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US 2010/0152254 A1Published application
Alpha-halo- and alpha-alkyl-cyclopropylcarboxy compounds and uses thereof
AssigneeYissum Research Development Company of the Hebrew University of Jerusalem
InventorsMeir Bialer, Boris Yagen, Neta Pessah
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Abstract
Novel Alpha-halo- and Alpha-alkyl-cyclopropylcarboxy compounds, and uses of these and related compounds in the treatment of a variety of neurological diseases and disorders, and particularly epilepsy, are provided.
Claims39
A compound having the general Formula I:
- an enantiomer, a prodrug, a hydrate, a solvate or a pharmaceutically acceptable salt thereof,
- wherein:
- X is halide or an alkyl having from 1 to 20 carbon atoms;
- R1-R4 are each independently an alkyl having from 1 to 20 carbon atoms;
- Y is selected from the group consisting of NR5, O and S;
- A is selected from the group consisting of O, N and S;
- and
- R5 is selected from the group consisting of hydrogen, alkyl and cycloalkyl;
- and
- D1 and D2 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, halide, hydroxy, alkoxy, hydroxyalkyl, thiohydroxy, thioalkoxy, thiohydroxyalkyl, aryloxy, thioaryloxy, haloalkyl, amine, carbonyl, amide, thioamide, carbamate, urea, alkyl-sulfonamide, aryl-sulfonamide, alkyl-aryl-sulfonamide, thiadiazole-sulfonamide, alkyl-thiadiazole-sulfonamide or absent;
- with the proviso that when X is halide, Y is O and A is N or O, at least one of D1 and D2 is selected from the group consisting of alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, hydroxy, alkoxy, hydroxyalkyl, thiohydroxy, thioalkoxy, thiohydroxyalkyl, aryloxy, thioaryloxy, haloalkyl, amine, carbonyl, amide, thioamide, carbamate, urea, alkyl-sulfonamide, aryl-sulfonamide, alkyl-aryl-sulfonamide, thiadiazole-sulfonamide, alkyl-thiadiazole-sulfonamide.
8 more elements
A pharmaceutical composition comprising, as an active ingredient, compound having the general Formula VIII:
- an enantiomer, a prodrug, a hydrate, a solvate or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier;
- wherein:
- X is halide or an alkyl having from 1 to 20 carbon atoms;
- R1-R4 are each independently an alkyl having from 1 to 20 carbon atoms;
- Y is selected from the group consisting of NR5, O and S;
- A is selected from the group consisting of O, N and S;
- R5 is selected from the group consisting of hydrogen, alkyl and cycloalkyl;
- and
- D1 and D2 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, halide, hydroxy, alkoxy, hydroxyalkyl, thiohydroxy, thioalkoxy, thiohydroxyalkyl, aryloxy, thioaryloxy, haloalkyl, amine, carbonyl, amide, thioamide, carbamate, alkyl-sulfonamide, aryl-sulfonamide, alkyl-aryl-sulfonamide, thiadiazole-sulfonamide, alkyl-thiadiazole-sulfonamide or absent.
6 more elements
A method of treating a neurological disease or disorder, the method comprising administering to a subject in need thereof a therapeutically effective amount of a compound having the general Formula VIII:
- an enantiomer, a prodrug, a hydrate, a solvate or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier;
- wherein:
- X is halide or an alkyl having from 1 to 20 carbon atoms;
- R1-R4 are each independently an alkyl having from 1 to 20 carbon atoms;
- Y is selected from the group consisting of NR5, O and S;
- A is selected from the group consisting of O, N and S;
- R5 is selected from the group consisting of hydrogen, alkyl and cycloalkyl;
- and
- D1 and D2 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, halide, hydroxy, alkoxy, hydroxyalkyl, thiohydroxy, thioalkoxy, thiohydroxyalkyl, aryloxy, thioaryloxy, haloalkyl, amine, carbonyl, amide, thioamide, carbamate, alkyl-sulfonamide, aryl-sulfonamide, alkyl-aryl-sulfonamide, thiadiazole-sulfonamide, alkyl-thiadiazole-sulfonamide or absent.
6 more elements
20-23. (canceled)
Dependencies are inferred from the claim text.