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 alpha or beta 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 alpha , beta or gamma 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. |