Blockade of voltage dependent sodium channels
AssigneeUniversity College London
InventorsGiti Garthwaite, David Selwood, Marcel Kling, Grant Wishart
Life of this patent
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Abstract
Compounds of formula (1), and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis.
Claims18
Use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in blockading voltage-dependent sodium channels
- 14
- wherein:
- —R1 is hydrogen, C1-C6 alkyl, aryl or —(C1-C6 alkyl)-aryl;
- —R2 is aryl, heteroaryl, 3- to 6-membered heterocyclyl, C3-C6 carbocyclyl or —XR wherein X is a divalent C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl group and R is aryl, heteroaryl, 3- to 6-membered heterocyclyl or C3-C6 carbocyclyl, or R2 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or —COR, —CONR′R″ or —CO2R′ wherein each R′ and R″ is the same or different and is selected from hydrogen, C1-C6 alkyl, aryl and heteroaryl and R is selected from C1-C6 alkyl, aryl and heteroaryl;
- and
- either R3 and R4, together with the carbon atoms to which they are attached, form a phenyl group, or R3 and R4 are the same or different and are selected from hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, aryl, heteroaryl, 3- to 6-membered heterocyclyl, —COR, —CONR′—NR″COR, —CONR′—NR″CS—R, —CO2R′, -CONR′—NR″—CO2R′, —CONR′—NR″—CS—OR′, —CONR′R″, —CONR′—NR″CO—NR′″R″″ and —conr′—NR″CS—NR′″R″″, wherein each R is the same or different and is selected from C1-C6 alkyl, aryl, -(C1-C6 alkyl)-aryl and heteroaryl and each R′, R″, R′″ and R″″ is the same or different and is selected from hydrogen, C1-C6 alkyl, aryl, —(C1-C6 alkyl)-aryl and heteroaryl:
Use according to any one of the preceding claims, wherein R2 is aryl, heteroaryl, 3- to 6-membered heterocyclyl, C3-C6 carbocyclyl, C1-C6 alkyl, C2-C6 alkenyl, —CONR′R″ or —CO2R′ wherein R′ and R″ are the same or different and are selected from hydrogen, C1-C6 alkyl, aryl and heteroaryl.
Use according to any one of the preceding claims, wherein R3 is hydrogen.
Use according to any one of the preceding claims, wherein R4 is C1-C6 alkyl, aryl, heteroaryl, —CONR′—NR″COR, —CONR′—NR″CS—R, —CO2R′, —CONR′R″, —CONR′—NR″CO—NR′″R″″ or —CONR′—NR″CS—NR′″ R″″ wherein each R is the same or different and is selected from C1-C6 alkyl, aryl, —(C1-C6 alkyl)-aryl and heteroaryl and each R′, R″, R′″ and R″″ is the same or different and is selected from hydrogen, C1-C6 alkyl, aryl, —(C1-C6 alkyl)-aryl and heteroaryl.
Use of a compound of formula (I), as defined in any one of the preceding claims, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in protecting neuronal white matter.
Use according to any one of the preceding claims, wherein the medicament is for use in protecting ganglion cells and axons of the optic nerve from damage.
Use according to any one of the preceding claims, wherein the medicament is for use in the treatment or prevention of normal tension glaucoma or multiple sclerosis.
Dependencies are inferred from the claim text.