Abstract: Disclosed are novel small molecules, methods of synthesis of the small molecules, and uses of the small molecules for modulating activity of the human serotonin receptor 2C (5-HT2c), preferably selectively. The small molecules have a substituted beta-carboline core structure, which optionally may be saturated at one or more bonds to provide a dihydro-beta-carboline core or a tetrahydro-beta-carboline core. The small molecules may be administered to treat and/or prevent diseases, disorders, and/or conditions associated with human serotonin receptor 2C (5-HT2C) including psychiatric, mental, and/or neurological diseases, disorders, and conditions such as cognitive impairment, addiction, and obsessive compulsive disorder. The disclosed small molecules also may be administered to treat and/or prevent obesity, for example, via appetite suppression.
Type:
Grant
Filed:
October 2, 2019
Date of Patent:
November 1, 2022
Assignee:
Northwestern University
Inventors:
Karl A. Scheidt, Herbert Y. Meltzer, Adam J. Csakai
Abstract: An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof. The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof. wherein the symbols in the formula are defined below: R1: e.g., a C1-C6 alkyl group; R2: a C1-C6 alkyl group; A: e.g., an oxygen atom; and R3: e.g., a C1-C6 alkyl group.
Abstract: The present invention relates to a process for making a compound of formula (I) as described herein Formula (I) comprising reducing a compound of formula (II) as described herein with hydrogen in the presence of a palladium catalyst and a solvent wherein the solvent is a polar, aprotic solvent or a C3-C10 alcohol Formula (II). The present invention further relates to a hydrochloride salt and a monohydrochloride salt of the compound of formula (I) as described herein and to a process for making the same Formula (I).
Type:
Grant
Filed:
June 20, 2019
Date of Patent:
October 18, 2022
Assignee:
CELLESTIA BIOTECH AG
Inventors:
Michael Bauer, Uwe Hahn, Erhard Bappert
Abstract: Disclosed herein are formulations and methods for reversing one or more symptoms of cannabinoid hyperemesis syndrome (CHS) or one or more symptoms thereof, comprising parenterally administering a CB1 antagonist in an amount sufficient to reverse the CHS or symptom(s).
Abstract: Provided are a crystal form of a tricyclic compound and a preparation process thereof. Also provided is an application of the crystal form in preparing a drug for treating a disease related to a sphingosine-1-phosphate subtype 1 (S1P1) receptor.
Abstract: A method for treating a tumor in a patient by administering to the patient an immunogenic composition including antigenic material inactivated by treatment with a metal-based coordination complex and electromagnetic radiation, wherein the immunogenic composition is effective to elicit an immune response to the antigenic material in the patient after administration and the metal-based coordination complex having a specified formula. An immunogenic composition and a method for preparing it are also disclosed.
Abstract: The present invention relates to a compound selected from (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine and a pharmaceutically acceptable salt thereof, and in particular to the phosphate salt of (R)-(+)-5-(p-cyanophenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine, both having preferably an enantiomeric excess of the (R) form higher than or equal to 97%. Furthermore, the present invention relates to pharmaceutical compositions comprising the same, their use as a medicament and in methods of treatment of diseases and disorders in humans including women of child bearing potential and pediatric patients in which aldosterone over-exposure contributes to the deleterious effects of said diseases or disorders, as well as processes for preparing said inventive compounds.
Type:
Grant
Filed:
August 12, 2020
Date of Patent:
September 20, 2022
Assignee:
DAMIAN PHARMA AG
Inventors:
Christoph Schumacher, Walter Fuhrer, Ronald Edward Steele
Abstract: The invention provides bipartite, dual-targeted inhibitors of bacterial RNA polymerase having the general structural formula (I): X-?-Y (I) wherein X is an moiety that binds to the Rif target of a bacterial RNA polymerase; Y is a moiety that binds to the bridge-helix N-terminus target of a bacterial RNA polymerase; and is a covalent bond or a linker. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.
Type:
Grant
Filed:
May 23, 2019
Date of Patent:
September 20, 2022
Assignee:
Rutgers, The State University of New Jersey
Inventors:
Richard H. Ebright, Yon W. Ebright, Chih-Tsung Lin
Abstract: A method of treating fungal infections using dabigatran etexilate is provided. The method can include administering a therapeutically effective amount of dabigatran etexilate to a subject in need thereof. In an embodiment, dabigatran etexilate may be effective as a broad-spectrum antifungal agent and may be used to treat infections resulting from a wide array of fungal pathogens. In an embodiment, dabigatran etexilate may be administered to treat either a topical or systemic fungal infection.
