Patents Examined by Kahsay Habte
  • IL-17 and IFN-gamma inhibition for the treatment of autoimmune diseases and chronic inflammation
    Patent number: 11292788
    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
  • Alkene spirocyclic compounds as farnesoid X receptor modulators
    Patent number: 11286252
    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.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: March 29, 2022
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jianxin Feng, Chunjian Liu, Yanting Huang
  • 1-imidazothiadiazolo-2H-pyrrol-5-one derivatives
    Patent number: 11286266
    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
  • Heterocyclic compound and use thereof
    Patent number: 11279713
    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.
    Type: Grant
    Filed: March 23, 2020
    Date of Patent: March 22, 2022
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masakuni Kori, Toshihiro Imaeda, Shinji Nakamura, Masashi Toyofuku, Eiji Honda, Yasutomi Asano, Osamu Ujikawa, Michiyo Mochizuki
  • Process for preparing benzothiophen-2yl boronate
    Patent number: 11274110
    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.
    Type: Grant
    Filed: October 18, 2018
    Date of Patent: March 15, 2022
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Jörg Gries, Johannes Platzek
  • NMDA receptor modulators and uses thereof
    Patent number: 11274107
    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
  • Fungicidal oxadiazoles
    Patent number: 11266147
    Abstract: The present invention relates to heterocyclylaminophenyloxadiazole and derivatives thereof that may be used and as fungicides.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: March 8, 2022
    Assignee: BAYER AKTIENGESELLSCHAFT
    Inventors: Anne-Sophie Rebstock, Sebastien Naud, Stephane Brunet, Mathieu Gourgues, Harald Jakobi, Andreas Goertz, Emmanuelle Hilt, Sophie Ducerf
  • Highly active amino-thiazole substituted indole-2-carboxamides active against the hepatitis B virus (HBV)
    Patent number: 11267825
    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.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: March 8, 2022
    Assignee: AICURIS GMBH & CO. KG
    Inventors: Alastair Donald, Andreas Urban, Susanne Bonsmann, Anita Wegert, Christiaan Gremmen, Jasper Springer
  • Small molecule inhibitors of galectin-3
    Patent number: 11267811
    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
  • Small molecules
    Patent number: 11261179
    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
  • Process for preparing substituted polycyclic pyridone derivative and crystal thereof
    Patent number: 11261198
    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.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: March 1, 2022
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Setsuya Shibahara, Kosuke Anan
  • Cyclohexyl acid isoxazole azoles as LPA antagonists
    Patent number: 11261180
    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
  • Compound as GLS1 inhibitor
    Patent number: 11254666
    Abstract: A compound as a GLS1 inhibitor as represented by formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 13, 2018
    Date of Patent: February 22, 2022
    Assignee: MEDSHINE DISCOVERY INC.
    Inventors: Yonggang Liao, Chaonan Liu, Changqing Wei, Hao Wu, Shuhui Chen
  • Capsaicinoid prodrug compounds and their use in treating medical conditions
    Patent number: 11254659
    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.
    Type: Grant
    Filed: January 17, 2020
    Date of Patent: February 22, 2022
    Assignee: Centrexion Therapeutics Corporation
    Inventors: James N. Campbell, Scott M. Duncan
  • Benzyl-, (pyridin-3-yl)methyl -or (pyridin-4-yl)-methyl-substituted oxadiazolopyridine derivatives as ghrelin O-acyl transferase (GOAT) inhibitors
    Patent number: 11254688
    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
  • Pyrazolo[1,5-A]pyrazin-4-yl and related derivatives
    Patent number: 11254668
    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
  • Inhibitors of MALT1 and uses thereof
    Patent number: 11248007
    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
  • Synthetic ligands that modulate the activity of the RhlR quorum sensing receptor
    Patent number: 11247976
    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
  • PD-1/PD-L1 inhibitors
    Patent number: 11236085
    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
  • Solid forms of [(1 S)-1 -[(2S,4R,5R)-5-(5-amino-2-oxo-thiazolo[4,5-D]pyrimidin-3-yl)-4-hydroxy-tetrahydrofuran-2-Yl]proptl] acetate
    Patent number: 11230559
    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.
    Type: Grant
    Filed: January 4, 2018
    Date of Patent: January 25, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Katja Grosse-Sender, Urs Schwitter, Frank Stowasser, Xuemei Wang, Jing Xiong