Abstract: The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e.
Type:
Grant
Filed:
October 30, 2023
Date of Patent:
February 11, 2025
Assignee:
Verrica Pharmaceuticals Inc.
Inventors:
Matthew Gene Davidson, Brian Matthew Eklov, Peter Wuts, Brad Melvin Loertscher, Steven R. Schow
Abstract: An object of the present invention is to provide a compound exhibiting an excellent drug efficacy as an anti-adenoviral agent, and an anti-adenoviral agent. The present invention provides a compound represented by General Formula [1] (in the formula, R1 represents a halogen atom, an amino group which may be substituted, a C1-6 alkoxy group which may be substituted, a hydroxyl group which may be protected, or the like; R2 represents a hydrogen atom or an amino protecting group; R3 represents a C1-20 alkoxy group which may be substituted, an aryloxy group which may be substituted, an amino group which may be substituted, or the like; R4 represents a C1-20 alkoxy group which may be substituted, an aryloxy group which may be substituted, an amino group which may be substituted, or the like); or a salt thereof.
Abstract: This disclosure relates to polymorphs of (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethenopyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to compositions including such polymorphs, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.
Abstract: The invention relates to the synthesis and provision of a new class of volatile metal organic compounds based on bis(alkylimine)glyoxal and bis(dialkylhydrazone)glyoxal ligands in combination with cyclopentadienide and alkyl ligands for use in ALD and CVD processes.
Type:
Grant
Filed:
July 26, 2019
Date of Patent:
December 31, 2024
Assignee:
UMICORE AG & CO. KG
Inventors:
Nicholas Rau, Joerg Sundermeyer, Andreas Rivas Nass, Ralf Karch, Annika Frey, Angelino Doppiu, Eileen Woerner
Abstract: Disclosed herein novel dopamine D3 receptor selective antagonists/partial agonists compounds with high affinity and metabolic stability useful for the treatment of psychiatric and neurological disorders and as research and diagnostic tools. Also disclosed are methods of making the compounds.
Type:
Grant
Filed:
March 3, 2022
Date of Patent:
December 10, 2024
Assignee:
The United States of America, as represented by the Secretary, Department of Health and Human Services
Abstract: The present invention relates to compounds of formula (I), wherein R1 to R6, m and n are I a described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
June 3, 2019
Date of Patent:
December 3, 2024
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Fabian Dey, Hong Shen, Hongtao Xu, Hongying Yun, Ge Zou, Wei Zhu
Abstract: Provided herein are compounds useful for the treatment of various proliferative diseases. These compounds, as well as pharmaceutically acceptable salts thereof may be formulated in pharmaceutical compositions, and may be used in methods of treatment and/or prophylaxis of proliferative diseases, including cancer, and more specifically, pancreatic cancer.
Type:
Grant
Filed:
September 4, 2020
Date of Patent:
November 26, 2024
Assignees:
The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard College
Inventors:
Srivatsan Raghavan, Bruce Kuan-Yee Hua, Shubhroz Gill, Stuart Schreiber, William Hahn, Paul Clemons, Raymond Ng, Partha Nag
Abstract: Disclosed are a novel tetrahydroisoquinoline compound, a method for preparing intermediates thereof, a pharmaceutical composition thereof and the use thereof. The tetrahydroisoquinoline compound of the present invention has a good inhibitory effect on phosphodiesterase (PDE4), and can be used in the prevention, treatment or auxiliary treatment of multiple diseases associated with the activity or expression of phosphodiesterase, especially PDE4-associated immune and inflammatory diseases, such as psoriasis and arthritis.
Type:
Grant
Filed:
February 3, 2019
Date of Patent:
November 19, 2024
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The invention relates to solid crystalline forms of Compound (I), such as e.g., Form VII, including pharmaceutical compositions thereof and processes for preparing crystalline Compound (I), Form VII. Compound (I) modulates or inhibits the activity of BET bromodomain-containing proteins, and is useful in the treatment of diseases such as cancer, inflammatory and cardiovascular diseases.
Type:
Grant
Filed:
September 13, 2019
Date of Patent:
November 19, 2024
Assignee:
ZENITH EPIGENETICS LTD.
