Abstract: The present invention relates to a compound of the Formula: and pharmaceutically salts thereof. The compound of the present invention inhibits Pol?. This novel therapeutic compound is therefore useful for the treatment and/or prevention of diseases and conditions in which Pol? activity is implicated, such as, for example but not limited to, the treatment and/or prevention of cancer. The present invention also relates to pharmaceutical compositions comprising the novel therapeutic compound defined herein, to processes for synthesising the compound and to their use for the treatment of diseases and/or conditions in which Pol? activity is implicated.
Type:
Grant
Filed:
March 8, 2024
Date of Patent:
November 19, 2024
Assignee:
Breakpoint Therapeutics GmbH
Inventors:
Andrea Guerrero Corella, Stuart Robert Flanagan, Jonathan Hollick, Julien Gilbert Jacques Malassis, Matthew Raymond Smith, Ian Andrew Yule, Jonathan Mark Bentley
Abstract: Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including autoimmune diseases, inflammatory diseases, chronic inflammatory diseases, diabetes, and infectious diseases, such as lupus, Sjögren's syndrome, rheumatoid arthritis, type 1 diabetes, inflammatory bowel disease, viral diseases, and nonalcoholic steatohepatitis. The compounds can also be used to generate cells, such as immune cells, for treating the conditions.
Type:
Grant
Filed:
May 20, 2022
Date of Patent:
November 19, 2024
Assignee:
NImmune Biopharma, Inc.
Inventors:
Josep Bassaganya-Riera, Andrew Leber, Raquel Hontecillas
Abstract: Compositions and methods for the treatment of tuberculosis, as well as other mycobacterial and gram positive bacterial infections are disclosed. These compositions contain a highly potent and selective oxazolidinone encapsulated with high efficiency to maximize dosing potential of low toxicity drugs, and are stable in the presence of plasma. The compositions are long circulating and retain their encapsulated drug while in the circulation following intravenous dosing to allow for efficient accumulation at the site of the bacterial or mycobacterial infection. The high doses that can be achieved when combined with the long circulating properties and highly stable retention of the drug allow for a reduced frequency of administration when compared to daily or twice daily administrations of other drugs typically utilized to treat these infections.
Type:
Grant
Filed:
December 13, 2022
Date of Patent:
November 19, 2024
Assignee:
Akagera Medicines, Inc.
Inventors:
Daryl C. Drummond, Suresh K. Tipparaju, Charles O. Noble, Alexander Koshkaryev, Dmitri B. Kirpotin
Abstract: Described herein are MK2 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of autoimmune disorders, chronic inflammatory disorders, acute inflammatory disorders, auto-inflammatory disorders, fibrotic disorders, metabolic disorders, neoplastic disorders, and cardiovascular or cerebrovascular disorders.
Type:
Grant
Filed:
May 2, 2023
Date of Patent:
November 12, 2024
Assignee:
XinThera, Inc.
Inventors:
Robert L. Hoffman, Lynnie Trzoss, Qing Dong, Stephen W. Kaldor
Abstract: The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted benzothiazole compounds of Formula (I), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
Type:
Grant
Filed:
June 25, 2019
Date of Patent:
November 12, 2024
Assignee:
PTC THERAPEUTICS, INC.
Inventors:
Nanjing Zhang, Suresh Babu, Scott J. Barraza, Anuradha Bhattacharyya, Guangming Chen, Gary Mitchell Karp, Andrew J. Kassick, Anthony R. Mazzotti, Young-Choon Moon, Jana Narasimhan, Nadiya Sydorenko, Anthony Turpoff, Matthew G. Woll, Wuming Yan
Abstract: 6,7-Dihydrothiazolo[5,4-c]pyridines substituted in the 5-position with heterocyclic rings are positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4) and may have use in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.
Type:
Grant
Filed:
April 18, 2024
Date of Patent:
November 12, 2024
Assignee:
Vanderbilt University
Inventors:
Craig W. Lindsley, Darren W. Engers, Kayla J. Temple, Alison R. Gregro, Madeline F. Long, Anna E. Ringuette, Julie L. Engers
Abstract: Provided herein are compounds, compositions including them, and methods of modulating GPR120 activity and treating diseases mediated by GPR120 by administering such compounds and compositions.
Type:
Grant
Filed:
October 3, 2022
Date of Patent:
October 15, 2024
Assignee:
Valo Health, Inc.
Inventors:
Brian Raimundo, Elena S. Koltun, John Griffin, Eric Stangeland
Abstract: Compositions and methods for the treatment of tuberculosis, as well as other mycobacterial and gram positive bacterial infections are disclosed. These compositions contain a highly potent and selective oxazolidinone encapsulated with high efficiency to maximize dosing potential of low toxicity drugs, and are stable in the presence of plasma. The compositions are long circulating and retain their encapsulated drug while in the circulation following intravenous dosing to allow for efficient accumulation at the site of the bacterial or mycobacterial infection. The high doses that can be achieved when combined with the long circulating properties and highly stable retention of the drug allow for a reduced frequency of administration when compared to daily or twice daily administrations of other drugs typically utilized to treat these infections.
