Abstract: A compound of formula (I) as defined herein, or a pharmaceutically acceptable salt thereof, being potent modulators of human TNF a activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
Type:
Grant
Filed:
October 23, 2019
Date of Patent:
January 17, 2023
Assignees:
UCB BIOPHARMA SRL, SANOFI
Inventors:
James Andrew Johnson, Ellen Olivia Gallimore, Mengyang Xuan
Abstract: Described herein is a process for the preparation of a compound of Formula I, wherein R1 and R2 each have the meanings provided in the description. Also described is a process for the preparation of pharmaceutically-active compounds including the process for the preparation of compounds of Formula I.
Abstract: The present disclosure provides compounds of Formula (I) or (II), pharmaceutically acceptable salt, isotopic variant, stereoisomer, or a mixture thereof. Also provided are pharmaceutical compositions comprising a compound, methods of treating a poly(ADP-ribose)polymerase-1-mediated disease or disorder in a subject, methods of detecting a poly(ADP-ribose)polymerase-1-mediated neurodegenerative disease or disorder, or methods of monitoring cancer treatment in a subject. In some embodiments, the poly(ADP-ribose)polymerase-1-mediated disease or disorder is a neurodegenerative disease or cancer.
Type:
Grant
Filed:
February 28, 2019
Date of Patent:
January 3, 2023
Assignee:
The Trustees of the University of Pennsylvania
Inventors:
Robert H. Mach, Sean W. Reilly, Mehran Makvandi, Laura Puentes
Abstract: A compound of Formula (I): pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof, wherein the variable substituents are disclosed herein.
Type:
Grant
Filed:
December 3, 2020
Date of Patent:
December 27, 2022
Assignee:
Gilead Sciences, Inc.
Inventors:
Stephen Ammann, Elizabeth M. Bacon, Gediminas Brizgys, Elbert Chin, Chienhung Chou, Jeromy J. Cottell, Marilyn Ndukwe, James G. Taylor, Nathan E. Wright, Zheng-Yu Yang, Sheila M. Zipfel
Abstract: Disclosed are spirocyclic compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and treating cancer, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.
Type:
Grant
Filed:
January 20, 2021
Date of Patent:
December 20, 2022
Assignee:
INCYTE CORPORATION
Inventors:
Le Zhao, Xiaozhao Wang, Wenyu Zhu, Haolin Yin, Liangxing Wu, Wenqing Yao
Abstract: The disclosure provides TNIK and/or MAP4K4 kinases inhibitors for the treatment of disease. In one aspect, disclosed herein are kinase inhibitors having a structure of Formula (A), (A*), (I), (IIA), or (IIB). Further described herein are pharmaceutical composition comprising these compounds and methods of using these compounds. In one aspect, disclosed herein are methods of treating a disease or condition by administering the kinases inhibitors described herein.
Type:
Grant
Filed:
February 23, 2022
Date of Patent:
December 20, 2022
Assignee:
Insilico Medicine IP Limited
Inventors:
Aleksandrs Zavoronkovs, Aleksandr Aliper, Vladimir Aladinskiy, Andrey Kukharenko
Abstract: The disclosure provides TNIK and/or MAP4K4 kinases inhibitors for the treatment of disease. In one aspect, disclosed herein are kinase inhibitors having a structure of Formula (A), (A*), (I), (IIA), or (IIB). Further described herein are pharmaceutical composition comprising these compounds and methods of using these compounds. In one aspect, disclosed herein are methods of treating a disease or condition by administering the kinases inhibitors described herein.
Type:
Grant
Filed:
February 23, 2022
Date of Patent:
December 20, 2022
Assignee:
Insilico Medicine IP Limited
Inventors:
Aleksandrs Zavoronkovs, Aleksandr Aliper, Vladimir Aladinskiy, Andrey Kukharenko
Abstract: Embodiments relate to a method for treatment of a sleep disorder and to compositions comprising tetrahydrocannabinol (THC), cannabidiol (CBD), and cannabinol (CBN), wherein the ratio of THC:CBD:CBN by weight is A:B:C where A is between 0.0001 and 1, B is 1, and C is between 0.05 and 1. Optionally A is between 0.001 and 0.02, B is 1 and C is between 0.2 and 0.7.
Type:
Grant
Filed:
October 24, 2018
Date of Patent:
November 22, 2022
Assignee:
DAY THREE LABS MANUFACTURING INC.
Inventors:
William Z. Levine, Shimon Lecht, Olga Gabay
Abstract: The invention relates to a process for the preparation of Lifitegrast of formula (I), which comprises: a) condensation of the compound of formula (II) with the compound of formula (III) to give the compound of formula (IV) wherein R1, R2 and R3 are independently selected from straight or branched C1-C6 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.
Type:
Grant
Filed:
June 13, 2019
Date of Patent:
November 15, 2022
Assignee:
OLON S.P.A.
