TRICYCLIC COMPOUNDS, PHARMACEUTICAL COMPOSITION CONTAINING THEM AND USING THEM FOR TREATING IMMUNOLOGICAL AND ONCOLOGICAL COMPOUNDS Russian patent published in 2015 - IPC C07D487/14 C07D471/14 C07D498/14 A61K31/4985 A61K31/4162 A61K31/407 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to a heterocyclic compound of formula and to its pharmaceutically acceptable salts, stereoisomers and isomers, wherein T: N, U: N, X: CR³ and Y: N; or T: CR⁶, U: CR⁴, X: CR³ and Y: N; or T: CR⁶, U: N, X: NR³ and Y: C; or T: O, U: N, X: CR³ and Y: C; or T: NR⁶, U: N, X: CR³ and Y: C; and R¹, R² and R⁵: H, heteroaryl substituted by 1-2 substitutes; or T: CR⁶, U: N, X: CR³ and Y: N; or T: N, U: CR⁴, X: CR³ and Y: N; and R¹ and R²: H, heteroaryl substituted by 1-2 substitutes; R⁵: heteroaryl substituted by 1-2 substitutes; R³: H, bridging (C₇-C₁₀)cycloalkyl; (C₁-C₈)alkyl optionally substituted by 1 substitute; (C₃-C₁₀)cycloalkyl optionally substituted by 1 substitute; (C₆-C₈)cycloalkenyl substituted by two (C₁-C₆)alkyl; (C₆)aryl optionally substituted by 1-2 substitutes; heteroaryl optionally substituted by (C₁-C₆)alkyl; heterocyclyl optionally substituted by (C₁-C₆)alkyl or heteroaryl; or R³: -A-D-E-G, wherein: A: a bond or (C₁-C₆)alkylene; D : (C_1-C₂)alkylene optionally substituted by (C₁-C₆)alkyl, bridging (C₆-C₁₀)cycloalkylene optionally substituted by (C₁-C₆)alkyl, (C₃-C₁₀)cycloalkylene optionally substituted by 1-2 substitutes, (C₄-C₆)cycloalkenylene optionally substituted by (C₁-C₆)alkyl, (C₆)arylene, heteroarylene or heterocyclylene optionally substituted by one (C₁-C₆)alkyl; E: a bond, -R^e-, -R^e-C(O)-R^e-, -R^e-C(O)O-R^e-, -R^e-O-R^e-, -R^e-S(O)₂-R^e-, -R^e-N(R^a)-R^e-, -R^e-N(R^a)C(O)-R^e-, -R^e-C(O)N(R^a)R^e-, -R^e-N(R^a)C(O)OR^e- or -R^e-N(R^a)S(O)₂-R^e-; wherein in each case, E is bound to either a carbon atom, or a nitrogen atom in D; G: H, -N(R^a)(R^b), halogen, -OR^a, S(O)₂R^a, -CN, -C(O)N(R^a)(R^b), -N(R^a)C(O)R^b, -C(O)R^a, -CF₃, N(R^a)S(O)₂R^b, -(C₁-C₆)alkyl optionally substituted by 1-3 substitutes; -(C₃-C₆)cycloalkyl optionally substituted by CN; -heteroaryl optionally substituted by 1-2 halogens, CN, -C(O)NH₂ or -CF₃; -heterocyclyl optionally substituted by 1-5 substitutes, -(C₆-C₁₀)aryl optionally substituted by 1-3 substitutes; wherein in a fragment containing -N(R^a)(R^b), nitrogen, R^a and R^b can form a ring so that -N(R^a)(R^b) represents (C₃-C₆)heterocyclyl optionally substituted by 1 substitute, wherein said (C₃-C₆)heterocyclyl is bound through nitrogen; R⁴ and R⁶: H, (C₁-C₄)alkyl optionally substituted by -OH, -COOH; (C₃-C₈)cycloalkyl, phenyl, optionally substituted by -SO₂CH₃ or -NHSO₂CH₃, halogen or -J-L-M-Q; wherein: J: (C₂-C₆)alkenylene; L: a bond; M: a bond; Q: -C(O)OR^a; R^a and R^b: H, (C₁-C₄)alkyl optionally substituted by cyano, -CF₃ or cyclopropane; (C₆)aryl optionally substituted by halogen or -O(C₁-C₄)alkyl; and R^e: a bond, (C₁-C₄)alkylene or (C₃)cycloalkylene. Besides, the invention refers to specific compounds, a pharmaceutical composition based on the compound of formula I, using the compound of formula I for treating and using the compounds of formulas 2-6

for preparing the compound of formula I.

EFFECT: prepared are the new compounds effective in treating a condition mediated by Jak1, Jak3 or Syk protein kinase activity.

51 cl, 34 tbl, 44 ex