Abstract: The invention provides methods of synthesis of enantiopure deuterium enriched R-pioglitazone with structure of compound (IV), or a pharmaceutically acceptable salt thereof: The invention further provides chemical intermediates useful in the synthesis of compound (IV), and methods of synthesizing those intermediates.
Type:
Grant
Filed:
June 28, 2021
Date of Patent:
September 26, 2023
Assignee:
Poxel SA
Inventors:
Laure Françoise Valérie Navarre, Vincent Jacques, Sébastien Bolze
Abstract: The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates.
Type:
Grant
Filed:
March 22, 2022
Date of Patent:
September 19, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Katrien Brak, Kae M. Bullock, Greg Cizio, Kathy Dao, Darryl D. Dixon, Joshua R. Dunetz, Luke D. Humphreys, Valerie Huynh, Michael A. Ischay, Trevor C. Johnson, Jeffrey E. Merit, Christopher S. Regens, Eric A. Standley, Dietrich P. Steinhuebel, Justin Y. Su, Tao Wu, Marshall D. Young
Abstract: A novel method for synthesizing deuterated amides and deuterated sulfonamides includes the following steps: (1) adding a compound M, DMAP, R3—X to a solvent to obtain a compound N after a reaction is complete; and (2) adding the compound N, R4—NH—R5, or a salt and base thereof to a solvent, and purifying after a reaction is complete to obtain a compound I.
Type:
Grant
Filed:
April 12, 2019
Date of Patent:
September 12, 2023
Assignee:
HINOVA PHARMACEUTICALS INC.
Inventors:
Wu Du, Kun Wen, Jinyun He, Haibo Li, Dekun Qin, Xinghai Li, Yuanwei Chen
Abstract: A process provides for minimizing an amount of fuel gas utilized in an absorber off-gas incinerator and better control of emissions. The process provides for less temperature deviations in the absorber off-gas incinerator firebox and for less deviation in an amount of oxygen in the absorber off-gas incinerator stack gas.
Type:
Grant
Filed:
May 4, 2017
Date of Patent:
September 5, 2023
Assignee:
INEOS EUROPE AG
Inventors:
Manoj Shrikant Shouche, Timothy Robert McDonel, Jay Robert Couch
Abstract: The present invention provides compositions and methods for inhibiting group II intron splicing for treating or preventing a disease or disorder associated with an organism harboring an active group II intron. The present invention also provides compositions and methods for inhibiting group II intron splicing for inhibiting, preventing or reducing growth of an organism harboring an active group II intron.
Type:
Grant
Filed:
January 25, 2019
Date of Patent:
August 29, 2023
Assignee:
YALE UNIVERSITY
Inventors:
Anna Pyle, Olga Fedorova, Erik Gunnar Jagdmann, Michael Van Zandt, Lin Yuan, Albert DeBerardinis
Abstract: The present invention relates to pharmaceutical tablet compositions comprising the compound niraparib as an active pharmaceutical ingredient, suitable for oral administration as well as to methods for their preparation. Also described herein are tablet compositions containing niraparib formed by the disclosed methods, and therapeutic uses of such tablet compositions for treating various disorders and conditions.
Type:
Grant
Filed:
September 26, 2018
Date of Patent:
August 22, 2023
Assignee:
Tesaro, Inc.
Inventors:
Simon McGurk, Padma Narayan, Aleksandar Rajlic
Abstract: Non-aqueous emulsion methods for producing polymeric or polymer-coated microparticles are provided. One method produces a sustained release microparticle composition by combining protein powder and a polymer into a hydrocarbon solvent to form a non-aqueous first solution and adding the first solution to a second solution, wherein the second solution comprises a fluorocarbon liquid and a fluorosurfactant to form a non-aqueous emulsion comprising multiple emulsion hydrocarbon droplets in the fluorocarbon liquid. The subsequent microparticle hardening process includes the steps of removing the hydrocarbon solvent from the formed emulsion droplets, which can be achieved through evaporation the hydrocarbon at ambient condition under stirring, or accelerated hardening through vacuum, or through adding hydrofluoroester into the fluorocarbon as a cosolvent.
Abstract: The present invention relates to compounds of formula (I): including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of, for example, cancer.
Type:
Grant
Filed:
August 29, 2018
Date of Patent:
August 22, 2023
Assignees:
MUSC Foundation for Research Development, Lukogene Therapeutics Incorporated
Inventors:
Nathan G. Dolloff, Reeder M. Robinson, Allen B. Reitz, Haiyan Bian
Abstract: Provided are crystals of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate, compositions comprising the same, and methods of making and using such crystals.
Type:
Grant
Filed:
August 27, 2021
Date of Patent:
August 15, 2023
Assignee:
Aeromics, Inc.
Inventors:
Paul Robert McGuirk, Robert Zamboni, Melanie Bevill, Stephan Parent
Abstract: The present application provides hydrogel microcapsules, particularly, canonized hydrogel microcapsules having improved substantivity. This application further relates to the use of hydrogel microcapsules for delivering encapsulated actives in a wide range of industries and applications including: agrochemicals, pharmaceuticals, cosmetics industry, personal care products, laundering detergents, homecare & cleaning products, dish washing detergents, oral care, dental care, textiles, paper, mining, oil industry, water treatment, adhesives, coatings, plastics, sealants, construction, paints, inks and dyes onto different substrate surfaces such as skin, hair, textiles.
