University College Cardiff Consultants Limited

Nucana Plc

Fabrizio Pertusati

Christopher McGuigan

Hugh Griffith

Magdalena Slusarczyk

Michaela Serpi

Emyr Lloyd-Evans

Edward James

Emily Maguire

Chirstopher McGuigan

Christopher Mcguigan

Samuele Di Ciano

The present invention relates to compounds comprising a salt of a diphosphate phosphoramidate of a nucleoside drug, e.g. clofarabine. The compounds are useful in the treatment of cancer, e.g. leukemia.

Salts of diphosphate phosphoramidate of nucleosides as anticancer compounds

Compounds of general formula (I): (Formula I)) wherein R, Q, R, R, R, R, Rand Arare as defined herein are inhibitors of class I histone deacetylases and are of use in the treatment of lysosomal storage disorders, especially Niemann-Pick type C disease, as well as other lysosomal storage disorders, defective autophagy, accumulation of free cholesterol and mycobacterial diseases. 

Phosphorodiamidates and other phosphorus derivatives of fingolimod and related S1P receptor modulators

Provided are phosphoramidate nucleoside compounds of Formula (I), or pharmaceutically acceptable salts or esters or solvates thereof, useful in the treatment of cancer, viral infections and other diseases: Also provided is a process for the synthesis of compounds of Formula (I) where a desired enantiomer, having regard to the asymmetric chiral center of the phosphorus atom P, is provided in an enriched amount. The process comprises admixing a nucleoside with a phosphorochloridate in the presence of a catalyst comprising a metal salt selected from the group consisting of salts of Cu, Fe, La and Yb.

Process for preparing nucleoside prodrugs

Provided are phosphoramidate nucleoside compounds of Formula (I), or pharmaceutically acceptable salts or esters or solvates thereof, useful in the treatment of cancer, viral infections and other diseases: Also provided is a process for the synthesis of the compounds of Formula (I) where a desired enantiomer, having regard to the asymmetric chiral center of the phosphorus atom P, is provided in an enriched amount. The process comprises admixing a nucleoside with a phosphorochloridate in the presence of a catalyst comprising a metal salt selected from the group consisting of salts of Cu, Fe, La and Yb.

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Cardiff, United Kingdom

Fabrizio Pertusati