| abstract |
The compounds can be used for the treatment of diseases depending on the estrogen such as breast cancer or benignant hyperplasia of the prostate gland. They have the formula where R1 is H, CH3, OCH3, NO2, NH2, CN, CF3, CHF2, CH2F or halogen, R2 is heterocycle radical selected from 1-imidazolyl, triazolyl, tetrazolyl, 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 in combination form a bond; or R3 is H, and R4 & R5 in combination form =0; R6 is methylene, ethylene, -CHOH-, CH2-CHOH-, -CH=CH- or -C(=O)- or R4 is H, and R5 and R6 in combination form =CH- or =CH-CH2. The invention also relates to stereoisomers of the compounds or their non-toxic, pharmaceutically acceptable acid additive salts which inhibit desmoslase and also selectively inhibit aromatase. 20 claims |