Lipomacrocycles and uses thereof
OwnerKunyuan Cui, Dong Lianginventors
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Abstract
What is described are macrocyclic compounds formed by reaction of a cyclic compound, which contains an amine, with an epoxide. The macrocyclic compound has the following structure: When substituents R and R′ that are hydrophobic substituents, the macrocyclic compound functions as a lipid and is compatible with lipid systems, including liposomes and lipid particles. When present in certain lipid systems, the macrocyclic compound enhances the ability of the lipid system to facilitate delivery of therapeutic molecules to target cells in a mammalian subject.
Claims55
A macrocyclic compound produced by reacting a cyclic compound consisting of formula I
- with an epoxide consisting of formula II or III
- wherein X is N, O or S, wherein X may vary in the cyclic compound;
- wherein when X is O or S, then R is nothing, and when X is N, then R is selected from a group consisting of H, a linear or branched alkyl, an aryl, a cholesterol, CH2CONH2, CH2CONHCH3, a methylene bridge between a pair of the amino groups of the cyclic compound, or an ethylene bridge between pairs of amino groups of the cyclic compound;
- wherein more than one R group may occur in the cyclic compound;
- wherein the CH2—XR—CH2 group of the cyclic compound repeats from m=2 to 10 times, wherein for every repeat of the CH2—XR—CH2 group, n is 0 or 1;
- and wherein R′ is C1 to C20.
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Dependencies are inferred from the claim text.