Heparanase inhibitors and their use as anti-cancer compounds
AssigneesWayne State University, Technion, Israel Institute of Technology, University of Iowa Research Foundation
InventorsHien M. Nguyen, Ravi Sankar Loka, Eric Sletten, Israel Vlodavsky
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Abstract
Anti-heparanase compounds for the treatment of cancer are described. The anti-heparanase compounds are high affinity, synthetic glycopolymers that result in minimal anticoagulant activity. Stereoselective fluorinated forms of these compounds are also provided.
Claims60
A method of treating cancer in a subject in need thereof comprising administering a therapeutically effective amount of a salt form of an anti-heparanase compound having the structure:
- wherein n=2-100 repeating units of the structure;
- the ring opening bonds designated as (*) are independently single or double bonds;
- and the salt form is selected from a sodium salt, a calcium salt, a magnesium salt, a lithium salt, a potassium salt, a cesium salt, or a triethylammonium salt.
A method of treating cancer in a subject in need thereof comprising administering a therapeutically effective amount of a salt form of an anti-heparanase compound to the subject wherein the anti-heparanase compound comprises a glycopolymer linked to a disaccharide.
A compound having the structure:
- wherein:
- X is —O— or
- Y is —O— or —CH2—;
- n=2-100 repeating units;
- R1 is OH or —N(H)-L-Ra;
- L is a linking group;
- Ra is a saccharide or disaccharide, which saccharide or disaccharide comprises one or more —SO3H groups;
- the carboxylic acid group is a salt thereof;
- and the dash bond --- is a single bond or a double bond.
The compound of 40 wherein the one or more F− groups comprise axial 2-fluoro-glycoside.
The compound of 41 wherein the one or more F− groups comprise axial 2-fluoro-glycoside.
The compound of 42 wherein the one or more F− groups comprise axial 2-fluoro-glycoside.
The compound of 43 wherein the one or more F− groups comprise axial 2-fluoro-glycoside.
Dependencies are inferred from the claim text.