Abstract: Disclosed herein are embodiments of a compound that can be used as a supramolecular sensor for determining the presence of analytes (e.g., illicit drugs), and for identifying and/or quantifying the analytes. Also disclosed herein is a parallel synthesis method for making compound embodiments, as well as method embodiments for using the compound embodiments. Array embodiments comprising one or more compound embodiments disclosed herein also are described.
Abstract: Described is a cannabinoid-terpenoid solution (CTS) and method of treating a disease state or condition in animals other than humans via cannabinoid-terpenoid therapy. The CTS includes a unique combination of cannabinoids, terpenoids (terpenes), and a lipophilic carrier to allow safely and effectively treat the animal.
Abstract: There is disclosed a compound, a pharmaceutical composition and a method of cancer treatment with an improved Myc inhibitor compound. More specifically, there is disclosed an improved compound having with improved solubility, improved binding characteristics and better efficacy and therapeutic activity inhibiting c-MYC wherein the improved compound comprises a tri-substituted pyridine having a thiazoyl moiety at position R1 versus an earlier disclosed genus of tri-substituted pyridine structures.
Abstract: A polycrystalline form of a dehydrophenylahistin-like compound, and a manufacturing and purification method and application thereof. A (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione monohydrate crystal and a (3Z,6Z-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione monohydrate crystal are more competitive crystalline forms with stable quality. The manufacturing and purification method is simple and easy to operate, and can effectively control the generation of a trans-isomer contaminant to obtain a high purity product. The polycrystalline form of the dehydrophenylahistin-like compound has a certain value in an application for manufacturing an antitumor pharmaceutical product.
Abstract: A composition inhibiting MEIS proteins. The MEIS proteins are effective in proliferation of hematopoietic stem cells. A formulation capable of easily passing through the cell membrane and perform its activity in the cell, and can inhibit MEIS activity in a dose dependent manner. The combination includes isolated cells, medium, growth factors and MEISi inhibitor. The isolated cells are isolated from mouse bone marrow, human bone marrow and human umbilical cord blood. The medium has a pH value of 7.2 and contains bovine serum albumin, recombinant insulin, transferrin, 2-mercaptoethanol and IMDM medium. The growth factors are hematopoietic stem cell factor SCF, fetus liver tyrosine kinase-3 ligand Flt3L, and thrombopoietin. A chemical formula of the MEISi-1 is 4-[2-(benzylamino)-2-oxoethoxy]-N-(2,3-dimethylphenyl) benzamide. A chemical formula of MEISi-2 is 4-hydroxy-N?-[(Z)-(2-oxonaphthalen-1-ylidene)methyl] benzohydrazide.
Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
Type:
Grant
Filed:
March 25, 2021
Date of Patent:
March 14, 2023
Assignee:
The Regents of the University of California
Inventors:
Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
Abstract: Provided are 2-aminoimidazole-phenyl derivative compounds of Formula (I): which compounds are useful in methods of controlling microbial growth, such as by enhancing the effects of an antibiotic administered in combination with the compound. Compositions including these compounds, devices including these compounds, and methods of using the same are also provided.
Type:
Grant
Filed:
March 8, 2018
Date of Patent:
February 21, 2023
Assignee:
North Carolina State University
Inventors:
Christian Melander, David Kendall Jung, Samuel Onofre Reyes
Abstract: The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS.
Type:
Grant
Filed:
June 22, 2018
Date of Patent:
February 21, 2023
Assignee:
University of Washington
Inventors:
Erkang Fan, Zhongsheng Zhang, Wenlin Huang, Frederick S. Buckner
Abstract: Compounds represented by the structural formula (1) R1, R2, R3, R4, R5, R6 are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
Type:
Grant
Filed:
April 15, 2019
Date of Patent:
February 21, 2023
Assignee:
MASARYKOVA UNIVERZITA
Inventors:
Kamil Paruch, Benoit Carbain, Stepan Havel, Jiri Damborsky, Jan Brezovsky, Lukas Daniel, Alexandra Sisakova, Fedor Nikulenkov, Lumir Krejci
Abstract: Oral pharmaceutical solution comprising a pharmaceutically acceptable salt of lisdexamfetamine, and a pharmaceutically acceptable aqueous carrier comprising a buffer and a cosolvent selected from the group consisting of a glycol, a polyol, and a mixture thereof, wherein the pH of the solution is from 5.5 to 9.0. The oral pharmaceutical solution presents excellent physicochemical stability, even under alkaline conditions.
Abstract: A polycrystalline form of a dehydrophenylahistin-like compound, and a manufacturing and purification method and application thereof. A (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione monohydrate crystal and a (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione monohydrate crystal are more competitive crystalline forms with stable quality. The manufacturing and purification method is simple and easy to operate, and can effectively control the generation of a trans-isomer contaminant to obtain a high purity product. The polycrystalline form of the dehydrophenylahistin-like compound has a certain value in an application for manufacturing an antitumor pharmaceutical product.
Abstract: Cationic radial catenane comprising a central cationic ring and two or more radial cationic rings mechanically interlocked central cationic ring and methods for making the same are disclosed herein.
Type:
Grant
Filed:
April 5, 2019
Date of Patent:
January 31, 2023
Assignees:
Northwestern University, King Abdulaziz City for Science and Technology (KACST)
Abstract: Disclosed herein are compounds which inhibit the kinase activity of dual leucine zipper (DLK) kinase (MAP3K12), pharmaceutical compositions, and methods of treatment of DLK-mediated diseases, such as neurological diseases that result from traumatic injury to central nervous system and peripheral nervous system neurons (e.g. stroke, traumatic brain injury, spinal cord injury), or that result from a chronic neurodegenerative condition (e.g. Alzheimer's disease, frontotemporal dementia, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, spinocerebellar ataxia, progressive supranuclear palsy, Lewy body disease, Kennedy's disease, and other related conditions), from neuropathies resulting from neurological damage (chemotherapy-induced peripheral neuropathy, diabetic neuropathy, and related conditions) and from cognitive disorders caused by pharmacological intervention (e.g. chemotherapy induced cognitive disorder, also known as chemobrain).
Type:
Grant
Filed:
October 20, 2020
Date of Patent:
January 24, 2023
Assignee:
Board of Regents, The University of Texas System
Inventors:
Michael J. Soth, Kang Le, Philip Jones, Jason Cross
Abstract: The present invention relates to peptide conjugates of microtubule-targeting agents such as maytansinoid derivatives which are useful for the treatment of diseases such as cancer.
Type:
Grant
Filed:
July 9, 2020
Date of Patent:
January 17, 2023
Assignee:
Cybrexa 3, Inc.
Inventors:
Daniel Richard Marshall, Johanna Marie Csengery, Robert John Maguire, Robert A. Volkmann
Abstract: Provided herein is a combination product comprising a Bcl-2 inhibitor, an anti-CD20 antibody and/or bendamustine or a combination product comprising a Bcl-2 inhibitor and CHOP, the combination product provides a use of the combination product for prevention and/or treatment of a disease (e.g., cancer, rheumatoid arthritis (RA), granulomatosis with polyangiitis (GPA), and microscopic polyangiitis).
Abstract: The purpose of the invention is to provide a novel hematopoiesis-promoting agent and a medicament comprising the hematopoiesis-promoting agent as an active ingredient for preventing or treating anemia, in particular refractory anemia. The present invention provides a hematopoiesis-promoting agent comprising an S-adenosylmethionine synthase inhibitor.
Type:
Grant
Filed:
February 25, 2019
Date of Patent:
January 17, 2023
Assignee:
TOHOKU UNIVERSITY
Inventors:
Kazuhiko Igarashi, Hiroki Kato, Yusho Ishii, Chi Long Nguyen, Hideo Harigae
Abstract: Provided herein are compounds, compositions and methods of using the compounds and compositions for the treatment of diseases modulated, as least in part, by AhR. The compounds are represented by formulae Formula (I), (II), (III), (iv): wherein the letters and symbols a, b, c, d, e, f, g, Z, R1b, R2a and R2b have the meanings provided in the specification.
Type:
Grant
Filed:
July 18, 2018
Date of Patent:
January 10, 2023
Assignee:
IDEA YA BIOSCIENCES, INC.
Inventors:
Muzaffar Alam, Hilary Plake Beck, Michael Patrick Dillon, Marcos Gonzalez-Lopez, Alice Chen Rico, James Clifford Sutton, Jr.
Abstract: Provided herein are compounds according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, and R7 are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) as well as the use of such compounds as M4 receptor agonists.
Type:
Grant
Filed:
October 7, 2020
Date of Patent:
January 10, 2023
Assignee:
NOVARTIS AG
Inventors:
Amy Calhoun, Xin Chen, Kevin Matthew Gardinier, Edward Charles Hall, Keith Jendza, Nancy Labbe-Giguere, James Neef, Daniel Steven Palacios, Ming Qian, Michael David Shultz, Christopher G. Thomson, Kate Yaping Wang, Fan Yang
Abstract: The present invention relates to a process for preparing 4-{[(2S)-2-{4-[5-chloro-2-(4-chloro-1H-1,2,3-triazol-1-yl)phenyl]-5-methoxy-2-oxopyridin-1(2H)-yl}butanoyl]amino}-2-fluorobenzamide (I) or 4-({(2S)-2-[4-{5-chloro-2-[4-(trifluoromethyl)-1H-1,2,3-triazol-1-yl]phenyl}-5-methoxy-2-oxopyridin-1(2H)-yl]butanoyl}amino)-2-fluorobenzamide (II) from 2,5-dimethoxypyridine (III), 1-(2-bromo-4-chlorophenyl)-4-chloro-1H-1,2,3-triazole (X-Cl) or 1-(2-bromo-4-chlorophenyl)-4-(trifluoromethyl)-1H-1,2,3-triazole (X-CF3), 4-amino-2-fluorbenzamide (XIII) and (2R)-2-aminobutanoic acid (XVII).
Type:
Grant
Filed:
March 8, 2019
Date of Patent:
January 3, 2023
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Julian Egger, Daniel Goetz, Michal Sowa
Abstract: Heterocycles having odoriferous ketone or odoriferous aldehyde groups may be suitable in compositions comprising washing agents, cleaning agents, cosmetic agents, air care agents, insect repellents, or combinations thereof where the heterocycles release the ketones and aldehydes during hydrolysis.
Type:
Grant
Filed:
October 16, 2018
Date of Patent:
January 3, 2023
Assignee:
Henkel AG & Co. KGaA
Inventors:
Sascha Wilhelm Schaefer, Benjamin Berntsson