Sulfamate derivative compound for use in preventing or treating epilepsy
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Publication Number
US-9937145-B2
Publication Date
2018-04-10
Expiration Date
Abstract
The present invention relates to a pharmaceutical composition for treating or preventing epilepsy containing a sulfamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention epilepsy comprising administering a sulfamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of epilepsy.
Core Innovation
The invention relates to a method of treating epilepsy in a subject in need thereof by administering a pharmaceutically effective amount of a pharmaceutical composition comprising a sulfamate derivative compound represented by Chemical Formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient. The sulfamate derivative compound is defined by substituent classes for R1 and R2, an aryl moiety or a heterocyclic moiety A, and additional substituent variables R3 and R4, together with integer indices l and m.
Chemical Formula 1 defines R1 and R2 as each independently hydrogen, C1-C5 alkyl, C2-C5 alkenyl, or C6-C10 aryl, with options that R1 and R2 together with the carbon atom to which they attach form a C3-C12 cycloalkyl group or that R1 and R2 together with the oxygen atom to which they attach form a carbonyl group. The moiety A is an aryl moiety or a heterocyclic moiety optionally substituted by hydroxyl, alkoxy, alkyl, alkenyl, aryl, alkoxycarbonyl, carboxyl, acyl, alkylthio, cyano, nitro, amine, alkyl amine, and halogen.
R3 and R4 are each independently hydrogen or C1-C3 alkyl, and l and m are each independently an integer of 0 to 4. The dependent claims further specify stereochemical forms, enumerated substituted sulfamate and related sodium sulfonamide/sulfonyl members, and narrow the scope by constraining l and m to 0 to 2 and R3 and R4 to hydrogen or methyl.
Claims Coverage
One independent claim is identified. The claim coverage centers on treating epilepsy by administering a pharmaceutically effective amount of a pharmaceutical composition containing a sulfamate derivative compound represented by Chemical Formula 1 or a pharmaceutically acceptable salt, with inventive features defined by the Chemical Formula 1 substituent classes and dependent narrowing by stereochemical form, enumerated members, and parameter limits.
Epilepsy treatment by administering a sulfamate derivative pharmaceutical composition
A method of treating an epilepsy in a subject in need thereof comprising administering a pharmaceutically effective amount of a pharmaceutical composition comprising a sulfamate derivative compound represented by Chemical Formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient.
Defined substituent classes for R1 and R2
R1 and R2 are each independently selected from hydrogen, C1-C5 alkyl, C2-C5 alkenyl, and C6-C10 aryl, or R1 and R2 together with the carbon atom to which they attach form a C3-C12 cycloalkyl group, or R1 and R2 are bond and together with the oxygen atom to which they attach form a carbonyl group.
Optional substitution on aryl or heterocyclic moiety A
A is an aryl moiety or a heterocyclic moiety optionally substituted by one or more substituents selected from hydroxyl, alkoxy, alkyl, alkenyl, aryl, alkoxycarbonyl, carboxyl, acyl, alkylthio, cyano, nitro, amine, alkyl amine, and halogen.
Defined substituents R3 and R4 and indices l and m
R3 and R4 are each independently hydrogen or C1-C3 alkyl, and l and m are each independently an integer of 0 to 4.
Stereochemical form selection
The method uses selected stereochemical forms including racemate, enantiomer, diastereomer, or mixtures of enantiomers or diastereomers.
Enumerated substituted sulfamate and related sodium sulfonamide/sulfonyl members
The active ingredient is limited to selected substituted sulfamate compounds and related sodium sulfonamide/sulfonyl members with specified aryl/heteroaryl substitution patterns and dioxolane or dioxaspiro ring structures.
Integer range constraint for l and m
l and m are each independently integers in the range 0 to 2.
R3 and R4 restricted to hydrogen or methyl
R3 and R4 are each independently hydrogen or methyl.
Overall, the claims cover an epilepsy-treatment method that administers a pharmaceutically effective composition containing a Chemical Formula 1 sulfamate derivative or pharmaceutically acceptable salt. The inventive scope is defined by the R1/R2, A, R3/R4, and l/m structural features, with dependent claims further narrowing stereochemical form, enumerated substituted sulfamate or related members, and the allowed ranges or values for l, m, R3, and R4.
Stated Advantages
Enhanced anti-epileptic activity with decreased side effects.
Documented Applications
Treatment of epilepsy in a subject in need thereof using a pharmaceutical composition containing the specified sulfamate derivative compounds of Chemical Formula 1 or pharmaceutically acceptable salts.
In vivo anti-epilepsy efficacy testing in MES and lithium-pilocarpine induced epilepsy (LI-PILO), with reported ED50 values and protection percentages for multiple listed examples.
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