17 beta -substituted 4-azaandrostane derivatives, pharmaceutical compositions containing them and process for preparing same

摘要

PCT No. PCT/HU93/00058 Sec. 371 Date Mar. 23, 1995 Sec. 102(e) Date Mar. 23, 1995 PCT Filed Oct. 1, 1993 PCT Pub. No. WO94/07909 PCT Pub. Date Apr. 14, 1994The invention relates to novel 17 beta -substituted 4-azaandrostane derivatives of general formula (I), <IMAGE> (I) wherein R means hydrogen or a C1-3alkyl group; R1 and R2 are the same or different and stand for hydrogen or a C1-4alkyl group with the proviso that both can mean hydrogen only in the case when n is higher than 5; or R1 and R2 together means an alpha , omega -alkylene group containing 5 to 7 carbon atoms, the terminal carbon atoms of said alkylene group being bound to the same ring carbon atom; n is 4, 5, 6 or 7; and +E,uns ---+EE bond line represents a single or double bond. Furthermore, the invention relates to pharmaceutical composition containing these compounds as well as a process for the preparation of the compounds of general formula (I). The compounds of general formula (I) exert a 5 alpha -reductase enzyme-inhibiting effect and therefore, they are useful for treating all diseases, where the aim is to reduce the tissue dihydrotestosterone level, such as the benign prostatic hyperplasia, acne, seborrhoea, female hirsutism or androgenic alopecia.