Naphthopyran derivatives and use thereof

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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549280, C07D31192, A61K 31365

Patent

active

049635816

ABSTRACT:
The present invention relates to an aromatase inhibiting composition which contains a compound of the formula: ##STR1## wherein R is hydroxy, lower alkoxy or amino which may be substituted by lower alkyl; R.sup.1 is hydrogen or lower alkyl; and A is hydrogen, a group of the formula ##STR2## in which R.sup.2 is hydroxy, lower alkoxy or amino which may be substituted by lower alkyl and R.sup.3 is hydrogen or lower alkyl, or a group of the formula ##STR3## in which R.sup.4 and R.sup.5 are independently hydrogen or lower alkyl, or a salt thereof.
The present composition is useful in the prevention and treatment of estrogen-dependent diseases, such as breast cancer.

REFERENCES:
patent: 4537858 (1985-08-01), O'Sullivan et al.
Akita et al., CA 91: 205062x.
Zeeck et al., CA 91: 20250p.
Sedmera et al., CA 96: 84032e.
Singh et al., CA 103: 140195n.
Pushpa Singh et al., "Two New Inhibitors of Phospholipase A.sub.2 Produced by Penicillium Chermesinum: Taxonomy, Fermentation, Isolation, Structure Determination and Biological Properties", The Journal of Antibiotics, vol. 38(6), pp. 706-712 (1985).
Axel Zeeck et al., "Isolierung des Antibioticums Semi-Vioxanthiaus Penicillium Citreo-Viride und Synthese des Xanthomegnins", Chem. Ber., vol. 112, pp. 957-978 (1979).

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