Novel steroids with pregnane skeleton, pharmaceutical...

C - Chemistry – Metallurgy – 07 – J

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C07J 43/00 (2006.01) A61K 31/58 (2006.01) C07D 239/42 (2006.01) C07D 239/48 (2006.01) C07D 239/50 (2006.01) C07D 491/10 (2006.01)

Patent

CA 2136546

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; R1 and R2 represent, independently from each other, a primary amino group bearing as substituent a branched-chain C4-8alkyl, -alkenyl or -alkynyl group, or a C4-10cyc- loalkyl group comprising 1 to 3 ring(s) and being optionally substituted by C1-3alkyl group(8); or R1 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 R1 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 secon- dary amino group, or a heterocyclic secondary amino group containing 4 to 7 carbon atoms and substituted by C1-4alkyl 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.

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