COMPOSES, COMPOSITIONS ET METHODE POUR LE TRANSPORT DES MOLECULES DE CYCLOSPORINE A TRAVERS LA BARRIERE HEMATO-ENCEPHALIQUE
New cyclosporin compounds (I) comprise at least one cyclosporin molecule (II) and at least one peptide vector (III) capable of transporting (III) across the blood-brain barrier. An Independent claim is included for bonding agents (IV) of formula C(O)-R4-NR1-C(O)-(CH2)n-NH-(CH2)m-C(O)- (IVA), C(O)-R4...
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Zusammenfassung: | New cyclosporin compounds (I) comprise at least one cyclosporin molecule (II) and at least one peptide vector (III) capable of transporting (III) across the blood-brain barrier. An Independent claim is included for bonding agents (IV) of formula C(O)-R4-NR1-C(O)-(CH2)n-NH-(CH2)m-C(O)- (IVA), C(O)-R4-NR1-C(O)-R2-NH-R3-C(O)- (IVB), C(O)-R4-NR1-Hyp-O-C(O)-R5-C(O) (IVC), C(O)-R4-NR1-C(O)-CH(NH2)-R5-O-C(O)-R8-C(O) (IVD), C(O)-R4-NR1-C(O)-R5-NH-O-R8-C(O) (IVE), C(O)-R4-NR1-C(O)-R5-O-NH-R8-C(O) (IVF), C(O)-R4-NR1-C(O)-R5-NR7-NR6-R8-C(O) (IVG) or C(O)-R4-NH-R5-C(O) (IVH). m, n = at least 1; R1 = H, OR6, NR6R7, alkyl, aryl, alkaryl, acyl or allyl; R2, R3 = alkyl, at least one of which is branched by one or two or a combination of alkyl, aryl, alkaryl, acyl or allyl or any other type of branched alkyl (optionally containing heteroatom groups); R4-R6 = linear alkyl or branched alkyl as defined for R2/R3; R1 = H, alkyl, aryl, alkaryl, acyl or allyl, and Hyp-O = hydroxyproline residue, in which the OH group is in the 2, 3 or 4-position of the proline and bonding is via the O of the OH group of the hydroxyproline. Asymmetric carbons have R- or S-configuration. |
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