Compounds for use in the treatment of cancer

C - Chemistry – Metallurgy – 07 – D

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C07D 251/70 (2006.01) A61K 31/53 (2006.01)

Patent

CA 2106868

2106868 9216513 PCTABS00016 Compounds of formula (I), wherein R3 is hydrogen, alkyl or hydroxymethyl, and R1 and R2 are hydrogen, alkyl or an electron withdrawing organic group containing at least two carbon atoms, at least one of R1 and R2 being an electron withdrawing group, and with the proviso that: when R3 is hydroxymethyl, R1 and R2 are electron withdrawing organic groups; are useful in the treatement of cancers, particularly cis-platin resistant ovarian cancer. The new compounds are obtainable by reacting formaldehyde with an intermediate of formula (II), wherein R3a and R3b are hydrogen, alkyl or hydroxymethyl, but not both hydroxymethyl, and R1 and R2 are hydrogen, alkyl or an electron withdrawing organic group containing at least two carbon atoms, and at least one of R1 and R2 is an electron-withdrawing organic group and where necessary, converting any N-hydroxy-methoxymethyl substituents to N-hydroxymethyl by treatment with an aqueous medium.

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