Lipid conjugates in the treatment of disease
View Patent ↗The invention relates to methods of use for compounds in treating, reducing the incidence, reducing the severity or pathogenesis of an intestinal disease or condition in a subject, including, inter alia, inflammatory bowel disease, Crohn's disease, ulcerative colitis, or a combination thereof.
1. A method of reducing the severity of neoplasia, or treating neoplasia in a subject suffering from a sarcoma comprising the step of administering to said subject suffering from a sarcoma a compound 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, wherein said spacer comprises —CO-alkylene-NH—, —CO-alkylene-CO—or a combination thereof;
wherein if Y is nothing the phospholipid moiety is directly linked to X via an amide bond and if Y is a spacer group, the spacer group is directly linked to X via an amide or an ester bond and to the phosphoethanolamine moiety via an amide bond;
X is hyaluronic acid, wherein the sugar rings of the glycosaminoglycan are intact; and
n is a number from 1 to 1000;
and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.
2. The method according to claim 1 , wherein R 1 and R 2 are both palmitoyl moieties.
3. The method according to claim 1 , wherein R 1 and R 2 are both myristoyl moieties.
4. A method of reducing the severity of or pathogenesis of cancer metastasis in a subject suffering from a sarcoma, comprising the step of administering to said subject suffering from a sarcoma a compound 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, wherein said spacer comprises —CO-alkylene-NH—, —CO-alkylene-CO—or a combination thereof;
wherein if Y is nothing the phospholipid moiety is directly linked to X via an amide bond and if Y is a spacer group, the spacer group is directly linked to X via an amide or an ester bond and to the phosphoethanolamine moiety via an amide bond;
X is hyaluronic acid, wherein the sugar rings of the glycosaminoglycan are intact; and
n is a number from 1 to 1000;
and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof.
5. The method according to claim 4 , wherein R 1 and R 2 are both palmitoyl moieties.
6. The method according to claim 4 , wherein R 1 and R 2 are both myristoyl moieties.