NOVEL SELECTIVE AROMATASE INHIBITING COMPOUNDS

New compounds of formula (I) wherein R1 is H, CH3, OCH3, NO2, NH2, CN, CF3, CHF2, CH2F or halogen, R2 is a heterocyclyl radical selected from 1-imidazolyl, triazolyl, pyrazolyl, pyrimidinyl, oxazolyl, thiazolyl, isoxazolyl and isothiazolyl, R3 is H or OH, R4 is H, R5 is H or OH; or R4 is H and R3 an...

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Bibliographische Detailangaben
Hauptverfasser:	S DERVALL, MARJA-LIISA, LAMMINTAUSTA, RISTO ARVO SAKARI, KALAPUDAS, ARJA MARKETTA, PELKONEN, REINO OLAVI, KARJALAINEN, ARTO JOHANNES, LAINE, AIRE MARJA
Format:	Patent
Sprache:	eng ; fre
Schlagworte:	BEER BIOCHEMISTRY CHEMISTRY COMPOSITIONS THEREOF CULTURE MEDIA ENZYMOLOGY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY MICROBIOLOGY MICROORGANISMS OR ENZYMES MUTATION OR GENETIC ENGINEERING ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS SPIRITS VINEGAR WINE
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Beschreibung
Zusammenfassung:	New compounds of formula (I) wherein R1 is H, CH3, OCH3, NO2, NH2, CN, CF3, CHF2, CH2F or halogen, R2 is a heterocyclyl radical selected from 1-imidazolyl, triazolyl, pyrazolyl, pyrimidinyl, oxazolyl, thiazolyl, isoxazolyl and isothiazolyl, R3 is H or OH, R4 is H, R5 is H or OH; or R4 is H and R3 and R5 combined form a bond; or R3 is H and R4 and R5 combined form ? O; R6 is methylene, ethylene, -CHOH-, -CH2-CHOH-, -CHOH-CH2-, -CH=CH- or -C(=O-)-; or R4 is H and R5 and R6 combined is ?CH- or =CH-CH2-; stereoisomers thereof and non-toxic pharmaceutically acceptable acid addition salts thereof exhibit selective aromase 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).