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US 9,221,866 B2Granted
Phosphoramidate derivatives of 5-fluoro-2′-deoxyuridine for use in the treatment of cancer
AssigneeNuCana BioMed Limited
InventorsChristopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
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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.
Claims69
A compound of formula (I):
- wherein
- Ar is a fused bicyclic aryl moiety or a monocyclic aryl moiety, either of which aryl moieties is carbocyclic or heterocyclic and is optionally substituted;
- R3 is alkyl, which is optionally substituted;
- R4 is H or alkoyl;
- R1 and R2 are independently selected from the group consisting of H and alkyl, or R1 and R2 together form an alkylene chain so as to provide, together with the C atom to which they are attached, a cyclic system, or one of R1 and R2 comprises an alkylene chain attached to N, the H atom attached to N is absent and one of R1 and R2 comprise H or alkyl, any of which said alkyl moieties or alkylene chains is optionally substituted;
- or a pharmaceutically acceptable salt, ester, salt of such ester, hydrate, solvate, crystalline form, or metabolite thereof, or any other compound which upon administration to a recipient is capable of providing (directly or indirectly) said compound of formula (I),
- wherein the compound is not a compound having, in combination, Ar as unsubstituted phenyl, R3 as CH3, R4 as H, one of R1 and R2 as H and one of R1 and R2 as CH3.
4 more elements
A compound of formula (I):
- wherein
- Ar is a fused bicyclic aryl moiety or a monocyclic aryl moiety, either of which aryl moieties is carbocyclic or heterocyclic and is optionally substituted;
- R3 is alkyl, which is optionally substituted;
- R4 is H or alkoyl;
- R1 and R2 are independently selected from the group consisting of H and alkyl, or R1 and R2 together form an alkylene chain so as to provide, together with the C atom to which they are attached, a cyclic system, or one of R1 and R2 comprises an alkylene chain attached to N, the H atom attached to N is absent and one of R1 and R2 comprise H or alkyl, any of which said alkyl moieties or alkylene chains is optionally substituted;
- or a pharmaceutically acceptable salt thereof,
- wherein the compound is not a compound having, in combination, Ar as unsubstituted phenyl, R3 as CH3, R4 as H, one of R1 and R2 as H and one of R1 and R2 as CH3.
4 more elements
Dependencies are inferred from the claim text.