Abstract: The present invention provides a process for the preparation of gemcitabine-[phenyl(benzoxy-L-alaninyl)] phosphate of Formula I in high yield and purity.
Abstract: Phosphoramidate derivatives of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.
Type:
Grant
Filed:
November 17, 2015
Date of Patent:
May 23, 2017
Assignee:
NuCana BioMed Limited
Inventors:
Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
Abstract: Phosphorodiamidate derivatives of e.g. gemcitabine are provided for use in treating cancer. In one embodiment, the two amidate motifs each comprises NR?R? where R? is H and R? is CR5R6CO2R7, where R6 is H, R5 is the side chain, including H and C1, of a naturally occurring alpha amino acid, and R7 is branched or unbranched, substituted or unsubstituted, acyclic or cyclic alkyl, including t-butyl-CH2-, benzyl and C3 to C6 cycloalkyl. Formula (I).
Abstract: Phosphoramidate derivatives of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.
Type:
Grant
Filed:
December 4, 2014
Date of Patent:
December 29, 2015
Assignee:
NuCana Biomed Limited
Inventors:
Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
Abstract: Phosphoramidate derivatives of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.
Type:
Grant
Filed:
February 29, 2012
Date of Patent:
January 13, 2015
Assignee:
NuCana BioMed Limited
Inventors:
Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
Abstract: The compounds are phosphoramidate derivatives of nucleoside compounds such as cladribine, isocladribine, fludarabine and clofarabine useful in the treatment of cancer.
Type:
Grant
Filed:
March 16, 2006
Date of Patent:
September 11, 2012
Assignee:
Nucana Biomed Limited
Inventors:
Christopher McGuigan, Kenneth Mills, Costantino Congiatu