Abstract: A first aspect of the invention relates to betahistine, or a pharmaceutically acceptable salt thereof, and a monoamine oxidase inhibitor, for use in the treatment or prevention of one or more symptoms of vertigo in a subject. A second aspect of the invention relates to a method of treating or preventing one or more symptoms of vertigo in a subject, said method comprising administering to the subject (i) betahistine, or a pharmaceutically acceptable salt thereof, and (ii) a monoamine oxidase inhibitor.
Abstract: The present invention relates to a compound of the following formula (A): or a pharmaceutically acceptable salt or hydrate thereof, for use in the prevention or treatment of a disease associated with a mitochondrial dysfunction.
Type:
Grant
Filed:
November 2, 2020
Date of Patent:
June 27, 2023
Assignee:
Amabiotics
Inventors:
Antoine Danchin, Agnieszka Sekowska, Patrice Garnier
Abstract: Provided are methods of producing Active Pharmaceutical Ingredient (API) grade migalastat hydrochloride, and for purifying intermediate grade migalastat hydrochloride. Further provided are methods of producing [(2R,3S,4R,5S)-1-butyl-2-(hydroxymethyl)piperidine-3,4,5-triol hydrochloride (lucerastat hydrochloride) and other 1-deoxygalactonojirimycin compounds, as well as methods of purifying intermediate grade lucerastat hydrochloride and other 1-deoxygalactonojirimycin compounds.
Abstract: Disclosed are 3,4-methylenedioxyphenylimidazolylethanonexime ether derivatives, a preparation method and use thereof, and a drug for the treatment of Alzheimer's disease, which relates to the technical field of preparation of acetophenone oxime ether compounds. The (Z)-3,4-methylenedioxyphenylimidazolylethanonexime ether derivatives provided by the present disclosure show a significant effect on the inhibition of NO production, with an EC50 of 2.07-5.41 ?mol/L. Compared with the positive control group of quercetin (with an EC50 of 9.56 ?mol/L) and oxiconazole (with an EC50 of 13.5 ?mol/L), the inhibitory effect is stronger without significant cytotoxicity (cell viability >90%), which can be used to prepare drugs for the treatment of Alzheimer's disease.
Abstract: The invention relates to pyridone amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.
Type:
Grant
Filed:
June 24, 2020
Date of Patent:
June 13, 2023
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Sara Sabina Hadida Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
Abstract: In one aspect, the present invention provides a method for treating or ameliorating the effects of a HER2 positive cancer in a subject. In some embodiments, the method comprises administering a combination therapy comprising an anti-HER2 antibody and tucatinib. In some embodiments, the method further comprises administering a chemotherapeutic agent (e.g., an antimetabolite) to the subject. Pharmaceutical compositions and kits are also provided herein.
Abstract: The present disclosure relates to the use of a compound of formula (I) or anyone of its pharmaceutically acceptable salts, in the treatment and/or prevention of an inflammatory disease; wherein: means an aromatic ring wherein V is C or N and when V is N; Q is N or O, provided that R? does not exist when Q is O; R? independently represent a hydrogen atom or a group chosen among a (C1-C3)alkyl group, a halogen atom, a hydroxyl group, a —COOR1 group, a —NO2 group, a —NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (C1-C3)fluoroalkyl group, a —O—P(?O)—(OR3)(OR4) group, a (C1-C4)alkoxy group and a —CN group, and can further be a group chosen among:
Type:
Grant
Filed:
August 17, 2020
Date of Patent:
May 16, 2023
Assignees:
ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE DE MONTPELLIER
Abstract: The present disclosure relates to the use of a compound of formula (I) or anyone of its pharmaceutically acceptable salts, in the treatment and/or prevention of an inflammatory disease; wherein: means an aromatic ring wherein V is C or N and when V is N; Q is N or O, provided that R? does not exist when Q is O; R? independently represent a hydrogen atom or a group chosen among a (C1-C3)alkyl group, a halogen atom, a hydroxyl group, a —COOR1 group, a —NO2 group, a —NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (C1-C3)fluoroalkyl group, a —O—P(?O)—(OR3)(OR4) group, a (C1-C4)alkoxy group and a —CN group, and can further be a group chosen among:
Type:
Grant
Filed:
December 7, 2020
Date of Patent:
May 16, 2023
Assignees:
ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE DE MONTPELLIER
Abstract: This invention is directed to selective androgen receptor degrader (SARD) compounds pharmaceutical compositions and uses thereof in treating early prostate cancer, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
Type:
Grant
Filed:
August 31, 2020
Date of Patent:
May 16, 2023
Assignee:
University of Tennessee Research Foundation
Inventors:
Ramesh Narayanan, Duane D. Miller, Thamarai Ponnusamy, Dong-Jin Hwang, Yali He
Abstract: A novel therapeutic agent effective for the treatment of intellectual disability or autism is disclosed. The therapeutic agent for intellectual disability or autism contains, as an active component(s), at least one selected from the group consisting of tipifarnib and lonafarnib. Examples of the intellectual disability include memory impairment. Examples of the memory impairment include memory impairment caused by abnormality of the Tsc1 gene and/or Tsc2 gene, and epilepsy-induced memory impairment. Also provided is a method of treating intellectual disability or autism, comprising administering an effective amount of at least one selected from the group consisting of tipifarnib and lonafarnib to a patient with intellectual disability or autism.
