Patents Examined by Paul V. Ward
  • Salt forms and polymorphs of (r)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl)acetamido) pyridazin-3-yl)-2-fluorobutyl)-n-methyl-1H-1,2,3-triazole-4-carboxamide
    Patent number: 11603365
    Abstract: Disclosed herein is the compound (R)-1-(4-(6-(2-(4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl)acetamido) pyridazin-3-yl)-2-fluorobutyl)-N-methyl-1H-1,2,3-triazole-4-carboxamide, and salt forms and polymorphs thereof demonstrating improved exposure after oral dosing. Methods of inhibition GLS1 activity in a human or animal subject are also provided.
    Type: Grant
    Filed: December 16, 2020
    Date of Patent: March 14, 2023
    Assignee: Board of Regents, the University of Texas System
    Inventors: Philip Jones, Michael J. Soth, Jason P. Burke, Kang Le, Gang Liu
  • Topical treatment of vitiligo by a JAK inhibitor
    Patent number: 11602536
    Abstract: The present disclosure relates to topical treatment of vitiligo using ruxolitinib, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 10, 2020
    Date of Patent: March 14, 2023
    Assignee: Incyte Corporation
    Inventors: Kathleen Butler, Jim Lee, Kang Sun, Fiona Kuo, Michael Howell
  • Neuro-attenuating ketamine and norketamine compounds, derivatives thereof, and methods
    Patent number: 11603348
    Abstract: The present invention is directed to novel neuro-attenuating norketamine (NANKET) compounds according to any one of formulas (I—shown below), (I-A) and (I-B), or any of the compounds described in Tables A-D, or in any of the Examples provided herein, and pharmaceutically acceptable salts thereof, novel pharmaceutical formulations and novel methods of uses thereof. The present invention also features novel oral neuro-attenuating ketamine (NAKET) and neuro-attenuating norketamine (NANKET) modified-release pharmaceutical formulations, and novel methods of administration thereof, which ensure the steady release of a therapeutically effective amount of ketamine, norketamine, or derivatives thereof from the oral modified-release pharmaceutical formulations without neurologically toxic spikes in plasma concentration of the ketamine, norketamine, or derivatives during the release periods.
    Type: Grant
    Filed: March 9, 2021
    Date of Patent: March 14, 2023
    Assignee: Amorsa Therapeutics, Inc.
    Inventors: Alex Nivorozhkin, Nelson Landrau
  • Use of Tapinarof for the treatment of chronic plaque psoriasis
    Patent number: 11590088
    Abstract: Topical compositions and methods for using topical compositions comprising tapinarof to treat mild to moderate atopic dermatitis or plaque psoriasis are described herein. Also described are clinical endpoints for treatment of subjects diagnosed with mild to moderate atopic dermatitis, wherein about 5% to about 35% of body surface area was affected, and Investigator Global Assessment (IGA) score was greater than or equal to 3. Also described are clinical endpoints for treatment of subjects diagnosed with chronic mild to moderate plaque psoriasis for greater than or equal to 6 months, wherein about 3% to about 20% of body surface area was affected, and Physician Global Assessment (PGA) score was greater than or equal to 2.
    Type: Grant
    Filed: July 22, 2022
    Date of Patent: February 28, 2023
    Assignee: DERMAVANT SCIENCES GMBH
    Inventors: John E. Kraus, James Lee
  • Process for preparing tetrahydrocarbazole carboxamide compound
    Patent number: 11591314
    Abstract: Disclosed is a process for preparing Compound 8: comprising the step of reacting Compound of 7: wherein R is C1-8 alkyl or benzyl in the presence of a base. Also disclosed are intermediates and processes for preparing the intermediates.
    Type: Grant
    Filed: November 23, 2020
    Date of Patent: February 28, 2023
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ronald Carrasquillo, Peng Geng, Eric C. Huang, Kishta Katipally, Andrew Lee, Boguslaw Mudryk, Xinhua Qian, Thomas M. Razler, Jianji Wang, Carolyn S. Wei, Steven R. Wisniewski, Ye Zhu
  • HIF-2a small-molecule inhibitor and use thereof
    Patent number: 11591330
    Abstract: The present invention belongs to the field of diagnosis and treatment of tumors, and relates to a HIF-2? small-molecule inhibitor and use thereof in treatment of tumors such as breast cancer and ovarian cancer. The small-molecule inhibitor is a compound represented by formula (I) or a stereoisomer, pharmaceutically acceptable salt, solvate or prodrug of the compound represented by formula (I). The small-molecule inhibitor mainly inhibits the proliferation of tumor cells by inhibiting HIF-2? protein, and can also inhibit the growth of CSCs with high expression of HIF-2?. The small-molecule inhibitor can be used as a novel anti-tumor drug to completely eliminate tumors and stem cells, and has broad application prospects.
    Type: Grant
    Filed: January 25, 2019
    Date of Patent: February 28, 2023
    Assignee: China Medical University
    Inventors: Minjie Wei, Yuanyuan Yan, Miao He, Yinuo Liu, Liwen Zhang
  • Topical treatment of vitiligo by a jak inhibitor
    Patent number: 11590138
    Abstract: The present disclosure relates to topical treatment of vitiligo using ruxolitinib, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 8, 2022
    Date of Patent: February 28, 2023
    Assignee: Incyte Corporation
    Inventors: Kathleen Butler, Jim Lee, Kang Sun, Fiona Kuo, Michael Howell
  • Methods to induce targeted protein degradation through bifunctional molecules
    Patent number: 11583586
    Abstract: The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.
    Type: Grant
    Filed: September 28, 2020
    Date of Patent: February 21, 2023
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: James Bradner, Dennis Buckley, Georg Winter
  • Substituted pyridopyrimidinonyl compounds useful as T cell activators
    Patent number: 11584747
    Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: R1, R2, R4, R5, and m are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGK?) and diacylglycerol kinase zeta (DGK?), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.
    Type: Grant
    Filed: August 27, 2020
    Date of Patent: February 21, 2023
    Inventors: Upender Velaparthi, Richard E. Olson, Chetan Padmakar Darne, Bireshwar Dasgupta, Jayakumar Sankara Warrier, Hasibur Rahaman, Prasada Rao Jalagam, Saumya Roy, Denise Christine Grunenfelder
  • Harmine synthesis
    Patent number: 11578070
    Abstract: Methods for the synthesis of harmine comprise reacting harmaline with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) in the presence of a diacid catalyst. In an embodiment, the synthesis is carried out using a reaction mixture of harmaline, DDQ, THF solvent, and succinic acid; the reaction is carried out under an inert atmosphere with refluxing for a period of 4-12 hours.
    Type: Grant
    Filed: September 1, 2020
    Date of Patent: February 14, 2023
    Assignee: Ankh Life Sciences Limited
    Inventors: Gene H. Zaid, Krishna Mohan Donavalli, Rajni Verma
  • Compositions and methods for an improved antitumor immune response
    Patent number: 11576933
    Abstract: The present disclosure provides compositions and methods for improving an antitumor response against non-inflamed solid tumors. Methods of this disclosure include use of an eIF4A inhibitor to promote infiltration of antitumor lymphocytes into a non inflamed solid tumor. Methods of treating cancer associated with a non-inflamed solid tumor are also provided.
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: February 14, 2023
    Assignee: eFFECTOR Therapeutics Inc.
    Inventors: Peggy A. Thompson, Kevin R. Webster
  • Biguanide compound and use thereof
    Patent number: 11572341
    Abstract: The present invention relates to a guanidine compound and a use thereof, and more specifically, to a guanidine derivative showing excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence; a preparation method thereof; and a pharmaceutical composition containing the same as an active ingredient. Compared to existing drugs, the guanidine derivative according to the present invention shows excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence even with small doses, and may thus be effectively used in preventing or treating various cancers such as uterine cancer, breast cancer, stomach cancer, brain cancer, rectal cancer, colorectal cancer, lung cancer, skin cancer, blood cancer, liver cancer, etc., inhibiting cancer cell proliferation and cancer metastasis.
    Type: Grant
    Filed: March 17, 2020
    Date of Patent: February 7, 2023
    Assignee: ImmunoMet Therapeutics Inc.
    Inventors: Hong Woo Kim, Jae Kap Jeong, Ji Sun Lee, Hye Jin Heo, Hong Bum Lee, Ji Ae Kook, Sung Wuk Kim
  • Targeting mitochondrial fission through mDIVI-1 derivatives
    Patent number: 11559527
    Abstract: Derivatives of mDIVI-1 may be used to target and eliminate cancer stem cells. Disruption in the mitochondrial dynamics balance plays a role in cancer. Proteins involved in regulating mitochondrial dynamics represent potential targets for cancer treatment. Mitochondrial fission protein DRP1 is such a target. Derivatives of mDIVI-1 inhibit DRP1, and have demonstrated inhibition of tumorsphere forming capacity, migration and stemness-related signaling in breast cancer cells. These properties result from induction of mitochondrial oxidative stress and reduction of mitochondrial metabolism in the target cancer cells. The potency of an mDIVI-1 derivative may be dramatically increased through addition of at least one membrane-targeting signal and/or a mitochondria-targeting signal.
