abstract |
The invention relates to bicyclo[3.3.0]octane derivatives of formula (I), and their enantioners. In formula (I) not more than one double bond is located between the carbon atoms of the centres a-b or b-c or b-d, and R?1 is (a'), (b'), (c'), (d') or COOR?5 stands for hydrogen or C1?-C10? alkyl, possibly substituted by halogen, phenyl, C1?-C4? alkoxy or di-(C1?-C4?)-alkylamino, C3?-C10? cycloalkyl, C7?-C16? aralkyl, Y-substituted phenacyl or C16?-C12? aryl or a 5- or 6-membered heterocyclic residue with at least one N, O or S atom, or -CONHR?7 with R?7 standing for hydrogen, C1?-C10? alkanyl or C1?-C10? alkane sulphonyl, X stands for a CH2? group or an O or S atom, n is 0-2, R?4 is a hydrogen atom, a free or functionally modified hydroxy group in which the OH group can be in the $g(a) or $g(b)position, Z stands for (e'), (f'), (g'), (h') or (i'), p=0 or 1, V is an O or an S atom, W stands for Y-substituted C1?-C10? alkyl, C3?-C10? cycloalkyl, (j'), (k'), (l'), (m'), (n'), (o'), (p'), (q') or (r'), Y1?, Y2? and Y3? are identical or different and stand for Y, Y stands for hydrogen, halogen, N3?, CF3?, OR?6, NO2?, COOR?6 or C1?-C10? alkyl, R?6 stands for hydrogen, C1?-C10? alkyl, possibly hydrogen substituted C6?-C12? aryl or C7?-C16? aralkyl, and, if R?5 stands for hydrogen, their salts with physiologically acceptable bases may stand for the $g(a), $g(b) or $g(g) cyclodextrin clathrates as well as the compounds of formula (I) encapsulated by liposomes. The invention also relates to a process for preparing them and their pharmaceutical use. |