Abstract: The present invention relates to novel alpha5 subunit-selective negative allosteric modulators of GABAA receptors that have been deuterated to improve their medicinal properties by prolonging their half-lives, rendering them useful as fast-acting pharmaceutical treatments for depression related disorders.
Type:
Grant
Filed:
August 28, 2018
Date of Patent:
October 4, 2022
Assignees:
UNIVERSITY OF MARYLAND, BALTIMORE, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
Inventors:
Scott Thompson, Adam Van Dyke, Craig Thomas, Patrick Morris
Abstract: Disclosed herein are compounds of formula I: or a salt thereof and compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof, alone or in combination with a bacterial efflux pump inhibitor.
Type:
Grant
Filed:
June 26, 2018
Date of Patent:
October 4, 2022
Assignee:
RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
Inventors:
Edmond J. LaVoie, Ajit Parhi, Hye Yeon Sagong
Abstract: N-benzylbenzamides that act as dual soluble epoxide hydrolase (sEH)/peroxisome proliferator-activated receptor ? (PPAR?) modulators and are useful as medications in the treatment of Metabolic Syndrome (MetS) cluster diseases, including diabetes. Methods of making and using the same are further provided.
Type:
Grant
Filed:
December 23, 2020
Date of Patent:
September 20, 2022
Assignees:
The Medical College of Wisconsin, Inc., Johann Wolfgang Goethe-Universität Frankfurt
Inventors:
John David Imig, Md. Abdul Hye Khan, Eugen Proschak, Rene Blocher
Abstract: The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter wherein R1-L- is R1—OC(O)—, or the like, R1 is hydrogen atom, optionally-substituted C1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R3 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like, the part of X, Y, and Z is X?Y—Z, X—Y?Z, or X—Y—Z, X is nitrogen atom, NR4 (R4 is hydrogen atom, optionally-substituted C1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.
Abstract: Provided is a long-acting method for preventing or treating glucose metabolism disorders that includes administering a beta-lactam compound or a pharmaceutically acceptable salt thereof to a subject in need thereof. The method for preventing or treating glucose metabolism disorders has a long-acting effect that lasts more than two days even after medication has been stopped.
Abstract: The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino] caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-V). The present invention also provides an amorphous form of SNAC.
Type:
Grant
Filed:
July 30, 2020
Date of Patent:
July 26, 2022
Assignee:
NOVO NORDISK NORTH AMERICA OPERATIONS A/S
Abstract: The present invention relates to a crystalline form of the compound (S)-3-{4-[5-(2-cyclopentyl-6-methoxy-pyridin-4-yl)-[1,2,4]oxadiazol-3-yl]-2-ethyl-6-methyl-phenoxy}-propane-1,2-diol.
Type:
Grant
Filed:
October 14, 2020
Date of Patent:
July 19, 2022
Assignee:
IDORSIA PHARMACEUTICALS LTD
Inventors:
Cyrille Lescop, Jasper Dingemanse, Andreas Krause
Abstract: The present invention relates to compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds; to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
Type:
Grant
Filed:
March 22, 2018
Date of Patent:
July 19, 2022
Assignee:
SYNGENTA PARTICIPATIONS AG
Inventors:
Jérôme Yves Cassayre, Myriem El Qacemi, Thomas Pitterna, André Stoller
Abstract: The present invention relates to a use of a carbamate compound represented by chemical formula 1, or a pharmaceutically acceptable salt, a solvate or a hydrate thereof for preventing, alleviating or treating myotonia.
Abstract: The present application provides process for preparation of siponimod, intermediates of siponimod, salts of siponimod, polymorphic forms and solid dispersions of siponimod and its salts thereof. The present application specifically provides crystalline polymorphic forms of siponimod base, siponimod hemifumarate and other salts and pharmaceutical compositions thereof. Also provided are solid dispersions of siponimod hemifumarate and pharmaceutical compositions containing them.
Abstract: The present disclosure relates generally to compounds that simultaneously bind both mutant huntingtin protein (mHTT) and an ubiquitin E3 ligase and their use as therapeutic agents, for example, in treating diseases, such as neurodegenerative disorders caused by aggregation of mHTT.
Type:
Grant
Filed:
February 24, 2020
Date of Patent:
July 19, 2022
Assignee:
CHDI Foundation, Inc.
Inventors:
Celia Dominguez, Jonathan Bard, Matthew R. Lee, Longbin Liu, Michael Edward Prime, Samuel Coe
Abstract: Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomer synthesis while maintaining overall yield and purity of a synthesized oligomer.
Type:
Grant
Filed:
November 16, 2020
Date of Patent:
July 12, 2022
Assignee:
Sarepta Therapeutics, Inc.
Inventors:
Baozhong Cai, Mitchell Martini, Ross Shimabuku, Katie Thomas, Diane Elizabeth Frank, Richard K. Bestwick
Abstract: The present invention relates to a compound according to formula I and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
Type:
Grant
Filed:
December 19, 2019
Date of Patent:
July 5, 2022
Assignee:
Leo Pharma A/S
Inventors:
Kevin Neil Dack, Xifu Liang, Mogens Larsen, Mark Andrews, Alan Stuart Jessiman, Mia Nørreskov Burhardt, Patrick Stephen Johnson, Peter Andersen, Lars Jørgensen
Abstract: Provided herein are dibenzocyclooctyne compounds useful as reagents in 1,3-dipolar cycloaddition reactions, and methods for their preparation.
Type:
Grant
Filed:
May 27, 2021
Date of Patent:
July 5, 2022
Assignee:
MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Inventors:
Ronald T. Raines, Brian Gold, Jesús M. Dones, Nile S. Abularrage, Brian James Graham
Abstract: The present disclosure provides solid forms of (E)-3-[2-(2-thienyl)vinyl]-1H-pyrazole, compositions thereof, and methods of making and using the same.
Abstract: The present invention relates to a modulator of 1,2,5-oxadiazole indoleamine-(2,3)-dioxygenase, a preparation method and use thereof, more particularly to compounds of Formula I and Formula II, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, and their use in preparing drugs for treating cancers, neurodegenerative diseases, eye diseases, mental disorders, depression, anxiety disorders, Alzheimer's diseases and/or autoimmune diseases. Specific meanings of R substituents in Formula I and Formula II are consistent with the description of the specification.
Abstract: In one aspect, the disclosure relates to compounds useful to regulate, limit, or inhibit the expression of AVIL (advillin), methods of making same, pharmaceutical compositions comprising same, and methods of treating disorders associated with AVIL dys-regulation using same. In aspects, the disclosed compounds, compositions and methods are useful for treating disorders or diseases in which the regulation, limitation, or inhibition of the expression of AVIL can be clinically useful, such as, for example, the treatment of cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
Type:
Grant
Filed:
October 26, 2018
Date of Patent:
June 28, 2022
Assignee:
University of Virginia Patent Foundation