- 17BETA-HETEROCYCLYL-DIGITALIS LIKE COMPOUNDS FOR THE TREATMENT OF HEART FAILURE
-
Disclosed are compounds of formula (I) wherein X, Y, Z are annular atoms comprised in a five-membered carbocyclic or heterocyclic ring, selected from the group consisting of CH, NH, N, O, S; said carbocyclic or heterocyclic ring being optionally substituted with amino (C1-C4) linear or branched alkyl or guanidine or guanidino (C1-C4) linear or branched alkyl; with the proviso that the heterocycle ring is not furyl; n is 0 or 1; R is H or OH; the dotted line represents an optional double bond C=C; the thick line represents a bond in the β configuration; the wavy line represents a bond both in the α and β configuration; their enantiomeric and/or diastereomeric mixtures, their pharmaceutically acceptable salts, their solvates, hydrates; their metabolite and metabolic precursors. The compounds of formula (I) are for use as medicaments, in particular for the treatment of acute or chronic heart failure. Oral administration is also possible.
- -
-
-
- Partial Syntheses of Cardenolides and Cardenolide Analogues. XIII. Synthesis of Substituted 14,21-Epoxy-5&β,14&β-card-20(22)-enolides
-
The 12-substituted 14,21-epoxy-5β,14β-card-20(22)-enolides 3 and 5 were synthesized by oxidation of the appropriate 17β-(3-furyl) derivatives 2b and 2c, respectively, with chromic acid. 5 was converted to the conjugated Δ9(11)-12-ketone 6 by dehydrogenation with selenium dioxide.The biological activities of the new compounds were investigated and are discussed.
- Courault, Klaus,Lindig, Claus
-
p. 445 - 452
(2007/10/02)
-
- 13C NMR Spectra of 5β,14β-Hydroxysteroids
-
The 13C chemical shifts of 30 substituted 5β,14β-hydroxysteroids are described and discussed.Substituent chemical shifts for 12α- and 12β-hydroxy groups were evaluated, and interesting γ effects were observed.A correlation is shown to exist between the 1H shifts of H-17 and the 13C shifts of C-17 for various C-12 substituents.A relationship for the distance of the substituent at C-12 from H-17 in the 14β,20-lactones was demonstrated, where an increased distance between these atoms is associated with smaller shift differences.
- Habermehl, Gerhard G.,Hammann, Peter E.,Wray, Victor
-
p. 959 - 963
(2007/10/02)
-