SUBSTITUTED OXAZOLE DERIVATIVES AND USE THEREOF AS TYROSINE KINASE INHIBITORS Russian patent published in 2012 - IPC C07D263/48 C07D413/04 C07D413/12 C07D417/12 C07D413/14 A61K31/4427 A61K31/423 A61K31/428 A61K31/422 A61K31/421 A61P29/00 A61P35/00 A61P37/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula I wherein the substitutes A, B, B', Q and R¹-R⁵ in formula I are specified as follows: A and B' are one of the following groups: (i) (R⁶)N(CH₂)_n, wherein n is 0 or 1; (ii) (CH₂)_n, wherein n is 0, 1 or 2; (iii) C(O)(CH₂)_n, wherein n is 0 or 1; or provided each of A and B' represents nitrogen, together they can form a bivalent radical of formula: -(CH₂)_s-X¹-(CH₂)_t- (a), wherein each s and t is independently 1 or 2, and X¹ represents (CH₂)_n, wherein n is 0 or 1; B is one of the following groups: (i) (R⁶)N; (ii) oxygen; (iii) C=δ, wherein δ represents oxygen or sulphur; (iv) C(R⁶)=C(R⁷); each R⁶ and R⁷ independently represent hydrogen, C_1-4-alkyl; R¹ is specified in the following groups: (i) phenyl group substituted by one or more substitute such as: - halogen specified in F, CI, Br or I, or alkyl¹ group; aryl¹ or heteroaryl group¹; cyano, NH-alkyl¹, N(alkyl¹)(alkyl¹) and amino; - NHCO-R or NHCOO-R, or COO-R, or CONH-R, wherein R represents hydrogen or alkyl group, or (ii) pyridinyl group which can be substituted by one substitute, such as halogen specified in I, F, Cl or Br; alkyl¹ group; aryl¹ group; cyano, NH-alkyl¹, N(alkyl¹)(alkyl¹), and amino; -NHCO-R or NHCOO-R, or COO-R, or CONH-R, wherein R represents hydrogen or alkyl¹ group; each R², R³, R⁴ and R⁵ are independently specified in hydrogen or linear or branched alkyl group containing 1 to 10 carbon atoms; Q is specified in the following groups: (i) alkyl¹; (ii) aryl¹; (iii) heteroaryl¹. The compounds of formula (I) are used for preparing a drug showing the c-kit inhibitor properties and aiming at treating a disease specified in neoplastic, allergic, inflammatory and autoimmune diseases.

EFFECT: use of oxazole derivatives as tyrosine kinase inhibitors.

13 cl, 1 tbl, 31 ex