Abstract: The present invention refers to a process for reacting an alkyl aryl ketone obtaining thereby the corresponding aryl oxirane or ?-functionalized alkyl aryl ketal, the aryl oxirane or ?-functionalized alkyl aryl ketal obtained by the process as well as the ?-functionalized ketone obtained by the process.
Abstract: A use of of ligustrazine nitrone derivatives and a pharmaceutical composition thereof in the preparation of medicine for preventing and treating diabetic complication diseases. The ligustrazine nitrone derivatives can be prepared into various dose forms together with drug carriers.
Type:
Grant
Filed:
May 25, 2018
Date of Patent:
December 14, 2021
Inventors:
Yuqiang Wang, Yewei Sun, Lipeng Xu, Mei Jing, Zaijun Zhang, Gaoxiao Zhang, Pei Yu, Peng Yi
Abstract: Embodiments of the present disclosure provide for biaryl ligands (also referred to herein as “biaryl compound”), biaryl complexes, methods of making biaryl compounds, methods of making single enantiomers of these biaryl compounds, methods of use (e.g., catalysis), and the like.
Type:
Grant
Filed:
February 17, 2020
Date of Patent:
December 14, 2021
Assignee:
University of Florida Research Foundation, Inc.
Abstract: Described herein are methods of administering the non-steroidal anti-inflammatory drug norketotifen, an isomer, an isomeric mixture, a prodrug, or a pharmaceutically acceptable salt thereof for the treatment of a respiratory disorders such as COPD and asthma to human patient in need of such treatment, without exposing said patient to adverse immune-suppressive effects. Methods include treating acute and potentially life-threatening exacerbations of COPD and asthma with norketotifen.
Type:
Grant
Filed:
February 17, 2021
Date of Patent:
December 14, 2021
Assignee:
BRIDGE PHARMA INC.
Inventors:
A. K. Gunnar Aberg, Vincent B. Ciofalo, Kresimir Pucaj
Abstract: The present disclosure provides a compound of Formula (I?): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein Rx, X1, X2, and R1 are as defined herein, and methods of making and using same.
Type:
Grant
Filed:
July 8, 2019
Date of Patent:
December 7, 2021
Assignee:
Novartis AG
Inventors:
Claire Adcock, Simone Bonazzi, Artiom Cernijenko, Philip Lam, Kathryn Taylor Linkens, Hasnain Ahmed Malik, Noel Marie-France Thomsen, Michael Scott Visser
Abstract: Disclosed herein are methods of making (4aR,6S,8aR)-6-((R)-1-hydroxyethyl)-6,8a-dihydropyrano[3,2-b]pyran-2-(4aH)-one (2) and methods of making (4aR,6S,8aR)-6-cyano-6,8a-dihydropyrano-[3,2-b]pyran-2(4aH)-one (4). Other pyranopyrans were also synthesized. Also compositions containing (4aR,6S,8aR)-6-cyano-6,8a-dihydropyrano-[3,2-b]pyran-2(4aH)-one (4) (or other pyranopyrans described herein) and optionally a carrier. In addition, methods for killing microorganisms or weeds on or in an object or area involving contacting the object or area with an effective microorganisms or weeds killing amount of a composition containing (4aR,6S,8aR)-6-cyano-6,8a-dihydropyrano-[3,2-b]pyran-2(4aH)-one (4) (or other pyranopyrans described herein) and optionally a carrier.
Type:
Grant
Filed:
September 23, 2019
Date of Patent:
December 7, 2021
Assignees:
The United States of America, as represented by The Secretary of Agriculture, Villanova University
Inventors:
Kevin Schrader, Stephen O. Duke, Robert M. Giuliano
Abstract: There is a continuing need for methods and compositions relating to hormone-receptor-dependent cancers, including pharmaceutical compositions including one or more compounds having activity against steroid hormone-receptor-dependent cancer and methods of treatment of a steroid hormone-receptor-dependent cancer in a subject using said pharmaceutical compositions. ELK1 is a steroid hormone receptor tethering, protein that is implicated in hormone receptor dependent cancers. Compositions and methods according to aspects of the present invention inhibit the association of steroid hormone receptors with ELK1 providing activity against steroid hormone-receptor-dependent cancer.
