Acetylated prodrugs for delivery across the blood-brain barrier
AssigneeThe General Hospital Corporation
InventorsDavid R. ELMALEH, Timothy M. SHOUP
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Abstract
The present disclosure relates to pharmaceutical compositions including a compound derived from a parent compound having a hydroxyl or amino moiety, wherein the hydroxyl in the parent compound is presented as an ester in the compound or the amino in the parent compound is presented as an amide in the compound, and their use to prevent or treat neurological disease.
Claims39
A compound selected from:
A compound selected from:
A pharmaceutical composition comprising a therapeutically or diagnostically effective amount of a compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient or solvent,
- wherein the compound is derived from a parent compound having a hydroxyl or amine moiety, and
- wherein the hydroxyl in the parent compound is presented as an ester or a carbonate in the compound, or the amine in the parent compound is presented as an alkyl amine amide in the compound,
- provided the parent compound is not morphine,
- provided the parent compound is not 5,5′-((2-hydroxypropane-1,3-diyl)bis(oxy))bis(4-oxo-4H-chromene-2-carboxylic acid);
- provided the compound is not heroin;
- provided the compound is not (2<S,3R,4R,5<S,6R)-6-(acetoxymethyl)-3-(3-iodobenzamido)tetrahydro-2H-pyran-2,4,5-triyl triacetate;
- provided the compound is not N-acetyl β-alanine;
- and
- provided the compound is not acetylcholine.
The composition of any preceding claim, wherein the excipient is a BBB disruptive excipient.
Dependencies are inferred from the claim text.