Abstract: The present invention relates to compounds of formula (I) and their use for treating or preventing a bacterial infection or as an antibacterial agent and/or as a ?-lactamase inhibitor.
Type:
Grant
Filed:
July 30, 2019
Date of Patent:
December 20, 2022
Assignee:
MUTABILIS
Inventors:
Julien Barbion, Audrey Caravano, Sophie Chasset, Francis Chevreuil, Nicolas Lecointe, Frédéric Le Strat, Chrystelle Oliveira, Christophe Simon
Abstract: A compound represented by the following formula (I): wherein each symbol in the formula is as described herein or a salt thereof has an NRF2 activating activity, and is expected to be useful as a preventive or therapeutic agent for diseases associated with oxidative stress, in particular, hepatic disease (for example, non-alcoholic steatohepatitis (NASH)), cardiovascular disease (for example, heart failure or pulmonary arterial hypertension), lung disease (for example, chronic obstructive pulmonary disease (COPD)), kidney disease (for example, chronic kidney disease (CKD) or acute kidney injury (AKI)), central nervous system disease (for example, Parkinson's disease), mitochondrial disease (for example, Friedreich motor ataxia, mitochondrial myopathy), inflammatory disease (for example, multiple sclerosis (MS), inflammatory bowel disease (IBD)), sickle cell disease, cancer, or the like.
Abstract: The invention relates to novel mTOR inhibitor compounds having the general formula (I), to compositions comprising said mTOR inhibitor compounds, methods for producing same, and the use thereof in compositions as a drug.
Abstract: The present invention relates to a new crystal modification of N-(aminoiminomethyl)-2-aminoacetic acid as well as a method for producing this crystal modification.
Type:
Grant
Filed:
June 25, 2020
Date of Patent:
November 29, 2022
Assignee:
Alzchem Trostberg GmbH
Inventors:
Thomas Güthner, Franz Thalhammer, Jürgen Sans
Abstract: Provided herein is a bulk composition comprising the trihydrate form of (3S, 4R, 3?R)-6-[4-(4-amino-5-chloro-2-methoxy-benzoylamino)-3-methoxy-piperidin-1-yl]-hexanoic acid 1-azabicyclo[2.2.2]oct-3?-yl ester di-hydrochloride salt. Provided are also pharmaceutical compositions and dosage forms comprising the trihydrate form, and methods and uses for treating a gastrointestinal disorder in a subject with the trihydrate form. In some embodiments, the gastrointestinal disorder is gastroesophageal reflux disease (GERD), dyspepsia (such as functional dyspepsia or functional motility disorder), gastroparesis, paralytic ileus, post-operative ileus, emesis, nausea, heartburn, intestinal pseudo-obstruction, irritable bowel syndrome (IBS), constipation, enteral feeding intolerance (EFI), or esophagitis. In some embodiments, the gastrointestinal disorder is post-operative ileus, chronic grass sickness, constipation, megacolon, gastritis, gastrointestinal stasis, or abomasal emptying defect.
Abstract: The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. See e.g., Formula I below. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).
Abstract: Compounds of Formula I are described as are pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric diseases and disorders in a subject in need are also disclosed.
Type:
Grant
Filed:
August 12, 2020
Date of Patent:
November 8, 2022
Assignees:
Sunovion Pharmaceuticals Inc., PGI Drug Discovery LLC
Inventors:
Carrie A. Bowen, Douglas F. Burdi, Michele L. R. Heffernan, Lee W. Herman, Linghong Xie
Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula I-A or I-B: wherein the variables are as defined herein.
Type:
Grant
Filed:
August 17, 2020
Date of Patent:
November 1, 2022
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Jean-Damien Charrier, Christopher John Davis, Damien Fraysse, Gorka Etxebarria I Jardi, Simon Pegg, Francoise Pierard, Joanne Pinder, John Studley, Carl Zwicker, Tapan Sanghvi, Michael Waldo, Ales Medek, David Matthew Shaw, Maninder Panesar, Yuegang Zhang, Naziha Alem
Abstract: The invention provides novel classes of HCV therapeutics that are orally available, safe and effective HCV NS3/4A protease inhibitors and are less susceptible to drug resistance than existing therapeutics. The invention also relates to pharmaceutical composition of these compounds and methods of preparation and use thereof.
