FIELD: pharmaceutics.
SUBSTANCE: invention relates to a compound represented by the following formula (IA):
(IA),
in which n is 0–2; A represents a C6-10 arylene group or a C3-5 heteroarylene group containing one or two nitrogen atoms or one sulfur atom; G represents a single bond, an oxygen atom or -CH2-; E represents a C3-5 nitrogen-containing non-aromatic heterocycle; R1 is a cyano group, mono-C1-6 alkylamino group, a di-C1-6 alkylamino group, C2-6 alkyl group, a C1-6 alkoxy group optionally substituted by 1 to 3 halogen atoms or one hydroxyl group, C1-6 alkoxy C1-6 alkyl group or a C1-6 alkoxy C1-6 alkoxy group; R2 represents a hydrogen atom, a halogen atom, a hydroxyl group, a C2-6 acyl group optionally substituted by one substituent selected from a group S described below, C1-6 alkyl group optionally substituted by 1 to 3 halogen atoms, a hydroxy C1-6 alkyl group or a C3-5 nitrogen-containing non-aromatic heterocyclic group; R3 represents a hydrogen atom, oxo group, a C1-6 alkyl group or a C1-6 alkoxy group; R4 represents a C1-6 alkyl group; with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom; and group S represents a group consisting of a hydroxyl group, a mono-C1-6 alkylamino group, a di-C1-6 alkylamino group, a C1-6 alkoxy group and a C3-5 nitrogen-containing non-aromatic heterocyclic group. Invention also relates to individual compounds, a pharmaceutical composition, therapeutic agents, a method of treatment, an FGFR inhibitor, and the use of a compound for the manufacture of a therapeutic agent.
EFFECT: new compounds of formula (IA) have been obtained which have inhibitory activity with regard to FGFR and can be useful in the treatment of the stomach cancer, lung carcinoma, bladder cancer or endometrial cancer.
25 cl, 43 tbl, 152 ex
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