Abstract: The invention discloses a 4-(N-methyl) aminopiperidine myricetin derivative containing dithiocarbamate, and its preparation method and application, whose structural general formula is shown as follows: wherein R is substituted phenyl and substituted aromatic heterocyclic group; n is the number of carbons in the carbon chain, which are 2, 3, 4 and 5 respectively; the substitute phenyl group is an alkyl group containing C1-6, alkoxy group containing C1-6, nitro group, halogen atom or hydrogen atom in ortho-, meta- and para-position on that benzene ring; the aromatic heterocyclic group is thienyl, furyl, pyrrolyl and pyridyl groups; the substituents on the substituted aromatic heterocycle are o-, m-, and p-containing C1-6 alkyl, C1-6 alkoxy, nitro, halogen, and hydrogen atoms. The invention has better inhibitory activity on cancer cells.
Type:
Grant
Filed:
December 5, 2019
Date of Patent:
July 23, 2024
Assignee:
Guizhou University
Inventors:
Wei Xue, Shichun Jiang, Ziyou Huai, Xu Tang, Yinjiu Huang, Liwei Liu, Mei Chen, Jun He, Shijun Su
Abstract: Disclosed multifunctional compounds, conjugates, macromolecules, and polymers that target dysregulated proteins for degradation. Also disclosed are methods of preparation, compositions, kits, and methods of use relating to the degraders.
Type:
Grant
Filed:
November 10, 2020
Date of Patent:
July 23, 2024
Assignees:
Massachusetts Institute of Technology, Dana-Farber Cancer Institute, Inc.
Inventors:
Jeremiah A. Johnson, Hung Vanthanh Nguyen, Yivan Jiang, Alexandre Detappe, Michael Agius, Irene Ghobrial, XueZhou Wang
Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting ALK2 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with ALK2 activity such as cancer.
Type:
Grant
Filed:
June 9, 2022
Date of Patent:
July 9, 2024
Assignee:
Incyte Corporation
Inventors:
Jun Pan, Jeremy Roach, Song Mei, Chunhong He, Liangxing Wu, Wenqing Yao
Abstract: This disclosure generally relates to therapeutic conjugates that covalently bind to a biological target. Methods of administering the compositions to a subject in need thereof are also provided herein.
Type:
Grant
Filed:
September 28, 2022
Date of Patent:
July 9, 2024
Assignee:
Totus Medicines Inc.
Inventors:
Neil Sonin Dhawan, James Abellera Blair, Robert B. Perni
Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1 or a salt thereof, wherein q, r, s, Q, R1, R2?, R2?, R3 and R4 are as defined herein.
Type:
Grant
Filed:
February 15, 2022
Date of Patent:
July 2, 2024
Assignee:
Heptares Therapeutics Limited
Inventors:
Giles Albert Brown, Julie Cansfield, Mark Pickworth, Benjamin Gerald Tehan, Barry John Teobald
Abstract: The present invention describes the administration of an NK1 antagonist, in combination with neostigmine methylsulfate, intravenously, via subcutaneous infusion, or both intravenously and via subcutaneous infusion to facilitate the treatment of a patient suffering from myasthenia gravis by providing a therapeutically effective neostigmine methylsulfate daily dose without the dose-limiting gastrointestinal adverse effects associated with neostigmine methylsulfate.
Abstract: The present disclosure relates to a ready-to-administer (RTA), intravenous (IV) bag presentation for hydromorphone. In particular, the present disclosure relates to terminally sterilized liquid formulations comprising hydromorphone hydrochloride in sodium chloride packaged in an RTA IV bag. The present disclosure also relates to methods of treating patients by administration of such formulations and RTA IV bags containing such formulations.
Abstract: Pulmonary hypertension is a progressive disease of various origins that is associated with vascular remodelling and results in right heart dysfunction. Accumulating evidence indicates important roles of immune cells and inflammatory chemokines in the pathogenesis and progression of pulmonary hypertension. We have identified CCL21 as anti-remodelling efficacy biomarker for pulmonary hypertension. CCL21 was found to be highly sensitive and specific in discriminating pulmonary hypertension patients from matched controls. CCL21 was upregulated in pulmonary hypertension and down-regulated with treatment with an anti-remodelling agent.
Type:
Grant
Filed:
February 17, 2022
Date of Patent:
June 18, 2024
Assignee:
Novartis AG
Inventors:
Marianna Rowlands, Clemence Anne Jeanne Marie Tessier, Paul Andrew Whittaker
Abstract: Disclosed are an oral solid dosage form composition comprising an active ingredient and a solubilizing carrier wherein a foaming ingredient is used to improve disintegration, dispersion or dissolution, and a preparation method therefor.
