Abstract: The present application provides a method for synthesis of Roxadustat. A compound as represented by formula (VIII) is used as a raw material, and is reacted with phenol, a vinyl-containing ether, an acid, hydroxylamine, and then the product is reacted with glycine. In addition, the present application also provides intermediate compounds as represented by formula (IX), formula (XI), formula (XII), formula (IV), and formula (V) for synthesis of Roxadustat.
Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof wherein Z, R1, R2, R3, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy. The present invention further provides methods of treating at least one disease, disorder, or condition associated with the glutamatergic and GABAergic signalling pathways regulated in full or in part by metabotropic glutamate receptor 7 (mGluR7) by administering a compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject. The compound may be a selective agonist of mGluR7, which modulates the release of at least one neurotransmitter in the subject.
Type:
Grant
Filed:
November 17, 2017
Date of Patent:
October 11, 2022
Assignee:
TAKEDA PHARMACEUTICAL COMPANY LIMITED
Inventors:
Martin Teall, Kathryn White, Stephen Mack, Gemma Liwicki, Anne Stephenson, Louise Dickson
Abstract: Toll-like receptor 8 (TLR8)-specific inhibitors and methods of using the same in individuals having an autoimmune disease or an inflammatory disorder.
Type:
Grant
Filed:
October 30, 2018
Date of Patent:
October 11, 2022
Assignee:
THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE
Inventors:
Hang Hubert Yin, Shuting Zhang, Zhenyi Hu
Abstract: Benzyl derivative compounds having peroxisome proliferator-activated receptor ? (PPAR?) agonistic activity, compositions containing such compounds, and methods of their use in enhancing PPAR? activity for treating diseases and/or conditions involving inflammation and/or angiogenesis, particularly ocular diseases and/or conditions such as but not limited to retinal inflammation, retinal neovascularization, retinal vascular leakage, retinopathy of prematurity, diabetic retinopathy, age-related macular degeneration, and diabetic macular edema are disclosed.
Type:
Grant
Filed:
March 15, 2019
Date of Patent:
September 20, 2022
Assignee:
The Board of Regents of the University of Oklahoma
Abstract: The present invention provides an anti-inflammatory compound, which is a compound having a structure (I) as shown below: The compound is a target that is important for autoimmune activation, and that has strong inhibitory effect on PDE4 and penetrates the skin easily, and is a new type anti-inflammatory compound that is easily degraded.
Abstract: The present invention provides, in part, a biodegradable compound of formula I, and sub-formulas thereof:Formula (I) or a pharmaceutically acceptable salt thereof, where each X independently is O or S, each Y independently is O or S, and each R1 independently is defined herein; and a liposome composition comprising the cationic lipid of formula I or a sub-formula thereof, and methods of delivering agents, such as nucleic acids including mRNA, in vivo, by administering to a subject the liposome comprising the cationic lipid of formula I or a sub-formula thereof, where the agent is encapsulated within the liposome.
Abstract: The present invention can synthesize lobaric acid and four analogues thereof, which are five phenolic lichen metabolites isolated from an extract of the Antarctic lichen Stereocaulon alpinum and selectively inhibit PTP1B, by a simple, economic and efficient chemical synthesis method.
Type:
Grant
Filed:
July 23, 2018
Date of Patent:
September 6, 2022
Assignee:
KOREA INSTITUTE OF OCEAN SCIENCE AND TECHNOLOGY
Inventors:
Joung Han Yim, Il-Chan Kim, Se Jong Han, Ui Joung Youn, Hong Kum Lee, Jun Hyuck Lee, Tai Kyoung Kim, Kwon Joo Yeo
Abstract: The present invention falls within the technical field of medicine, and in particular relates to PDE9 inhibitor compounds as shown in formula (I) or pharmaceutically acceptable salts or stereoisomers thereof, and also relates to pharmaceutical preparations and pharmaceutical compositions of the compounds and the uses thereof. X1, X2, X3, X4, R1, R2, ring A, L and m are as defined in the description. The compounds can be used to prepare drugs for treating or preventing related diseases mediated by PDE9.
Abstract: Disclosed herein are compounds, compositions, and methods of their use for the treatment of diabetes.
Type:
Grant
Filed:
August 20, 2020
Date of Patent:
August 30, 2022
Assignees:
THE SCRIPPS RESEARCH INSTITUTE, UNIVERSITÄT BREMEN
Inventors:
Hank Michael James Petrassi, Murali Mohan Reddy Peram Surakattula, Kathrin Maedler, Amin Ardestani, Jason T. Roland, Tyler D. Baguley, Matthew S. Tremblay, Weijun Shen, Peter G. Schultz, Arnab K. Chatterjee
Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Grant
Filed:
January 23, 2020
Date of Patent:
August 30, 2022
Assignee:
ChemoCentryx, Inc.
