Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein Ar, Z and Y are as described herein and R1 is a group of the structure wherein n is 0 or 1; R2 is H, deuterium or methyl; R3 is methyl, trifluoromethyl, ethyl, or taken with R2 together forms a cyclopropyl group, or R3 forms a methylene bridge to the carbon atom marked *, which are suitable for the treatment of autoimmune diseases and chronic inflammation.
Type:
Grant
Filed:
September 6, 2018
Date of Patent:
April 5, 2022
Assignee:
Immunic AG
Inventors:
Jakob Felding, Hella Kohlhof, Manfred Groppel, Rolf Andreas Muhler, Daniel Vitt, Carine Chevrier, Mirko Zaja, Stefan Tasler
Abstract: The present invention provides compounds of Formula (I), or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
Abstract: The present invention relates to 1-imidazothiadiazolo-2H-pyrrol-5-one derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
Type:
Grant
Filed:
May 6, 2019
Date of Patent:
March 29, 2022
Inventors:
Hugues Chanteux, Yannick Quesnel, Claude Delatour, Laurent Provins
Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.
Abstract: A process for preparing the benzothiophen-2-yl boronate of formula (VI) which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of proliferative disorders, such as cancer and tumor diseases.
Abstract: Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated to modulate the NMDA receptor.
Type:
Grant
Filed:
December 22, 2017
Date of Patent:
March 15, 2022
Assignee:
Cadent Therapeutics, Inc.
Inventors:
David R. Anderson, Robert A. Volkmann, Frank Menniti, Christopher Fanger, Yuelian Xu
Abstract: The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
Abstract: The present disclosure relates to compounds of formula I, which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.
Type:
Grant
Filed:
September 27, 2018
Date of Patent:
March 8, 2022
Assignee:
Bristol-Myers Squibb Company
Inventors:
Prasada Rao Jalagam, Satheesh Kesavan Nair, Manoranjan Panda, Ramakanth Sarabu, Jacob Swidorski, Brett R. Beno, Alicia Regueiro-Ren
Abstract: Compounds having the general structure A-L-B are presented wherein A and B are independently an E3 ubiquitin ligase protein binding ligand compound of formula 1A or 1B. Pharmaceutical compositions comprising these compounds and methods of use are also presented.
Type:
Grant
Filed:
April 13, 2018
Date of Patent:
March 1, 2022
Assignee:
University of Dundee
Inventors:
Alessio Ciulli, Chiara Maniaci, Scott J. Hughes, Andrea Testa
Abstract: The present invention provides a process for preparing a compound of the formula (II): wherein R2 is unsubstituted alkyl, characterized by reacting a compound of the formula (I): wherein R1 is hydrogen or a protecting group other than unsubstituted alkyl, with a compound of the formula: R2—OH, wherein R2 is as defined above, in the presence of a sodium salt and/or a magnesium salt.
Abstract: The present invention provides compounds of Formula (Ia) or (Ib):Formula (Ia) or (Ib), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
Type:
Grant
Filed:
December 18, 2018
Date of Patent:
March 1, 2022
Assignee:
Bristol-Myers Squibb Company
Inventors:
Peter Tai Wah Cheng, Yan Shi, Hao Zhang
Abstract: The invention provides capsaicinoid prodrug compounds (e.g., prodrugs of resiniferatoxin, tinyatoxin, iodoresiniferatoxin, and related compounds), pharmaceutical compositions, and their use in the treatment of medical conditions, such as pain, and in agonizing TRPV1 activity.
Abstract: The present invention relates to compounds of general formula (I), wherein the groups R1 and R2 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) 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 obesity.
Type:
Grant
Filed:
January 28, 2019
Date of Patent:
February 22, 2022
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Thomas Trieselmann, Cedrickx Godbout, Christoph Hoenke, Viktor Vintonyak
Abstract: A compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein variables are defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.
Type:
Grant
Filed:
August 9, 2018
Date of Patent:
February 22, 2022
Assignee:
Pfizer Inc.
Inventors:
Brian Stephen Gerstenberger, Andrew Fensome, Dafydd Rhys Owen, Matthew Frank Brown, Matthew Merrill Hayward, Felix Vajdos, Li Huang Xing, Stephen Wayne Wright
Abstract: Provided herein are compounds that inhibit MALT1, a protein whose activity is responsible for constitutive NF-?B signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating MALT1-related diseases and disorders (e.g., cancer) with the compounds in a subject, by administering the compounds and/or compositions described herein.
Type:
Grant
Filed:
March 8, 2018
Date of Patent:
February 15, 2022
Assignees:
Cornell University, Dana-Farber Cancer Institute, Inc.
Inventors:
Nathanael S. Gray, David A. Scott, John Hatcher, Ari M. Melnick, Lorena Fontan Gabas
Abstract: RhlR modulators including agonist and antagonists which are useful for modulating QS phenotypes in Gram-negative bacteria. Certain compounds of general formula A-W-HG having various carbocyclic ad heterocyclic head groups (HG) and various tail groups (A), where —W— is —CO—NH—, —SO2—NH—, —CO—NH—CH2—, or —SO2—NH—CH2— are RhlR agonists or antagonists. The compounds are useful in methods of modulating quorum sensing in Gram-negative bacteria, particularly in Pseudomonas. Compositions including certain RhlR modulators are useful for decreasing the virulence of Gram-negative bacteria. Pharmaceutical compositions comprising certain RhlR modulators are useful for treatment of infections of Gram-negative bacteria.
Type:
Grant
Filed:
April 30, 2017
Date of Patent:
February 15, 2022
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Helen Blackwell, Michelle E. Boursier, Joseph D. Moore
Abstract: Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
Type:
Grant
Filed:
October 22, 2019
Date of Patent:
February 1, 2022
Assignee:
Gilead Sciences, Inc.
Inventors:
Zhimin Du, Michael Graupe, Paulo A. Machicao Tello, Jonathan William Medley, Samuel E. Metobo, Eric Q. Parkhill, Barton W. Phillips, Scott P. Simonovich, Peiyuan Wang, Jie Xu, Christopher A. Ziebenhaus
Abstract: The present invention relates to novel solid forms of compound (I) [(1S)-1-[(2S,4R,5R)-5-(5-amino-2-oxo-thiazolo[4,5-d]pyrimidin-3-yl)-4-hydroxy-tetrahydrofuran-2-yl]propyl] acetate and pharmaceutical compositions comprising the solid forms thereof disclosed herein, which may be used as a TLR7 agonist, or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.