Abstract: The invention provides a pyrrole compound, which compound is (a) 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide or a deuterated derivative thereof, or (b) 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)-3-hydroxyphenyl)-2-oxoacetamide or a deuterated derivative thereof, or (c) a prodrug of compound (a) or a prodrug of compound (b), or a pharmaceutically acceptable salt or agriculturally acceptable salt of (a), (b) or (c). Also provided are combinations and compositions comprising the compound and known antifungal agents. The invention also relates to the therapeutic use of a compound of the invention in prevention or treatment of fungal diseases.
Type:
Grant
Filed:
February 10, 2020
Date of Patent:
July 20, 2021
Assignee:
F2G Limited
Inventors:
Graham Edward Morris Sibley, Derek Law, Jason David Oliver, Michael Birch
Abstract: A method of identifying an antifungal agent which targets a DHODH protein (alias PyrE, dihydroorotate dehydrogenase, EC: 1.3.99.11) of a fungus comprising contacting a candidate substance with a fungal DHODH protein and determining whether the candidate substance binds or modulates the DHODH protein, wherein binding or modulation indicates that the candidate substance is an antifungal agent. Specific examples concern Aspergillus fumigatus and Candida albicans DHODH proteins. DHODH inhibitors with a Quinazolinone core are also disclosed.
Type:
Grant
Filed:
May 1, 2009
Date of Patent:
May 19, 2015
Assignee:
F2G Limited
Inventors:
Jason David Oliver, John Leslie Thain, Michael John Bromley, Graham Edward Morris Sibley, Michael Birch
Abstract: The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: R1, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
Type:
Grant
Filed:
May 21, 2008
Date of Patent:
September 3, 2013
Assignee:
F2G Limited British Body Corporate
Inventors:
Lloyd James Payne, Robert Downham, Graham Edward Morris Sibley, Philip Edwards, Gareth Morse Davies
Abstract: The invention relates to a mutant bank of diploid micro-organisms which consists of a population of mutant cells in which at least one cell has a random mutation which disrupts the activity of at least one gene, wherein the micro-organism is inducible into haploid form. The invention further relates to a method of using the mutant bank to identify the genes which contribute to a chosen phenotype.
Type:
Application
Filed:
October 25, 2007
Publication date:
April 23, 2009
Applicant:
F2G Limited
Inventors:
David Wemys Denning, Jayne Louise Brookman, Andre Rickers, Mike Birch
Abstract: The invention relates to a mutant bank of diploid micro-organisms which consists of a population of mutant cells in which at least one cell has a random mutation which disrupts the activity of at least one gene, wherein the micro-organism is inducible into haploid form. The invention further relates to a method of using the mutant bank to identify the genes which contribute to a chosen phenotype.
Type:
Grant
Filed:
April 11, 2001
Date of Patent:
December 4, 2007
Assignee:
F2G Limited
Inventors:
David Wemys Denning, Jayne Louise Brookman, Andre Rickers, Mike Birch