3-aryloxy and 3-arylthioazetidinecarboxamides as anticonvulsants

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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540515, 540596, 544111, 544349, 544359, 546208, 546256, 546275, 548336, 548524, 548952, A61K 31395

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active

049563599

ABSTRACT:
Novel 3-aryloxy and 3-arylthioazetidinecarboxamides having utility in a method of treating convulsions and epilepsy and compositions therefor are disclosed having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo-substituted-pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, aryl, allyl, substituted allyl, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl, diloweralkylaminoloweralkyl, and R.sup.1 and R.sup.2 when taken with the adjacent nitrogen atom may form a heterocyclic radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof, excepting that when R.sup.3 is hydrogen, Z is oxygen, B is oxygen, and Ar is phenyl or phenyl substituted by trifluoromethyl or aminocarbonyl, then R.sup.1 and R.sup.2 cannot be a combination of hydrogen and loweralkyl, and the further exception that when R.sup.3 is hydrogen, Z is oxygen, B is oxygen, and Ar is phenyl or phenyl substituted by fluoro, loweralkyl, loweralkoxy, trifluoromethyl, acetyl, or aminocarbonyl, then R.sup.1 and R.sup.2 cannot both be hydrogen.

REFERENCES:
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patent: 4571393 (1986-02-01), Teng
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Albertson, et al., Chem. Abstracts vol. 101 (1984), entry 183856e.
Osman, et al., Chem. Abstracts vol. 102 (1985), entry 72276S.

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