Type:
Grant
Filed:
December 1, 2022
Date of Patent:
October 15, 2024
Assignee:
Akagera Medicines, Inc.
Inventors:
Daryl C. Drummond, Suresh K. Tipparaju, Charles O. Noble, Alexander Koshkaryev, Dmitri B. Kirpotin
Abstract: The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
Type:
Grant
Filed:
May 9, 2022
Date of Patent:
October 8, 2024
Assignee:
Lighthouse Pharmaceuticals, Inc.
Inventors:
Andrei W. Konradi, Robert A. Galemmo, Jr., Stephen S. Dominy, Casey C. Lynch, Leslie J. Holsinger
Abstract: Disclosed herein are WD40 repeat domain protein 5 (WDR5) degradation/disruption compounds including a WDR5 ligand, a degradation/disruption tag, and a linker, and methods of using such compounds in the treatment of WDR5-mediated diseases.
Type:
Grant
Filed:
June 21, 2019
Date of Patent:
October 8, 2024
Assignees:
Icahn School of Medicine at Mount Sinai, The University of North Carolina at Chapel Hill
Inventors:
Jian Jin, Gang Wang, Jing Liu, Xufen Yu, Dongxu Li
Abstract: This disclosure is drawn to pyridine derivatives, compositions thereof, and associated methods, useful for inhibition of SARM1 activity and/or for treating or preventing neurological disorders.
Type:
Grant
Filed:
March 3, 2023
Date of Patent:
October 8, 2024
Assignee:
NURA BIO, INC.
Inventors:
Rao Kolluri, Christopher Michael Tegley, Liusheng Zhu, Sean Pomeroy Brown, Charles Howard Reynolds, Andrew Stewart Tasker, Cheryl A. Grice
Abstract: Compounds of formula (I), or the pharmaceutically acceptable salts and/or the solvates thereof, wherein m, n, R1, R2, R3, R4, R5, L, Ar1 and Ar2 are as defined as disclosed, which are useful as inhibitors of METTL3 (N6-adenosine-methlytransferase subunit) activity, in particular for the treatment of proliferative diseases such as cancers.
Abstract: The present disclosure provides compounds that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
Type:
Grant
Filed:
July 17, 2023
Date of Patent:
September 17, 2024
Assignees:
IMMUNESENSOR THERAPEUTICS, INC., THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
Qi Wei, Heping Shi, Matt Tschantz, Jian Qiu, Youtong Wu, Huiling Tan, Lijun Sun, Chuo Chen, Zhijian Chen
Abstract: The present disclosure relates to calixpyrrole compounds and compositions thereof. The calixpyrrole compounds are chemical groups which are located in such a manner so as to be useful for the selective extraction of specific salts. Also provided herein are compositions and methods of use thereof.
Type:
Grant
Filed:
May 23, 2019
Date of Patent:
September 3, 2024
Assignees:
Board of Regents, The University of Texas System, GYEONGSANG NATIONAL UNIVERSITY
Inventors:
Jonathan L. Sessler, Qing He, Sung Kuk Kim
Abstract: The present invention relates to a heterocyclic amide inhibiting RIP1 kinase and the use thereof, and specifically, to a compound of formula I, its pharmaceutically acceptable salts, stereoisomers, enantiomers, diastereomers, atropisomers, optical isomers, racemates, polymorphs, solvates or isotopically labeled compounds, a pharmaceutical composition comprising the compound, and the pharmaceutical use thereof. The compound is particularly effective for treatment of diseases or disorders mediated by RIP1 kinase.
Type:
Grant
Filed:
October 8, 2022
Date of Patent:
August 20, 2024
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
Type:
Grant
Filed:
June 3, 2022
Date of Patent:
August 20, 2024
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Nikolaos Papaioannou, Jeremy Mark Travins, Sarah Jocelyn Fink, John Mark Ellard, Alastair Rae
Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 5, 2024
Date of Patent:
August 6, 2024
Assignee:
SLAP Pharmaceuticals LLC
Inventors:
Sunil Paliwal, Ahmed Abdi Samatar, Lawrence Saunders Cripe
Abstract: The present disclosure relates to tri-substituted aryl and heteroaryl derivatives. pharmaceutical compositions containing them, and methods of using them, including methods for modulating autophagy or preventing, reversing, slowing or inhibiting the PI3K-AKT-MTOR pathway, and methods of treating diseases that are associated with autophagy or the PI3K-AKT-MTOR pathway.
Type:
Grant
Filed:
November 7, 2022
Date of Patent:
July 30, 2024
Assignee:
Neuropore Therapies, Inc.
Inventors:
Emily M. Stocking, Wolfgang J. Wrasidlo