Pyrimidine compounds as anti-ictogenic and/or anti-epileptogenic agents
AssigneeQueen's University
InventorsDonald F. Weaver, Buhendwa Musole Guillain, John R. Carran, Kathryn Jones
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Abstract
Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and/or epileptogenesis. Methods for preparing the compounds of the invention are also described. Particularly preferred compounds of the invention include: 1
Claims63
An anti-ictogenic or anti-epileptogenic compound of the formula
- 69
- where
- R9 is hydrogen, alkyl, alkynyl, aryl, amino, hydroxy, halogen, nitro, carboxyl, or R9 and R10 together form a 5- or 6-membered carbocyclic or heterocyclic ring;
- R10 is hydrogen, alkyl, aryl, carboxyl, or R9 and R10 together form a 5- or 6-membered carbocyclic or heterocyclic ring;
- R11 is hydrogen, alkyl, amino, thioether, or tetrahydrofuranyl;
- and
- R12 is hydrogen, alkyl, amino, or thioether;
- or pharmaceutically acceptable salts or esters thereof.
A method of treating or preventing ictogenesis in a subject in need thereof comprising administering to said subject an amount of a compound of any one of claims 1, 29, 30, 31, 32, 36, 37, 55-63 effective to inhibit ictogenesis in said subject so that ictogenesis is treated or prevented in said subject.
A method of treating or preventing epileptogenesis in a subject comprising administering to a subject an amount of a compound of any one of claims 1, 29, 30, 31, 32, 36, 37, 55-63 effective to inhibit epileptogenesis so that epileptogenesis is treated or prevented in said subject.
A kit for treating or preventing ictogenesis in a subject comprising said compound of any one of claims 1, 29, 30, 31, 32, 36, 37, 55-63 and instructions for administering a therapeutically effective amount of a compound to said subject so that ictogenesis is treated or prevented in said subject.
A kit for treating or preventing epileptogenesis in a subject comprising said compound of any one of claims 1, 29, 30, 31, 32, 36, 37, 55-63 and instructions for administering a therapeutically effective amount of a compound to said subject so that epileptogenesis is treated or prevented in said subject.
A method of diagnosing an epileptogenic condition in a subject comprising administering a compound of any one of claims 1, 29, 30, 31, 32, 36, 37, 55-63 labeled with a detectable marker to said subject;
- and measuring increased binding of the compound to the NMDA receptors of the neurons of said subject's brain so that an epileptogenic condition is diagnosed in said subject.
A method of treating or preventing seizures in a subject suffering from head trauma comprising administering to said subject an amount of a compound of any one of claims 1, 29, 30, 31, 32, 36, 37, 55-63 so that seizures are treated or prevented in said subject.
An anti-ictogenic or anti-epileptogenic compound of the formula
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Dependencies are inferred from the claim text.