USE OF LIPID CONJUGATES IN THE TREATMENT OF INFLAMMATORY DISORDERS
This invention provides for the use of compounds represented by the structure of the general formula (A): wherein L is a lipid or a phospholipid, Z is either nothing, ethanolamine, serine, inositol, choline, or glycerol, Y is either nothing or a spacer group ranging in length from 2 to 30 atoms, X is a physiologically acceptable monomer, dimer, oligomer, or polymer, wherein X is a glycosaminoglycan; and n is a number from 2 to 1000, wherein any bond between L, Z, Y and X is either an amide or an esteric bond in treating a subject suffering from a disease associated with harmful angiogenic processes such as cancer.
1 . A method of treating osteoarthritis in a subject in need thereof, comprising the step of administering to said subject a composition comprising a compound 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 a glycosaminoglycan; and
n is a number from 1 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 a straight or branched chain alkylene selected from the group consisting of —CO-alkylene-CO, —NH-alkylene-NH—, —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 treating osteoarthritis in said subject.
2 . The method of claim 1 , wherein said glycosaminoglycan is hyaluronic acid, heparin, heparan sulfate, chondroitin, chondroitin sulfate, keratan, keratan sulfate, dermatan sulfate or a derivative thereof.
3 . The method of claim 1 , 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 glycosaminoglycan has a molecular weight of 500,000 to 1,000,000 Daltons.
6 . The method of claim 1 , wherein said glycosaminoglycan has a molecular weight of 1,000,000 to 2,000,000 Daltons.
7 . The method of claim 1 , wherein n is a number from 2 to 100.
8 . The method of claim 1 , wherein joint pain is alleviated in said subject in need thereof.
9 . The method of claim 1 , wherein knee pain is alleviated in said subject in need thereof.
10 . The method of claim 1 , wherein progressive stiffness of a joint is alleviated in said subject in need thereof.
11 . The method of claim 1 , wherein progressive stiffness of a knee is alleviated in said subject in need thereof.
12 . The method of claim 1 , wherein inflammation of a joint lining is alleviated in said subject in need thereof.
13 . The method of claim 1 , wherein said composition is administered via the intravenous route.
14 . The method of claim 1 , wherein said composition is administered via the subcutaneous route.
15 . The method of claim 1 , said method further comprises administering a second drug for treating osteoarthritis.
16 . The method of claim 15 , wherein said second drug is selected from the group consisting of: steroid, glucosamine, chondroitin, and methylsulfonylmethane (MSM).