Back to results
US 2007/0191310 A1Published application
Phospholipid derivatives of non-steroidal anti- inflammatory drugs
AssigneeD-Pharm Ltd.
InventorsAlexander Kozak, Israel Shapiro
Life of this patent
Estimating the term…
Abstract
Disclosed are compounds having non-steroidal anti-inflammatory drugs (NSAIDS) covalently linked to a phospholipid moiety via a bridging group. Also disclosed are a process for the synthesis of the compounds, pharmaceutical compositions comprising the compounds and the use thereof for the treatment of diseases and disorders related to inflammatory conditions, such as the treatment of ischemia.
Claims33
A compound of the general formula I
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is a saturated or unsaturated, substituted or unsubstituted hydrocarbon chain having from 2 to 30 carbon atoms;
- R2 is H or a phospholipid head group;
- D is a residue of a nonsteroidal anti-inflammatory drug having a functional group selected from the group consisting of carboxyl, hydroxyl, amine and thiol, wherein D is attached through said functional group to a bridging group, —C(O)-Z-X—, wherein Z is a saturated or unsaturated hydrocarbon chain having from 2 to 15 carbon atoms, and X is selected from amino, hydroxy, thio and carbonyl groups, such that when the functional group of D is carboxyl, X is selected from amino, hydroxy and thio, and when the functional group of D is amino, hydroxy or thio, X is a carbonyl group.
1 more element
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and, as an active ingredient, a compound of the general formula I
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is a saturated or unsaturated, substituted or unsubstituted hydrocarbon chain having from 2 to 30 carbon atoms;
- R2 is H or a phospholipid head group;
- D is a residue of a nonsteroidal anti-inflammatory drug having a functional group selected from the group consisting of carboxyl, hydroxyl, amine and thiol, wherein D is attached through said functional group to a bridging group, —C(O)-Z-X—, wherein Z is a saturated or unsaturated hydrocarbon chain having from 3 to 15 carbon atoms, and X is selected from amino, hydroxy, thio and carbonyl groups, such that when the functional group of D is carboxyl, X is selected from amino, hydroxy and thio, and when the functional group of D is amino, hydroxy or thio, X is a carbonyl group.
1 more element
(canceled)
Dependencies are inferred from the claim text.