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AssigneeOrion-yhtyma Oy
InventorsArto Johannes Karjalainen, Maria-Liisa Sodervall, Arja Marketta Kalapudas, Reino Olavi Pelkonen, Aire Maria Laine, Risto Arvo Sakari Lammintausta, Jarmo Sakari Salonen
Estimating the term…
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 --(O); R.sub.6 is methylene, ethylene, --CHOH--, --CH.sub.2 --CHOH--, --CHOH--CH.sub.2 --, --CH--CH-- or --C(--O)--; or R.sub.4 is H and R.sub.5 and R.sub.6 combined is --CH-- or --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).
A compound of formula (I) ##STR20## 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;
A process for the preparation of a compound of formula ##STR21## 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 1,2,4-triazolyl R.sub.6 is methylene or ethylene;
Dependencies are inferred from the claim text.