Use of lipid conjugates in the treatment of diseases associated with vasculature
View Patent ↗This invention provides for the use of compounds represented by the structure of the general formula (I): wherein R 1 is a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms; R 2 is a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms; Y is either nothing or a spacer group ranging in length from 2 to 30 atoms; X is either a physiologically acceptable monomer, dimer, oligomer or a physiologically acceptable polymer, wherein X is a glycosaminoglycan; and n is a number from 2 to 1,000; wherein if Y is nothing the phosphatidylethanolamine is directly linked to X via an amide bond and if Y is a spacer, said spacer is directly linked to X via an amide or an esteric bond and to said phosphatidylethanolamine via an amide bond, thereby inhibiting the development of a psoriatic plaque or reducing plaque size in a subject.
1. A method of inhibiting the accumulation of LDL in a subject in need thereof, comprising the step of administering to said subject a composition comprising a compound of general formula (I):
wherein
R 1 is a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms;
R 2 is a linear, saturated, mono-unsaturated, or poly-unsaturated, alkyl chain ranging in length from 2 to 30 carbon atoms;
Y is either nothing or a spacer group ranging in length from 2 to 30 atoms;
X is a glycosaminoglycan; and
n is a number from 2 to 1000;
wherein if Y is nothing, the phosphatidylethanolamine is directly linked to X via an amide bond and if Y is a spacer, said spacer is a straight or branched chain alkylene selected from the group consisting of —CO-alkylene-CO—, —NH-alkylene-NH—, and —CO-alkylene-NH—, and said spacer is directly linked to X via an amide or an esteric bond and to said phosphatidylethanolamine via an amide bond, thereby inhibiting the accumulation of LDL in a said subject.
2. The method of claim 1 , wherein said glycosaminoglycan is hyaluronic acid, heparin, heparin sulfate, chondroitin, chondroitin sulfate, keratan, keratan sulfate, dermatan sulfate or a derivative thereof.
3. The method of claim 2 , wherein said compound comprises sugar rings of said glycosaminoglycan, which are intact.
4. The method of claim 1 , wherein each of R1 and R2 is dipalmitoyl or dimyristoyl.
5. The method of claim 1 , wherein said subject has atherosclerosis.
6. The method of claim 1 , wherein said LDL is oxidized LDL.
7. The method of claim 1 , wherein said glycosaminoglycan has a molecular weight of 5000 to 10,000 Daltons.
8. The method of claim 1 , wherein said glycosaminoglycan has a molecular weight of 10,000 to 20,000 Daltons.
9. The method of claim 1 , wherein n is a number from 2 to 100.
10. The method of claim 1 , wherein said compound is administered intravenously.