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US 5,977,080 AGranted
Sulfated disaccharide inhibitors of selectins, methods for synthesis and therapeutic use
AssigneeThe Regents of the University of California
InventorsSteven D. Rosen, Carolyn Bertozzi
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Abstract
Sulfated disaccharides characterized by the ability to inhibit the binding of selectin to its physiologically-relevant ligand are disclosed. Included are efficient and inexpensive methods for producing the sulfated disaccharides, and methods for their therapeutic use and in in vivo and in vitro assays.
Claims23
A sulfated lactose compound having the formula:
- ##STR6## wherein R.sub.1 and R.sub.5 are each independently H or SO.sub.3.sup.-, R.sub.2, R.sub.4, R.sub.6, and R.sub.7 are each independently H, alkyl, or an acyl group;
- R.sub.3 is SO.sub.3.sup.-, H, alkyl, or an acyl group;
- and R.sub.8 is an alkyl group, an acetyl group, an acetic acid derivative group, or a linking group, wherein at least one of R.sub.1, R.sub.3 and R.sub.5 is SO.sub.3.sup.- and said compound binds to a selectin receptor.
A method of determining a site of inflammation in a patient, comprising the steps of:
- administering to a patient an effective amount of a labeled sulfated lactose compound, wherein said compound has the formula:
- ##STR7## wherein R.sub.1 and R.sub.5 are each independently H or SO.sub.3.sup.-, R.sub.2, R.sub.4, R.sub.6, and R.sub.7 are each independently H, alkyl, an acyl group;
- R.sub.3 is SO.sub.3.sup.-, H, an alkyl group, or an acyl group;
- and R.sub.8 is an alkyl group, an acetyl group, an acetic acid derivative group, or a linking group wherein at least one of R.sub.1, R.sub.3 and R.sub.5 is SO.sub.3.sup.- ;
- allowing the labeled compound sufficient time to circulate in the patient and attach to selectin in the patient;
- and
- detecting the label and its location in the patient and thereby determining the site of inflammation.
4 more elements
Dependencies are inferred from the claim text.