Inventors:
Christopher Lange, Viengkham Malathong, Darren J. McMurtrie, Sreenivas Punna, Rajinder Singh, Ju Yang, Penglie Zhang
Abstract: Provided herein are amino isoquinolinyl amide and sulfonamide compounds that affect the function of kinases and other proteins in a cell and that are useful as therapeutic agents. In particular, these compounds are useful in the treatment of eye diseases such as glaucoma and retinal diseases, as anti-inflammatory agents, for the treatment of cardiovascular diseases, and for diseases characterized by abnormal growth, such as cancers.
Type:
Grant
Filed:
September 13, 2019
Date of Patent:
August 30, 2022
Assignee:
Aerie Pharmaceuticals, Inc.
Inventors:
Mitchell A. deLong, Jill M. Sturdivant, Cynthia L. Lichorowic, Andriy Kornilov
Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
Type:
Grant
Filed:
May 1, 2020
Date of Patent:
August 16, 2022
Assignee:
VENATORX PHARMACEUTICALS, INC.
Inventors:
Christopher J. Burns, Denis Daigle, Bin Liu, Daniel McGarry, Daniel C. Pevear, Robert E. Lee Trout, Randy W. Jackson
Abstract: Described herein are compounds that are somatostatin modulators, 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 that would benefit from modulation of somatostatin activity.
Type:
Grant
Filed:
October 26, 2020
Date of Patent:
August 16, 2022
Assignee:
CRINETICS PHARMACEUTICALS, INC.
Inventors:
Jian Zhao, Sangdon Han, Sun Hee Kim, Shimiao Wang, Yunfei Zhu
Abstract: The present invention relates to a compound of formula (I): wherein P1, P3, P4 and P5 are amino acid residues or amino acid like structures. 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:
September 26, 2018
Date of Patent:
August 9, 2022
Assignees:
UNIVERSITE DE PARIS, INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE, SORBONNE UNIVERSITE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
Abstract: The present invention provides novel compounds (e.g., compounds of Formulae (I), (II), (III), (IV)) having tumor vascular remodeling effect and/or anti-CAF (Cancer Associated Fibroblasts) activity, or pharmaceutically acceptable salts thereof, optionally in a pharmaceutically acceptable carrier, and a medical uses thereof.
Type:
Grant
Filed:
November 15, 2018
Date of Patent:
August 9, 2022
Assignees:
President and Fellows of Harvard College, Eisai R&D Management Co., LTD.
Abstract: A method for preventing and/or treating fibrosis associated with a reproductive tract or digestive tract disease or disorder includes administering an effective amount of a multikinase inhibitor to an animal or human in need thereof. The multikinase inhibitor comprises axitinib, nintedanib, sunitinib, lenvatinib, regorafenib, ponatinib, pazopanib, riociguat, or a salt thereof. The reproductive tract or digestive tract disease or disorder comprises uterine fibroids or primary sclerosing cholangitis, including Intra uterine surgery, intra uterine synechiae, Asherman's syndrome, biliary duct fibrosis, biliary duct sclerosis, and primary biliary cirrhosis.
Abstract: The Invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, or diastereomers thereof: wherein W1, W2, W3, J1, J2, A, R1, R2, R3, R4, R5, a, and b are defined as set forth in the specification. The Invention also provides uses of the compounds of any one of Formulae (I)-(VIII) and the pharmaceutically acceptable salts, solvates, hydrates, N-oxides, or diastereomers thereof. Compounds of the Invention are useful for treating a disorder responsive to blockade of one or more sodium channels. In certain embodiments, Compounds of the Invention are useful for treating pain.
Abstract: Disclosed herein are compounds that can act as inhibitors of the Kelch-like ECH-associated protein 1/nuclear factor (erythroid-derived 2)-like 2 (“KEAP1/NRF2”) protein-protein interaction, and methods of using the compounds to treat and prevent diseases and disorders, such as COPD, multiple sclerosis, and diabetes, and in the promotion of wound healing. The compounds described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: formula (I), wherein the substituents are as described.
Type:
Grant
Filed:
April 2, 2019
Date of Patent:
July 26, 2022
Assignee:
THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Inventors:
Terry Moore, Phillip Lazzara, Brian David, Benjamin Richardson, Atul D. Jain
Abstract: Compounds useful in the modulation of ion channel activity in cells are disclosed herein. This disclosure also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation.
Type:
Grant
Filed:
May 17, 2019
Date of Patent:
July 12, 2022
Assignee:
BIONOMICS LIMITED
Inventors:
Belinda Huff, Courtney Hollis, Hamish Toop, Nathan Kuchel, Lorna Helen Mitchell, Rajinder Singh