Abstract: Disclosed is a compound of Formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions comprising thereof. Also disclosed is a method of treating PI3K? related disorders or diseases by using the compound disclosed herein.
Abstract: The invention relates to methods and compositions for treatment of IL13R?2-overexpressing cancer, wherein the treatment comprises administering a protein tyrosine phosphatase-1B (PTP1B) inhibitor.
Type:
Grant
Filed:
December 3, 2021
Date of Patent:
January 30, 2024
Assignee:
CONSEJO SUPERIOR DE INVESTIGACIONES CIENTÍFICAS (CSIC)
Inventors:
José Ignacio Casal Álvarez, Rubén Álvaro Bartolomé Conde
Abstract: Disclosed is a composition for preventing or treating chronic obstructive pulmonary disease containing regorafenib as an active ingredient, and particularly a pharmaceutical composition for preventing or treating chronic obstructive pulmonary disease containing regorafenib or a pharmaceutically acceptable salt thereof as an active ingredient, in which regorafenib is capable of effectively inhibiting increased immune response, which is a symptom of chronic obstructive pulmonary disease, and of improving and restoring changed lung structure and damaged lung function, and can be effectively used for the manufacture of a medicament for the prevention, amelioration, or treatment of chronic obstructive pulmonary disease, such as emphysema, chronic bronchitis, asthma, or pneumonia.
Type:
Grant
Filed:
July 6, 2022
Date of Patent:
January 23, 2024
Assignee:
Chungbuk National University Industry-Academic Cooperation Foundation
Inventors:
Eung Gook Kim, Eun Young Shin, Kwang Seok Oh
Abstract: The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof wherein X1, X2, R1, R2, R3 and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula (I) compounds as well as methods for utilizing the compounds of Formula (I) and the pharmaceutically acceptable compositions of Formula (I) compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.
Type:
Grant
Filed:
August 6, 2021
Date of Patent:
January 23, 2024
Assignee:
eFFECTOR Therapeutics Inc.
Inventors:
Justin T Ernst, Paul A. Sprengeler, Siegfried H. Reich, Samuel Sperry
Abstract: The invention provides substituted imidazo[1,2-b]pyridazine compounds, substituted imidazo[1,5-b]pyridazine compounds, related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted imidazo[1,2-b]pyridazine compounds described herein include substituted imidazo[1,2-b]pyridazine-3-carboxamide compounds and variants thereof.
Type:
Grant
Filed:
July 26, 2021
Date of Patent:
January 23, 2024
Assignee:
Bial—R&D Investments, S.A.
Inventors:
Renato T. Skerlj, Elyse Marie Josee Bourque, William J. Greenlee, Peter T. Lansbury
Abstract: The present application provides dihydropyrido[2,3-d]pyrimidone inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.
Type:
Grant
Filed:
June 10, 2021
Date of Patent:
January 9, 2024
Assignee:
Incyte Corporation
Inventors:
Alexander Sokolsky, Liangxing Wu, Wenqing Yao
Abstract: The present disclosure provides certain uracil derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.
Type:
Grant
Filed:
April 13, 2022
Date of Patent:
January 2, 2024
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Florian Paul Christian Binder, Martin Thomas Fleck, Jens Willwacher
Abstract: The invention provides novel heterocyclic compounds having the general formula (I), and pharmaceutically acceptable salts thereof, wherein X, D, R1 to R4, and R6 to R10 are as described herein. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
Type:
Grant
Filed:
July 14, 2022
Date of Patent:
January 2, 2024
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Mathis Braendlin, Sandra Marie Joseph Grall-Ulsemer, Xingchun Han, Christian Lerner, Mingming Li, Yongqiang Liu, Sébastien Schmitt, Jianhua Wang, Yongguang Wang, Min Wang, Song Yang, Chengang Zhou
Abstract: The present disclosure relates generally to methods and compositions for preventing or arresting cell death and/or inflammation.
Type:
Grant
Filed:
October 5, 2021
Date of Patent:
December 26, 2023
Assignee:
Denali Therapeutics Inc.
Inventors:
Giorgio Bonanomi, Anthony A. Estrada, Jianwen A. Feng, Brian Fox, Cinzia Maria Francini, Cheng Hu, Colin Philip Leslie, Maksim Osipov, Anantha Sudhakar, Zachary K. Sweeney, Javier De Vicente Fidalgo
Abstract: The present application is directed to compounds of Formula (I): compounds of Formula (II): compounds of Formula (III): and compounds of Formula (IV): compositions comprising these compounds and their uses, for example as medicaments and/or diagnostics. Specifically claimed are: (1) compounds containing reactive functional groups (compound of formula I), compounds containing compounds to be linked together (compound of formula II) and compounds having a reactive functional group/a compound to be linked (compound of formula IV), (2) an antibody-drug conjugate (compound of formula III), wherein the antibody is covalently attached by a linker to one or more drugs, (3) pharmaceutical compositions comprising compounds of Formula (II) or Formula (III), (4) treatment/diagnosis of disease comprising compounds of Formula (II) or Formula (III), and (5) methods of preparing an ADC of Formula III.
Type:
Grant
Filed:
December 20, 2018
Date of Patent:
December 26, 2023
Assignee:
ONTARIO INSTITUTE FOR CANCER SEARCH (OICR)
Abstract: Disclosed is a compound of formula (I): wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the compounds, compositions and kits for treatment of disorders associated with TREK-1, TREK-2 or both TREK-1 and TREK-2 dysfunction in a mammal.
Type:
Grant
Filed:
May 24, 2021
Date of Patent:
December 26, 2023
Assignees:
ONO PHARMACEUTICAL CO., LTD., VANDERBILT UNIVERSITY
Inventors:
Craig W. Lindsley, Joshua M. Wieting, Kevin M. Mcgowan, Jerod S. Denton, Kentaro Yashiro, Haruto Kurata, Yoko Sekioka, Takahiro Mori, Yuzo Iwaki
Abstract: The present invention relates to a new class of non-fused thiophene derivatives and their uses for treating diseases such as infection, cancer, metabolic diseases, cardiovascular diseases, iron storage disorders and inflammatory disorders.
Type:
Grant
Filed:
February 8, 2019
Date of Patent:
December 12, 2023
Assignee:
ENYO PHARMA
Inventors:
Eric Meldrum, Benoît De Chassey, Peter Machin, Karine Fabienne Malagu, Paul Colin Michael Winship, Mark Chambers, Jamie David Knight, Roberta Lanaro
Abstract: Provided herein are novel polymorphic forms of metopimazine mesylate. These polymorphic forms are useful in methods, compositions, and kits for the treatment of an enteric nervous system disorder.
Abstract: The present application provides bifunctional compounds of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 8 (CDK8). The present application also relates to methods for the targeted degradation of CDK8 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 which can be utilized in the treatment of disorders modulated by CDK8.
Type:
Grant
Filed:
December 23, 2021
Date of Patent:
November 28, 2023
Assignee:
DANA-FARBER CANCER INSTITUTE, INC.
Inventors:
Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski
Abstract: This disclosure relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The description also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Abstract: Automated oligonucleotide synthesis-compatible fluorescent dye phosphoramidite compounds, solid supports, and labeled polynucleotides incorporating the compounds are provided. The compounds allow universal incorporation of the fluorescent label into any position of the polynucleotide.
Type:
Grant
Filed:
July 13, 2021
Date of Patent:
November 7, 2023
Assignee:
Cepheid
Inventors:
Kevin P. Lund, Dmitri Sergueev, Alexander Gall
Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
Type:
Grant
Filed:
June 15, 2021
Date of Patent:
October 31, 2023
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Ashok Arasappan, Ian M. Bell, Christopher James Bungard, Christopher S. Burgey, Jason M. Cox, Michael J. Kelly, III, Mark E. Layton, Hong Liu, Jian Liu, James J. Perkins, Akshay A. Shah, Michael David VanHeyst, Zhe Wu
Abstract: The invention relates to functionalized dihydro- and tetrahydro-quinazoline compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds as heparanase inhibitors for the treatment of diseases or conditions related to heparanase.
Type:
Grant
Filed:
December 13, 2017
Date of Patent:
October 17, 2023
Assignee:
Beta Therapeutics Pty Ltd
Inventors:
Keats Nelms, Brett Schwartz, Colin Jackson, Martin Banwell, Edward Hammond
Abstract: The present disclosure belongs to the field of pharmaceutical preparations, and discloses a pharmaceutical composition and a preparation method therefor and uses thereof. The pharmaceutical composition comprising EGFR inhibitor (C-005) and the pharmaceutical tablets prepared therefrom of the present disclosure are suitable for the treatment of cancer, preferably lung cancer, particularly non-small cell lung cancer.