Abstract: Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
Abstract: The present invention relates to a boron hydroxyl-containing organic compound having a structural formula shown in formula I. The present invention also relates to a method for preparing the boron hydroxyl-containing organic compound and use thereof in an organic electronic device, particularly an organic light-emitting diode. The present invention further relates to an organic electronic device, particularly an organic light-emitting diode, including the boron hydroxyl-containing organic compound according to the present invention and use thereof in display and lighting technology. By optimizing the structure of the device and altering the concentration of the boron hydroxyl-containing organic compound in the substrate, the optimal device performance can be achieved so as to produce an OLED device with high efficiency, high brightness and high stability, which provides a better material option for use in full-color display and lighting.
Type:
Grant
Filed:
December 14, 2020
Date of Patent:
November 5, 2024
Assignee:
JIANGSU UNIVERSITY OF SCIENCE AND TECHNOLOGY
Abstract: A method for producing a first vadadustat intermediate represented by the following formula (3) comprising reacting a compound represented by the following formula (1) with glycine or a glycine derivative represented by the following formula (2) or a salt of the glycine or the glycine derivative in the presence of carbon monoxide. The method produces a vadadustat intermediate through a clean reaction with high atom conversion efficiency.
Type:
Grant
Filed:
March 5, 2020
Date of Patent:
November 5, 2024
Assignee:
KANEKA CORPORATION
Inventors:
Koji Machida, Hiroaki Yasukouchi, Akira Nishiyama
Abstract: The present invention is related to methods of stabilizing an ophthalmic drug by adding a surfactant and a viscosity enhancer to the ophthalmic drug to create a composition wherein the composition has a viscosity of about 25 centipoise or less at a shear rate of 1/1000 per second at 25 degrees Celsius and a viscosity of about 70 centipoise or more at shear rate of 1 per second at 25 degrees Celsius, filling the composition into a container; and storing the container at a temperature from about 2 degrees Celsius to about 25 degrees Celsius. The present invention is further directed to a container prepared by the methods of the present invention.
Abstract: A related substance of linagliptin intermediate 2-(chloromethyl)-4-methylquinazoline, 4,4?-(2-methylpropane-1,3-diyl)bis(2-(chloromethyl)quinazoline) and a method for synthesizing the related substance (impurity) by reacting 2-(chloromethyl)-4-methylquinazoline with acetaldehyde under an alkaline condition and a purification method are provided. The preparation method is simple and convenient to operate, short in reaction time, high in product purity, and high in yield. The synthesized related substance can be used for qualitative and quantitative analysis of the linagliptin intermediate 2-(chloromethyl)-4-methylquinazoline and API impurities of linagliptin, so that the medication safety of the linagliptin is improved.
Type:
Grant
Filed:
June 9, 2021
Date of Patent:
October 22, 2024
Assignee:
WISDOM PHARMACEUTICAL CO., LTD
Inventors:
Xiaolong Qiu, Hu Wang, Tao Xu, Lin Hu, Ping Zou, Zhiwei Zuo, Wenbo Liu, Lingling Chu
Abstract: The invention provides methods of chemical synthesis of the pharmacological agent 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate, also called CV-8972. The methods entail formation of a free base form of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethanol, also called CV-8814, as intermediate without producing a salt form of CV-8814.
Type:
Grant
Filed:
August 29, 2023
Date of Patent:
October 8, 2024
Assignee:
IMBRIA PHARMACEUTICALS, INC.
Inventors:
Neil Buckley, Dan Belmont, Bryan Hauser, Myoung Goo Kim, Kumar Kannan
Abstract: Provided herein are methods of using 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiomer, a mixture of enantiomers, a tautomer, an isotopolog, or a pharmaceutically acceptable salt thereof, alone or in combination with rituximab, for treating, preventing or managing non-Hodgkin lymphoma.
Type:
Grant
Filed:
June 24, 2022
Date of Patent:
October 1, 2024
Assignee:
Celgene Corporation
Inventors:
Maria Soraya Carrancio Anton, Tonia J. Buchholz, Antonia Lopez-Girona, Rama Krishna Narla, Michael Pourdehnad
Abstract: The present invention belongs to the pharmaceutical field, and provides the pharmaceutically acceptable salts of the compound (S)-7-(4-(1-(methylsulfonyl)piperidin-4-yl)phenyl)-N-(morpholin-2-ylmethyl)pyrido[3,4-b]pyrazin-5-amine and the crystalline forms thereof, the solvates and the crystalline forms thereof, the pharmaceutical compositions comprising the same as well as the methods of preparing the same and the use thereof.
Abstract: The present disclosure provides compounds useful as ionizable cationic lipids. The ionizable cationic lipids are useful for preparing lipid nanoparticles for the delivery of therapeutic nucleic acids to cells. Cationic ionizable lipids were engineered with improved stability to oxidative degradation while in storage.
