Substituted azabicycloheptanes, the use thereof, pharmaceutical

Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acids and salts thereof

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560 48, 560 12, 260544N, 260545R, 260544F, 556418, 544466, 562430, C07C101447

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active

047646403

ABSTRACT:
1-phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.

REFERENCES:
patent: 2673205 (1954-03-01), Hoffmann et al.
patent: 2848455 (1958-08-01), Hoffmann et al.
A. Alder, et al. Helv. Chim. Acta 65: p. 2405 (1982).
A. Alder, et al. J. Am. Chem. Soc. 105: p. 6712 (1983).

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