Abstract: An isocyanate production method is characterized by having: a carbamation step in which a carbonic acid ester, an inorganic acid salt of an amino acid derivative, and a basic compound are reacted to obtain a reaction mixture containing a carbamic acid ester derived from the carbonic acid ester, a hydroxy compound derived from the carbonic acid ester, and the carbonic acid ester; and a thermal decomposition step in which the carbamic acid ester is subjected to a thermal decomposition reaction to obtain an isocyanate.
Abstract: The present invention provides a method of administering magnesium threonate to a subject in need of supplementing magnesium. At least a portion of magnesium (Mg) and threonate (T) is present in a salt form of MgT2. The method may comprise administration of magnesium threonate at two different time points per day. The method may comprise administering, at a first time point, a first oral dosage form comprising magnesium threonate. The method may comprise administering, at a second time point, a combination of the first oral dosage form and a second oral dosage form comprising magnesium threonate. The first and second oral dosage forms may exhibit different dissolution profiles in a dissolution medium.
Abstract: The present invention relates to an aqueous ophthalmic solution for treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma, the solution comprising at least 0.5 w/v % brinzolamide dissolved in the solution; hydroxy-propyl-?-cyclodextrin; polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer; and water and/or the process for preparation thereof.
Abstract: A method for preparing the cyclic phosphonate compound of Formula I is described. The method significantly improves the stereoselectivity of the compound with the required configuration.
Type:
Grant
Filed:
April 15, 2021
Date of Patent:
April 5, 2022
Assignee:
GANNEX PHARMA CO., LTD.
Inventors:
Jinzi Jason Wu, Bailing Yang, Bin Liang
Abstract: The present invention provides an improved process for preparing an aminopyrimidine derivative or pharmaceutically acceptable salt thereof having a selective inhibitory activity against protein kinases, especially against the protein kinases for mutant epidermal growth factor receptors. Additional, the present invention provides novel intermediates useful for said process and processes for preparing the same.
Type:
Grant
Filed:
December 8, 2020
Date of Patent:
March 29, 2022
Assignee:
Yuhan Corporation
Inventors:
Sang-Ho Oh, Ja-Heouk Khoo, Jong-Chul Lim, Seong-Ran Lee, Hyun Ju, Woo-Seob Shin, Dae-Gyu Park, Su-Min Park, Yoon-Ah Hwang
Abstract: Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3 and R6, R11a, and R11b are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
Type:
Grant
Filed:
July 30, 2020
Date of Patent:
March 22, 2022
Assignee:
SAGE THERAPEUTICS, INC.
Inventors:
Francesco G. Salituro, Albert Jean Robichaud, Gabriel Martinez Botella, Boyd L. Harrison, Andrew Griffin, Daniel La
Abstract: Methods for stimulating the G protein receptor (Gpr91) pathway in intestinal cells to release IL-25 and enhance a type II immune response in the subject are useful in the treatment or prevention of bacterial or parasitic infection. Similarly methods and compositions used therein to inhibit or stimulate GPR91 are useful for the treatment or inhibition of certain diseases, such as irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), and Crohn's disease.
Abstract: Novel C-2-substituted bicyclic compounds of Formula I have been prepared and found to be useful as inhibitors of by inhibiting geranylgeranylation of proteins. The application is directed to these compounds, to compositions comprising these compounds and to their use, in particular as medicaments to cancer and other conditions treatable by inhibiting human geranylgeranylation pyrophosphate hGGPPS activity.
Abstract: Methods for modifying neuronal functional activity and/or treating a neurological disorder by using agents that raise neuronal intracellular concentration of magnesium are disclosed. Also provided herein are methods of determining the amenability of an individual to treatment for a neurological disorder, by measuring changes in intracellular magnesium concentration.
Abstract: The present disclosure provides compositions and methods of modulating abhydrolase domain-containing protein-2 (ABHD2). The present disclosure provides methods of identifying agents that modulate ABHD2 activity.
Type:
Grant
Filed:
August 1, 2016
Date of Patent:
March 15, 2022
Assignee:
The Regents of the University of California
Inventors:
Polina V. Lishko, Yuriy Kirichok, Melissa R. Miller
Abstract: The invention relates to compounds of Formula (I), (II) or (III), salts thereof, pharmaceutical compositions thereof, as well as therapeutic methods of treatment and prevention.
Type:
Grant
Filed:
October 24, 2018
Date of Patent:
March 15, 2022
Assignee:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Inventors:
David Favre, Robert G. Ferris, Jun Tang
Abstract: The disclosed subject matter provides N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.
Type:
Grant
Filed:
October 5, 2020
Date of Patent:
March 15, 2022
Assignee:
Cardioxyl Pharmaceuticals, Inc.
Inventors:
Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost, John P. Toscano
Abstract: The present application relates to a process for the preparation of piperine of high purity having low concentrations of isomeric impurities.
Abstract: Disclosed are compounds that can modulate DDAH and the amount of asymmetric dimethylarginine (ADMA) in a subject. Also provided are pharmaceutical compositions comprising these compounds, as well as methods of using these compositions to treat and/or prevent diseases associated with elevated or low levels of DDAH and ADMA.
Abstract: The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.
Type:
Grant
Filed:
March 4, 2020
Date of Patent:
February 22, 2022
Assignee:
C4 Therapeutics, Inc.
Inventors:
Roger Norcross, Annick Goergler, Fabian Dey, Eric Andre Kusznir
Abstract: The invention relates to compounds of Formula (I) and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by mycobacterium, such as tuberculosis.
Type:
Grant
Filed:
August 15, 2018
Date of Patent:
February 22, 2022
Assignees:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED, BIOVERSYS AG
Inventors:
Esther Porras De Francisco, Modesto Jesús Remuiñan-Blanco, Marilyne Bourotte, Benoit Deprez, Nicolas Willand
Abstract: The invention provides a combination comprising: (i) a compound of formula (Io): or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims; and (ii) a compound which is SGI-110 or a tautomer or a solvate or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions containing the combinations and medical uses of the combinations.
Type:
Grant
Filed:
March 28, 2018
Date of Patent:
February 1, 2022
Assignees:
ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED
Abstract: The invention relates to a new method for preparing a complex of forskolin and cyclodextrin and inclusion complexes of forskolin and ?-cyclodextrins having a weight ratio of 1:0.2 to 1:4 (w/w). Pharmaceutical compositions comprising said complex and their use are also provided.