Patents Examined by Brenda L. Coleman
  • Saturated-ring-fused dihydropyrimidinone or dihydrotriazinone compounds and pharmaceutical use thereof
    Patent number: 11834421
    Abstract: The present invention relates to saturated-ring-fused dihydropyrimidinone or dihydrotriazinone compounds, or pharmaceutically acceptable salts having ROR? antagonist activity, pharmaceutical compositions comprising the same, and pharmaceutical use thereof. A compound of Formula [I] or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and pharmaceutical use thereof are provided: wherein each substituent is defined as defined in the description.
    Type: Grant
    Filed: May 28, 2021
    Date of Patent: December 5, 2023
    Assignee: Japan Tobacco Inc.
    Inventors: Masahiro Yokota, Noriyoshi Seki, Eiichi Watanabe, Shingo Fujioka
  • Heterocyclic compounds as pad inhibitors
    Patent number: 11833156
    Abstract: Heterocyclic compounds of Formula (I), (II), and (III) are described herein along with their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The compounds described herein, their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cancer, cystic fibrosis, asthma, multiple sclerosis and psoriasis.
    Type: Grant
    Filed: September 20, 2018
    Date of Patent: December 5, 2023
    Assignee: JUBILANT EPIPAD LLC
    Inventors: Gurulingappa Hallur, Athisayamani Jeyaraj Duraiswamy, Buchi Reddy Purra, N. V. S. K. Rao, Sridharan Rajagopal
  • Methods of preparing cell-binding agent-drug conjugates
    Patent number: 11833214
    Abstract: The present invention provides methods of preparing a cell-binding agent-cytotoxic agent conjugate comprising a cell-binding agent (CysCBA) having one or more unpaired cysteine residues covalently linked to a cytotoxic agent. Also provided are conjugates prepared by the methods described herein and pharmaceutical composition and methods of use thereof.
    Type: Grant
    Filed: March 20, 2020
    Date of Patent: December 5, 2023
    Assignee: IMMUNOGEN, INC.
    Inventors: Scott A Hilderbrand, Daniel F. Milano
  • Tridentate macrocyclic compounds
    Patent number: 11827653
    Abstract: Photoredox catalysis has emerged as a powerful strategy for C—O cross-coupling reactions. We herein report a new class of tridentate pyridinophane ligands RN3 that allow for detailed mechanistic studies of the photocatalytic C—O coupling reaction. The derived (RN3)Ni complexes are active C—O cross-coupling photocatalysts under mild conditions and without an additional photocatalyst. We also utilized the RN3 ligands to study the essential but so far putative steps involving paramagnetic Ni species in a proposed catalytic cycle: the oxidative addition of an aryl bromide to a Ni(I) species, the ligand exchange at a Ni(III) center, and the C—O reductive elimination from a Ni(III) species.
    Type: Grant
    Filed: June 6, 2022
    Date of Patent: November 28, 2023
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Liviu M. Mirica, Hanah Na
  • Hydroxamic acid derivative, method for producing same and use thereof
    Patent number: 11827612
    Abstract: The present disclosure is related to the field of enzyme inhibitors, and in particular to a hydroxamic acid derivative, a method for producing the same and use thereof. The hydroxamic acid group of the hydroxamic acid derivative can be chelated with zinc ions in the LpxC active area, and the derivative has a hydrophobic side chain which can bind to hydrophic channels in the enzyme LpxC. These guarantee that the hydroxamic acid derivative has good bactericidal activity against Gram-negative bacteria and low toxicity. The present disclosure also provides a method for producing the hydroxamic acid derivative, which requires a shorter reaction time and can provide the derivative with a high yield.
    Type: Grant
    Filed: September 16, 2020
    Date of Patent: November 28, 2023
    Assignee: INSTITUTE OF MEDICINAL BIOTECHNOLOGY, CHINESE ACADEMY OF MEDICAL SCIENCES
    Inventors: Yucheng Wang, Xuefu You, Juxian Wang, Xiaonan Du, Minghua Wang, Mei Zhu, Guoning Zhang
  • Oral formulation of clonidine and midazolam for sedation in dental procedures
    Patent number: 11826371
    Abstract: A drug composition in solid drug matrix formulation comprising clonidine, midazolam, and fentanyl. The amounts of the drug contained in the solid drug matrix are sufficient to induce sedation in preparation for a clinical procedure. When administered in the mouth, the drug ingredients are absorbed by transmucosal passage. This solid drug matrix formulation may be particularly useful in pediatric dentistry practice. Also disclosed is a method of inducing sedation in a patient by administering the solid drug matrix formulation to the patient prior to performing a clinical procedure.
    Type: Grant
    Filed: December 6, 2021
    Date of Patent: November 28, 2023
    Assignee: Therapeutic Sedation Solutions, LLC
    Inventors: Pamala Lea Wilson, James Liddell McCarley
  • Pyrazolopyridine derivative having GLP-1 receptor agonist effect
    Patent number: 11814381
    Abstract: The present invention provides the compound, 3-[(1S,2S)-1-[5-[(4S)-2,2-Dimethyloxan-4-yl]-2-[(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methylindazol-5-yl)-2-oxoimidazol-1-yl]-4-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carbonyl]indol-1-yl]-2-methylcyclopropyl]-4H-1,2,4-oxadiazol-5-one, or a pharmaceutically acceptable salt of the compound, as well as a preventative agent or a therapeutic agent for non-insulin-dependent diabetes mellitus (Type 2 diabetes) or obesity containing such compound.
    Type: Grant
    Filed: October 7, 2020
    Date of Patent: November 14, 2023
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hitoshi Yoshino, Satoshi Tsuchiya, Atsushi Matsuo, Tsutomu Sato, Masahiro Nishimoto, Kyoko Oguri, Hiroko Ogawa, Yoshikazu Nishimura, Yoshiyuki Furuta, Hirotaka Kashiwagi, Nobuyuki Hori, Takuma Kamon, Takuya Shiraishi, Shoshin Yoshida, Takahiro Kawai, Satoshi Tanida, Masahide Aoki
  • Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors
    Patent number: 11814359
    Abstract: The present disclosure relates to certain (2,S)-N-[(1,S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
    Type: Grant
    Filed: September 10, 2022
    Date of Patent: November 14, 2023
    Assignee: AstraZeneca AB
    Inventors: Hans Roland Lönn, Stephen Connolly, Steven Swallow, Staffan Po Karlsson, Carl-Johan Aurell, John Fritiof Pontén, Kevin James Doyle, Amanda Jane Van De Poël, Graham Peter Jones, David Wyn Watson, Jacqueline Anne Macritchie, Nicholas John Palmer
  • Macrocyclic compounds for the treatment of medical disorders
    Patent number: 11814391
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce excessive activation of complement.
    Type: Grant
    Filed: September 6, 2019
    Date of Patent: November 14, 2023
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Venkat Rao Gadhachanda, Kyle J. Eastman, Godwin Pais
  • Pyrazolopyridine compounds and uses thereof
    Patent number: 11795166
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
    Type: Grant
    Filed: January 7, 2021
    Date of Patent: October 24, 2023
    Assignee: Incyte Corporation
    Inventors: Oleg Vechorkin, Jun Pan, Kai Liu, Alexander Sokolsky, Anlai Wang, Hai Fen Ye, Wenqing Yao
  • Albofungin and its derivatives specifically recognize HIV-1 LTR-III G-quadruplex
    Patent number: 11787817
    Abstract: The subject invention pertains to compositions comprising albofungin and/or derivatives thereof, including, chloroalbofungin, 477-albo, 492-albo, 505-albo, 506-1-albo, 506-2-albo, 519-albo, and 562-albo. The subject invention further pertains to methods of treating a subject with HIV using albofungin and/or derivatives thereof, including, chloroalbofungin, 477-albo, 492-albo, 505-albo, 506-1-albo, 506-2-albo, 519-albo, and 562-albo.
    Type: Grant
    Filed: June 1, 2022
    Date of Patent: October 17, 2023
    Assignees: The Hong Kong University of Science and Technology, Southern Marine Science and Engineering Guangdong Laboratory (Guangzhou)
    Inventors: Peiyuan Qian, Aifang Cheng, Changdong Liu, Wenkang Ye, Guang Zhu
  • Method of treating amyotrophic lateral sclerosis
    Patent number: 11779588
    Abstract: The present invention relates to the treatment of a sporadic ALS patient with oral fausdil at a dose of 180-240 mg/day. This results in an anticipated 25-50% reduction in the average decline over at least three months as measured using the revised ALS Functional Rating Scale.
    Type: Grant
    Filed: October 15, 2021
    Date of Patent: October 10, 2023
    Assignee: Woolsey Pharmaceuticals, Inc.
