Compounds that act as a vehicle for delivery through the blood-brain barrier and charge delivery vehicle constructions
OwnerErnest Giralt Lledó, Meritxell Teixidó Turàinventors
Life of this patent
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Abstract
Compounds of formula (I), where R1 and R3 are H or (C1-C4)-alkyl; R2 is H or a C-radical derived from one of the known ring systems with 1-4 rings; X1 is a (C1-C6)-alkyl biradical derived from a linear or branched carbon chain; and X2 is —NH—, —NH—(CH2)1-3—COO—, —NH—(CH2)1-3—S—, or —NH—CO—(CH2)1-3—S—, are useful as blood-brain barrier shuttles (BBB). BBB shuttle-cargo constructs, the cargo being a substance susceptible to form an amide or an ester or a disulfide bound with X2 and being unable to cross the blood-brain barrier by itself, are useful as medicaments.
Claims9
A compound of formula (I), or a pharmaceutically acceptable salt thereof, including any stereoisomer or mixtures of stereoisomers,
- wherein:
- R1 and R3 are radicals independently selected from the group consisting of H and (C1-C4)-alkyl, wherein either R1 or R3 is methyl;
- or alternatively, R1 and R3 are both methyl;
- R2 is phenyl, cyclohexyl,2-napthtyl, or 1-pyrenyl;
- X1 is —CH2 or CH2—CH2;
- and
- X2 is a biradical selected from the group consisting of —NH—, —NH—(CH2)1-3—COO—, —NH—(CH2)1-3—S—, and —NH—CO—(CH2)1-3—S—.
Dependencies are inferred from the claim text.