also disclosed herein.
    Type: Grant
    Filed: July 2, 2019
    Date of Patent: February 2, 2021
    Assignee: Knopp Biosciences LLC
    Inventors: Lynn Resnick, George T. Topalov, Justin K. Belardi, James S. Hale, Scott S. Harried, Charles A. Flentge, David A. Mareska
  • PPAR agonists, compounds, pharmaceutical compositions, and methods of use thereof
    Patent number: 10906885
    Abstract: Provided herein are compounds and compositions useful in increasing PPAR? activity. The compounds and compositions provided herein are useful for the treatment of PPAR? related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).
    Type: Grant
    Filed: November 13, 2019
    Date of Patent: February 2, 2021
    Assignees: Mitobridge, Inc., The Salk Institute for Biological Studies
    Inventors: Michael Downes, Ronald M. Evans, Arthur Kluge, Bharat Lagu, Masanori Miura, Sunil Kumar Panigrahi, Michael Patane, Susanta Samajdar, Ramesh Senaiar, Taisuke Takahashi
  • Aryl or heteroaryl triazolone derivatives or salts thereof, or pharmaceutical compositions comprising the same
    Patent number: 10899719
    Abstract: The present technology provides aryl or heteroaryl triazolone derivatives or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and the use thereof. The aryl or heteroaryl triazolone derivatives or their pharmaceutically acceptable salts exhibit selective inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: January 26, 2021
    Assignee: YUHAN CORPORATION
    Inventors: Tae Dong Han, Hee Jae Tak, Eun Kyung Kim, Su Bin Choi, Dong Hoon Kim, Sol Park, Eun Hye Jung, Hyun Ho Choi, Tae Wang Kim, Mi Kyeong Ju, Na Ry Ha
  • Modulators of indoleamine 2,3-dioxygenase
    Patent number: 10899754
    Abstract: Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases such as chronic viral infection, chronic bacterial infections, cancer, sepsis or a neurological disorder.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: January 26, 2021
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Martha Alicia De La Rosa, Wieslaw Mieczyslaw Kazmierski, Vicente Samano
  • Salt of (R)-(-methylpyrrolidine--yl)methyl(-chloro--fluoro-[-biphenyl]--yl)carbamate and crystal form thereof
    Patent number: 10894768
    Abstract: The present invention relates to a novel salt of (R)-(1-methylpyrrolidine-3-yl)methyl(3?-chloro-4?-fluoro-[1,1?-biphenyl]-2-yl)carbamate and a crystal form thereof. Also, the novel salt of (R)-(1-methylpyrrolidine-3-yl)methyl(3?-chloro-4?-fluoro-[1,1?-biphenyl]-2-yl)carbamate and the crystal form thereof according to examples of the present invention have remarkably excellent stability, hygroscopicity and solubility.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: January 19, 2021
    Assignee: Dong-A St Co., Ltd.
    Inventors: Woo Young Kwak, Chang-Yong Shin, Punna Reddy Ullapu, Sun-Ho Choi, Min-Jung Lee, Ji-Su Kim
  • Method for the manufacturing of delmopinol
    Patent number: 10894778
    Abstract: The present invention relates to a new process for producing 2-(3-(4-propylheptyl)morpholino)ethan-1-ol with the INN name Delmopinol. The invention also relates to three key intermediates 1-chloro-4-propylhept-3-ene, 1-iodo-4-propylhept-3-ene and 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: January 19, 2021
    Assignee: Lundbeck Pharmaceuticals Italy S.P.A.
    Inventors: Carla De Faveri, Mariano Stivanello
  • Amide compounds and use thereof
    Patent number: 10882837
    Abstract: Disclosed are compounds of formula (I) below and pharmaceutically acceptable salts thereof, in which each of variables R1, R2, L, and Z is defined herein. Also disclosed are methods for reducing the glycemic level and treating glucagon-associated disorders with a compound of formula (I) or a salt thereof and a pharmaceutical composition containing same.
    Type: Grant
    Filed: January 22, 2018
    Date of Patent: January 5, 2021
    Assignee: ALPHALA CO., LTD.
    Inventors: Cheng-Ho Chung, Shi-Liang Tseng, Yung-Ning Yang, Yen-Fu Chen
  • Bicyclic heteroaryl derivatives and preparation and uses thereof
    Patent number: 10882832
    Abstract: The present invention relates compounds of Formula (A), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of dysfunctional glutamate transmission. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological and psychiatric disorders and diseases as well as cancer in humans.
    Type: Grant
    Filed: February 14, 2020
    Date of Patent: January 5, 2021
    Assignee: XW LABORATORIES INC.
    Inventors: Jia-Ning Xiang, Xuesong Xu, Wei Zhou
  • Compounds useful as immunomodulators
    Patent number: 10882844
    Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: January 5, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kap-Sun Yeung, Katharine A. Grant-Young, Li-Qiang Sun, David R. Langley, Denis R. St. Laurent, Paul M. Scola
  • Process for the preparation of a triaryl phosphate ester composition
    Patent number: 10882875
    Abstract: The invention relates to a process for the preparation of a triaryl phosphate ester composition comprising a. reacting a phosphorous oxyhalide with a (C1-C15-alkyl)phenol to obtain a first product; b. reacting the first product with phenol to obtain a triaryl phosphate ester composition; wherein in step a., for every mol of phosphorous oxyhalide 1.3 to 1.6 mols of (C1-C15-alkyl)phenol are used. The invention also relates to a triaryl phosphate ester composition obtainable according to the process of the invention.
    Type: Grant
    Filed: February 13, 2017
    Date of Patent: January 5, 2021
    Assignee: PCC ROKITA SA
    Inventors: Lukasz Gorecki, Grzegorz Janus, Uwe Storzer
  • Trifluoromethylpropanamide derivatives as HTRA1 inhibitors
    Patent number: 10870623
    Abstract: The invention provides novel compounds having the general formula (I) wherein R2, R3, R4, R5, R6, R7, R8, X, A and R11 are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: February 22, 2019
    Date of Patent: December 22, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Benoit Hornsperger, Hans Peter Maerki, Peter Mohr, Michael Reutlinger, Markus Rudolph
  • Histone deacetylase inhibitors and uses thereof
    Patent number: 10870618
    Abstract: Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of cancer.
    Type: Grant
    Filed: October 13, 2017
    Date of Patent: December 22, 2020
    Assignee: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Chung-Jen James Chou, Jesse McClure, Cheng Zhang, Elizabeth Inks