    Inventors: Thomas MacAllister, Sven Jacobson
  • Benzothiazepine compounds and their use as bile acid modulators
    Patent number: 11773071
    Abstract: The invention relates to 1,5-benzothiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
    Type: Grant
    Filed: January 20, 2021
    Date of Patent: October 3, 2023
    Assignee: Albireo AB
    Inventors: Per-Göran Gillberg, Jan Mattsson, Ingemar Starke, Santosh S. Kulkarni
  • Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors
    Patent number: 11773069
    Abstract: The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
    Type: Grant
    Filed: September 9, 2022
    Date of Patent: October 3, 2023
    Assignee: AstraZeneca AB
    Inventors: Hans Roland Lönn, Stephen Connolly, Steven Swallow, Staffan Po Karlsson, Carl-Johan Aurell, John Fritiof Pontén, Kevin James Doyle, Amanda Jane Van De Poël, Graham Peter Jones, David Wyn Watson, Jaqueline Anne Macritchie, Nicholas John Palmer
  • Process for preparing levoketoconazole
    Patent number: 11760750
    Abstract: The present disclosure relates to a process for the preparing levoketoconazole, its salts, solvates, and solid-state forms thereof.
    Type: Grant
    Filed: March 9, 2023
    Date of Patent: September 19, 2023
    Assignee: Nuray Chemicals Private Limited
    Inventors: Ramasamy Venkatragavan, Senthilkumaran Paramanandam, Jayakumar Ayyamuthu, Andi Selvamani, Sengodan Manickam, Ravi Silambarasan, Murugan Arunkumar, Sorakka Pichandi Parthipan
  • Process for manufacturing 4-(2,2,3,3-tetrafluoropropyl)morpholine
    Patent number: 11760737
    Abstract: The present application relates to a novel, cost-saving and efficient process for preparing 4-(2,2,3,3-tetrafluoropropyl)morpholine which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: January 15, 2020
    Date of Patent: September 19, 2023
    Assignee: ADVERIO PHARM GmbH
    Inventors: Peter Fey, Sergii Pazenok, Christian Funke, Natalya Pavlovna Kolesnik, Olexandr Ivanovich Guzyr, Yuriy Grigorievich Shermolovich
  • Thienopyranones and furanopyranones as kinase, bromodomain, and checkpoint inhibitors
    Patent number: 11760762
    Abstract: The invention relates to compounds and methods of treating diseases including but not limited to, cancer, non-cancer proliferative disease, sepsis, autoimmune disease, viral infection, atherosclerosis. Type 1 or 2 diabetes, obesity, inflammatory disease, or Myc-dependent disorder including by modulating biological processes by the inhibition of cell cycle checkpoint targets CDKs, and/or PI3 kinase, and/or bromodomain protein binding to substrates, comprising the administration of a compound(s) of Formula 1-V1 (or pharmaceutically acceptable salts thereof) as defined herein.
    Type: Grant
    Filed: January 26, 2018
    Date of Patent: September 19, 2023
    Assignee: SignalRx Pharmaceuticals, Inc.
    Inventors: Guillermo A. Morales, Joseph R. Garlich, Donald L. Durden
  • Quinoline derivatives with other anti-viral agents
    Patent number: 11752145
    Abstract: Compositions and methods for the treatment or prophylaxis of viral and other infections (e.g., coronavirus) are provided. The compositions typically comprise a quinoline derivative and an additional anti-viral agent. Incorporations of these agents into fabrics for use as filtration devices which forestall infection is also disclosed.
    Type: Grant
    Filed: March 30, 2021
    Date of Patent: September 12, 2023
    Inventor: Sanjay Gupta
  • Treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders with Alpha5-containing GABAreceptor agonists
    Patent number: 11753412
    Abstract: Provided herein are alpha5-containing GABAA receptor agonists and pharmaceutical compositions and methods of treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders using them.
    Type: Grant
    Filed: December 15, 2020
    Date of Patent: September 12, 2023
    Assignees: UWM Research Foundation, Inc., Centre for Addiction and Mental Health, University of Belgrade—Faculty of Pharmacy
    Inventors: James M. Cook, Guanguan Li, Michael Ming-Jin Poe, Miroslav M. Savic, Etienne Sibille
  • Cyclic phosphate substituted nucleoside derivatives for the treatment of liver diseases
    Patent number: 11730748
    Abstract: The present invention relates to Compounds of Formula (I) or Formula (II): or a pharmaceutically acceptable salt, solvate or enantiomer thereof, wherein A, B, R1, R2, R3, R4, Q and V are as defined herein. The present invention also relates to pharmaceutical compositions comprising a Compound of Formula (I) or Formula (II) and to their use in therapy.
    Type: Grant
    Filed: November 24, 2020
    Date of Patent: August 22, 2023
    Assignee: MSD International GMBH
    Inventors: Cyril B. Dousson, David Dukhan, Christophe C. Parsy, Stephane L. Bogen