Methane-sulfonamide derivatives, the preparation thereof and composition comprising the same
AssigneeDainippon Pharmaceutical Co., Ltd.
InventorsHitoshi Uno, Mikio Kurokawa, Yoshinobu Masuda
Life of this patent
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Abstract
Methane-sulfonamide derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen or a halogen atom, R.sub.2 and R.sub.3 are the same or different and are each hydrogen or a straight or branched alkyl having 1 to 3 carbon atoms, and one of X and Y is a carbon atom and another is a nitrogen atom, provided that the group: --CH.sub.2 SO.sub.2 NR.sub.2 R.sub.3 is bonded to the carbon atom of either of X and Y, and an alkali metal salt thereof, and a process for the preparation of said methane-sulfonamide derivatives. Said compounds have an excellent anticonvulsant activity and are useful as anticonvulsants for controlling convulsions and seizures in patients with epilepsy.
Claims24
A compound of the formula:
- ##STR12## wherein R.sub.1 is hydrogen or a halogen atom, R.sub.2 and R.sub.3 are the same or different and are each hydrogen or an alkyl having 1 to 3 carbon atoms, and one of X and Y is carbon atom and another is nitrogen atom, provided that the group:
- --CH.sub.2 SO.sub.2 NR.sub.2 R.sub.3 is bonded to the carbon atom of either of X and Y, or an alkali metal salt thereof.
A compound of the formula:
- ##STR13## wherein R.sub.1 is hydrogen or a halogen atom, and R.sub.2 and R.sub.3 are the same or different and are each hydrogen or an alkyl having 1 to 3 carbon atoms, or an alkali metal salt thereof.
A compound of the formula:
- ##STR14## wherein R.sub.1 is hydrogen or a halogen atom, and R.sub.2 and R.sub.3 are the same or different and are each hydrogen or an alkyl having 1 to 3 carbon atoms, or an alkali metal salt thereof.
3-Sulfamoylmethyl-1,2-benzisoxazole or an alkali metal salt thereof.
5-Fluoro-3-sulfamoylmethyl-1,2-benzisoxazole or an alkali metal salt thereof.
5-Chloro-3-sulfamoylmethyl-1,2-benzisoxazole or an alkali metal salt thereof.
5-Bromo-3-sulfamoylmethyl-1,2-benzisoxazole or an alkali metal salt thereof.
6-Fluoro-3-sulfamoylmethyl-1,2-benzisoxazole or an alkali metal salt thereof.
2-Sulfamoylmethylbenzoxazole or an alkali metal salt thereof.
A pharmaceutical composition comprising as an active ingredient a compound of the formula:
- ##STR15## wherein R.sub.1 is hydrogen or a halogen atom, R.sub.2 and R.sub.3 are the same or different and are each hydrogen or an alkyl group having 1 to 3 carbon atoms, and one of X and Y is carbon atom and another is nitrogen atom, provided that the group:
- --CH.sub.2 SO.sub.2 NR.sub.2 R.sub.3 is bonded to the carbon atom of either of X and Y, or an alkali metal salt thereof and a pharmaceutically acceptable carrier.
A method for controlling convulsions and seizures in patients with epilepsy which comprises administering an effective amount of a compound of the formula:
- ##STR18## wherein R.sub.1 is hydrogen or a halogen atom, R.sub.2 and R.sub.3 are the same or different and are each hydrogen or an alkyl having 1 to 3 carbon atoms, and one of X and Y is carbon atom and another is nitrogen atom, provided that the group:
- --CH.sub.2 SO.sub.2 NR.sub.2 R.sub.3 is bonded to the carbon atom of either of X and Y, or an alkali metal salt thereof to said patients.
Dependencies are inferred from the claim text.