Abstract: Disclosed herein are compounds of the formula: as well as analogs thereof, wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used to modulate the activity of IL-17 and ROR?. Also provided are methods of administering compounds and composition provided herein to a patient in need thereof, for example, for the treatment or prevention of diseases or disorders associated with inflammation or for autoimmune disorders.
Type:
Grant
Filed:
June 17, 2019
Date of Patent:
May 28, 2024
Assignee:
REATA PHARMACEUTICALS, INC
Inventors:
Xin Jiang, Melean Visnick, Christopher F. Bender, Gary Bolton, Bradley Caprathe, Chitase Lee, Brian Kornberg, Patrick O'Brien, Martha R. Hotema
Abstract: This disclosure provides compositions and methods for altering or changing the tissue tropism, e.g., liver tropism, of adeno-associated viruses (AAV).
Type:
Grant
Filed:
May 10, 2019
Date of Patent:
May 21, 2024
Assignees:
Massachusetts Eye and Ear Infirmary, The Schepens Eye Research Institute, Inc.
Inventors:
Luk H. Vandenberghe, Pauline Schmit, Christopher Tipper, Carmen Unzu, Eric Zinn
Abstract: Disclosed are small molecule PTPRD inhibitors and uses thereof. Methods of using the PTPRD inhibitors include methods of treating, preventing, or delaying the progression of a disorder responsive to PTPRD inhibition, including for example nicotine dependence, addiction, obesity, metabolic syndrome, and substance-use disorders such as stimulant-use disorders and opioid-use disorders.
Type:
Grant
Filed:
May 2, 2022
Date of Patent:
May 21, 2024
Assignees:
Arizona Board of Regents on Behalf of the University of Arizona, The United States Government as respresented by the Department of Veterans Affairs, The University of Kentucky Research Foundation
Inventors:
George Richard Uhl, Ian M. Henderson, Wei Wang, Thomas Prisinzano
Abstract: The present invention relates to a solid pharmaceutical preparation comprising ?-lipoic acid, dicalcium phosphate and a binder. The solid pharmaceutical preparation has an improved stability and thereby improved bioavailability.
Abstract: Methods are provided for preventing, reducing, and/or treating contrast-induced acute kidney injury which include administering an inhibitor of fatty acid oxidation to a patient in need thereof. Also provided are methods involving use of trimetazidine or pharmaceutically acceptable salts thereof for the prevention and/or treatment of contrast-induced acute kidney injury. Methods are also provided for preventing and/or treating contrast-induced acute kidney injury which include administration of one or more of trimetazidine, etomoxir, oxfenicine, perhexiline, mildronate, or ranolazine, or pharmaceutically acceptable salts of any of the preceding.
Abstract: The present disclosure relates to the use of 1-[4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl]-2-fluorophenyl]-3-phenylurea or 1-(5-(7-amino-1-ethyl-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-4-bromo-2-fluorophenyl)-3-phenylurea, or a pharmaceutically acceptable salt thereof, in combination with a MAPKAP kinase inhibitor for the treatment of cancers, including c-KIT-mediated cancers, such as GIST.
Type:
Grant
Filed:
July 30, 2020
Date of Patent:
May 21, 2024
Assignee:
Deciphera Pharmaceuticals, LLC
Inventors:
Daniel L. Flynn, Bryan D. Smith, Anu Gupta
Abstract: The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof, is useful as an agent for the prophylaxis or treatment of narcolepsy.
Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
Type:
Grant
Filed:
June 23, 2021
Date of Patent:
May 21, 2024
Assignee:
Celgene Quanticel Research, Inc.
Inventors:
Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
Abstract: The invention concerns methods for preventing the reduction of disulfide bonds during the recombinant production of disulfide-containing polypeptides. In particular, the invention concerns the prevention of disulfide bond reduction during harvesting of disulfide-containing polypeptides, including antibodies, from recombinant host cell cultures.
Type:
Grant
Filed:
January 11, 2024
Date of Patent:
May 21, 2024
Assignee:
Genentech, Inc.
Inventors:
Yung-Hsiang Kao, Michael W. Laird, Melody Trexler Schmidt, Rita L. Wong, Daniel P. Hewitt
Abstract: A new synthetic route to 4,4?-diiodoazobenzene compound using homooxidative cross-coupling of an aryl diazonium salt using a Cu-catalyzed Sandmeyer-style reaction.
Abstract: The present disclosure relates generally to aromatic derivatives that are inhibitors of FGFR4 and are useful in treating FGFR4-associated diseases or conditions. Compositions containing the compounds of the present disclosure are also provided.
Type:
Grant
Filed:
February 19, 2020
Date of Patent:
May 7, 2024
Assignee:
BIOARDIS LLC
Inventors:
Ding Wang, Ning Shao, Hongbin Yuan, Frank Kayser
Abstract: Disclosed herein are methods for preparing [(2S,3R)āNā[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound āGā): and precursors thereof.
Type:
Grant
Filed:
October 13, 2022
Date of Patent:
May 7, 2024
Assignee:
KEZAR LIFE SCIENCES, INC.
Inventors:
Henry Johnson, Sean Dalziel, Dustin McMinn
Abstract: Provided herein are compounds of Formula (I). Methods for the preparation of the compounds of Formula (I) and intermediates useful in the preparation of the compounds of Formula (I) are described herein. The compounds of Formula (I) may be useful as inhibitors of the MYST family of lysine acetyltransferases (KATs) for the treatment of and/or prophylaxis of hyperproliferative diseases, disorders or conditions such as cancer. In particular, the compounds of Formula (I) are useful for the inhibition of KAT6A and KAT6B which are enzymes frequently mutated, overexpressed, amplified and/or translocated in cancer altering their normal expression, activity and function. The use of the compounds of Formula (I) in the manufacture of pharmaceutical compositions or for treating cancers is further described, including for treating cancer in combination with other anti-cancer agents.
Abstract: This invention provides methods for synthesizing phentolamine mesylate from phentolamine and methanesulfonic acid in the presence of acetone and water. The methods of the present invention provide highly pure phentolamine mesylate. The invention also provides highly pure phentolamine mesylate.
Abstract: The present invention provides salts and crystalline forms of Linsitinib (OSI-906; cis-3-[8-amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutanol). These forms of Linsitinib provide increased solubility and improved pharmacokinetic profiles for orally administered pharmaceutical formulations. Accordingly, the invention enables improved methods for treating human insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) mediated conditions.