Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof: which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
December 6, 2022
Date of Patent:
May 28, 2024
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Joseph D. Panarese, Samuel Bartlett, Yat Sun Or
Abstract: The invention relates to methods for decreasing adverse effects associated with solriamfetol ([R]-2-amino-3-phenylpropylcarbamate) therapy in subjects with impaired renal function. In particular, the invention provides an optimized dose escalation scheme for subjects with moderate renal impairment which results in the subjects having increased tolerance to adverse effects associated with the administration of solriamfetol. The invention also provides adjusted dosing for safe therapeutic use of solriamfetol in subjects having severe renal impairment.
Abstract: The invention relates to methods for decreasing adverse effects associated with solriamfetol ([R]-2-amino-3-phenylpropylcarbamate) therapy in subjects with impaired renal function. In particular, the invention provides an optimized dose escalation scheme for subjects with moderate renal impairment which results in the subjects having increased tolerance to adverse effects associated with the administration of solriamfetol. The invention also provides adjusted dosing for safe therapeutic use of solriamfetol in subjects having severe renal impairment.
Abstract: Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Type:
Grant
Filed:
March 19, 2022
Date of Patent:
May 14, 2024
Assignee:
Arvinas Operations, Inc.
Inventors:
Erika Marina Vieira Araujo, Michael Berlin, Hanqing Dong, Steven M. Sparks, Jing Wang, Wei Zhang
Abstract: The present invention relates to Compounds of Formula I and Ia and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, X, A and B are as defined herein. The present invention also relates to compositions comprising at least one compound of Formula I or Ia, and methods of using the compounds of Formula I or Ia for treating or preventing HIV infection in a subject.
Type:
Grant
Filed:
March 16, 2020
Date of Patent:
May 7, 2024
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Wensheng Yu, Joseph A. Kozlowski, Dane James Clausen, Jian Liu, James Fells
Abstract: The subject invention provides oligo(carbamoylated guanidine)s (OCGs) having fast and selective mycobactericidal effects via disruption of the mycobacterial membrane potential. OCGs also potentiates bedaquiline, an oxidative phosphorylation-targeting anti-TB drug. The combination of OCG and anti-TB drug can be used as an effective therapy for treating tuberculosis.
Type:
Grant
Filed:
November 10, 2023
Date of Patent:
May 7, 2024
Assignee:
THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES
Abstract: The present disclosure provides for a method of inhibiting the growth of a microorganism including contacting the microorganism with zinc porphyrin (ZnPor). The present disclosure also provides for a method of treating or preventing biofilm formation of one or more microorganisms including contacting the biofilm with zinc porphyrin (ZnPor). Further, the present disclosure provides for a method of treating a disease associated with biofilm formation in a subject including administering to the subject a composition comprising a therapeutically effective amount of ZnPor.
Abstract: The invention relates to methods for decreasing adverse effects associated with solriamfetol ([R]-2-amino-3-phenylpropylcarbamate) therapy in subjects with impaired renal function. In particular, the invention provides an optimized dose escalation scheme for subjects with moderate renal impairment which results in the subjects having increased tolerance to adverse effects associated with the administration of solriamfetol. The invention also provides adjusted dosing for safe therapeutic use of solriamfetol in subjects having severe renal impairment.
Abstract: The present disclosure relates to compounds having an improved solubility thereby increasing their bioavailability, lower dosages, etc. The target compounds, may include but are not limited to, macrophage migration inhibitory factor (MIF) inhibitors, epidermal growth factor receptor (EGRF) inhibitors, kinase inhibitors and prodrugs of alpha4 beta1 and alpha4 beta7 integrin antagonists.
Type:
Grant
Filed:
September 22, 2020
Date of Patent:
April 23, 2024
Assignee:
Rutgers, The State University of New Jersey
Abstract: A 6-(6-bromo-2-oxo-2H-chromen-3-yl)-4-(4-chlorophenyl)-2-alkoxynicotinonitrile compound, its synthesis, and its use as an antimicrobial agent.
Type:
Grant
Filed:
October 9, 2023
Date of Patent:
April 16, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
Abstract: The present invention relates to the technical field of photosensitizers, and particularly to a near-infrared nano-photosensitizer and a preparation method and use thereof. The near-infrared nano-photosensitizer in the present invention is modified by conjugation extension of the boron dipyrromethene core, achieving absorption and emission spectra close to the near-infrared region. A polyfluoroalkyl group and a polyethylene glycol group are introduced to the boron dipyrromethene structure to obtain an amphiphilic photosensitizer. By means of the strong fluorine-fluorine interaction between the polyfluoroalkyl group and the hydrophilic interaction of the polyethylene glycol group, a nano-photosensitive micelle with an ultra-low CMC value is ultimately constructed. Boron dipyrromethene is induced by fluorine-fluorine interaction to undergo J-aggregation, causing the maximum absorption peak to red-shift to the near-infrared region, beneficial to the deep phototherapy of tumors.
