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
Abstract: The present disclosure relates to an ADAM9 inhibitor compound of formula (I), including salts, hydrates and stereoisomers thereof, compositions thereof, and methods of use therefor, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
Abstract: The present invention relates to novel halogen-substituted compounds, to processes for their preparation and to their use for controlling animal pests, in particular arthropods and especially insects and arachnids.
Type:
Grant
Filed:
June 27, 2019
Date of Patent:
June 14, 2022
Assignee:
Bayer Animal Health GmbH
Inventors:
Joachim Telser, Ursula Krenz, Kirsten Boerngen, Andreas Turberg, Klein Sofia, Franziska Schmidt
Abstract: Provided herein are compounds that can exhibit activity as biofilm modulating agents (e.g., activity as biofilm inhibitors and/or activity as biofilm dispersal agents). The compounds can exhibit potent activity against Gram positive biofilms. The compounds can also exhibit activity against Gram negative biofilms. In some cases, the compounds can exhibit both biofilm modulation properties and antimicrobial activity. Compositions comprising these compounds, as well as methods of using thereof, are also described. For example, the compounds described herein can be used in human and animal health (e.g., for the treatment of infection), agriculture, marine coatings, and other coating applications related to prevention of biofilm (e.g., dental, medical, etc.).
Abstract: The invention relates to novel liquid formulations suitable for topical administration to animals, which formulations comprise a fluorine-containing antiparasitic active compound and also triethyl phosphate, and to their use for the control and prevention of animal parasites.
Type:
Grant
Filed:
September 3, 2018
Date of Patent:
May 31, 2022
Assignee:
Bayer Animal Health GmbH
Inventors:
Wolfgang Wiehl, Petra Ohage-Spitzlei, Franziska Schmidt
Abstract: Provided is a pharmaceutical composition containing pemafibrate, a salt thereof or a solvate thereof and having excellent storage stability. The pharmaceutical composition is provided to contain pemafibrate, a salt thereof or a solvate thereof, wherein a pH value of a solution produced by dissolving or dispersing the pharmaceutical composition in water is 7 or more.
Abstract: The present invention provides a therapeutic agent or a prophylactic agent of dementia containing xanthine oxidase inhibitor such as a compound represented in formula (I), (II), (III) or (IV), or a pharmaceutically acceptable salt thereof as an active ingredient.
Type:
Grant
Filed:
February 17, 2017
Date of Patent:
May 31, 2022
Assignees:
NATIONAL UNIVERSITY CORPORATION TOTTORI UNIVERSITY, Tejin Pharma Limited
Abstract: Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.
Abstract: The present disclosure relates to an improved process for the preparation of a sulfonamide structured kinase inhibitor, namely N-(2?,4?-difluoro-5-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)-[1,1?-biphenyl]-3-yl)cyclopropanesulfonamide (1A) and pharmaceutically acceptable salts thereof. Compound of formula (1A) is a selective inhibitor of FGFR/VEGFR kinase families and is useful in the treatment of cancer.
Abstract: T-PLL Therapy There is provided tinostamustine or a pharmaceutically acceptable salt thereof for use in the treatment of T-cell prolymphocytic leukemia (T-PLL) in a patient in need thereof.
Abstract: Provided are methods useful for preventing and mitigating radiation injury, including acute radiation syndrome, comprising administering to a subject a therapeutically effective amount of a compound represented by formula I: or a pharmaceutically acceptable salt thereof, wherein Z is —O— or —N(H)—.
Type:
Grant
Filed:
March 31, 2017
Date of Patent:
April 26, 2022
Assignees:
Georgetown University, The Board of Regents of the University of Oklahoma
Inventors:
Milton L. Brown, Yali Kong, Courtney Houchen, Sripathi M. Sureban, Parthasarathy Chandrakesan
Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.
Abstract: The present invention encompasses compounds of formula (I), wherein the groups R1 to R, A1 to A4 and n have the meanings given in the claims and specification, their use as inhibitors of PHGDH, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
Type:
Grant
Filed:
March 13, 2018
Date of Patent:
April 19, 2022
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Harald Weinstabl, Georg Dahmann, Matthias Treu, Bernd Wellenzohn, Stephan Karl Zahn
Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
Type:
Grant
Filed:
October 12, 2020
Date of Patent:
April 12, 2022
Assignees:
CYTOKINETICS, INC., AMGEN INC.
Inventors:
Luke Ashcraft, Alessandro Boezio, John Butler, Aroop Chandra, Chihyuan Chuang, Scott E. Collibee, Mikkel V. Debenedetto, Vincent DiMassa, Russell Graceffa, Justin Malinowski, David Moebius, Bradley Paul Morgan, Joshua Payette, Antonio Romero, David St. Jean, Jr., Richard Vargas, John Yeoman, Hanmo Zhang, Alan Cheng, Felix Gonzalez Lopez De Turiso, Michael Garrett Johnson
Abstract: Provided is a pharmaceutical composition which contains pemafibrate, a salt thereof or a solvate thereof and has excellent stability. A pharmaceutical composition is provided containing pemafibrate, a salt thereof or a solvate thereof and having a moisture content of 2.4 mass % or less.
Abstract: The invention relates to functionalised dioxaborolane or dioxaborinane derivatives of formula (I), wherein R1 is covalently bonded to the boron atom by a carbon atom; one of R2, R3, R?3 or R4 is a radical of formula —X; or one of R1, R2, R3, R?3 or R4 is a radical of formula —X; and X is a functionalised radical. The invention relates to the method for preparing same and the uses thereof.
Type:
Grant
Filed:
May 30, 2017
Date of Patent:
March 22, 2022
Assignees:
ECOLE SUPERIEURE DE PHYSIQUE ET DE CHIMIE INDUSTRIELLES DE LA VILLE DE PARIS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE