Abstract: Provided herein are compounds of the Formula (I): (I) and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein Rx, Ry, W, X, Y, Z, Ring A and (AA) have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
Type:
Grant
Filed:
September 6, 2019
Date of Patent:
April 23, 2024
Assignee:
ARRAY BIOPHARMA INC.
Inventors:
James F. Blake, Donghua Dai, Julia Haas, Yutong Jiang, Dean Kahn, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L McKenney, Andrew T. Metcalf, David A. Moreno, Brett Prigaro, Ginelle A. Ramann, Li Ren, Shane M. Walls, Hailong Zhang
Abstract: Provided are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, and R3 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to novel compounds having a histone deacetylase 6 (HDAC6) inhibitory activity, optical isomers thereof or pharmaceutically acceptable salts thereof, a pharmaceutical use thereof, and a method for preparing the same. According to the present invention, the novel compounds, optical isomers thereof or pharmaceutically acceptable salts thereof have the histone deacetylase 6 (HDAC6) inhibitory activity, and are effective in preventing or treating HDAC6-related diseases, comprising infectious diseases; neoplasm; internal secretion; nutritional and metabolic diseases; mental and behavioral disorders; neurological diseases; eye and ocular adnexal diseases; circulatory diseases; respiratory diseases; digestive diseases; skin and subcutaneous tissue diseases; musculoskeletal system and connective tissue diseases; and teratosis or deformities, and chromosomal aberration.
Type:
Grant
Filed:
July 25, 2019
Date of Patent:
April 16, 2024
Assignee:
Chong Kun Dang Pharmaceutical Corp.
Inventors:
Chang Sik Lee, Jung Taek Oh, Hokeun Yun, Hyeseung Song, Hyunjin Michael Kim
Abstract: In one aspect, the disclosure relates to methods for preparation of terpene and terpene-like molecules. In a further aspect, the disclosure relates to the products of the disclosed methods, i.e., terpene and terpene-like molecules prepared using the disclosed methods. Intermediates for the synthesis of a wide variety of terpenoids are ?-allyl Knoevenagel adducts or quasi ?-allyl Knoevenagel adducts are disclosed. In various aspects, methods of preparing terpenoids through these intermediates are disclosed. The methods can comprise ?-alkylation of an allylic electrophile followed by ring-closure metathesis to a polycyclic terpenoid structure. In a further aspect, the disclosure pertains to terpenoid frameworks, and compounds prepared via disclosed oxidation and substitution reactions on the disclosed terpenoid frameworks. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
Type:
Grant
Filed:
September 15, 2017
Date of Patent:
April 9, 2024
Assignee:
University of Florida Research Foundation, Inc.
Abstract: Substituted cyclohexyl chemical entities of Formula (I): wherein Ra, G, and Rb have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.
Type:
Grant
Filed:
June 15, 2022
Date of Patent:
April 2, 2024
Assignee:
Dart Neuroscience, LLC
Inventors:
Jillian Basinger Thompson, Brett C. Bookser, Scott Burley, Pablo Garcia-Reynaga, Andrew Hudson, Marco Peters, Benjamin Pratt, Aaron Thompson, Joe Tran, Lino Valdez
Abstract: Pharmaceutical compositions are provided according to aspects of the present disclosure which include a compound having chemical structural formula I: where R1 is selected from the group consisting of: an alkyl group, a heteroalkyl group, an aryl group, a heteroaryl group, an alkenyl group, a heteroalkenyl group, an alkynyl group, a heteroalkynyl group, a cycloalkyl group, a hetercycloalkyl group, an alkylcycloalkyl group, a heteroalkyl cycloalkyl group, an aralkyl group, a heteroaralkyl group, an alkoxy group, a polar group, an ester and a charged group; a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof; and/or a pharmaceutically acceptable salt thereof; where R4? is H or an alkoxy group; where both R5 and R3? are OH, or where one or both OH groups is optionally modified as a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof; and/or a deuterated form thereof; and/or a pharmaceutically acceptable salt thereof; and a pharma
Abstract: A method for the oxidation of ethylene to form ethylene oxide which comprises treating an aqueous stream in a cycle water treatment unit containing an anion exchange resin to reduce the content of the impurities.
Type:
Grant
Filed:
March 4, 2022
Date of Patent:
March 12, 2024
Assignee:
Scientific Design Company, Inc.
Inventors:
Saurabh Katiyar, Saurabh H. Parikh, Jason P. Durand
Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
Type:
Grant
Filed:
November 8, 2022
Date of Patent:
March 5, 2024
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Steven John Durrant, Nadia M. Ahmad, Elizabeth Mary Beck, Lidio Marx Carvalho Meireles, Ewa Iwona Chudyk, Gorka Etxebarria Jardi, Bhairavi Galan, Sara S. Hadida Ruah, Dennis James Hurley, Ronald Marcellus Knegtel, Timothy Donald Neubert, Joanne Louise Pinder, Joseph Pontillo, Robert Pullin, Yvonne Schmidt, David Matthew Shaw, Sarah Skerratt, Dean Stamos, Stephen Andrew Thomson, Anisa Nizarali Virani, Christopher Wray
Abstract: Provided herein are compounds of Formula (I), Formula (II), and Formula (III) or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7 and A are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I), Formula (II), or Formula (III) and methods of using a compound of Formula (I), Formula (II), or Formula (III), e.g., in the treatment of a mental health disease or disorder.
