Abstract: This invention relates to 4-(4-fluorobenzylamino)-1-methylpiperidine trihydrate and a process for the preparation of 4-(4-fluorobenzylamino)-1-methylpiperidine trihydrate comprising treating 4-(4-fluorobenzylamino)-1-methylpiperidine with water. The invention also relates to a process for the preparation of pimavanserin comprising reacting 4-(4-fluorobenzylamino)-1-methylpiperidine trihydrate with 1-isobutoxy-4-(isocyanatomethyl)benzene; to a process for the preparation of a pimavanserin acid addition salt comprising reacting 4-(4-fluorobenzylamino)-1-methylpiperidine trihydrate with 1-isobutoxy-4-(isocyanatomethyl)benzene and converting pimavanserin into a pimavanserin acid addition salt, pimavanserin and pimavanserin acid addition salts obtainable by the process, and to the use of 4-(4-fluorobenzylamino)-1-methylpiperidine trihydrate for preparing pimavanserin or an acid addition salt thereof.
Abstract: The present invention provides non-peptide compounds that mimic the streptococcal SspB Adherence Region (BAR) and function as inhibitors of P. gingivalis adherence to streptococci. The invention also provides methods of making and using the inhibitors.
Type:
Grant
Filed:
July 19, 2019
Date of Patent:
February 4, 2025
Assignee:
University of Louisville Research Foundation, Inc.
Abstract: Compositions attractive to mice include one or more long-range volatiles and one or more short-range volatiles. The long-range volatiles can include butyric acid, 2-methylbutyric acid, and 4-heptanone. Devices and methods of using the compositions are also disclosed.
Type:
Grant
Filed:
May 2, 2019
Date of Patent:
January 28, 2025
Assignee:
OMS Investments, Inc.
Inventors:
Elana Varner, Gerhard J. Gries, Regine M. Gries, Stephen J. Takacs
Abstract: Disclosed herein are crystalline forms of compounds for the inhibition of RhoGTPase. Also disclosed herein are compounds, pharmaceutical compositions, and methods of treatment of RhoGTPase-mediated diseases, such as hyperproliferative and neoplastic diseases.
Type:
Grant
Filed:
October 5, 2022
Date of Patent:
January 28, 2025
Assignee:
MBQ Pharma
Inventors:
Jocelyn M. Jiménez Cruz, Vilmalí López-Mejías, Torsten Stelzer
Abstract: Disclosed herein are new compounds, pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
Type:
Grant
Filed:
September 27, 2019
Date of Patent:
January 21, 2025
Assignee:
CALLIDITAS THERAPEUTICS SUISSE SA
Inventors:
Peter Machin, Mark Chambers, Alastair Hodges, Andrew Sharpe, Grant Wishart, Benjamin Perry, Sylvain Celanire, Freddy Heitz
Abstract: DP-2 antagonists reversed PGD2-mediated human hair growth inhibition in a dose-dependent manner in vitro by reducing PGD2-triggered apoptosis and maintaining proliferation of keratinocytes. Hair follicles from approximately half of the alopecia patients exhibited little susceptibility to PGD2's effect in vitro. SNPs in the human DP-2 gene were identified that are associated with hair growth inhibition by PGD2. These findings underscore the role of DP-2 in regulating hair growth and indicate that DP-2 can be an effective approach in preventing and/or treating androgenetic alopecia in patients sensitive to PGD2. Furthermore, the SNPs identified here can be used to identify patients who will benefit from treatment.
Type:
Grant
Filed:
July 28, 2016
Date of Patent:
January 21, 2025
Assignee:
The Trustees of the University of Pennsylvania
Inventors:
George Cotsarelis, Ying Zheng, Jen-Chih Hsieh, David Collins, Joan O'Brien
Abstract: Disclosed are formulations/compositions comprising ibrutinib: as well as processes for preparing such formulations/compositions and methods of treatment of a disease or condition that comprises the use of such formulations/compositions.
Abstract: Provided is an injectable sustained release pharmaceutical formulation, including 3-acyl-naltrexone or a pharmaceutically acceptable salt thereof, a biocompatible organic solvent, and optionally a biocompatible polymeric material. Also provided is a method for treating opioid use disorder or alcoholism, including administering the injectable sustained release pharmaceutical formulation to a subject in need thereof. The pharmaceutical formulation provides a sustained release profile after one single injection, and the plasma levels of naltrexone in minipigs could provide a sustained release for 2 months.
Abstract: The present application provides compounds and methods of treating bacterial infection, including bacterial infection caused by P. acnes.
Type:
Grant
Filed:
November 23, 2021
Date of Patent:
January 14, 2025
Assignees:
The General Hospital Corporation, Rhode Island Hospital, A Lifespan-Partner, Temple University—Of The Commonwealth System of Higher Education
Inventors:
Frederick M. Ausubel, Wooseong Kim, Eleftherios Mylonakis, William M. Wuest
Abstract: Nasal formulations of metoclopramide, which remain stable and/or colorless upon storage over a period of time, are provided. Also provided are methods of treating disorders treatable with metoclopramide, comprising administering the nasal solutions to patients in need thereof.
