Abstract: The present invention discloses a compound, which comprises the structure shown in FIG. 1; and further discloses a preparation method thereof, a precursor material used in the preparation method, explosives comprising the compound, and the application thereof in the field of explosives, in particular in the application of green environmentally-friendly primers. The compound disclosed by the invention may provide green environmental protection type primer, and meets the problem of requiring green environmental protection primers in many fields such as military industry, firework and civil explosion engineering.
Type:
Grant
Filed:
January 28, 2019
Date of Patent:
February 15, 2022
Assignee:
INSTITUTE OF CHEMICAL MATERIALS OF CHINA ACADEMY OF ENGINEERING AND PHYSICS
Abstract: The invention relates to compounds of formula (I), and pharmaceutical uses thereof. Particular aspects of the invention relate to methods of synthesising the compounds and the use of those compounds in treating, ameliorating, or preventing a microbial infection.
Abstract: Disclosed herein is a very efficient method to make 5-(alkoxycarbonyl)furan-2-carboxylic acids (ACFC) from feedstocks comprised of furoates. When a feedstock comprised of methyl 5-methylfuran-2-carboxylate (MMFC) is used a product comprised of (5-(methoxycarbonyl)furan-2-carboxylic acid (MCFC) is obtained in high yield.
Abstract: The present disclosure relates to a method for preparing 3-[(3S)-7-bromo-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1H-[1,4]-benzodiazepin-3-yl] propionic acid methyl ester from (2-amino-5-bromo-phenyl)-pyridin-2-yl-methanone. Also disclosed are compounds useful as intermediates in the method, methyl (4S)-4-amino-5-[4-bromo-2-(pyridin-2-carbonyl)anilino]-5-oxo-pentanoate hydrobromide salt and methyl (4S)-4-(benzyloxycarbonylamino)-5-[4-bromo-2-(pyridin-2-carbonyl)anilino]-5-oxo-pentanoate.
Abstract: Provided are novel salts and polymorphs of 5-(2,4-diamino-pyrimidin-5-yloxy)-4-isopropyl-2-methoxy-benzenesulfonamide, which are potentially useful for modulating a condition mediated by a P2X3 or P2X2/3 receptor. Also provided are pharmaceutical formulations and methods of administration and dosing of these salts and polymorphs to subjects in need thereof.
Type:
Grant
Filed:
April 30, 2020
Date of Patent:
January 25, 2022
Assignee:
AFFERENT PHARMACEUTICALS, INC.
Inventors:
Prabha Ibrahim, Ronald Charles Hawley, Anthony P. Ford, Steven A. Smith
Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia Formula (I).
Type:
Grant
Filed:
November 12, 2018
Date of Patent:
January 18, 2022
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Steven L. Colletti, Duane DeMong, Kevin D. Dykstra, Zhiyong Hu, Michael Miller
Abstract: The present embodiments are directed, in part, to compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof for modulating the activity of delta opioid receptor, biased and/or unbiased, and/or methods for treating pain, migraines, headaches, depression, Parkinsons Disease, anxiety, and/or overactive bladder, and other disorders and conditions described herein or any combination thereof.
Type:
Grant
Filed:
February 15, 2018
Date of Patent:
January 18, 2022
Assignee:
Trevena, Inc.
Inventors:
Aimee Crombie Speerschneider, Dennis Shinji Yamashita, Philip Michael Pitis, Michael John Hawkins, Guodong Liu, Tamara Ann Miskowski Daubert, Catherine C. K. Yuan, Robert Borbo Kargbo, Robert Jason Herr, Donna Romero
Abstract: The present invention relates to metallo-?-lactamase inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-?-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more ?-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
Type:
Grant
Filed:
July 12, 2018
Date of Patent:
December 28, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Alexander Pasternak, Shuzhi Dong, Jack D. Scott, Haiqun Tang, Zhiqiang Zhao, Dexi Yang, Xin Gu, Jinlong Jiang, Li Xiao
Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I) Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Type:
Grant
Filed:
July 30, 2018
Date of Patent:
December 28, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Hua Zhou, Abdelghani Achab, Xavier Fradera, Yongxin Han, Derun Li, Meredeth A. McGowan, Nunzio Sciammetta, David L. Sloman, Wensheng Yu
Abstract: Novel 3-(N-piperidinyl)methyl benzamide derivatives are disclosed. The compounds can be used in treating diseases and conditions which are associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic ?-cell dysfunction and death, for example in the treatment of diabetes.
