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US 5,858,994 AGranted
Carbohydrate conjugates as inhibitors of cell adhesion
AssigneeHoechst Aktiengesellschaft
InventorsGerhard Kretzschmar, Wolfgang Schmidt, Ulrich Sprengard, Eckart Bartnik, Dirk Seiffge, Horst Kunz
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Abstract
The invention relates to novel conjugates of tetrasaccharides, preferably of sialyl-Lewis X (SLeX) and sialyl-Lewis A (SLeA), having improved activity as inhibitors of cell adhesion, a process for the preparation of these compounds, and their use as pharmacological active compounds and as diagnostics and pharmaceuticals which contain these conjugates.
Claims34
A compound having the formula I,
- Z--Y--(CH.sub.2).sub.n --NH(CO)!.sub.p --R.sup.2 (I)
- in which
- Z is a branched tetrasaccharide,
- Y is oxygen or NH(CO) and
- R.sup.2 is an amino acid or oligopeptide radical of up to 6 amino acids,
- a lipophilic radical formed from aliphatic or cycloaliphatic units,
- a combination of aliphatic and heterocyclic units or
- a triphenylmethane dye, where
- for Y=oxygen
- p is 1 and
- n is an integer from 2 to 10, and
- for Y.dbd.NH(CO) and p=0
- n is an integer from 0 to 10, and
- for Y.dbd.NH(CO) and p=1,
- n is an integer from 1 to 10, and wherein said compound binds to a selection receptor.
12 more elements
Dependencies are inferred from the claim text.