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US 5,470,842 AGranted
Carbohydrate-based anti-inflammatory agents
AssigneeGlycomed Incorporated
InventorsBrian K. Brandley, Michael Tiemeyer, Stuart J. Swiedler, Margaret Moreland, Hans Schweingruber
Life of this patent
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Abstract
Ligands in the form of N-acetyllactosamines which bind to endothelial leukocyte adhesion molecule-1 (ELAM-1) are disclosed. The ligand compounds can be formulated into pharmaceutical compositions and/or assay compositions used to alleviate inflammation and assay for the presence of (qualitative) and amount of (quantitative) ELAM-1 and thereby determine the presence, location and degree of inflammation.
Claims9
An injectable pharmaceutical composition, comprising:
- a pharmaceutically acceptable, injectable excipient carrier;
- and
- a compound which binds to ELAM-1 wherein the compound has the following structure:
- ##STR9## each of the saccharide rings shown, is connected at its 1-position to the next saccharide ring at a position selected from the group consisting of the 3-position and the 4-position and wherein the variables are defined as follows:
- ##STR10## wherein R.sup.4 is selected from the group consisting of H, and an alkyl containing 1 to 6 carbons;
- R.sup.5 is selected from the group consisting of H, alkyl containing 1 to 6 carbons, and COCH.sub.3 ;
- and
- R.sup.6 is selected from the group consisting of H, and an alkyl containing 1 to 6 carbons;
- E and D are each independently H or fucose wherein E or one D is fucose connected to the 3-position or 4-position of the sugar to which it is bound and the bond is in an alpha configuration;
- R.sup.3 is selected from the group consisting of OH and NAc with the proviso that R.sup.3 is OH if n is O;
- n is an integer of from 0 to 10 with the proviso that if n is O, then R.sup.3 is OH and E is fucose;
- F is a linking group bound to a pharmaceutically active drug;
- X is O;
- wherein the compound which binds to ELAM-1 is present in the composition in an amount in the range of about 1% to about 95% by weight.
11 more elements
Dependencies are inferred from the claim text.