Type:
Grant
Filed:
December 28, 2022
Date of Patent:
February 27, 2024
Assignee:
EmpathBio, Inc.
Inventors:
Robert B. Perni, Glenn Short, Tanweer A. Khan
Abstract: The invention provides a material comprising (i) a crown ether of formula (I), (ii) a crown ether of formula (II), and/or (iii) a crown ether of formula (III), or a salt thereof, wherein each m independently is an integer from 1 to 8, p is an integer from 1 to 1000, each “” designates an optionally present bond and/or structure, each X is an optionally present substituent, each * independently represents —H, ?O, or a bond to a remainder of the material, provided that at least one * is a bond to the remainder of the material, and wherein the remainder of the material is bound via a sp3-sp3 carbon-carbon bond, a method of making the material, and a method of using the material.
Type:
Grant
Filed:
November 4, 2022
Date of Patent:
February 20, 2024
Assignee:
Pall Corporation
Inventors:
Andrew Kocen, Yiren Zhang, Rehanah Sejoubsari, Ahmad Arabi Shams Abadi
Abstract: The present invention provides processes for preparing a compound of formula (I) and pharmaceutically acceptable salts thereof, comprising deprotecting a compound of formula (II), wherein each R3 independently represents a tertiary alkyl group, preferably wherein each R3 is tertiary butyl. The invention also provides intermediates useful for preparing compounds of formula (I) and processes for preparing these intermediates. Additionally the invention provides polymorphic forms of the dichloride salt of the compound of formula (I) and their use in the treatment of proliferative disorders.
Type:
Grant
Filed:
April 24, 2018
Date of Patent:
February 6, 2024
Inventors:
Gregor Welti, Markus Heubes, David Tagliaferri
Abstract: The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.
Type:
Grant
Filed:
April 30, 2021
Date of Patent:
January 9, 2024
Assignee:
Corsair Pharma, Inc.
Inventors:
Xiaoming Zhang, Meenakshi S. Venkatraman, Cyrus K. Becker
Abstract: Provided herein are, inter alia, compounds inhibiting poly(ADP-ribose) Glycohydrolase (PARG) in a cancer cell and methods of treating cancer using compounds of the invention.
Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
Type:
Grant
Filed:
June 13, 2019
Date of Patent:
January 2, 2024
Assignee:
Pfizer Inc.
Inventors:
Gary Erik Aspnes, Scott W. Bagley, Edward L. Conn, John M. Curto, David J. Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Chris Limberakis, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound useful in the treatment of a neurodegenerative disorder and their combined use as a medicament, in particular for the treatment of neurodegenerative and/or cognitive disorders.
Type:
Grant
Filed:
December 12, 2018
Date of Patent:
December 26, 2023
Assignee:
H. Lundbeck A/S
Inventors:
Jan Kehler, Karsten Juhl, Mauro Marigo, Paulo Jorge Vieira Vital, Mikkel Jessing, Morten Langgård, Lars Kyhn Rasmussen, Carl Martin Sebastian Clementson
Abstract: The disclosure provides chemical compounds possessing therapeutic and/or protective properties against oxidative damage. Methods of making such therapeutic and/or protective compounds and associated compositions are also provided, as are methods for their use, which include protecting cells from oxidative damage and/or inhibiting production of ROS in a cell or subject, as well as preventing or reducing the extent of tissue damage caused by an ischemic event in a subject at elevated risk of such an event.
Type:
Grant
Filed:
November 15, 2021
Date of Patent:
December 5, 2023
Assignee:
University of South Alabama
Inventors:
Gary Piazza, Xi Chen, Herbert Weissbach, Shailaja Kesraju Allani
Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
Type:
Grant
Filed:
December 4, 2020
Date of Patent:
December 5, 2023
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Steven John Durrant, Nadia Ahmad, Elizabeth Mary Beck, Lidio Marx Carvalho Meireles, Ewa Iwona Chudyk, Gorka Etxebarria Jardi, Bhairavi Galan, Sara S. Hadida Ruah, Dennis James Hurley, Ronald Marcellus Knegtel, Timothy Donald Neubert, Joanne Louise Pinder, Joseph Pontillo, Robert Pullin, Yvonne Schmidt, David Matthew Shaw, Sarah Skerratt, Dean Stamos, Stephen Andrew Thomson, Anisa Nizarali Virani, Christopher Wray