Type:
Grant
Filed:
July 2, 2021
Date of Patent:
January 14, 2025
Assignee:
Evoke Pharma, Inc.
Inventors:
Matthew J. D'Onofrio, David A. Gonyer, Shirish A. Shah, Stuart J. Madden
Abstract: Nasal formulations of metoclopramide, which remain stable and/or colorless upon storage over a period of time, are provided. Also provided are methods of treating disorders treatable with metoclopramide, comprising administering the nasal solutions to patients in need thereof.
Type:
Grant
Filed:
July 2, 2021
Date of Patent:
January 14, 2025
Assignee:
Evoke Pharma, Inc.
Inventors:
Matthew J. D'Onofrio, David A. Gonyer, Shirish A. Shah, Stuart J. Madden
Abstract: The invention relates to compound of formula (I): in particular flavonoid derivatives (quercetin and catechin derivatives), for use in the prevention and/or the treatment of a disease or disorder involving both carbonyl and oxidative stresses.
Type:
Grant
Filed:
July 12, 2019
Date of Patent:
January 14, 2025
Assignees:
Centre National de la Recherche Scientifique (CNRS), Universite De Montpellier, Ecole Nationale Superieure de Chimie, Institut National de la Sante et de la Recherche Medicale (INSERM)
Inventors:
Céline Crauste, Espérance Moine, Philippe Brabet, Thierry Durand, Joseph Vercauteren
Abstract: The present invention relates to compositions, formulations, and methods for treating pulmonary disorders having fibrosis as part of the underlying pathology, such as IPF and ARDS, by administration of a UPase inhibitor, with or without supplemental UR, a UR prodrug, or a UR mimetic to a subject in need thereof.
Type:
Grant
Filed:
July 7, 2021
Date of Patent:
January 14, 2025
Assignee:
Tosk, Inc.
Inventors:
William A. Garland, Philip Liaw, Brian D. Frenzel
Abstract: Described herein are compositions and methods for the conversion of chlorophyll-derived phytol into useful and economically viable surfactants. The provided compositions utilize the hydrophobic phytol structure and added functional groups to increase hydrophilicity at one end of the molecule.
Type:
Grant
Filed:
October 21, 2022
Date of Patent:
January 14, 2025
Assignee:
Alliance for Sustainable Energy, LLC
Inventors:
Tao Dong, Robert David Allen, Lieve Laurens
Abstract: Emulsion formulations and systems for the intravenous or parenteral administration of neurokinin-1 (NK-1) receptor antagonists for treatment of emesis are provided. Methods for preparing the stable NK-1 receptor antagonist emulsions and pharmaceutical formulations are further provided. The emulsion formulations are prepared and characterized as a formulation and process that will allow an NK-1 receptor antagonist compound to be incorporated into an emulsion for intravenous injection and remain stable during the shelf life of the formulation. Specifically, emulsion formulations have an oil phase that includes oil, ethanol, egg lecithin, and the further addition of sodium oleate that is mixed with an aqueous phase and processed to form the emulsion formulation.
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 disclosure relates to compounds of formula (I) useful in the treatment of tauopathies and Alzheimer's disease wherein A, R, W, Q, n, and m are described herein.
Type:
Grant
Filed:
April 30, 2021
Date of Patent:
January 7, 2025
Assignee:
Asceneuron SA
Inventors:
Anna Quattropani, Santosh S. Kulkarni, Awadut Gajendra Giri
Abstract: In various aspects and embodiments the invention provides a method of treating epilepsy in a subject in need thereof, the method comprising providing to the subject an effective amount of an FLNA modulator. In various embodiments, the FLNA modulator is PTI-125 or kartogenin. In various embodiments, the epilepsy is epilepsy associated with focal cortical dysplasia (FCD) type II or tuberous sclerosis complex (TSC).
Abstract: Compositions including a complex of fatty acids (e.g., including one or more C4 to C40 fatty acids, such as a C4 to C20 fatty acid) and one or more amino acids (and particularly one or more amino acids having electrically charged basic side chains, e.g., Arginine, Lysine, etc.) for use as an anti-pathogenic composition. In particular, described herein are compositions of decanoic acid: Arginine in which the decanoic acid and Arginine for a complex having a lamellar supramolecular structure.
Abstract: Provided herein are compounds of the Formula (I), (II), and (III): as well as pharmaceutically acceptable salts thereof, wherein the substituents are those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of oncologic diseases.
Type:
Grant
Filed:
October 19, 2020
Date of Patent:
January 7, 2025
Assignee:
XRAD Therapeutics, Inc.
Inventors:
Jianmin Fu, Yaode Wang, Yue Sun, Guosheng Wu, Aijun Lu, Shuang Zhang, Robert Goodnow, Tona Gilmer, Michael Kastan, David Kirsch