NONSTEROID (HETERO) CYCLIC SUBSTITUTED ACYLANYLIDES OF MIXED GESTAGENOUS AND ANDROGENOUS ACTIVITY

摘要

The nonsteroid gestagens can be used individually or in combination with estrogens in contraceptive preparations, in the treatment of endometriosis, as well as of gynaecological distrurbances. The compounds can find also application in the treatment of premenstrual complaints and in substitution treatment. Their androgenous activity makes them suitable for controlling the male fertility, in male hormonosubstituting therapy (HRT) and in the treatment of andrological syndromes. They have the general formula where R1 & R2 are the same or different and mean hydrogen atom, C1-5 alkyl group or halogen atom or together with C-atom of the chain form a total of 3-7 member ring; R3 means C1-5 alkyl group or completely or partially fluorized C1-5 alkyl group; A means optionally substituted mono- or bicyclic aromatic ring, ester group -COOR4, alkenyl group -CR5=CR6R7, alkynyl group -C CR5 or partially or completely fluorized C1-5 alkyl group. B is carbonyl or CH2 group and Ar is a ring system selected from the following group of general partial formulae in case that B in the general formula I means CH2 group, Ar can mean phenyl residue with general partial formula The new compounds have very high affinity to the gestagen receptor. 33 claims