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US 2010/0249055 A1Published application
Clofarabine phospholipid derivatives
AssigneeHeidelberg Pharma GmbH
InventorsChristoph Mueller, Brigitte Heckl-Oestreicher, Christian Lutz
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Abstract
The subject of the present invention are specific phospholipidesters of clofarabine and the use of such lipidesters in the treatment of tumors.
Claims11
A nucleotide derivative of formula I
- wherein
- R1 and R2 are independently selected from the group consisting of a straight-chain or branched, saturated or unsaturated alkyl chain having 1-20 carbon atoms,
- their tautomers, their optically active forms, including single diastereomeric forms, mixtures thereof, racemic mixtures of these compounds, and their physiologically acceptable salts of inorganic and organic acids or bases.
A method of synthesis of compounds of the formula I:
- wherein R1 and R2 are independently selected from the group consisting of a straight-chain or branched, saturated or unsaturated alkyl chain having 1-20 carbon atoms, their tautomers, their optically active forms, including single diastereomeric forms, mixtures thereof, racemic mixtures of these compounds, and their physiologically acceptable salts of inorganic and organic acids or bases
- comprising reacting of 2-Chloro-9-(2′-deoxy-2′-fluoro-β-arabino-furanosyl)adenine:
- with an activated form of the compound:
- in an inert solvent to provide the compound of formula
1 more element
Dependencies are inferred from the claim text.