Inhibition of DYRK1A kinase
AssigneeAnkh Life Sciences Limited
InventorsGene H. Zaid, Brian Scott Johnathan Blagg, Cameron E. West
Life of this patent
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Abstract
Novel compounds which inhibit DYRK1A activity comprise thymoquinone derivatives including a pair of substituted or unsubstituted six-membered carbon rings selected from phenyl and cyclohexadiene linked by an alkyl or alkenyl linker. Each six-membered ring includes at least one oxygen-bearing substituent selected from carbonyl oxygens, hydroxyls, alkoxyls, and halogenated derivatives thereof. The compounds can be administered to mammalian subjects for inhibition of DYRK1A kinase proteins.
Claims21
One or more compounds having the structure I and/or II:
- wherein:
- the linker -[ ]n- is a branched or unbranched alkyl or alkenyl group, where n is from 1-6;
- each R1, R2, R4, R1′, R2′, and R4′ are independently selected from the group consisting of —H, branched alkyl groups, and unbranched alkyl groups;
- each R3 is independently selected from the group consisting of hydroxyls, alkoxyls, straight and branched alkyl groups, halogenated derivates thereof, and halogens, provided that at least one of the six-membered rings in a pair comprises at least one oxygen-bearing substituent;
- optionally wherein one or more carbon atoms of the linker and/or any of R1, R2, R3, R4, R1′, R2′, and R4′ may be independently substituted with a halogen or hydroxyl group, subject to the proviso that at least one of R2 and R4 in compound I is an isopropyl group, and/or at least one of R2′ and R4′ in compound II is an isopropyl group.
A method of inhibiting DYRK1A activity comprising the step of contacting DYRK1A kinase with an effective amount of a thymoquinone derivative comprising a pair of substituted or unsubstituted six-membered carbon rings selected from the group consisting of phenyl and cyclohexadiene linked by a linker bonded to both of said six-membered rings, at least one of said six-membered rings having a pair of oxygen-bearing substituents selected from the group consisting of carbonyl oxygens, hydroxyls, alkoxyls, and halogenated derivatives thereof, said linker being a straight or branched chain alkyl or alkenyl group having from 1-6 carbon atoms.
Dependencies are inferred from the claim text.