NOVEL STEROIDS WITH PREGNANE SKELETON, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME

摘要

The invention relates to novel, therapeutically active 21-aminosteroids of formula (I) with pregnane skeleton, wherein two of X, Y and Z mean a nitrogen atom each and the third one is a methine group; R?1 and R2¿ represent, independently from each other, a primary amino group bearing as substituent a branched-chain C¿4-8?alkyl, -alkenyl or -alkynyl group, or a C4-10cycloalkyl group comprising 1 to 3 ring(s) and being optionally substituted by C1-3alkyl group(s); or R?1 and R2¿ stand together for a spiro-heterocyclic secondary amino group containing at most 10 carbon atoms and optionally at least one oxygen atom as additional heteroatom; or one of R?1 and R2¿ means an unsubstituted heterocyclic secondary amino group containing 4 to 7 carbon atoms and the other one is an above-identified primary amino group, an above-identified spiro-heterocyclic secondary amino group, or a heterocyclic secondary amino group containing 4 to 7 carbon atoms and substituted by C¿1-4?alkyl group(s); and n is 1 or 2, as well as their acid addition salts and pharmaceutical compositions containing these compounds. Furthermore, the invention relates to a process for the preparation of the above compounds. The compounds of formula (I) possess antioxidant, particularly lipid peroxidation-inhibiting effect, and therefore they may useful for the treatment of pathologic sequels of lipid peroxidation occurring in mammals, including man.