The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Dec. 10, 1996
Filed:
Dec. 23, 1994
Alberto Cerri, Gessate, IT;
Giuseppe Bianchi, Milan, IT;
Patrizia Ferrari, Varese, IT;
Elena Folpini, Milan, IT;
Piero Melloni, Bresso, IT;
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.