    Type: Grant
    Filed: December 18, 2018
    Date of Patent: January 24, 2023
    Assignee: LUNELLA BIOTECH, INC.
    Inventors: Michael P. Lisanti, Federica Sotgia
  • Compounds and methods for regulating insulin secretion
    Patent number: 11555031
    Abstract: Disclosed herein are methods for inducing insulin secretion in a glucose-dependent manner and compounds for use in these methods. The compounds may have the structure of formula I(a): wherein the substituents are as described in the description; or a pharmaceutically acceptable form thereof.
    Type: Grant
    Filed: March 19, 2018
    Date of Patent: January 17, 2023
    Assignees: The Broad Institute, Inc., The General Hospital Corporation, Instituto Carlos Slim de la Salud, A.C.
    Inventors: Sean M. Burns, Bridget K. Wagner, Amedeo Vetere
  • 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor
    Patent number: 11554120
    Abstract: Compounds according to formula I are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.
    Type: Grant
    Filed: July 31, 2019
    Date of Patent: January 17, 2023
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yam B. Poudel, Sanjeev Gangwar, Liqi He, Prasanna Sivaprakasam, Matthias Broekema, Matthew Cox, Christine M. Tarby, Qian Zhang, Naidu S. Chowdari
  • Preparation method of selenium-containing heterocyclic compounds
    Patent number: 11548862
    Abstract: A reaction of azacyclopropane derivative with elemental selenium and TMSCN to construct a selenium-containing heterocycle under metal-free and additive-free conditions is provided. The new strategy features no metal participation, no additive promotion, a wide substrate selection range and a good functional group compatibility, and provides an efficient and green approach to constructing a variety of selenium-containing heterocyclic compounds in a highly concise way.
    Type: Grant
    Filed: November 16, 2021
    Date of Patent: January 10, 2023
    Assignee: WENZHOU UNIVERSITY
    Inventors: Miaochang Liu, Liguo Lu, Chuanli Chen, Yunbing Zhou, Huayue Wu
  • Use of formin agonists in overcoming brain tumor radio- and chemo-resistance by targeting tumor microtubes
    Patent number: 11547682
    Abstract: Compositions and methods for inhibiting brain tumor proliferation, or for inhibiting or halting TM formation, invasion, and/or proliferation, or for rendering brain tumor cells sensitive to chemotherapy or radiation, or for treating a brain tumor, or for inducing cell death, involving mDia agonists such as IMM01 and IMM02, are described.
    Type: Grant
    Filed: March 10, 2020
    Date of Patent: January 10, 2023
    Assignee: The University of Toledo
    Inventors: Kathryn Eisenmann, Krista M. Pettee, Kathryn Becker
  • Peptide pharmaceuticals for treatment of NASH and other disorders
    Patent number: 11541028
    Abstract: The disclosure provides peptide products comprising a peptide covalently attached to a surfactant moiety which have improved properties, including increased duration of action and bioavailability. The peptide products are useful for treating insulin resistance, diabetes, obesity, metabolic syndrome and cardiovascular diseases, and conditions associated therewith, such as NASH and PCOS.
    Type: Grant
    Filed: January 3, 2019
    Date of Patent: January 3, 2023
    Assignee: Altimmune Inc.
    Inventor: John J Nestor
  • Compounds and compositions for the treatment of neurodegenerative and inflammatory diseases
    Patent number: 11541023
    Abstract: The invention relates to compounds exhibiting kallikrein inhibitory activity, and to compositions comprising at least one of these compounds for use in the treatment of diseases or disorders in which kallikrein activity is dysregulated, particularly neurodegenerative and inflammatory diseases.
    Type: Grant
    Filed: February 13, 2019
    Date of Patent: January 3, 2023
    Assignees: SARBONNE UNIVERSITE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE, ASSISTANCE PUBLIQUE—HÔPITAUX DE PARIS, INSTITUT DU CERVEAU ET DE LA MOELLE EPINIERE, UNIVERSITÉ DE MONTPELLIER, ECOLE NATIONALE SUPERIEURE DE CHIMIE DE MONTPELLIER
    Inventors: Chahrazade El Amri, Feryel Soualmia, Nicolas Masurier, Sabrina Aït Amiri, Brahim Nait Oumesmar, Cyrille Deboux
  • Method of preparing a composition comprising ferulic acid
    Patent number: 11541025
    Abstract: The present invention relates to a method of preparing a composition comprising ferulic acid. An aspect of the invention is a composition comprising hydrolysed wheat bran for use in the treatment or prevention of metabolic disease.
    Type: Grant
    Filed: April 3, 2018
    Date of Patent: January 3, 2023
    Assignee: Societe des Produits Nestle S.A.
    Inventor: Rachid Bel-Rhlid