Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1987-07-31
1989-06-13
Hollrah, Glennon H.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546219, A61K 3145, C07D21188
Patent
active
048393703
ABSTRACT:
Novel 3-aryl-3-cycloalkyl-piperidine-2,6-dione derivatives of the general formula I: ##STR1## in which A is a 4-aminophenyl radical or a pyridyl-(4)-radical and R.sub.1 is a saturated or unsaturated C.sub.3 -C.sub.10 -cycloalkyl radical or a C.sub.3 -C.sub.12 -alkenyl radical as well as physiologically acceptable salts thereof. The compounds are useful as inhibitors of estrogen biosynthesis. The compounds are made by a process which includes the step of heating a compound of the formula II ##STR2## wherein A and R.sub.1 have the meanings given above, and in addition A may also be a phenyl radical or a 4-nitrophenyl radical, X and Y are the same or different and repesent CN or COOC.sub.1 -C.sub.6 -alkyl and X or Y may also be COOH or a carboxylic acid ester group of the formula COOC.sub.1 -C.sub.6 -alkyl group, in a high boiling solvent at a temperature between 50.degree. and 200.degree. C. in particular between 80.degree. and 100.degree. C., optionally in the presence of condensation agents to form a piperidine dione ring.
REFERENCES:
patent: 2848455 (1958-08-01), Hoffmann et al.
patent: 3057867 (1962-10-01), Taub
Allan B. Foster et al, J. Med. Chem. (1983), vol. 26, pp. 50-54.
Allan B. Foster et al, J. Med. Chem. (1985), vol. 28, pp. 200-204.
Rolf W. Hartmann et al, J. Med. Chem. (1986), vol. 29, pp. 1362-1369.
Batzl Christine
Hartmann Rolf W.
Asta-Pharma AG
Hollrah Glennon H.
Treanor Susan P.
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