NOVEL AMIDE DERIVATIVE FOR INHIBITING GROWTH OF CANCER CELLS Russian patent published in 2011 - IPC C07D403/12 C07D239/94 A61K31/517 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel amide derivatives of formula (I), isomers and pharmaceutically acceptable salt thereof, which have cancer cell selective inhibiting properties, caused by an epidermal growth factor receptor (EGFR), selected from EGFR or caused by EGFR mutation. In formula (I): (I) (a) or (b), A denotes a group (a) or (b), R₄, R₅, R₆ and R₇, each independently denote hydrogen, halogen, N-C₁-₆alkyl or N-hydroxyamido or inverse C-C_1-6alkylamido (-NHCOC_1-6alkyl), hydroxycarbonyl(-COOH), C_1-6 alkyloxycarbonyl(-COOC_1-6), C_1-6alkyl or C_1-6alkyl, substituted with a hydroxy group, C_1-6dialkylamino or a saturated 5-6-member heterocyclic group with 1-2 heteroatoms and selected from nitrogen and oxygen atoms; R₁ denotes a phenyl or a 6-member heteroaryl group with a nitrogen atom as a heteroatom, each of which is substituted with 1-3 X, or C_1-6alkyl, substituted with a phenyl, which can be substituted with halogen atoms; R₂ denotes hydrogen, hydroxy, C_1-6alkoxy or C_1-6alkoxy, substituted C_1-6alkoxy or 5-6-member saturated heterocyclic group; R₃ denotes hydrogen, -COOH, C_1-6alkyloxycarbonyl or amido, N-unsubstituted or N-substituted Y; n_a and n_b each is a whole number ranging from 1 to 3; where: X denotes hydrogen, halogen, hydroxy, cyano, nitro, (mono-, di- or trihalogen)methyl, mercapto, C_1-6alkylthio, acrylamido, C_1-6alkyl, C_2-6alkenyl, C_2-6alkynyl, C_1-6alkoxy, phenyloxy, C_1-6dialkylamino or C_1-6alkyl or C_1-6alkoxy, substituted with Z, provided that when the number of substitutes X equals two or more, groups X can be condensed with each other to form a 5-member cyclic structure, possibly containing 2 nitrogen atoms in the ring as heteroatoms; Y denotes hydroxy, C_1-6alkyl or C_1-6alkyl substituted with Z, C_1-6alkyl has 1-4 fragments selected from a group consisting of N, O, S, SO and SO₂; and Z denotes C_1-6alkyl, phenyl or a 6-member heterocyclic group containing one or more heteroatoms selected from N or O. Said phenyl or heterocyclic group is unsubstituted or substituted with a halogen.

EFFECT: improved properties of the derivatives.

4 cl, 7 tbl, 144 ex