Abstract: Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.
Type:
Grant
Filed:
October 16, 2019
Date of Patent:
May 11, 2021
Assignee:
Shy Therapeutics LLC
Inventors:
Yaron R. Hadari, Luca Carta, Michael Schmertzler, Theresa M. Williams, Charles H. Reynolds, Rebecca Hutcheson
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:
November 27, 2018
Date of Patent:
May 11, 2021
Assignee:
The Trustees of the University of Pennsylvania
Abstract: The present invention pertains to an antiviral drug for severe fever with thrombocytopenia syndrome, which contains a compound represented by formula (I) or a salt thereof, or a solvate of the compound or salt (In the formula, R1 and R2 are the same or different from each other, and each represents a substituted or unsubstituted C1-10 alkyl group, R1 and R2 may form a substituted or unsubstituted 5- or 6-member ring in conjunction with an adjacent nitrogen atom, and X represent a halogen atom.
Abstract: The present invention relates to compounds which can act as aryl hydrocarbon receptor (AhR) modulators and, in particular, as AhR antagonists. The invention further relates to the use of the compounds for the treatment and/or prophylaxis of diseases and/or conditions through binding of said aryl hydrocarbon receptor by said compounds.
Type:
Grant
Filed:
February 1, 2018
Date of Patent:
April 20, 2021
Assignee:
Phenex Pharmaceuticals AG
Inventors:
Christoph Steeneck, Ulrich Deuschle, Michael Albers, Thomas Hoffmann
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 29, 2019
Date of Patent:
April 20, 2021
Assignees:
ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE MONTPELLIER
Abstract: Compounds and compositions for selectively inhibiting Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.
Type:
Grant
Filed:
February 5, 2020
Date of Patent:
April 20, 2021
Assignee:
Augusta University Research Institute, Inc.
Inventors:
Samir N. Khleif, Mikayel Mkrtichyan, Iryna Lebedyeva, Thomas Albers
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:
April 24, 2020
Date of Patent:
April 13, 2021
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
Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
Abstract: The present invention relates to a compound of formula (I) wherein P1, P3, P4 and P5 are amino acid residues. The invention also relates to a compound of formula (I) for its use as a Caspase-2 inhibitor and for its therapeutical use. It also concerns the use of a compound of formula (I) as activity base probe to selectively detect Caspase-2 activity.
Type:
Grant
Filed:
March 21, 2017
Date of Patent:
March 30, 2021
Assignees:
INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), UNIVERSITE PARIS DIDEROT-PARIS 7
Abstract: Provided herein are compounds useful for modulating the activity of an androgen receptor, or a variant thereof, and related compositions and methods. Compounds of the invention are useful for antagonizing the androgen receptor splice variant AR-v7, and for the treatment of castration-resistant prostate cancer.
Type:
Grant
Filed:
November 21, 2018
Date of Patent:
March 30, 2021
Assignee:
Massachusetts Institute of Technology
Inventors:
David Freeman, Nicholas B. Struntz, Shelby K. Doyle, Andre Richters, Angela N. Koehler
Abstract: Described herein are compounds that are farnesoid X receptor agonists, 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 farnesoid X receptor activity.
Type:
Grant
Filed:
March 14, 2018
Date of Patent:
March 30, 2021
Assignee:
METACRINE, INC.
Inventors:
Nicholas D. Smith, Steven P. Govek, Johnny Y. Nagasawa
Abstract: Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.
Type:
Grant
Filed:
October 16, 2019
Date of Patent:
March 9, 2021
Assignee:
Shy Therapeutics LLC
Inventors:
Yaron R. Hadari, Luca Carta, Michael Schmertzler, Theresa M. Williams, Charles H. Reynolds, Rebecca Hutcheson
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: Provided herein are methods and compositions for treating cancers, inflammatory diseases, rasopathies, and fibrotic disease involving aberrant Ras superfamily signaling through the binding of compounds to the GTP binding domain of Ras superfamily proteins including, in certain cases, K-Ras and mutants thereof, and a novel method for assaying such compositions.
Type:
Grant
Filed:
October 16, 2019
Date of Patent:
March 2, 2021
Assignee:
Shy Therapeutics LLC
Inventors:
Yaron R. Hadari, Luca Carta, Michael Schmertzler, Theresa M. Williams, Charles H. Reynolds, Rebecca Hutcheson
Abstract: Described herein are compounds that are farnesoid X receptor agonists, 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 farnesoid X receptor activity.
Type:
Grant
Filed:
May 28, 2020
Date of Patent:
February 23, 2021
Assignee:
METACRINE, INC.
Inventors:
Nicholas D. Smith, Stephen P. Govek, Johnny Y. Nagasawa
Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a beta-3 adrenergic receptor-mediated disorder, such as, heart failure; cardiac performance in heart failure; mortality, reinfarction, and/or hospitalization in connection with heart failure; acute heart failure; acute decompensated heart failure; congestive heart failure; severe congestive heart failure; organ damage associated with heart failure (e.g.
Type:
Grant
Filed:
May 12, 2020
Date of Patent:
February 23, 2021
Assignee:
Arena Pharmaceuticals, Inc.
Inventors:
Thuy-Anh Tran, Quyen-Quyen Do, Brett Ullman, Anthony C. Blackburn, Maiko Nagura
Abstract: The complexes disclosed herein are cyclometalated metal complexes of Formula (I) that are useful for full color displays and lighting applications.
Type:
Grant
Filed:
November 26, 2018
Date of Patent:
February 23, 2021
Assignee:
Arizona Board of Regents on behalf of Arizona State University
Abstract: [Problem] The present invention pertains to a safer and more effective respiratory infection treating agent. [Solution] A respiratory infection treating agent containing, as an active ingredient, 7-[(3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrrolidine-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
November 13, 2018
Date of Patent:
February 16, 2021
Assignee:
KYORIN PHARMACEUTICAL CO., LTD.
Inventors:
Kota Kume, Hisao Yoshida, Hirotaka Ando, Yuta Tanaka
Abstract: The invention relates to a process for the preparation of avibactam sodium in polymorphic form C comprising the steps (i) providing a mixture comprising avibactam or a salt thereof and a solvent, wherein the mixture has a water content of less than 2% by weight based on the weight of the mixture; (ii) increasing the temperature of the mixture provided in (i) to at least 55° C. and providing a positive pressure; adding a sodium source to the mixture in step (i) and/or (ii) if the form of avibactam provided in (i) is not avibactam sodium; thereby obtaining avibactam sodium in polymorphic form C.
Type:
Grant
Filed:
February 7, 2018
Date of Patent:
February 16, 2021
Assignee:
Sandoz AG
Inventors:
Michael Fischer, Veronika Werner, Andreas Lechner, Brigitte Staggl
Abstract: The present invention relates to compounds of general formula I, wherein the groups R, R1, R2, R3, m and n are defined herein, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
Type:
Grant
Filed:
January 22, 2018
Date of Patent:
February 16, 2021
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Matthias Eckhardt, Holger Wagner, Stefan Peters