Type:
Grant
Filed:
January 25, 2022
Date of Patent:
April 16, 2024
Assignee:
SOOCHOW UNIVERSITY
Inventors:
Zhengqing Guo, Hui He, Mengke Shi, Han Xu, Dandan Ji, Yangyang Huang, Qiujin He
Abstract: The present technology is related to reducing or treating neurological swelling and related conditions with SUR1-TRPM4 channel inhibitors. In some embodiments, the methods include: reducing late neurological deterioration or preventing death, reducing cerebral midline shift, reducing the degree of disability in a subject, counteracting blood glucose levels in a subject receiving a SUR1-TRPM4 channel inhibitor, preventing brain swelling, monitoring liver enzyme activity along with treating injury or conditions related to CNS edema, or monitoring cardiac activity along with treating injury or conditions related to CNS edema.
Abstract: Compositions comprising fatty acid analogs are provided for treating metabolic syndrome, anemia, cancer, cardiovascular disease, diabetes, dyslipidemia, hypertension, inflammation, insulin resistance, prediabetes, fatty liver disease, steatohepatitis, iron overload, neurodegenerative diseases, including Alzheimer's disease and other forms of dementia, and other related conditions. Methods for the diagnosis and monitoring of metabolic syndrome and other conditions are also provided.
Type:
Grant
Filed:
July 17, 2020
Date of Patent:
April 9, 2024
Assignee:
EPITRACKER, INC.
Inventors:
Stephanie Venn-Watson, John Reiner, Richard Lumpkin
Abstract: Disclosed herein is a complex, a contrast agent and the method for treating a disease related to CXCR4 receptor. The complex is configured to bind the CXCR4 receptor, and is used as a medicament for diagnosis and treatment of cancers and other indications related to the CXCR4 receptor.
Type:
Grant
Filed:
December 18, 2020
Date of Patent:
April 9, 2024
Assignee:
INSTITUTE OF NUCLEAR ENERGY RESEARCH, ATOMIC ENERGY COUNCIL, EXECUTIVE YUAN, R.O.C
Abstract: An 2-benzo-[3,4-b]quinolino-[b,g]indeno[1?,2?:3,4]fluoreno-[1,2-d]oxonine-24-flouro-5,11,16,21-tetraone compound, its synthesis, and its use as an antimicrobial agent.
Type:
Grant
Filed:
November 7, 2023
Date of Patent:
April 9, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Antar Ahmed Abdelhamid Ahmed
Abstract: Provided herein are pharmaceutical compositions comprising a phosphatidylinositol 3-kinase inhibitor or a pharmaceutically acceptable form thereof, and a Bcl-2 inhibitor or a pharmaceutically acceptable form thereof. Also provided herein are methods for treating cancer comprising administration the compositions, and uses of the compositions, e.g., for the treatment of cancer.
Abstract: Provided are aminopyridine compounds and pharmaceutically acceptable compositions thereof which exhibit inhibition activity against certain mutated forms of EGFR.
Type:
Grant
Filed:
August 26, 2022
Date of Patent:
April 2, 2024
Assignees:
YUHAN CORPORATION, JANSSEN BIOTECH, INC.
Inventors:
Hyunjoo Lee, Su Bin Choi, Young Ae Yoon, Kwan Hoon Hyun, Jae Young Sim, Marian C. Bryan, Scott Kuduk, James Campbell Robertson, Jaekyoo Lee, Paresh Devidas Salgaonkar, Byung-Chul Suh, Jong Sung Koh, So Young Hwang
Abstract: Compositions and methods for treating progressive neurodegenerative diseases, and their associated symptoms by administration of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine).
Type:
Grant
Filed:
July 2, 2021
Date of Patent:
April 2, 2024
Assignee:
MediciNova, Inc.
Inventors:
Michael E. Kalafer, Kenneth W. Locke, Kazuko Matsuda, Richard E. Gammans
Abstract: Concentrated methotrexate solutions are described which are suitable for the use of an active substance in the production of a parenterally administered medicament for the treatment of inflammatory autoimmune diseases. The methotrexate is added to a pharmaceutically acceptable solvent at a concentration of more than 25 mg/ml.
Type:
Grant
Filed:
February 25, 2020
Date of Patent:
April 2, 2024
Assignee:
MEDAC GESELLSCHAFT FUER KLINISCHE SPEZIALPRAEPARARATE MBH