Type:
Grant
Filed:
February 28, 2022
Date of Patent:
September 20, 2022
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Mahmoud Kandeel Elsayed, Naser Abdullah Alhumam, Abdulla Yousef Al-Taher
Abstract: The present application provides improved processes for the synthesis of eribulin intermediate, which generally comprise the steps of: a) De-protecting the eribulin-enone (compound 1) in tetrahydrofuran by using TBAF solution, buffered with imidazole HCl in the presence of molecular sieve and sodium sulphate to get an insitu mixture of eribulin-dione diastereomer at C12 carbon (compound 2). Then ketalization may be performed of eribulin-dione insitu intermediate containing mixture of diastereomer at C12 carbon (compound 2) with PPTS in dichloromethane to yield eribulin-diol (compound 3).
Abstract: Disclosed herein a process for the preparation of highly pure dexmethylphenidate hydrochloride (Formula-I) which comprises the steps of neutralization of dl-threomethylphenidate hydrochloride to dl-threo methylphenidate; subsequent resolution of dl-threo methylphenidate using amino acid or its derivatives as chiral resolution agent to yield dexmethylphenidate salt; hydrolysis of the salt and further conversion of dexmethylphenidate into its hydrochloride salt.
Abstract: Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I): including stereoisomers, salts and tautomers thereof, R1, R2, R3, L1, L2, L3, L4, L5, L6, M1, M2, A, q, w and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.
Type:
Grant
Filed:
March 2, 2021
Date of Patent:
September 6, 2022
Assignee:
Sony Corporation
Inventors:
Tracy Matray, Hesham Sherif, C. Frederick Battrell
Abstract: The present invention relates to the synthesis of intermediate compounds which can be used in the synthesis of mint lactone and related compounds, including 3,6-dimethylhexahydrobenzofuran-2-ones, isomers, and other derivatives.
Type:
Grant
Filed:
April 15, 2021
Date of Patent:
September 6, 2022
Assignee:
P2 SCIENCE, INC.
Inventors:
Patrick Foley, Yonghua Yang, Tania Salam
Abstract: Novel compounds of formula (II) are disclosed. Compounds of formula (II) comprise ornithine derivatives or compounds that can metabolize under physiological conditions to ornithine. The pH and plasma stability of compounds of formula (II) is also described. Also disclosed are methods for the treatment of neurodegenerative diseases such as Alzheimer's Disease using compounds of formula (II).
Type:
Grant
Filed:
March 22, 2021
Date of Patent:
September 6, 2022
Assignee:
Resilio Therapeutics, LLC
Inventors:
Francis Xavier Tavares, Michael Peter Vitek
Abstract: Provided herein are salt forms of a complement component 5a receptor having the formula of Compound 1 Also provided herein are pharmaceutical compositions and methods of treatment using the salt forms of Compound 1, described herein.
Type:
Grant
Filed:
November 6, 2020
Date of Patent:
August 30, 2022
Assignee:
ChemoCentryx, Inc.
Inventors:
Rajinder Singh, Kwok Yau, Yibin Zeng, Penglie Zhang, Rebecca M. Lui, Ju Yang, Howard S. Roth
Abstract: A stable crystal of a salt of N—[(R)-1-{(S)-2-hydroxy-2-phenylpropylamino}propan-2-yl]isoquinoline-6-sulfonamide may have desirable properties for a pharmaceutical drug substance, and more specifically N—[(R)-1-{(S)-2-hydroxy-2-phenylpropylamino}propan-2-yl]isoquinoline-6-sulfonamide dihydrochloride anhydride. A crystal of the anhydride may have characteristic peaks at 2? angles of 6.8±0.1°, 10.0±0.1°, 12.7±0.1°, 14.6±0.1°, 14.8±0.1°, 16.2±0.1°, 17.4±0.1°, 17.8±0.1°, 19.5±0.1°, 20.0±0.1°, 21.6±0.1°, 24.7±0.1°, 25.5±0.1°, 25.8±0.1°, 29.8±0.1°, 39.5±0.1°, and/or 44.9±0.1° in powder X-ray diffraction spectrum.
Abstract: Sugar-based mono and diesters are prepared by esterification of 2,5-furan-dicarboxylic acid (FDCA) with an alcohol in the presence of low loadings of a homogeneous organotin (IV) catalyst.
Type:
Grant
Filed:
February 3, 2021
Date of Patent:
August 23, 2022
Assignees:
Archer Daniels Midland Company, DUPONT INDUSTRIAL BIOSCIENCES USA, LLC
Abstract: The present invention provides a heterocyclic compound having an activity to promote the maturation of a cardiomyocyte. A compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof has an activity to promote the maturation of a cardiomyocyte, and is useful as a cardiomyocyte maturation promoter.
Abstract: The present disclosure relates to compounds for activating the enzymatic activity of an E3 ubiquitin ligase and methods for treating a disease or disorder in a subject with diminished E3 ubiquitin ligase enzymatic activity. In some embodiments, the present disclosure provides a compound of Formula (I) or a compound of Formula (II) or pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
July 28, 2017
Date of Patent:
August 2, 2022
Assignee:
Mayo Foundation for Medical Education and Research
Inventors:
Wolfdieter Springer, Fabienne C. Fiesel, Thomas R. Caulfield