1-substituted alkyl-1,2-dihydro-2-pyrazinone derivatives

Details 1-substituted alkyl-1,2-dihydro-2-pyrazinone derivatives 1-substituted alkyl-1,2-dihydro-2-pyrazinone derivatives

1987-02-25

1989-06-06

Berch, Mark L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

540575, 540598, 540599, 544116, 544295, 544354, 544408, C07D40306, C07D40314, C07D40106, C07D40312

Patent

active

048373192

ABSTRACT:
1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkyl; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene and R is selected from the group consisting of hydroxyl, hologen, lower alkanoyloxy R.sub.4 -carbamoyloxy, arylthio, 1-methyltetrazole-5-yl-thio, 1-imidazole, morpholino, ##STR2## in which R.sub.4 is lower alkyl or aryl, R.sub.5 is lhydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A, R.sub.1, R.sub.2 and R.sub.3 are as defined above, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

REFERENCES:
patent: 3935214 (1976-01-01), Zellner
patent: 4181724 (1980-01-01), Hall et al.
Abstracts of Papers 16th Congress of Heterocyclic Chemistry, Osaka, Japan, 1984, No. 1B-08, pp. 65-68.
"Pharmacological Study on Tetramethyl Pyrazine", Chinese Medical Journal, 4(4), Jul. 1978, pp. 319-322.
Derwent for JP 59-212269.

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