Abstract: The disclosure provides crystalline forms for certain synthetic intermediates for making belzutifan, a HIF-2? inhibitor, useful for the treatment of cancer. The disclosure also provides processes for isolating the crystalline forms.
Inventors:
Stephen M. Dalby, Clinton Scott Shultz, Chintal Desai, Joshua Lee, Zhiwei Chen, Jungchul Kim, Nastaran Salehi Marzijarani, Tao Wang, Eric M. Phillips, Patrick Larpent, Het P. Patel, Haiheng Guo, Xin Wang, Kangze Dai, Lu Chen, Teng Li, Taotao Lu, Jianjun Duan
Abstract: The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.
Type:
Grant
Filed:
January 14, 2022
Date of Patent:
November 21, 2023
Assignee:
JANSSEN PHARMACEUTICA NV
Inventors:
Manuel Jesus Alcazar Vaca, Jose Ignacio Andres Gil, Christa C. Chrovian, Heather R. Coate, Meri De Angelis, Curt A. Dvorak, Christine F. Gelin, Michael A. Letavic, Brad M. Savall, Akinola Soyode-Johnson, Brice M. Stenne, Devin M. Swanson
Abstract: The invention relates to a compound according to general formula (I), which acts as a bradykinin (BK) B2 receptor antagonist; to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament.
Type:
Grant
Filed:
January 18, 2022
Date of Patent:
November 21, 2023
Assignee:
PHARVARIS NETHERLANDS B.V.
Inventors:
Christoph Gibson, Joern Saupe, Horst-Dieter Ambrosi, Lars Ole Haustedt
Abstract: Crystalline forms of Compound (I): are disclosed. Pharmaceutical compositions comprising the same, methods of treating disorders and conditions mediated by BTK activity using the same, and methods for making Compound (I) and crystalline forms thereof are also disclosed.
Type:
Grant
Filed:
January 21, 2021
Date of Patent:
November 14, 2023
Assignee:
Principia Biopharma Inc.
Inventors:
Pasit Phiasivongsa, Kolbot By, Jean Baum
Abstract: Compounds including triphenylamine and luminol moieties exhibiting near-infrared chemiluminescence useful as reactive oxygen sensors, pharmaceutical compositions including the same, and methods of preparation and use thereof.
Type:
Grant
Filed:
March 1, 2021
Date of Patent:
November 14, 2023
Assignee:
The Hong Kong University of Science and Technology
Abstract: Methods and uses for diagnosing and treating anxiety disorders are encompassed, wherein diagnosis and treatment may be based upon an assessment of genetic alterations in metabotropic glutamate receptor (mGluR) network genes and wherein treatment is with nonspecific activators of mGluRs such as fasoracetam.
Abstract: A TLR9 inhibitor includes a compound of general formula (I): wherein the meanings of the variables are explained in the specification, or a stereoisomeric form or a mixture of stereoisomeric forms, or pharmaceutically acceptable salts thereof. A pharmaceutical composition can include compounds of the invention, which can be used in a method for inhibiting TLR9 activity in vitro or in vivo. The method can be performed by administering the compound to a subject to inhibit TLR9 activity, which can be used to treat a disease or disorder associated with TLR9.
Type:
Grant
Filed:
April 26, 2021
Date of Patent:
November 7, 2023
Assignee:
Insilico Medicine IP Limited
Inventors:
Aleksandrs Zavoronkovs, Vladimir Aladinskiy, Aleksandr Aliper
Abstract: Methods for diagnosing and treating conduct disorder are encompassed, wherein diagnosis and treatment may be based upon an assessment of genetic alterations in metabotropic glutamate receptor (mGluR) network genes and wherein treatment is with nonspecific activators of mGluRs such as fasoracetam.
Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(arylsulfinyl)-acetamide compounds that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-t RNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.
Type:
Grant
Filed:
October 6, 2017
Date of Patent:
October 31, 2023
Assignee:
Oxford Drug Design Limited
Inventors:
Paul William Finn, Michael Charlton, Grace Edmund, Aigars Jirgensons, Einars Loza
Abstract: The present invention aims to provide a compound acting as a specific agonist for LPA4 receptors, and a pharmaceutical composition containing the compound. The present invention relates to a novel lysophosphatidic acid derivative having an agonistic action on LPA4 receptors and useful for the prophylaxis and/or treatment of diseases associated with angiogenesis abnormalities involving LPA4 receptors, diseases associated with vascular disorders, or the symptoms associated therewith, and a pharmaceutical composition containing the derivative.
