Compounds, compositions and method for transporting cyclosporin molecules through the blood brain barrier
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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