Methods of treating a seizure disorder with a maxi-K channel opener or a pharmaceutically acceptable salt thereof are provided. In embodiments, suitable maxi-K channel openers are be fluoro-oxindole or chloro-oxindole compounds. In some embodiments, the maxi-K channel opener may be (3S)-(+)-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6 -(trifluoromethyl)-2H-indole-2-one or pharmaceutically acceptable salts thereof. The methods provide therapeutic compositions that may be used to improve one or more symptoms of a seizure disorder.

Ovid Therapeutics Inc.

OVID THERAPEUTICS INC.

Methods of treating seizure disorders

A class of pyridazino[4,5-b]indole-1,4-dione derivatives, substituted in the 2-position by an optionally substituted phenyl moiety, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment and/or prevention of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA antagonist.

Merck, Sharp &amp; Dohme, Ltd.

Pyridazino-indole derivatives

A 5-phenyl-1,3,3a,4,5,9b-hexahydro-3H-benz(e)indole compound of the formula I: ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-6 alkyl, R.sup.2 is hydrogen or C.sub.1-3 alkyl in the 3a- or 4-position, R.sup.3 and R.sup.4 are each hydrogen, hydroxyl, halogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, C.sub.1-3 alkylthio or trifluoromethyl, acetylamino or amino and R.sup.5 is hydrogen or C.sub.1-3 alkyl, or a salt thereof with a physiologically tolerated acid. The compounds and compositions are useful for treating depression or trating convulsions and which exhibit a sedative and tranquilizing effect when administered to a patient.

BASF Aktiengesellschaft

5-phenyl-1,2,3a,4,5,9b-hexahydro-3H-benz(e)indotes preparation and use thereof as drugs

Coupled to the N-methyl-D-aspartate (NMDA) receptor-channel complex is a strychnine-insensitive binding site for glycine. Pharmacological antagonism of glycine binding at this site can produce anticonvulsant activity. Derivatives of kynurenic acid, pyridine and 2-carboxy-indole were synthesized and evaluated as antagonists of glycine binding and for anticonvulsant effects. Compounds were tested in mice against seizures induced by electroshock and pentylenetetrazole, and in the rotorod assay for neurologic deficit. The derivatives were also assayed for binding at the NMDA-associated glycine site. The most potent anticonvulsant was ethyl 4-methylamino-5,7-dichloro-2-quinoline carboxylate. This compound provided protection against maximal electroshock (MES) induced seizures at a dose of 30 mg/kg. Other compounds were active at 100 mg/kg dose level, including 5-fluoro-2-indole carboxylic acid and the diethyl ester of 2,6-pyridine dicarboxylic acid.

indole/seizures

Methods of treating seizure disorders

Pyridazino-indole derivatives

5-phenyl-1,2,3a,4,5,9b-hexahydro-3H-benz(e)indotes preparation and use thereof as drugs

Anticonvulsive agents and uses thereof

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