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    17-iminomethylalkenyl-5 .beta., 14 .beta.-androstane and 17-iminoalkyl-5 .beta., 14 .beta.-androstane derivatives active on the cardiovascular system, and pharmaceutical compositions containing same
    4.
    发明授权
    17-iminomethylalkenyl-5 .beta., 14 .beta.-androstane and 17-iminoalkyl-5 .beta., 14 .beta.-androstane derivatives active on the cardiovascular system, and pharmaceutical compositions containing same 失效

    公开(公告)号：US5583127A

    公开(公告)日：1996-12-10

    申请号：US363060

    申请日：1994-12-23

    申请人： Alberto Cerri ,  Giuseppe Bianchi ,  Patrizia Ferrari ,  Elena Folpini ,  Piero Melloni

    发明人： Alberto Cerri ,  Giuseppe Bianchi ,  Patrizia Ferrari ,  Elena Folpini ,  Piero Melloni

    IPC分类号： A61K31/575 ,  A61K31/573 ,  A61K31/58 ,  A61P9/00 ,  A61P9/12 ,  C07J41/00 ,  C07J43/00 ,  C07J75/00 ,  A61K31/57 ,  C07J9/00

    CPC分类号： C07J41/005 ,  C07J43/003 ,  C07K2319/00

    摘要： Disclosed are 17-iminomethylalkenyl and 17-iminoalkyl-14.beta.-hydroxy-5.beta.-androstane derivatives of the formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration or a Z or E configuration; A represents (CH.sub.2).sub.m or --(CH.dbd.CH).sub.n --; m represents an integer number from 1 to 6; n represents an integer number from 1 to 3; R.sup.2 represents hydrogen or hydroxy; R.sup.1 represents hydrogen, C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5, which may be the same or different, represent hydrogen, C.sub.1 -C.sub.4 alkyl or R.sup.4 and R.sup.5 may form, when taken together with the nitrogen atom, a five- or six- membered heterocyclic ring optionally containing one or more heteroatoms selected from oxygen and nitrogen; R.sup.3 represents NHC(.dbd.X)NR.sup.6 R.sup.7 or OR.sup.8 wherein R.sup.6 and R.sup.7, which may be the same or different, represent hydrogen, methyl, or C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 have the previously defined meanings; R.sup.8 represents hydrogen, methyl, C.sub.2 -C.sub.6 alkyl, unsubstituted or substituted by one or more NR.sup.4 R.sup.5 or NHC(.dbd.NH)NH.sub.2, wherein R.sup.4 and R.sup.5 have the previously defined meanings; X represents O, S, or NR.sup.9 ; R.sup.9 represents hydrogen, methyl, C.sub.2 -C.sub.4 alkyl, C.sub.2 -C.sub.4 acyl or phenyl, where the C.sub.2 -C.sub.4 alkyl and C.sub.2 -C.sub.4 acyl are unsubstituted or substituted by NR.sup.4 R.sup.5, wherein R.sup.4 and R.sup.5 have the previously defined means; and R.sup.6, R.sup.7, and R.sup.9, taken two by two, may form, together with the heteroatoms to which they are linked, a five- , six- , or seven-membered heterocyclic ring; or mixtures of .alpha. and .beta. isomers at the 3-position; or mixtures of Z and E isomers of the group A--CH.dbd.NR.sup.3 ; or pharmaceutically acceptable salts thereof. The compounds are useful for the treatment of cardiovascular disorders, such as heart failure and hypertension. Also, disclosed is a process for preparing the derivatives by reaction of the corresponding 17-alkyl or 17-methylalkenyl aldehyde with a compound of the formula H.sub.2 NNHC(.dbd.X)NR.sup.6 R.sup.7 or H.sub.2 NOR.sup.8.