Abstract: Compounds of the formula I in which X1, X2, X3, X4, R1, R2, R3, Q and Y have the meanings indicated in claim 1, are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.
Type:
Grant
Filed:
February 20, 2020
Date of Patent:
November 30, 2021
Assignee:
MERCK PATENT GMBH
Inventors:
Dieter Dorsch, Mathilde Muzerelle, Lars Burgdorf, Margarita Wucherer-Plietker, Paul Czodrowski, Christina Esdar, Christos Tsaklakidis
Abstract: The present disclosure provides a compound of Formula (I?): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein Ra, Rb, Rx, R1, R2, X2, and q are as defined herein, and methods of making and using same.
Type:
Grant
Filed:
July 8, 2019
Date of Patent:
November 30, 2021
Assignee:
Novartis AG
Inventors:
Rohan Eric John Beckwith, Simone Bonazzi, Artiom Cernijenko, Fupeng Ma, Nathaniel F. Ware
Abstract: Disclosed is a new crystal form of a 5-aminopyrazole carboxamide compound as shown in Formula (I). Also disclosed are a preparation method for said crystal form of said compound, a pharmaceutical composition of said crystal form of said compound, and uses thereof.
Type:
Grant
Filed:
November 8, 2018
Date of Patent:
November 23, 2021
Assignee:
SinoMab BioScience Limited
Inventors:
Yuchuan Wu, Xi Chen, Shaoqiang Huang, Yonghan Hu
Abstract: Processes for converting a hydrocarbon reactant into an alcohol compound and/or a carbonyl compound are disclosed, and these processes include the steps of forming a supported chromium catalyst comprising chromium in a hexavalent oxidation state, irradiating the hydrocarbon reactant and the supported chromium catalyst with a light beam at a wavelength in the UV-visible spectrum to reduce at least a portion of the supported chromium catalyst to form a reduced chromium catalyst, and hydrolyzing the reduced chromium catalyst to form a reaction product comprising the alcohol compound and/or the carbonyl compound. The supported chromium catalyst can be formed by heat treating a supported chromium precursor, contacting a chromium precursor with a solid support while heat treating, or heat treating a solid support and then contacting a chromium precursor with the solid support.
Type:
Grant
Filed:
September 14, 2020
Date of Patent:
November 23, 2021
Assignee:
Chevron Phillips Chemical Company, LP
Inventors:
Carlos A. Cruz, Masud M. Monwar, Max P. McDaniel, Jared L. Barr, Kathy S. Clear, William C. Ellis
Abstract: Two enantiomers of a SElective Glucocorticoid Receptor Agonistic Modulator (SEGRAM) of Formula 1 or a derivative thereof; to a deuterated form of a SEGRAM of Formula 1 or a derivative thereof; and to the two deuterated enantiomers of a SEGRAM of Formula 1 or a derivative thereof: or a pharmaceutically acceptable salt, solvate and/or prodrug thereof. The present invention also relates to a SEGRAM of Formula 1 or a derivative thereof, or a pharmaceutically acceptable enantiomer, deuterated form, salt, solvate and/or prodrug thereof, for use in the prevention or treatment of an inflammatory disorder in a subject in need thereof.
Type:
Grant
Filed:
October 23, 2018
Date of Patent:
November 23, 2021
Assignee:
ASSOCIATION POUR LA RECHERCHE À L'IGBMC (ARI)
Abstract: Compounds and pharmaceutical compositions for use in the treatment of psoriasis are disclosed. Preferred compounds have demonstrated efficacy in reducing skin scaling, erythema and skin thickness in the mouse model of Aldara-induced psoriasis.
Type:
Grant
Filed:
March 22, 2018
Date of Patent:
November 23, 2021
Assignees:
SOLVOTRIN THERAPEUTICS LTD, THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH, NEAR DUBLIN
Inventors:
John Francis Gilmer, Mark Ledwidge, Pat O'Flynn, Francis Quilty, Kate O'Donnell
Abstract: The present invention concerns new therapeutical uses, including low dosage administration of the highly potent H3-ligand: (3S)-4-{4-[3-(3-methylpiperidin-1-yl)propoxy]phenyl}pyridine 1-oxide.
