1-(2-Aryl-2-halo-1-ethenyl)-1H-azoles, and anticonvulsant use thereof
AssigneeJanssen Pharmaceutica NV
InventorJan Heeres
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Abstract
1-(2-Aryl-2-halo-1-ethenyl)-1H-azoles having anticonvulsant properties which are particularly useful in the treatment of generalized forms of epilepsy.
Claims12
A chemical compound having the formula ##STR9## a pharmaceutically acceptable acid addition salt or a stereochemically isomeric forms thereof, wherein
- Q is CH or N;
- R is hydrogen, lower alkyl, aryl, aryllower alkyl or halo;
- and
- Ar is aryl;
- wherein aryl is phenyl, substituted phenyl, naphthalenyl, substituted naphthalenyl, thienyl or substituted thienyl, wherein said substituted naphthalenyl and substituted thienyl are naphthalenyl, respectively thienyl, having 1 or 2 substituents each independently selected from the group consisting of halo, lower alkyl and lower alkyloxy and wherein said substituted phenyl is phenyl having from 1 to 3 substituents each independently selected from the group consisting of halo, lower alkyl, lower alkyloxy, trifluoromethyl, nitro, amino, phenyllower alkyl and a radical R.sup.2, said R.sup.2 being phenyl optionally substituted with halo and/or lower alkyl;
- provided that not more than one substituent on said substituted phenyl is a radical R.sup.2.
An anticonvulsant composition comprising an inert carrier and an anticonvulsant effective amount of a compound having the formula ##STR10## a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein
- Q is CH or N;
- R is hydrogen, lower alkyl, aryl, aryllower alkyl or halo;
- and
- Ar is aryl;
- wherein aryl is phenyl, substituted phenyl, naphthalenyl, substituted naphthalenyl, thienyl or substituted thienyl, wherein said substituted naphthalenyl and substituted thienyl are naphthalenyl, respectively thienyl, having 1 or 2 substituents each independently selected from the group consisting of halo, lower alkyl and lower alkyloxy and wherein said substituted phenyl is phenyl having from 1 to 3 substituents each independently selected from the group consisting of halo, lower alkyl, lower alkyloxy, trifluoromethyl, nitro, amino, phenyllower alkyl and a radical R.sup.2, said R.sup.2 being phenyl optionally substituted with halo and/or lower alkyl;
- provided that not more than one substituent on said substituted phenyl is a radical R.sup.2.
A method of treating warm-blooded animals suffering from convulsions which method comprises the systemic administration to said warm-blooded animals of an effective anticonvulsant amount of at least one compound having the formula ##STR11## a pharmaceutically acceptable acid addition salt or a stereochemically isomeric form thereof, wherein
- Q is CH or N;
- R is hydrogen, lower alkyl, aryl, aryllower alkyl or halo;
- and
- Ar is aryl;
- wherein aryl is phenyl, substituted phenyl, naphthalenyl, substituted naphthalenyl, thienyl or substituted thienyl, wherein said substituted naphthalenyl and substituted thienyl are naphthalenyl, respectively thienyl, having 1 or 2 substituents each independently selected from the group consisting of halo, lower alkyl and lower alkyloxy and wherein said substituted phenyl is phenyl having from 1 to 3 substituents each independently selected from the group consisting of halo, lower alkyl, lower alkyloxy, trifluoromethyl, nitro, amino, phenyllower alkyl and a radical R.sup.2, said R.sup.2 being phenyl optionally substituted with halo and/or lower alkyl;
- provided that not more than one substituent on said substituted phenyl is a radical R.sup.2.
Dependencies are inferred from the claim text.