Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-09-15
1999-10-05
Morris, Patricia L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5483361, A61K 31415, C07D23361
Patent
active
059624957
ABSTRACT:
##STR1## New compounds of formula (I) wherein R.sub.1 is H, CH.sub.3, OCH.sub.3, NO.sub.2, NH.sub.2, CN, CF.sub.3, CHF.sub.2, CH.sub.2 F or halogen, R.sub.2 is a heterocyclyl radical selected from 1-imidazolyl, triazolyl, tetrazolyl, pyrazolyl, pyrimidinyl, oxazolyl, thiazolyl, isoxazolyl and isothiazolyl, R.sub.3 is H or OH, R.sub.4 is H, R.sub.5 is H or OH; or R.sub.4 is H and R.sub.3 and R.sub.5 combined form a bond; or R.sub.3 is H and R.sub.4 and R.sub.5 combined form .dbd.O; R.sub.6 is methylene, ethylene, --CHOH--, --CH.sub.2 --CHOH--, --CHOH--CH.sub.2 --, --CH.dbd.CH-- or --C(.dbd.O)--; or R.sub.4 is H and R.sub.5 and R.sub.6 combined is .dbd.CH-- or .dbd.CH--CH.sub.2 --; stereoisomers thereof and non-toxic pharmaceutically acceptable acid addition salts thereof exhibit selective aromatase inhibiting properties, compared with their desmolase inhibiting properties. The compounds of the invention are valuable in the treatment of estrogen dependent diseases, e.g. breast cancer or benign prostatic hyperplasia (BPH).
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Kalapudas Arja Marketta
Karjalainen Arto Johannes
Laine Aire Marja
Lammintausta Risto Arvo Sakari
Pelkonen Reino Olavi
Morris Patricia L.
Risto Arvo Sakari Lammintausta
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