Type:
Grant
Filed:
November 7, 2018
Date of Patent:
May 9, 2023
Assignee:
TOKYO METROPOLITAN INSTITUTE OF MEDICAL SCIENCE
Abstract: The invention provides novel asymmetric and symmetric bisaminoquinolmes and related compounds, methods of treatment and syntheses. The novel compounds exhibit effective anticancer activity and are useful in the treatment of a variety of autophagy-related disorders.
Type:
Grant
Filed:
April 13, 2021
Date of Patent:
May 2, 2023
Assignee:
THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
Abstract: Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R1 or R2 is independently selected from Cl, F, —CF3, or —CH3, and the other is hydrogen, and methods for their use are provided.
Type:
Grant
Filed:
September 2, 2021
Date of Patent:
April 25, 2023
Assignee:
Eli Lilly and Company
Inventors:
Jolie Anne Bastian, Jeffrey Daniel Cohen, Almudena Rubio, Daniel Jon Sall, Jennifer Anne McMahon
Abstract: Disclosed herein are compounds having a structure of formula (I), compositions and methods useful for the treatment of a disease or infection, such as a viral infection (e.g.
Type:
Grant
Filed:
September 10, 2018
Date of Patent:
April 18, 2023
Assignees:
President and Fellows of Harvard College, The Brigham and Women's Hospital, Inc.
Inventors:
James Morgan Cunningham, Hu Liu, Ye Tian, Katie Kyungae Lee
Abstract: Provided are methods of producing a batch of 1,2,3,6-tetrapivaloyl-D-galactofuranoside; 5-azido-5-deoxy-1,2,3,6-tetrapivaloyl-D-galactofuranoside; intermediate grade migalastat hydrochloride; and/or migalastat hydrochloride. Also provided are methods of determining the purity of a batch of 1,2,3,6-tetrapivaloyl-D-galactofuranoside; 5-azido-5-deoxy-1,2,3,6-tetrapivaloyl-D-galactofuranoside; intermediate grade migalastat hydrochloride; and/or migalastat hydrochloride. Also provided are methods of distributing a batch of 1,2,3,6-tetrapivaloyl-D-galactofuranoside; 5-azido-5-deoxy-1,2,3,6-tetrapivaloyl-D-galactofuranoside; intermediate grade migalastat hydrochloride; and/or migalastat hydrochloride. Also provided are methods of assessing suitability of migalastat hydrochloride for medical use.
Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
Type:
Grant
Filed:
April 28, 2021
Date of Patent:
April 4, 2023
Assignee:
Aerie Pharmaceuticals, Inc.
Inventors:
Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
Abstract: The invention provides novel compounds having the general formula I: wherein R1, R2, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.
Abstract: Described herein is a crystalline hydrate form of LNP023 hydrochloride and to a process for its preparation. Furthermore, described herein is a pharmaceutical composition comprising the crystalline hydrate form of LNP023 hydrochloride, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition described herein can be used to treat a disease and disorder mediated by complement activation.
Type:
Grant
Filed:
May 17, 2021
Date of Patent:
March 14, 2023
Assignee:
Novartis AG
Inventors:
Zichen Jia, Philipp Lustenberger, Marie Meyer, Massimo Moratto
Abstract: The present invention relates to a compound, which can be used in the prevention and treatment of infections with pathogenic Neisseria species, in particular N. gonorrhoeae and N. meningitidis (the gonococcus and the meningococcus, respectively), and other pathogenic bacteria (e.g. Haemophilus species or Moraxella catarrhalis), and which can be used for disinfecting a substrate from said bacteria. Moreover, the present invention relates to a corresponding pharmaceutical composition comprising said compound.
Type:
Grant
Filed:
December 14, 2018
Date of Patent:
March 7, 2023
Assignee:
Universität Konstanz
Inventors:
Thomas Böttcher, David Szamosvari, Christof Hauck, Tamara Schuhmacher, Petra Muenzner-Voight
Abstract: The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula I: or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X1, X2, X3, A1, A2, Y, R1, R2, R3, and R4 are as described herein.
Type:
Grant
Filed:
February 18, 2021
Date of Patent:
February 28, 2023
Assignee:
Fulcrum Therapeutics, Inc.
Inventors:
Ivan Viktorovich Efremov, Steven Kazmirski, Qingyi Li, Lorin A. Thompson, III, Owen Brendan Wallace, Shawn Donald Johnstone, Feng Zhou, Peter Rahl