Type:
Grant
Filed:
June 19, 2018
Date of Patent:
October 18, 2022
Assignee:
University of Massachusetts
Inventors:
Celia Schiffer, Akbar Ali, Ashley Matthew
Abstract: This invention provides compounds of formula (I) and salts thereof, which have activity as inhibitors of N-myristoyl transferase (NMT). The invention also relates to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of N-myristoyl transferase provides a therapeutic or prophylactic effect, including protozoan infections (such as malaria and leishmaniasis), viral infections (such as human rhinovirus and HIV), and hyperproliferative disorders (such as B-cell lymphoma).
Type:
Grant
Filed:
July 8, 2020
Date of Patent:
October 11, 2022
Assignee:
IMPERIAL COLLEGE INNOVATIONS LIMITED
Inventors:
Andrew Simon Bell, Edward William Tate, Robin John Leatherbarrow, Jennie Ann Hutton, James Antony Brannigan
Abstract: Methods for producing enantiodefined polycyclic compounds, particularly tetracyclic compounds, are provided. More particularly, synthetic methods for producing biologically active enantiodefined steroidal compositions of both natural (“nat-”) and unnatural (“ent-”) absolute stereochemistry are provided. An exemplary method for manufacturing a tetracyclic compound comprises a step of forming a hydrindane intermediate through coupling of a suitably functionalized enyne with a suitably functionalized alkyne and subsequently performing an intramolecular ring-closing reaction to form the tetracyclic compound. Steroidal compounds obtained by this method and methods of using such steroidal compounds in human and/or animal therapeutics and medicines are also provided.
Abstract: The present invention relates to the technical field of polymer spectral probes, and particularly to a perchloroethylene derivative and use thereof. The perchloroethylene derivative is prepared by reacting a compound A and a perchloroethylene resin. According to the present invention, the fluorescent polymer can be used as a high-selectivity and high-sensitivity enhanced colorimetric and fluorescent polymer probe for Fe3+ and Cr3+ As compared with the organic small molecule spectral probe, the polymer spectral probe has improved mechanical property, film forming property and excellent recyclability, and thus has a strong practicability.
Abstract: This invention relates to: (a) compounds of formula Ia (with R1, R4 to R6, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-?-hydroxylase inhibitors; (b) pharmaceutical compositions (comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.
Type:
Grant
Filed:
November 30, 2018
Date of Patent:
September 6, 2022
Assignee:
BIAL—PORTELA & CA, S.A.
Inventors:
Laszlo Erno Kiss, Alexander Beliaev, Tino Rossi, Pedro Nuno Leal Palma, Patrício Manuel Vieira Araujo Soares Da Silva, Rui Pinto, Francisco Cardona
Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein.
Type:
Grant
Filed:
October 29, 2020
Date of Patent:
September 6, 2022
Assignee:
Agency for Science, Technology and Research
Abstract: The present invention provides compounds of formula I, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
Type:
Grant
Filed:
July 24, 2020
Date of Patent:
September 6, 2022
Assignee:
Nimbus Lakshmi, Inc.
Inventors:
Craig E. Masse, Jeremy Robert Greenwood, Donna L. Romero, Geraldine C. Harriman, Ronald T. Wester, Mee Shelley, Joshua Jahmil Kennedy-Smith, Markus Dahlgren, Sayan Mondal, Shaughnessy Robinson
Abstract: The present invention relates to a dioxinoquinoline compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention also provides a preparation method of the compound of formula (I) and a pharmaceutically acceptable salt thereof, as well as uses thereof as a drug, wherein the drug acting as a tyrosine kinase (i.e. VEGFR-2 and c-MET) inhibitor is used for treating disorders related to tyrosine kinase.
Abstract: Provided herein are compounds, compositions and methods of using the compounds and compositions for the treatment of diseases modulated, as least in part, by AhR. The compounds are represented by formulae: wherein the letters and symbols X1, X2, Z, R1b, R1c, R1d, R1e, R2a, R2b, R2c and R2d have the meanings provided in the specification.
Type:
Grant
Filed:
September 17, 2020
Date of Patent:
August 9, 2022
Assignee:
IDEAYA BIOSCIENCES, INC.
Inventors:
Muzaffar Alam, Hilary Plake Beck, Michael Patrick Dillon, Marcos Gonzalez-Lopez, James Clifford Sutton, Jr.