| 摘要 |
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to organic chemistry, namely to a heterocyclic compound of formulaand to its pharmaceutically acceptable salts, stereoisomers and isomers, wherein T: N, U: N, X: CRand Y: N; or T: CR, U: CR, X: CRand Y: N; or T: CR, U: N, X: NRand Y: C; or T: O, U: N, X: CRand Y: C; or T: NR, U: N, X: CRand Y: C; and R, Rand R: H, heteroaryl substituted by 1-2 substitutes; or T: CR, U: N, X: CRand Y: N; or T: N, U: CR, X: CRand Y: N; and Rand R: H, heteroaryl substituted by 1-2 substitutes; R: heteroaryl substituted by 1-2 substitutes; R: H, bridging (C-C)cycloalkyl; (C-C)alkyl optionally substituted by 1 substitute; (C-C)cycloalkyl optionally substituted by 1 substitute; (C-C)cycloalkenyl substituted by two (C-C)alkyl; (C)aryl optionally substituted by 1-2 substitutes; heteroaryl optionally substituted by (C-C)alkyl; heterocyclyl optionally substituted by (C-C)alkyl or heteroaryl; or R: -A-D-E-G, wherein: A: a bond or (C-C)alkylene; D : (CC)alkylene optionally substituted by (C-C)alkyl, bridging (C-C)cycloalkylene optionally substituted by (C-C)alkyl, (C-C)cycloalkylene optionally substituted by 1-2 substitutes, (C-C)cycloalkenylene optionally substituted by (C-C)alkyl, (C)arylene, heteroarylene or heterocyclylene optionally substituted by one (C-C)alkyl; E: a bond, -R-, -R-C(O)-R-, -R-C(O)O-R-, -R-O-R-, -R-S(O)-R-, -R-N(R)-R-, -R-N(R)C(O)-R-, -R-C(O)N(R)R-, -R-N(R)C(O)OR- or -R-N(R)S(O)-R-; wherein in each case, E is bound to either a carbon atom, or a nitrogen atom in D; G: H, -N(R)(R), halogen, -OR, S(O)R, -CN, -C(O)N(R)(R), -N(R)C(O)R, -C(O)R, -CF, N(R)S(O)R, -(C-C)alkyl optionally substituted by 1-3 substitutes; -(C-C)cycloalkyl optionally substituted by CN; -heteroaryl optionally substituted by 1-2 halogens, CN, -C(O)NHor -CF; -heterocyclyl optionally substituted by 1-5 substitutes, -(C-C)aryl optionally substituted by 1-3 substitutes; wherein in a fragment containing -N(R)(R), nitrogen, Rand Rcan form a ring so that -N(R)(R) represents (C-C)heterocyclyl optionally substituted by 1 substitute, wherein said (C-C)heterocyclyl is bound through nitrogen; Rand R: H, (C-C)alkyl optionally substituted by -OH, -COOH; (C-C)cycloalkyl, phenyl, optionally substituted by -SOCHor -NHSOCH, halogen or -J-L-M-Q; wherein: J: (C-C)alkenylene; L: a bond; M: a bond; Q: -C(O)OR; Rand R: H, (C-C)alkyl optionally substituted by cyano, -CFor cyclopropane; (C)aryl optionally substituted by halogen or -O(C-C)alkyl; and R: a bond, (C-C)alkylene or (C)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 2-6for 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 |