Type:
Grant
Filed:
June 15, 2018
Date of Patent:
December 21, 2021
Assignee:
The Board of Regents of the University of Oklahoma
Abstract: Provided are methods for continuously administering to a subject in need of treatment a formulation comprising an immunomodulatory imide compound. In some embodiments, the method are for use in treating multiple myeloma, transfusion-dependent anemia due to low- or intermediate-1-risk myelodysplastic syndromes, mantle cell lymphoma, hematologic cancers, or solid tumor cancers.
Type:
Grant
Filed:
April 21, 2020
Date of Patent:
December 14, 2021
Assignee:
Starton Therapeutics, Inc.
Inventors:
Marina Borovinskaya, Fotios Plakogiannis, Nisarg Modi, Tamanna Lather, Rod L. Hartwig, James C. Oliver, Yuliya Levintova
Abstract: Provided is a novel process for producing a (2S)-2-[(1H-pyrazol-1-yl)methyl]-1,3-oxazinane derivative. More specifically, provided is a process for producing a (2S)-2-[(1H-pyrazol-1-yl)methyl]-1,3-oxazinane derivative represented by formula (1): the process comprising reacting 3-aminopropan-1-ol with glyoxylic acid.
Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
Type:
Grant
Filed:
August 20, 2018
Date of Patent:
December 7, 2021
Assignee:
VIVACE THERAPEUTICS, INC.
Inventors:
Andrei W. Konradi, Tracy Tzu-Ling Tang Lin
Abstract: The disclosure relates to compounds of formula (I), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
Type:
Grant
Filed:
June 8, 2018
Date of Patent:
November 30, 2021
Assignee:
Bristol-Myers Squibb Company
Inventors:
Nicholas R. Wurtz, Pravin Sudhakar Shirude, Andrew Quoc Viet
Abstract: Methods and kits for improving tear production are described, along with topical pharmaceutical compositions. In certain instances, the composition comprises pentoxifylline and a pharmaceutically acceptable carrier. The compositions also may further comprise another active agent, such as an anti-bacterial agent, antiviral agent, antifungal agent, or immunosuppressant agent, and combinations thereof.
Abstract: The present disclosure provides compounds of Formula (I?), Formula (II), and Formula (III). The compounds described herein may useful in treating and/or preventing protozoan infections in a subject in need thereof, treating and/or preventing trypanosomal infections (e.g., Trypanosoma cruzi (T. cruzi) or Trypanosoma brucei infections) and/or plasmodial infections in a subject in need thereof, treating and/or preventing diseases in a subject in need thereof (e.g., Chagas disease, malaria, and/or sleeping sickness), and may be useful in treating and/or preventing infectious diseases in a subject in need thereof. Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein.
Type:
Grant
Filed:
January 17, 2017
Date of Patent:
November 23, 2021
Assignees:
University of Central Florida Research Foundation, Inc., The Regents of the University of California, Memorial Sloan-Kettering Cancer Center, The Broad Institute, Inc.
Inventors:
Derek Shieh Tan, Corinne N. Foley, Gustavo Moura-Letts, James McKerrow, Sivaraman Dandapani, Rahul Edwankar, Alyssa Verano, Debopam Chakrabarti, Bracken Roberts
Abstract: Disclosed are a 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, a preparation method therefor and an application thereof. Specifically, disclosed are three crystalline forms, i.e., crystalline forms A, B, and C, of 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride (formula I), preparation methods for the three crystalline forms, and use of the three crystalline forms in preparation of drugs.
Type:
Grant
Filed:
May 31, 2018
Date of Patent:
November 16, 2021
Assignees:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, FUKANG (SHANGHAI) HEALTH TECHNOLOGY CO., LTD.
Inventors:
Chunhao Yang, Zehong Miao, Cun Tan, Xiajuan Huan, Jian Ding, Yi Chen