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US 5,962,660 AGranted
Sialyl Lewis X mimetics incorporating fucopeptides
AssigneeThe Scripps Research Institute
InventorsChi-Huey Wong, Chun-Cheng Lin, Tetsuya Kajimoto
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Abstract
Sialyl Lewis X mimetics incorporating fucopeptides are synthesized and shown to mimic the configuration and essential functional groups of sialyl Lewis X in space. The fucopeptides exhibit substantially the same biological activity as sialyl Lewis X in the E-selectin binding assay and can be employed for blocking neutrophil inflamatory conditions.
Claims8
A compound of the formula:
- ##STR117## wherein R.sub.1 is a radical selected from a group represented by one of the following structures:
- ##STR118## wherein 1.ltoreq.n.ltoreq.5;
- R.sub.2 is a radical selected from the group consisting of H and --OH;
- R.sub.3 is a radical selected from the group consisting of --OM, --O--(C.sub.1 -C.sub.18 (alkyl)), --NH(CH.sub.2).sub.m CONHR.sub.y wherein 1.ltoreq.m.ltoreq.5 and NHR.sub.y wherein R.sub.y is a radical represented by the following structure:
- ##STR119## wherein 1.ltoreq.p.ltoreq.20;
- 1.ltoreq.q.ltoreq.3;
- 1.ltoreq.r.ltoreq.20;
- and
- M is a counter ion;
- with the proviso that the compound cannot be represented by the following structures:
- ##STR120##
8 more elements
Dependencies are inferred from the claim text.