Process for preparing a compound useful to treat mycoses
Inventors
COLLEY, Thomas Christopher • Ito, Kazuhiro • RAPEPORT, Garth • Strong, Peter • Murray, Peter John • Onions, Stuart Thomas • Sunose, Mihiro
Assignees
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Publication Number
US-12269814-B2
Publication Date
2025-04-08
Expiration Date
Abstract
A combination therapy including one or more compounds of formula (I): wherein R represents hydrogen, halo, cyano, C1-4 haloalkyl, C1-4 haloalkoxy, or SO2NR5R6, R1a and R1b independently represent hydrogen or halo; R2 represents hydrogen, halo, cyano, C1-4 alkyl, C1-4 alkoxy, or C1-4 haloalkoxy; R3 represents halo, cyano, C1-4 alkyl, or C1-4 hydroxyalkyl; R4 represents hydrogen or C1-4 alkyl; X represents CH or N; Y represents N or CH which carbon atom may optionally be substituted by R, R1a or R1b; R5 and R6 independently represent hydrogen or C1-4 alkyl; or a pharmaceutically acceptable salt thereof; and a second or further active ingredient.
Core Innovation
The invention provides antifungal therapeutic use of compounds of formula (I), described as benzamide-piperazine scaffold compounds having defined substituent ranges for R, R1a, R1b, R2-R6, X, and Y, together with pharmaceutically acceptable salts. The subject matter includes enantiomeric, polymorph, stable isotope/deuterium, and salt extensions, and it identifies the compound of formula (I) as a primary antifungal agent for use in treating mycoses.
The document states antifungal efficacy against fungi such as Aspergillus fumigatus and other Aspergillus spp., and also encompasses Candida spp., Rhizopus spp., Cryptococcus spp., Chaetomium spp., Penicillium spp., and Trichophyton spp. The reported results provide evidence of antifungal activity against fungal growth and fungal burden in relevant in vitro and in vivo contexts, including lung effects and measures such as CFU and galactomannan.
The document further discloses pharmaceutical compositions and administration formats associated with the compound of formula (I), including topical lung or nose administration and intranasal administration formats such as aerosol, nebulizer, and dry powder with particle size ranges. It also discloses combination therapy concepts in which the compound of formula (I) is used together with a second or further active ingredient, with example second actives including antifungal agents and cholesterol-pathway inhibitors.
Claims Coverage
The independent claims cover two inventive features: combination therapy using compounds of formula (I) with a second or further active ingredient, and a kit of parts including a formula (I) pharmaceutical composition, additional active ingredient compositions, and administration instructions.
Formula (I) combination therapy with second or further active ingredient
A combination therapy comprising one or more compounds of formula (I), defined by substituent parameters R, R1a, R1b, R2-R6, X, and Y, or pharmaceutically acceptable salts thereof, together with a second or further active ingredient.
Kit of parts with formula (I) composition, additional active ingredients, and instructions
A kit of parts comprising a pharmaceutical composition containing one or more compounds of formula (I) or pharmaceutically acceptable salts thereof, a pharmaceutical composition containing a second active ingredient, optionally one or more further pharmaceutical compositions each containing a third or further active ingredient, and instructions for administration of the pharmaceutical compositions to a subject in need thereof.
The claim set primarily covers combination therapy where compounds of formula (I) are administered with a second or further active ingredient, and a corresponding kit-of-parts format that packages the formula (I) composition with additional active ingredient compositions plus instructions.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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