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US 2002/0173468 A1Published application
Modified cytostatic agents
OwnerHans-Georg Lerchen, Karsten Von Dem Bruch +2inventors
InventorsHANS-GEORG LERCHEN, KARSTEN VON DEM BRUCH, JORG BAUMGARTEN, MICHAEL SPERZEL
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Abstract
The present invention relates to conjugates of cytostatics and N-thiocarbonyl-modified amino acids or peptides, processes for their preparation and their use as medicaments, in particular in connection with carcinomatous disorders.
Claims9
Compounds of the general formula (I)
- 31
- in which
- 32
- represents 1 to n′ groups
- 33
- which are identical to or different from one another, where n is a number 1 to n′ and n′ corresponds to the maximum number of possible linkage sites of M,
- in which
- Ar represents an aryl radical having up to 10 carbon atoms, which additionally to X can optionally be mono- or polysubstituted by alkyl having up to 6 carbon atoms, alkoxy having up to 6 carbon atoms, alkoxycarbonyl having up to 6 carbon atoms, hydroxyl, carboxyl, carboxyalkyl having up to 6 carbon atoms, cyano, nitro, isocyanato, isothiocyanato, halogen, sulphonyl and/or sulphonamide,
- X represents a direct single bond or alkylene having up to 6 carbon atoms,
- M represents a mono-, di-, tri- or tetrapeptide, which is linked via the α-amino group and/or via amino and/or hydroxy groups of the side chains to the n groups
- 34
- which are identical to or different from one another, where further functional groups of the peptide can optionally carry protective groups,
- C represents a radical of a cytostatic or of a cytostatic derivative which is linked to m via an amino function or via an oxygen atom,
- and their stereoisomers, stereoisomer mixtures and salts.
11 more elements
Dependencies are inferred from the claim text.