Patent ID: 6413949
Filing Date: 2002-07-02
Classification: A61K,C07F,Y10S

Abstract:
A method for treating epilepsy in a mammal comprising administering to a mammal in need of treatment, an amount of a pharmaceutically acceptable prodrug effective to treat epilepsy,said prodrug comprising valproic acid or a pharmaceutically acceptable derivative thereof covalently bonded to an intracellular transporting adjuvant, said intracellular transporting adjuvant comprising a compound selected from the group consisting of C3-20 fatty acid monoglycerides, C3-20 fatty acid diglycerides, hydroxy-C2-6-alkyl esters of C3-20 fatty acids, hydroxy-C2-6-alkyl esters of lysophosphatidic acids, lyso-plasmalogens, lysophospho-lipids, lysophosphatidic acid amides, glycerophosphoric acids, lyso-phosphatidalethanolamine lysophosphatidyl-ethanolamine, N-mono-(C1-4)-alkyl and N,N-di-(C1-4)-alkyl and quaternary derivatives of the amines thereof, wherein said covalent bond is scission-sensitive to supranormal intracellular enzyme activity; said prodrug being cell membrane permeable and said covalent bond being cleaved in the presence of said supranormal intracellular enzyme activity and wherein cleavage of said covalent bond results in selective intracellular accumulation of therapeutic amounts of valproic acid within cells having said supranormal intracellular enzyme activity.