Inventors:
Giorgio Bertolini, Lazzaro Feliciani, Davide Longoni, Mara Sada, Matteo Valli
Abstract: The compounds provided herein are phenoxazines that can be used as far red to near-infrared nerve-sparing fluorescent compounds in medical procedures.
Type:
Grant
Filed:
July 26, 2019
Date of Patent:
November 8, 2022
Assignee:
Oregon Health & Science University
Inventors:
Summer L. Gibbs, Lei G. Wang, Connor W. Barth
Abstract: The present invention relates to a compound, 4-amino-N-(1-((3-chloro-2-fluoro-4-hydroxyphenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide, and pharmaceutically acceptable salts thereof having inhibitory activity for protein kinases.
Type:
Grant
Filed:
November 29, 2018
Date of Patent:
November 8, 2022
Assignee:
Hanmi Pharm. Co., Ltd.
Inventors:
In Hwan Bae, Seung Hyun Jung, Young Gil Ahn, Kwee Hyun Suh
Abstract: Embodiments of the present invention provide for syntheses and uses of mechanism-based nutritional colorants from vitamin C and amino-containing compounds, wherein the amino-containing compounds can be one of natural compounds or synthetic compounds, wherein the amino-containing compounds can be made through environmentally-friendly radical reactions that follow the antioxidant mechanism of action of vitamin C.
Abstract: Disclosed herein are tetrahydropyranoindole compounds and derivatives thereof, as well as their methods of synthesis and use. The disclosed compounds may be synthesized by methods that utilize a cooperative hydrogen bond donor/Brønsted acid system. The disclosed compounds may be useful for treating a disease, disorder, or a symptom thereof in a subject in need thereof, such as pain, swelling, and joint stiffness. The disclosed compounds also may be useful for treating cell proliferative diseases and disorders such as cancer.
Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
Type:
Grant
Filed:
November 3, 2020
Date of Patent:
October 11, 2022
Assignee:
Vernalis (R&D) Limited
Inventors:
Samantha Jane Bamford, Roger John Gillespie, Richard Simon Todd
Abstract: Provided are compounds and compositions for prevention and/or elimination of Zika virus infection. Also provided are methods for preventing and treating a subject in need of prevention or treatment of Zika virus.
Type:
Grant
Filed:
March 19, 2018
Date of Patent:
October 11, 2022
Assignees:
Cornell University, The University of North Carolina at Chapel Hill
Inventors:
Shuibing Chen, Ting Zhou, Lei Tan, Qisheng Zhang
Abstract: A series of substituted spirocyclic indane derivatives of Formula (I), and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.
Type:
Grant
Filed:
July 8, 2019
Date of Patent:
October 4, 2022
Assignee:
UCBBiopharma Srl
Inventors:
Gareth Neil Brace, Daniel Christopher Brookings, Gregory Foulkes, Fabien Claude Lecomte
Abstract: In an aspect, the disclosure provides for compounds (II), compositions, and methods of administering the compounds and compositions to a patient in need thereof. In another aspect, the disclosure relates to compounds and compositions for treating cancer, for example, lymphoid leukemia. The disclosure further provides for compounds which inhibit two phosphoinositide 3-kinase (PI3K) isoforms, y and ?, pharmaceutical compositions comprising said compounds, and methods of using said compounds and pharmaceutical compositions for treatment, amelioration, and/or prevention of non-Hodgkin lymphoma.
Type:
Grant
Filed:
July 31, 2018
Date of Patent:
October 4, 2022
Assignee:
The Trustees of Columbia University in the City of New York
Inventors:
Donald W. Landry, Shi-Xian Deng, Xiaoming Xu, Thomas Diacovo
Abstract: Provided herein are methods for treating, delaying progression of, or reducing the severity of amyotrophic lateral sclerosis (ALS) in a subject through administration of therapeutically effective amounts of agents (e.g., JAK kinase inhibitors (e.g., tofacitinib)) capable of interfering with central nervous system related natural killer cell (NK) levels and function.
Type:
Grant
Filed:
April 22, 2020
Date of Patent:
September 27, 2022
Assignee:
The Regents of the University of Michigan
Inventors:
Eva L. Feldman, Ben Murdock, Stephen Goutman, Stacey Jacoby
Abstract: Disclosed are quinazoline compounds inhibiting ErbBs (e.g. HER2), pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds which are useful in treating diseases associated ErbBs. The compound and the pharmaceutical composition can effectively treat diseases associated ErbBs (especially HER2), including cancer.
Abstract: 10H-phenothiazine derivatives capable of inhibiting ferroptosis has structural formula (I). The derivatives, pharmaceutically acceptable salts thereof, crystal forms thereof, or solvates thereof exhibit inhibitory effect on ferroptosis, and therapeutic effect on a rat model of focal cerebral ischemia and thus can be used as a main active ingredient in the preparation of ferroptosis inhibitors. The compounds and the inhibitors prepared by the compounds have good medicinal potential and are expected to be used as drug candidates for the treatment of stroke.