DERIVATIVES OF 1,5- AND 1,7-NAPHTHYRIDINE USEFUL IN TREATMENT OF FGFR-MEDIATED DISEASES Russian patent published in 2017 - IPC C07D471/04 A61K31/4375 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a novel derivative of 1,5- and 1,7-naphthyridine of the formulas

or ,

as well as to its tautomeric or isomeric form, and a pharmaceutically acceptable salt, wherein X¹ is N and X² is CR^3a or X² is N and X¹ is CR^3a; Each R² is independently selected from halogen and C₁-₄alkoxy; Y is -E-D; D is a 5- or 6-membered aromatic monocyclic heterocyclyl containing one or two N atoms, wherein said heterocyclyl may be optionally substituted with one or two R¹ groups; E is a chain; R¹ is C₁-₆alkyl; R^3a is hydrogen or chlorine; R³ is C₂-₆alkynyl, halo C1-6alkyl, hydroxyC₁-₆alkyl, cyano C₁-₆alkyl, C₁-₆alkoxyC₁-₆alkyl, C₁-₆alkyl, substituted R⁹, C₁-₆alkyl substituted with -NR¹⁰R¹¹, C₁-₆alkyl substituted with -C(=O)-NR¹⁰R¹¹, R¹³; R⁹ is a 5- or 6-membered saturated or aromatic monocyclic heterocyclyl containing one, two or three heteroatoms selected from N or O, wherein mentioned 5- or 6-membered monocyclic heterocyclyl is optionally and independently substituted with 1 or 2 substituents, wherein each substituent is independently selected from =O, C₁-₄alkyl, -S(=O)₂-NR¹⁴R¹⁵ and phenyl C₁-₆alkyl; R¹⁰ and R¹¹ are each independently hydrogen, C₁-₆alkyl, C₁-₆alkyl substituted with -NR¹⁴R¹⁵; R¹³ is a saturated 6-membered monocyclic heterocyclyl containing one N atom; R¹⁴ and R¹⁵ are each independently hydrogen or C₁-₄alkyl; N is independently an integer of 2, 3 or 4. The invention also relates to a pharmaceutical composition based on a compound of formulas (IA) or (IB), the use of mentioned compound, a method for treating or preventing a condition mediated by FGFR kinase, a product based on a compound of formulas (IA) or (IB).

EFFECT: new naphthyridine derivatives, useful in the treatment of cancer, have been obtained.

36 cl, 4 tbl, 38 ex