1-(pyridinylamino)-2-pyrrolidinones as pain relievers

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546256, 546281, 546 15, 514343, A61K 3144, C07D40100, C07D21100

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active

049944720

ABSTRACT:
This invention relates to 1-(pyridinylamino)-2-pyrrolidinones of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl or heteroaryl substituted cycloalkane; X is hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m is an integer of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and where appropriate the geometrical, optical and stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesics, for enhancing memory and for the treatment of Alzheimer's disease.

REFERENCES:
patent: 4324884 (1982-04-01), White et al.
patent: 4752610 (1988-06-01), Effland
Blokhina et al., Khim. Geterotsikl. Soedin., 4, 474-478 (1987).
Baldwin et al., Tetrahedron, vol. 42, No. 15, pp. 4247-4252, (1986).
Baldwin et al., J. Chem. Soc., Chem. Commun., (16), 1095-1096, (1984).

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