Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1994-12-23
1996-12-10
Kestler, Kimberly J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514174, 514176, 514182, 540108, 540109, 540110, 540112, 540113, 552540, 552548, 552554, 552559, 552563, 552582, A61K 3157, A61K 31575, A61K 3158, C07J 900
Patent
active
055831273
ABSTRACT:
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.
REFERENCES:
patent: 4689410 (1987-08-01), Barton et al.
Lindig, et al., Tetrahedron, 28(6), pp. 1847-1858 (1972).
Krasso, et al., Helv. Chim Acta, 55(5), pp. 1352-1371 (1972).
Thomas, et al., J. of Pharmac. & Exp. Ther., pp. 219-231 (1974).
Gelbart, et al., J. of Med. Chem., 21(3), pp. 284-288 (1978).
Bianchi Giuseppe
Cerri Alberto
Ferrari Patrizia
Folpini Elena
Melloni Piero
Kestler Kimberly J.
Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
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