SUBSTITUTED QUINAZINE DERIVATIVES AS FGFR-KINASE INHIBITORS FOR TREATMENT OF CANCER Russian patent published in 2016 - IPC C07D403/04 A61K31/502 A61P35/00 

Abstract RU 2602233 C2

FIELD: pharmaceutics.

SUBSTANCE: invention is related to compounds of formula I, pharmaceutical compositions based thereon, use thereof for treating cancer, FGFR-kinase mediated, and methods of their production. In general formula I n is any integer, equal to 0, 1 or 2; R1 is C1-6alkyl; each group R1a represents hydrogen; each group R2 is C1-4alkoxy; R3a is-NR10R11, hydroxyl, gidroksiC1-6alkyl, cianoC1-6alkyl, C1-6alkyl substituted R9, C1-6alkyl substituted -NR10R11, C1-6alkyl substituted hydroxyl and -NR10R11, C1-6alkyl substituted -C(=O)-NR10R11; R3b is hydrogen or hydroxyl; provided that if R3a is -NR10R11, then R3b is hydrogen; or R3a and R3b are taken together to form =O, to make cyclopropyl together with carbon atom, with which they are bonded or to make =CH-C0-4alkyl, substituted R3c; R3s is-NR10R11 or cyano; R9 is a 5-7-member monocyclic heterocyclic ring, containing at least one heteroatom, selected from N, O or S, where 5-7-member monocyclic heterocyclyl is optionally substituted = O; R10 and R11 group each independently represents hydrogen, C1-6alkyl, C1-6alkyl substituted-NR14R15, or halogenC1-6alkyl; R14 and R15 group each independently denotes hydrogen or C1-4alkyl.

EFFECT: treatment of cancer.

34 cl, 4 tbl, 10 ex

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Authors

Saksti Gordon

Mjurrej Kristofer Uilljam

Berdini Valerio

Bezong Gilbert Ebaj

Khamlett Kristofer Charlz Frederik

Vudkhed Stiven Dzhon

Lini Jannik Eme Eddi

Anzhibo Patrik Rene

Dates

2016-11-10Published

2011-11-29Filed