Type:
Grant
Filed:
December 1, 2011
Date of Patent:
August 8, 2023
Assignee:
ISP Investments LLC
Inventors:
Kishor Kumar Mistry, Abdul Wahab Hussain, Petra Helga Beck, David Vaughan Palmer, Benjamin Roger Sales, Andrew Mint
Abstract: Presented herein is a coupling method for the preparation of 1,2-di(thiophen-2-yl)ethane-1,2-diol compounds, including (E)-1,2-di(thiophen-2-yl)ethene-1,2-diol, via a Cu(II) catalyst.
Type:
Grant
Filed:
December 30, 2021
Date of Patent:
August 8, 2023
Assignee:
QATAR UNIVERSITY
Inventors:
Ismail K. Warad, Amjad M. Shraim, Anas Al-Ali, Kifah S M Salih, Abdelkader Zarrouk, Yousef Hijji
Abstract: The present disclosure relates to the use of cannabidiol (CBD) for the reduction of total convulsive seizure frequency in the treatment of “treatment-resistant epilepsy” (TRE). In particular, the disclosure relates to the use of CBD of treating TRE when the TRE is Dravet syndrome; myoclonic absence seizures or febrile infection related epilepsy syndrome (FIRES). The disclosure further relates to the use of CBD in combination with one or more anti-epileptic drugs (AEDs).
Type:
Grant
Filed:
September 10, 2021
Date of Patent:
July 18, 2023
Assignee:
GW Research Limited
Inventors:
Geoffrey Guy, Stephen Wright, Orrin Devinsky
Abstract: The present disclosure relates generally to certain tetracyclic compounds, pharmaceutical compositions comprising said compounds, and methods of making said compounds and pharmaceutical compositions. The compounds of the disclosure are useful in treating or preventing human immunodeficiency virus (HIV) infection.
Type:
Grant
Filed:
February 23, 2021
Date of Patent:
July 11, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Lan Jiang, David W. Lin, Michael L. Mitchell, Ezra Roberts, Gregg M. Schwarzwalder
Abstract: A method of making a hydroxyl-terminated thioketal diol is provided, the method comprising reacting a thioketal ester with a non-pyrophoric reducing agent to form a hydroxyl-terminated thioketal diol. The hydroxyl-terminated thioketal diol can be 2,2-(propane-2,2-diylbis(sulfanediyl)) diethanol. The non-pyrophoric reducing agent can be a sodium aluminum hydride, for example, sodium bis (2-methoxyethoxy)aluminum hydride. The thioketal ester can be dimethyl 2,2-(propane-2,2-diylbis(sulfanediyl)) diacetate. A biodegradable matrix prepared by reacting a hydroxyl-terminated thioketal diol with an isocyanate is provided. A method of making a biodegradable polyurethane composite is also provided.
Type:
Grant
Filed:
May 24, 2021
Date of Patent:
June 20, 2023
Assignee:
Warsaw Orthopedic, Inc.
Inventors:
Roger E. Harrington, Jerbrena C. Jacobs, Robert Doyle
Abstract: The present disclosure is directed to novel crystalline forms of ozanimod and ozanimod hydrochloride, as well as preparation method thereof. Said crystalline forms of ozanimod and ozanimod hydrochloride can be used for treating autoimmune diseases, particularly used for preparing drugs for treating multiple sclerosis and ulcerative colitis. The crystalline forms of the present disclosure have one or more advantages in solubility, melting point, stability, dissolution, bioavailability and processability and provide new and better choices for the preparation of ozanimod drug product, and are very valuable for drug development.
Abstract: A colloidal dispersion of particles of silica having a particle size of from 3 nm to 100 nm, to which ions of one or more metals are adsorbed, selected from metals having atomic numbers 21-31, 39-46, 48-50, 57-82, and 89-93, and a method for preparing the dispersion. The dispersion may be used in various fields of use of metals.
Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Grant
Filed:
November 4, 2020
Date of Patent:
June 13, 2023
Assignee:
NOVARTIS AG
Inventors:
Kamlesh Jagdis Bala, Andrew Brearley, James Dale, Anne-Marie Edwards, Mahbub Ahmed, David Porter, Robert Alexander Pulz, Lisa Ann Rooney, David Andrew Sandham, Duncan Shaw, Nichola Smith, Jessica Louise Taylor, Roger John Taylor, Thomas Josef Troxler, Joe Wrigglesworth
Abstract: 4-Hydroxyphenyl-2H-indazol-5-ol compounds are estrogen receptor beta ligands that have immunomodulatory properties and increase oligodendrocyte survival, differentiation, and remyelination. The compounds, compositions, and kits are useful in the treatment of multiple sclerosis and endometriosis.
Type:
Grant
Filed:
May 23, 2019
Date of Patent:
June 13, 2023
Assignees:
The Board of Trustees of the University of Illinois, The Regents of the University of California
Inventors:
John A. Katzenellenbogen, Seema K. Tiwari-Woodruff, Sung Hoon Kim, Benita Katzenellenbogen
Abstract: Compositions comprising nanoparticles are described herein. At least a portion of the nanoparticles comprises a lipid and/or polymer which is water-insoluble, and an agent incorporated in the lipid and/or polymer. The nanoparticles are optionally associated with a surface of water-soluble particles which comprise a water-soluble compound. The polymer is optionally a polyanhydride. Further described herein are processes for preparing such compositions, comprising contacting a solution comprising the lipid and/or polymer dissolved in a non-aqueous solvent with an anti-solvent (in which the lipid and/or polymer and agent are insoluble) which is miscible with the non-aqueous solvent. Further described herein are uses of the compositions for nasal administration, and devices configured for nasal administration of the composition upon atomization.
Type:
Grant
Filed:
July 20, 2018
Date of Patent:
May 30, 2023
Assignees:
INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION, YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD.