Medicaments useful in cancer therapy and having...

C - Chemistry – Metallurgy – 07 – D

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C07D 313/12 (2006.01) A61K 31/135 (2006.01) A61K 31/335 (2006.01) A61K 31/395 (2006.01) A61K 31/40 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) A61K 31/55 (2006.01) C07C 211/32 (2006.01) C07D 213/55 (2006.01) C07D 213/56 (2006.01) C07D 223/20 (2006.01) C07D 295/03 (2006.01) C07D 295/073 (2006.01) C07D 295/096 (2006.01) C07D 295/155 (2006.01) C07D 403/06 (2006.01) C07D 405/06 (2006.01)

Patent

CA 2059127

2059127 9015599 PCTABS00002 Use of compounds of formula (I) wherein A represents a group selected from (II) or (III), X represents -CH- or -N-; R1 represents a hydrogen or halogen atom, a C1-4 alkoxy group, a C1-4 alkyl group, or a C1-4 alkyl group substituted by 1 to 3 halogen atoms; R2 represents a hydrogen or halogen atom, a C1-4 alkoxy group, benzyloxy or a group -R7COOR8 (wherein R7 represents a single bond or a C1-7 bivalent aliphatic hydrocarbon group and R8 represents a hydrogen atom or a C1-4 alkyl group) or a group R7CONR8aR8b (wherein R8a and R8b each represent a hydrogen atom or a C1-4 alkyl group, or together with the nitrogen atom to which they are attached form a 4-6 membered saturated heterocyclic ring); R3 and R4, which may be the same or different each represent a hydrogen atom or a C1-4 alkyl group, or R3 and R4 together with the nitrogen atom to which they are attached form a 4-6 membered saturated heterocyclic ring, which may optionally contain an oxygen atom or a further nitrogen atom, which may itself be substituted by a C1-4 alkyl group; R5 and R6 each represent a hydrogen atom or together form a linking group between the aromatic rings, said group being selected from -CH2CH2-, -CH2O-, -OCH2-, -NHCH2, or -CH2NH; n is zero or an integer from 1 to 3; and p and q are each independently an integer from 1 to 4, with the provisos that (a) when R5 and R6 form a linking group, A is not (IV) and (b) when A represents a group (V) and n is 1, R1 is methyl, NR3R4 is pyrrolidino and R5 and R6 are both hydrogen then R2 is not hydrogen or -CH=CHCO2H, and pharmaceutically acceptable salts thereof in the manufacture of a medicament for enhancing the therapeutic effect of an antineoplastic agent.

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