Type:
Grant
Filed:
December 12, 2022
Date of Patent:
September 3, 2024
Assignee:
Akagera Medicines, Inc.
Inventors:
Daryl C. Drummond, Dmitri B. Kirpotin, Mark E. Hayes
Abstract: The present disclosure discloses a compound 1,1,3,3-tetramethylguanidine (R)-(tert-butoxycarbonyl)(2-(5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dicarbonyl-3,6-dihydropyrimidine-1(2H)-yl)-1-phenylethyl) sulfamate (of structural formula I) and a preparation method thereof.
Type:
Grant
Filed:
November 24, 2020
Date of Patent:
September 3, 2024
Assignee:
Nanjing Chempion Biotechnology Co., Ltd.
Inventors:
Jian Chen, Xianqiang Zhang, Yaoqiang Li
Abstract: Disclosed herein are Notch transcriptional activation complex kinase (“MACK”) inhibitors, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein include compounds of Formula (Ia) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.
Type:
Grant
Filed:
September 6, 2022
Date of Patent:
September 3, 2024
Assignee:
University of Miami
Inventors:
Anthony J. Capobianco, Stephan C. Schürer, Xiaoxia Zhu, Tanya T. Kelley
Abstract: This invention is for improving the manufacturing pharmaceutical grade CBD and other cannabinoids following current Good Manufacturing Practices (cGMP) of the US FDA for use in clinical trials for CNS and other indications by the NIH and other researchers. The major cannabinoids in marijuana (Cannabis) and hemp originate from Cannabigerolic Acid (CBGA) present in the biomass of the plant. Plant enzymes that are specific to different strains of biomass converts CBGA to different carboxylic acids of cannabinoids including Cannabidiolic Acid (CBDA) and ?9-Tetrahydrocannabinolic Acid (?9-THCA). These are relatively stable in the growing and fresh-cut plants. These are converted by thermal decarboxylation to Cannabidiol (CBD) and ?9-Tetrahydrocannabinol (?9-THC), carbon dioxide and water. Cannabinoids can be manufactured by first heating the Cannabis biomass to convert carboxylic acids prior to extraction and purification.
Abstract: Compounds represented by general Formulae I to IV as described herein are disclosed. Further disclosed are composition utilizing the herein disclosed compounds and using the same for the treatment of glycogen storage disorders.
Type:
Grant
Filed:
October 27, 2022
Date of Patent:
August 20, 2024
Assignees:
HADASIT MEDICAL RESEARCH SERVICES AND DEVELOPMENT LTD., RAMOT AT TEL-AVIV UNIVERSITY LTD.
Inventors:
Or Kakhlon, Miguel Enrique Weil, Leonardo Javier Solmesky
Abstract: Pharmaceutical compositions for the topical administration of a drug to the pilosebaceous unit and methods for administering the same. As disclosed herein, the inventors of the present invention have made the surprising discovery that pharmaceutical compositions comprising small particles of an active pharmaceutical ingredient can be administered to the pilosebaceous unit. The pharmaceutical composition can comprise SHR0302 or spironolactone as an active pharmaceutical ingredient.
Abstract: The present disclosure relates to compounds of Formula (I) and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inflammatory, autoinflammatory and autoimmune diseases and cancers.
Type:
Grant
Filed:
June 11, 2020
Date of Patent:
August 6, 2024
Assignee:
NodThera Limited
Inventors:
Mark G. Bock, David Harrison, Jane E. Scanlon
Abstract: Highly efficient process for the preparation of 4-Fluoro-1H-pyrazole or salts thereof by reaction of pyrazole with an electrophilic fluorinating reagent is disclosed.
Type:
Grant
Filed:
January 27, 2023
Date of Patent:
July 30, 2024
Assignee:
F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.
Abstract: The present disclosure encompasses crystalline polymorphs of Rivoceranib and Rivoceranib mesylate (Apatinib mesylate), processes for preparation thereof, and pharmaceutical compositions thereof.
Abstract: Disclosed herein are safened compositions comprising (a) a pyridine carboxylate herbicide or an agriculturally acceptable N-oxide, salt or ester thereof and (b) a safener comprising isoxadifen or agriculturally acceptable salt or ester thereof. Also disclosed herein are methods of controlling undesirable vegetation, comprising applying to vegetation or an area adjacent the vegetation or applying in soil or water to control the emergence or growth of vegetation (a) a pyridine carboxylate herbicide or an agriculturally acceptable N-oxide, salt or ester thereof and (b) a safener comprising isoxadifen or agriculturally acceptable salt or ester thereof.
Abstract: The invention provides safe and efficacious treatments for Female Sexual Disorders, genitopelvic pain/penetration disorders; vulvovaginal atrophy, vestibulodynia, dyspareunia, sexual interest/arousal disorder, low female libido, and female orgasmic disorder.