Inventors:
Feng Wen, Jiahui Chen, Xianghui Wen, Mark T. Edgar, Henrik C. Hansen
Abstract: Disclosed are a 3-aryloxyl-3-five-membered heteroaryl propylamine compound and use thereof. Specifically disclosed is a compound or a pharmacologically acceptable salt thereof or a prodrug thereof. The compound has the structure of formula I. The compound or the pharmacologically acceptable salt thereof or the prodrug thereof has excellent inhibition to transient receptor potential (TPR) channel proteins, and has good therapeutic effect on diseases related to the TPR channel proteins.
Abstract: Polyethylene glycol derivatives of the following formula I and uses thereof are disclosed. A method for manufacturing the polyethylene glycol derivatives is also disclosed.
Type:
Grant
Filed:
December 20, 2022
Date of Patent:
November 12, 2024
Assignee:
HANMI PHARM. CO., LTD.
Inventors:
Dae Jin Kim, Jong Soo Lee, Sung Min Bae, Se Chang Kwon
Abstract: The invention relates to certain 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives as defined herein. These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
Type:
Grant
Filed:
January 12, 2023
Date of Patent:
November 5, 2024
Assignee:
Albireo AB
Inventors:
Per-Göran Gillberg, Ingemar Starke, Santosh S. Kulkarni
Abstract: The disclosure is directed to compounds of Formula I pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.
Type:
Grant
Filed:
December 17, 2021
Date of Patent:
October 29, 2024
Assignee:
Prelude Therapeutics Incorporated
Inventors:
Xiaowei Wu, Andrew W. Buesking, Andrew Paul Combs, Ryan Holmes, Sarah Pawley, Katarina Rohlfing
Abstract: A method for therapeutic treatment of pain-associated anxiety or depression in a mammalian subject in need thereof, that includes administering to the subject an effective amount of a pharmaceutical composition containing a morphinan derivative that exhibits an opioid ? receptor agonist activity.
Abstract: Provided is a thiobenzopyran-based compound of Formula I and its pharmaceutically acceptable salt, and its use in the preparation of drugs for the treatment of rheumatoid arthritis, wherein X is selected from oxygen, sulfur, —SO—, and —SO2—; Y is a sulfur atom and Z is H, Na, or K. Through preliminary tests of anti-inflammatory activity, compounds of formula I have anti-rheumatoid arthritis effects.
Abstract: Disclosed herein are novel carborane hydroxamic acid matrix metalloproteinase (“MMP”) inhibitors and agents bearing borane-containing moieties and methods for their use in treating or preventing a disease, such as cancer and rheumatoid arthritis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: Formula (I) wherein the substituents are as described.
Type:
Grant
Filed:
February 28, 2023
Date of Patent:
October 8, 2024
Assignee:
LOYOLA UNIVERSITY OF CHICAGO
Inventors:
Daniel Paul Becker, Marlon Ray Lutz, Jr.
Abstract: The present disclosure relates generally to inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions thereof, and methods of using said compounds and compositions thereof. More specifically, the present disclosure relates to triazolopyrimidine and imidazolopyrimidine inhibitors of ENPP1 and methods of their use for treating disease mediated by ENPP1.
Type:
Grant
Filed:
June 15, 2021
Date of Patent:
September 17, 2024
Assignee:
Volastra Therapeutics, Inc.
Inventors:
Sarah Bettigole, Michael Su, Derek A. Cogan, Leon Van Berkom, Piotr Nieczypor, Gydo Van Der Heijden, Prashanna Vijayachandran
Abstract: A deuterated compound having structural formula I or a pharmaceutically acceptable salt thereof: Values and example values of the variable in formula (I) are disclosed herein. Also disclosed are the use of compounds of formula (I) in the methods of treating a disease selected from cancer, an autoimmune disease, and an infectious disease, and methods of enhancing an immune response to an antigen.
Abstract: The present invention relates to a method for racemizing (5R)-4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-2-methyl-benzoic acid.
Abstract: The present invention relates to a new process for the synthesis of 3?-hydroxy-5?-pregnan-20-one, commonly known as brexanolone, wherein the corresponding cyclic 20-ketal or cyclic 20-thioketal compound of formula (IV) is deprotected with the use or iodine in an organic solvent: (I).