Abstract: The present disclosure provides compounds useful for the prevention of amyloid formation and the treatment of amyloid related disorders, including synucleopathies such as Parkinson's Disease.
Type:
Grant
Filed:
August 6, 2018
Date of Patent:
November 22, 2022
Assignee:
Axial Therapeutics, Inc.
Inventors:
Anthony Stewart Campbell, Bridget Cole, Alessandra Bartolozzi
Abstract: Compounds having a structure according to formula are modulators of TLR7 activity and can be used to treat conditions amenable to treatment by the modulation of TLR7 activity.
Type:
Grant
Filed:
April 23, 2019
Date of Patent:
November 1, 2022
Assignee:
BRISTOL-MYERS SQUIBB COMPANY
Inventors:
Ashok V. Purandare, Honghe Wan, Liqi He, Sanjeev Gangwar, Shoshana L. Posy, Yam B. Poudel, Prasanna Sivaprakasam, Naidu S. Chowdari
Abstract: The present invention relates to desmethylanethole trithione (AOX) and derivatives thereof, especially derivatives of formula (I), for the prevention and treatment of diseases whose initiation and/or evolution relates to the production and effects of reactive oxygen species (ROS) of mitochondrial origin,
Type:
Grant
Filed:
March 7, 2018
Date of Patent:
November 1, 2022
Assignees:
OP2 Drugs, Centre Hospitalier Universitaire de Bordeaux, Institut National de la Santé et de la Recherche Médicale (INSERM), Université de Bordeaux
Inventors:
Philippe Diolez, Frédéric Marin, Olivier Petitjean
Abstract: A new analgesic has been developed for T-type calcium channels as therapeutic targets. The present invention provides a T-type calcium channel inhibitor which is a compound represented by formula (1): wherein each of R1 and R2 independently represents —H or —OH; R3 represents —OH; R4 represents —OH or —H; R5 represents a straight or branched alkyl or cycloalkyl-alkyl group having one to ten carbon atoms or a straight or branched alkenyl or cycloalkyl-alkenyl group having two to ten carbon atoms, or a pharmaceutically acceptable salt or solvate thereof. The present invention also provides this T-type calcium channel inhibitor, a medicament containing the T-type calcium channel inhibitor, and a therapeutic or prophylactic agent for a disease having an effective T-type calcium channel inhibitory action.
Type:
Grant
Filed:
September 21, 2018
Date of Patent:
October 25, 2022
Assignees:
KINKI UNIVERSITY, NATIONAL UNIVERSITY CORPORATION UNIVERSITY OF TOYAMA, FUSO PHARMACEUTICAL INDUSTRIES, LTD.
Abstract: Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
Type:
Grant
Filed:
August 10, 2020
Date of Patent:
October 25, 2022
Assignee:
CRINETICS PHARMACEUTICALS, INC.
Inventors:
Jian Zhao, Yunfei Zhu, Shimiao Wang, Mi Chen, Joseph Pontillo
Abstract: The present invention provides novel heterocyclic compounds of the general formula (I), including novel compounds of formula (Ia), and pharmaceutical compositions containing them. Moreover, the compounds of formula (I) or (Ia) and the pharmaceutical compositions containing them are provided for use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. The compounds of formula (I) or (Ia) can act as modulators of nervous system receptors sensitive to glutamate, in particular as modulators of metabotropic glutamate receptors (mGluRs), which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.
Type:
Grant
Filed:
May 14, 2018
Date of Patent:
October 18, 2022
Assignee:
Domain Therapeutics
Inventors:
Anne-Laure Blayo, Thomas Catelain, Ismet Dorange, Cédric Genet, Baptiste Manteau, Stanislas Mayer, Stephan Schann
Abstract: The present invention relates to a process for the preparation of enantiomerically enriched 3-aminopiperidine, as in particular of its R-enantiomer (R)-3-aminopiperidine. The invention also relates to an enantiomerically enriched intermediate of said process and to specific acid-addition salts of 3-aminopiperidine (hereinafter also APIP) that are useful for obtaining a single enantiomer of APIP, and to crystalline (R)-3-aminopiperidine-dihydrochloride-monohydrateand crystalline (S)-3-aminopiperidine-dihydrochloride-monohydrate.
Type:
Grant
Filed:
September 23, 2019
Date of Patent:
October 18, 2022
Inventors:
Karl Reuter, Tobias Wedel, Viktor Meier, Mark Kantor, Vasyl Andrushko, Florian Stolz
Abstract: The present disclosure provides compounds represented by Formula (I): and pharmaceutically acceptable salts, solvates, e.g., hydrates, and prodrugs thereof wherein X and n are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat diseases and conditions, e.g., cancer, wherein inhibition of HDAC provides a benefit.
Type:
Grant
Filed:
March 29, 2018
Date of Patent:
October 18, 2022
Assignees:
The George Washington University, The Board of Trustees ofthe University of Illinois
Inventors:
Alejandro Villagra, Alan P. Kozikowski, Sida Shen
Abstract: Inhibitors of oxidized low-density lipoprotein receptor 1 (LOX-1), compositions comprising inhibitors of LOX-1, and methods of using thereof are described.
