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.
Claims14
A pharmaceutical composition comprising, as an active ingredient, a compound having the general Formula:
- an enantiomer, a prodrug, a hydrate, a solvate or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier;
- wherein:
- X is halide;
- 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, the pharmaceutical composition being formulated for administration.
A method of substantially inhibiting, slowing the progression of, or substantially ameliorating clinical or aesthetical symptoms of a neurological disease or disorder, the neurological disease or disorder being selected from the group consisting of epilepsy, convulsions, seizure disorders, status epilepticus, a chemically-induced convulsion and/or seizure disorder, a febrile convulsion condition, hypoglycemia, hyponatremia, hypoxia, a substance withdrawal condition, spasticity, skeletal muscle spasms, restless leg syndrome, anxiety, stress, multiple sclerosis, stroke, head trauma, spinal cord injury, amytrophic lateral sclerosis (ALS), Parkinson's Disease, Huntington's Disease, Alzheimer's Disease, amyotrophic lateral sclerosis, neuropathic pain, deafferentation pain, myoclonus, schizophrenia, migraine, headaches and bipolar disorder, the method comprising administering to a subject in need thereof a therapeutically effective amount of a compound having the general Formula I:
- an enantiomer, a prodrug, a hydrate, a solvate or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier;
- wherein:
- X is halide;
- 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.
Dependencies are inferred from the claim text.