Type:
Grant
Filed:
March 21, 2018
Date of Patent:
November 23, 2021
Assignee:
BIOPROJET PHARMA
Inventors:
Jeanne-Marie Lecomte, Jean-Charles Schwartz, Olivier Labeeuw, Marc Capet
Abstract: Compounds of the formula I in which X1, X2, X3, X4, R1, R2, R3, Q and Y have the meanings indicated in Claim 1, are inhibitors of c-Kit kinase, and can be employed for the treatment of cancer.
Type:
Grant
Filed:
February 20, 2020
Date of Patent:
November 16, 2021
Assignee:
MERCK PATENT GMBH
Inventors:
Dieter Dorsch, Mathilde Muzerelle, Lars Burgdorf, Margarita Wucherer-Plietker, Paul Czodrowski, Christina Esdar, Christos Tsaklakidis
Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a triazole-methyl-piperidinyl-pyrolyl-propenone structure which function as modulators of shared epitope (SE)—calreticulin (CRT) binding and/or interaction, and their use as therapeutics for the treatment of immunoregulatory abnormalities (e.g., autoimmune diseases, inflammatory diseases (e.g., chronic inflammatory disease), and bone erosive diseases) by selectively inhibiting SE-CRT interactions and/or signal transduction pathways commonly overactive or dysregulated in arthritic and/or other diseases or conditions.
Type:
Grant
Filed:
June 9, 2020
Date of Patent:
November 9, 2021
Assignee:
The Regents of the University of Michigan
Abstract: An object of the present invention is to provide a novel composition for use in activating a sympathetic nerve. The present invention provides a composition for use in activating a sympathetic nerve, comprising a polyphenol as an active ingredient. The polyphenol comprises 25% by mass or more of monomeric to tetrameric polyphenols, and the monomeric to tetrameric polyphenols include at least catechin, epicatechin, procyanidin B2, procyanidin B5, procyanidin C1 and cinnamtannin A2.
Abstract: The present invention relates to a pharmaceutical composition comprising a DUSP1 inhibitor. The pharmaceutical composition comprising the DUSP1 inhibitor according to the present invention can solve the problems of inhibitors that target the active site because it inhibits DUSP1 by an allosteric inhibitory mechanism, and is effective for preventing or treating diseases involving DUSP1 enzymes, for example, a cancer such as a liver cancer, a breast cancer and a pancreatic cancer, a hepatitis C, and a depression. In particular, the DUSP1 inhibitor according to the present invention is very effective in treating a depression because it directly acts on neuronal growth.
Type:
Grant
Filed:
February 28, 2018
Date of Patent:
October 19, 2021
Assignees:
INDUSTRY-UNIVERSITY COOPERATION FOUNDATION HANYANG UNIVERSITY, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
Inventors:
Seong Eon Ryu, Tae Hyun Park, Kwang Hwan Lee, Ju Seop Kang, Shin Hee Kim, Kyoung Tae Nam, Hyeon Kyu Lee
Abstract: The present disclosure provides methods and compositions for the prevention, amelioration, or alleviation of one or more neurological disorders associated with microbially-induced amyloid formation. Methods of inhibiting, ameliorating, reducing the likelihood, delaying the onset of, treating, or preventing an amyloid disorder are disclosed. Methods of identifying compounds capable of inhibiting the formation of microbially-induced amyloid fibrils are disclosed.
Type:
Grant
Filed:
May 14, 2018
Date of Patent:
October 19, 2021
Assignees:
AXIAL THERAPEUTICS, INC., CALIFORNIA INSTITUTE OF TECHNOLOGY
Inventors:
Timothy Sampson, Sarkis Mazmanian, Anthony Stewart Campbell
Abstract: The present invention relates to a process for preparing a compound of formula (6) which is an intermediate for the preparation of eribulin mesylate with high yields and high purity, and an intermediate therefor.