Type:
Grant
Filed:
October 30, 2018
Date of Patent:
May 14, 2024
Assignee:
SAMYANG HOLDINGS CORPORATION
Inventors:
Sang Yeob Park, Hye Jung Lim, Jae Young Lee, Min Hyo Seo, Sa Won Lee
Abstract: Disclosed herein is a method for preparing a 2-arylmalonic acid derivative. In this method, a cyclohexadiene compound is used as a raw material, and sequentially undergoes an isomerization reaction, a halogenation reaction in the presence of a halogenating agent and a dehydrohalogenation-aromatization reaction to obtain a 2-arylmalonic acid derivative (3). An intermediate for preparing the 2-arylmalonic acid derivative (3) and use of the intermediate are also disclosed.
Abstract: The present disclosure provides compounds having the general formula P-L-U, or pharmaceutically acceptable salts thereof, wherein P is a FOXO1 fusion protein binding moiety, L is a bivalent linker, and U is an ubiquitin ligase binding moiety. Also provided are pharmaceutical compositions containing such compounds and methods of using such compounds.
Type:
Grant
Filed:
September 16, 2022
Date of Patent:
April 23, 2024
Assignees:
Massachusetts Institute of Technology, Universität Zürich
Inventors:
Angela Nicole Koehler, Shelby Doyle, Becky Leifer, Madeleine Henley, Beat W. Schaefer, Marco Wachtel
Abstract: Composition for use in the prevention and/or treatment of a mitochondrial dysfunction-related neurodegenerative diseases, the composition comprising an active agent, said active agent containing the amino acids leucine, isoleucine, valine, threonine, lysine and citric acid, succinic acid, malic acid.
Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.
Type:
Grant
Filed:
August 4, 2023
Date of Patent:
April 9, 2024
Assignee:
LABORATORIOS LEON FARMA SA
Inventors:
Philippe Perrin, Jose Luis Velada, Dominique Drouin
Abstract: Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising a Cbl-b inhibitor and a cancer vaccine, as well as methods for treating cancer using a Cbl-b inhibitor and a cancer vaccine; and pharmaceutical compositions comprising a Cbl-b inhibitor and an oncolytic virus, as well as methods for treating cancer using a Cbl-b inhibitor and an oncolytic virus.
Type:
Grant
Filed:
July 13, 2022
Date of Patent:
April 9, 2024
Assignee:
NURIX THERAPEUTICS, INC.
Inventors:
Arthur T. Sands, Neil F. Bence, Christoph W. Zapf, Frederick Cohen, Chenbo Wang, Thomas Cummins, Hiroko Tanaka, Hunter Shunatona, Mario Cardozo, Dahlia Weiss, Jennifa Gosling
Abstract: Disclosed are conjugate molecules formed from an active agent which is linked to a cannabinoid moiety through a specified linker having ester and amide end groups. The active agent can be a COX-2 inhibitor moiety, and the cannabinoid moiety can be a cannabidiol moiety. These conjugate molecules are contemplated to potentially be effective in the treatment of medical conditions.
Type:
Grant
Filed:
April 21, 2023
Date of Patent:
April 2, 2024
Assignee:
AKOS BIOSCIENCES, INC.
Inventors:
Paul M. Hershberger, Yinghui Liu, Kirk William Hering, James Bernard Kramer, Ramanathan S. Lalgudi
Abstract: Disclosed herein are 5-Substituted 4-amino-1H-benzo[c][1,2,6]thiadiazine 2,2-dioxide compounds useful as sweet flavor modifiers. Also disclosed herein are ingestible compositions that include one or more of these compounds in combination with a natural or artificial sweetener.
Type:
Grant
Filed:
August 6, 2019
Date of Patent:
April 2, 2024
Assignee:
FIRMENICH INCORPORATED
Inventors:
Joseph R. Fotsing, Catherine Tachdjian, Guy Servant, Brett Weylan Ching, Timothy Davis
Abstract: The present invention relates to compounds of Formula I, pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I increase significantly low density lipoprotein receptor and are useful for preventing and treating of elevated cholesterol.
Type:
Grant
Filed:
May 23, 2022
Date of Patent:
March 19, 2024
Assignee:
Montréal Heart Institute
Inventors:
Steve Poirier, Brent Richard Stranix, Gaétan Mayer
Abstract: This invention relates to new crystalline forms of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile(lorlatinib) maleate. The invention also relates to pharmaceutical compositions comprising lorlatinib maleate, and to methods of using lorlatinib maleate and compositions comprising it in the treatment of abnormal cell growth, such as cancer, in mammals.
Abstract: The present disclosure relates to a JAK inhibitor upadacitinib intermediate and a preparation method therefor, and to a preparation method for a JAK inhibitor upadacitinib. The upadacitinib intermediate of the present application is as shown in Formula (II) or Formula (III), wherein, R is a protective group of nitrogen atoms, and R1 is an open-chain or cyclic amine group. Compared with the prior art, the method for the synthesis of upadacitinib of the present application, significantly reduces cost, is environmentally-friendly. And the quality of the final product is well controlled.