Type:
Grant
Filed:
November 3, 2021
Date of Patent:
October 31, 2023
Assignees:
MITSUBISHI TANABE PHARMA CORPORATION, OSAKA UNIVERSITY
Abstract: The present disclosure is directed toward uses of compound 1 (or its stereoisomers) and compositions and/or dosage forms containing compound 1: or a pharmaceutically acceptable salt thereof. Some uses of Compound 1 and/or its stereoisomers include treating a variety of diseases and disorders, including pain, depression, and schizophrenia. In some embodiments, Compound 1 and/or its stereoisomers may be useful in the treatment of a substance use disorder while inducing fewer withdrawal symptoms than a standard-of-care opioid addiction treatment.
Abstract: The present invention relates to the use of 7-hydroxy-cannabidol (7-OH-CBD) and/or 7-hydroxy-cannabidivarin (7-OH-CBDV) in the treatment of epilepsy. Preferably the cannabinoid metabolites are isolated from plants to produce a highly purified extract or can be reproduced synthetically.
Type:
Grant
Filed:
September 10, 2021
Date of Patent:
October 24, 2023
Assignee:
GW Research Limited
Inventors:
Colin Stott, Nick Jones, Benjamin Whalley, Gary Stephens, Claire Williams
Abstract: The present invention relates to a composition comprising, in a physiologically acceptable medium: a) at least one saccharide, b) at least one amino acid, c) DMSO or at least one C3-C5 alkanediol, d) at least one antioxidant, and e) cells for therapeutic purposes, said composition having a pH between 7.0 and 8.5, preferably between 7.0 and 8.3. It also relates to a method for the cryopreservation of at least one sample of cells for therapeutic purposes, comprising the following steps: i) mixing the sample of cells for therapeutic purposes with ingredients a) to d) above and a physiologically acceptable medium, so as to obtain a composition having a pH between 7.0 and 8.5, preferably between 7.0 and 8.3, then ii) freezing the composition obtained in step i).
Type:
Grant
Filed:
November 27, 2018
Date of Patent:
October 17, 2023
Assignee:
Laboratoire Francais du Fractionnement et des Biotechnologies
Inventors:
Joffrey De Larichaudy, Sandy Cazalon Nemorin
Abstract: The invention provides methods of chemical synthesis of the pharmacological agent 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate, also called CV-8972. The methods entail formation of a free base form of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethanol, also called CV-8814, as intermediate without producing a salt form of CV-8814.
Type:
Grant
Filed:
June 28, 2021
Date of Patent:
October 10, 2023
Assignee:
IMBRIA PHARMACEUTICALS, INC.
Inventors:
Neil Buckley, Dan Belmont, Bryan Hauser, Myoung Goo Kim, Kumar Kannan
Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.
Type:
Grant
Filed:
May 18, 2021
Date of Patent:
October 3, 2023
Assignee:
SRX CARDIO, LLC
Inventors:
Thomas E Barta, Jonathan W Bourne, Kyle D Monroe, Michael M Muehlemann
Abstract: The present invention provides dihydrooxydiazinone compounds of general formula (I) in which R1, R2, R3, and R4, are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative diseases, as a sole agent or in combination with other active ingredients.
Type:
Grant
Filed:
July 14, 2022
Date of Patent:
October 3, 2023
Assignees:
Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft, The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc.
Inventors:
Manuel Ellermann, Stefan Nikolaus Gradl, Charlotte Christine Kopitz, Martin Lange, Adrian Tersteegen, Philip Lienau, Christa Hegele-Hartung, Detlev Sülzle, Timothy A. Lewis, Heidi Greulich, Xiaoyun Wu, Matthew Meyerson, Alex Burgin
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:
June 16, 2021
Date of Patent:
October 3, 2023
Assignee:
ORGANOVO, INC.
Inventors:
Nicholas D. Smith, Steven P. Govek, Karensa L. Douglas, Andiliy G. Lai
Abstract: The present disclosure provides 1) an enantiomerically purified compound SRR G-1, or a derivative thereof, including specific crystal forms, salts and co-crystals that modulates G protein-coupled estrogen receptor activity, 2) pharmaceutical and cosmetic compositions comprising an enantiomerically purified SRR G-1, or a derivative thereof, and 3) methods of treating or preventing disease states and conditions and cosmetic conditions mediated through these receptors and related methods thereof in humans and animals.
Type:
Grant
Filed:
February 25, 2021
Date of Patent:
September 19, 2023
Assignee:
Linnaeus Therapeutics, Inc.
Inventors:
Christopher Natale, Patrick T. Mooney, Tina Garyantes, Wayne Luke