4,5-dihydro and 4,5,6,7-tetrahydropyrazolo(1,5-A)-pyrimidines

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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544281, 546328, 548375, 548377, 564194, 564342, 564345, 558440, C07D47104, A61K 31505

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active

048472565

ABSTRACT:
Novel compounds having the following structural formula: ##STR1## wherein - - - may represent the presence of a double bond between the C.sub.6 and C.sub.7 position, Ia, or the absence of a double bond between the C.sub.6 and C.sub.7 position, Ib; R.sub.1 is selected from the group consisting essentially of hydrogen, bromo, chloro, carbamoyl, carboxyl, carboxyalkoxyl where alkoxyl is (C.sub.1 -C.sub.3), cyano, --CO--CF.sub.3, COONa, ##STR2## --CO--C(CH.sub.3).sub.3, and ##STR3## where X is hydrogen, cyano, halogen and nitro; R.sub.2, R.sub.4 and R.sub.5 may be hydrogen and lower alkyl (C.sub.1 -C.sub.3); R.sub.3 is hydrogen, alkyl (C.sub.1 -C.sub.3), ##STR4## where R.sub.7 and R.sub.8 may be the same or different and are selected from the group consisting essentially of hydrogen, halogen, alkyl (C.sub.1 -C.sub.3), nitro, alkoxy (C.sub.1 -C.sub.3), trifluoro-methyl, acetylamino or N-alkylacetylamino where alkyl is (C.sub.1 -C.sub.3), and R.sub.3 may also be selected from a monovalent radical selected from the class consisting essentially of 3-thienyl, 2-pyridinyl, 3-pyridinyl and 4-pyridinyl, either of said pyridinyl radicals being optionally substituted with an alkyl radical R.sub.9, where alkyl is (C.sub.1 -C.sub.4), and the structures of the monovalent 2-pyridinyl, 3-pyridinyl and 4-pyridinyl moieties are depicted respectively as: ##STR5## R.sub.6 is hydrogen or alkyl-(C.sub.1 -C.sub.3); pharmaceutical compositions of matter containing the above-defined compounds; methods for using the compounds as anxiolytic agents, antihypertensive agents or antidepressant agents in mammals; processes for the preparation of the compounds.

REFERENCES:
patent: 4521422 (1985-06-01), Dusza et al.
patent: 4576943 (1986-03-01), Tomcufcik et al.
patent: 4654347 (1987-03-01), Dusza et al.

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