new kardioaktive 17 iminomethylalkenyl - 5 - beta - 14 - beta - androstan and 17 iminoalkyl 5 beta, 14 beta androstan derivatives, a process for their manufacture and pharmaceutical preparations thereof

摘要

The present invention provides 17-Iminomethylalkenyl- and 17-iminoalkyl-14 beta -hydroxy-5 beta -androstane derivatives of general formula (I): CHEM wherein: the symbol @ means alpha or beta configuration or a Z or E configuration; A represents (CH2)m or -(CH=CH)n-; m represents an integer number from 1 to 6; n represents an integer number from 1 to 3. R1 represents hydrogen, C2-C4 alkyl unsubstituted or substituted by NR4R5 wherein R4, R5 which may be the same or different, represent hydrogen, C1-C4 alkyl or R4 and R5 may form, taken together with the nitrogen atom, a five- or six-membered heterocyclic ring optionally containing one or more further heteroatoms selected from oxygen and nitrogen; R2 represents hydrogen or hydroxy; R3 represents NHC(=X)NR6R7 or OR8 wherein R6, R7 which may be the same or different, represent hydrogen, methyl or C2-C4 alkyl unsubstituted or substituted by NR4R5 wherein R4 and R5 have the previously defined meanings; R8 represents hydrogen; methyl; C2-C6 alkyl, unsubstituted or substituted by one or more NR4R5 or NHC(=NH)NH2, wherein R4 and R5 have the previously defined meanings; X represents O, S or N @ R9; R9 represents hydrogen, methyl, C2-C4 alkyl, C2-C4 acyl or phenyl, where the C2-C4 alkyl, C2-C4 acyl are unsubstituted or substituted by NR4R5, wherein R4 and R5 have the previously defined meanings; and R6, R7, R9 taken two by two may form, together with the heteroatoms they are linked to, and where possible, a five- or six- or seven-membered heterocyclic ring.