Type:
Grant
Filed:
December 19, 2019
Date of Patent:
October 11, 2022
Assignees:
THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS, BIOVENTURES, LLC
Inventors:
Jawahar L. Mehta, Magomed Khaidakov, Kottayil I. Varughese, Shraddha Thakkar, Yao Dai, Peter Crooks, Narsimha Reddy Penthala
Abstract: Provided is a method for treating or preventing cancer, containing, as an active ingredient, a compound having a specific chemical structure and an activity of inhibiting the formation of a c-Myc/Max/DNA complex, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
July 27, 2017
Date of Patent:
October 11, 2022
Assignee:
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
Inventors:
Kyung Chae Jeong, Hwan Jung Lim, Seong Jun Park, Ho Kyung Seo, Kyung Ohk Ahn, Sang Jin Lee, Eun Sook Lee
Abstract: This invention is directed to compositions, methods and kits that can be used for the treatment or amelioration of pain.
Type:
Grant
Filed:
March 12, 2018
Date of Patent:
October 4, 2022
Assignees:
The Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, University of Alcala De Henares, South Rampart Pharma, LLC
Inventors:
Nicolas Bazan, Hernan Bazan, Julio Alvarez-Builla, Dennis Paul, Carolina Burgos
Abstract: The invention relates to benzimidazole derivatives of the general formula I, and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
Type:
Grant
Filed:
August 20, 2018
Date of Patent:
September 27, 2022
Assignee:
Merck Patent GmbH
Inventors:
Eva-Maria Tanzer, Kai Schiemann, Markus Klein
Abstract: An object of the present invention is to provide an ?,?-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like. The ?,?-unsaturated amide compound represented by the following formula (I) or a pharmaceutically acceptable salt or the like thereof has anticancer activity and the like: [wherein, “A” represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO2—, —NRX1— (wherein, RX1 represents hydrogen atom or lower alkyl), —CHRX2— (wherein, RX2 represents hydrogen atom or hydroxy), —CH?CH—, ?CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].
Abstract: Disclosed herein are polymers containing repeating units of formula (I) or copolymers containing the repeating units of formula (I) and (II), where R1 to R12, m, n, p, q, x and y are as defined herein. The polymers and copolymers have an antimicrobial effect and may be used therapeutically or in formulations intended for use as detergents.
Type:
Grant
Filed:
April 18, 2018
Date of Patent:
September 13, 2022
Assignees:
Nanyang Technological University, Massachusetts Institute of Technology
Inventors:
Bee Eng Mary Chan, Paula T. Hammond, Bo Liu, Wenbin Zhong
Abstract: The present disclosure relates to a salt of phenyl pyrimidinone compound, a polymorph thereof and a pharmaceutical composition comprising the same and a use thereof, particularly relates to the hydrochlorate of phenyl pyrimidinone compound of following formula (I-A) and a pharmaceutically acceptable polymorph, solvate, hydrate, co-crystal, anhydrous substance, or amorphous form thereof, a pharmaceutical composition and a pharmaceutical unit dosage comprising the same, the preparing method and use thereof.
Type:
Grant
Filed:
January 7, 2020
Date of Patent:
September 6, 2022
Assignees:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, SUZHOU VIGONVITA LIFE SCIENCES CO., LTD., TOPHARMAN SHANGHAI CO., LTD.
Abstract: Sulcardine salts other than sulfuric acid salts of sulcardine, including crystalline sulcardine salts, are provided herein. Pharmaceutical compositions comprising such salts and methods of treating arrhythmias comprising administering effective amounts of such salts are also provided.
Type:
Grant
Filed:
January 28, 2020
Date of Patent:
August 30, 2022
Assignee:
HUYABIO International, LLC
Inventors:
Suzanne J. Romano, Hayley Ann Reece, Joseph Edward Gordon Benson, Sarah Collins, Gary T. Elliott, Mireille Gillings, Robert Goodenow, Curtis Tyree
Abstract: This invention relates to compounds that are useful as cancer therapies. The compounds comprise azithromycin derivatives having a phosphonium cation tethered to the azithromycin macrocycle. The invention also relates to methods of using said compounds and the pharmaceutical formulations comprising said compounds.
Type:
Grant
Filed:
April 20, 2018
Date of Patent:
August 30, 2022
Inventors:
Tim Sparey, Andrew Ratcliffe, Brett Stevenson, Franz Lagasse, Edward Cochrane
Abstract: A lactone compound is represented by general formula (A), and an ether compound is represented by general formula (B). In formula (A), R is a hydrogen atom or R1. When R is a hydrogen atom, R? is R1, the carbon bond (1) is a single bond or a double bond, and the carbon bond (2) is a single bond. When R is R1, R? is a hydrogen atom or R1, both the carbon bonds (1) and (2) are a single bond, or one of them is a double bond and the other is a single bond. In formula (B), R? is R1. R1 represents a specific alkyl group, a specific alkenyl group, a specific alkynyl group, or an aryl group. In formulas (A) and (B), n is 0 or 1.