Patent RU-2545023-C9 (RU)
Inventor: UIShART Nejl
IPC: C07D498/14
Filed: 2009-06-09
Granted: 2016-06-20
Abstract: 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: CR 3  and Y: N; or T: CR 6 , U: CR 4 , X: CR 3  and Y: N; or T: CR 6 , U: N, X: NR 3  and Y: C; or T: O, U: N, X: CR 3  and Y: C; or T: NR 6 , U: N, X: CR 3  and Y: C; and R 1 , R 2  and R 5 : H, heteroaryl substituted by 1-2 substitutes; or T: CR 6 , U: N, X: CR 3  and Y: N; or T: N, U: CR 4 , X: CR 3  and Y: N; and R 1  and R 2 : H, heteroaryl substituted by 1-2 substitutes; R 5 : heteroaryl substituted by 1-2 substitutes; R 3 : H, bridging (C 7 -C 10 )cycloalkyl; (C 1 -C 8 )alkyl optionally substituted by 1 substitute; (C 3 -C 10 )cycloalkyl optionally substituted by 1 substitute; (C 6 -C 8 )cycloalkenyl substituted by two (C 1 -C 6 )alkyl; (C 6 )aryl optionally substituted by 1-2 substitutes; heteroaryl optionally substituted by (C 1 -C 6 )alkyl; heterocyclyl optionally substituted by (C 1 -C 6 )alkyl or heteroaryl; or R 3 : -A-D-E-G, wherein: A: a bond or (C 1 -C 6 )alkylene; D : (C 1- C 2 )alkylene optionally substituted by (C 1 -C 6 )alkyl, bridging (C 6 -C 10 )cycloalkylene optionally substituted by (C 1 -C 6 )alkyl, (C 3 -C 10 )cycloalkylene optionally substituted by 1-2 substitutes, (C 4 -C 6 )cycloalkenylene optionally substituted by (C 1 -C 6 )alkyl, (C 6 )arylene, heteroarylene or heterocyclylene optionally substituted by one (C 1 -C 6 )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) 2 R a , -CN, -C(O)N(R a )(R b ), -N(R a )C(O)R b , -C(O)R a , -CF 3 , N(R a )S(O) 2 R b , -(C 1 -C 6 )alkyl optionally substituted by 1-3 substitutes; -(C 3 -C 6 )cycloalkyl optionally substituted by CN; -heteroaryl optionally substituted by 1-2 halogens, CN, -C(O)NH 2  or -CF 3 ; -heterocyclyl optionally substituted by 1-5 substitutes, -(C 6 -C 10 )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 (C 3 -C 6 )heterocyclyl optionally substituted by 1 substitute, wherein said (C 3 -C 6 )heterocyclyl is bound through nitrogen; R 4  and R 6 : H, (C 1 -C 4 )alkyl optionally substituted by -OH, -COOH; (C 3 -C 8 )cycloalkyl, phenyl, optionally substituted by -SO 2 CH 3  or -NHSO 2 CH 3 , halogen or -J-L-M-Q; wherein: J: (C 2 -C 6 )alkenylene; L: a bond; M: a bond; Q: -C(O)OR a ; R a  and R b : H, (C 1 -C 4 )alkyl optionally substituted by cyano, -CF 3  or cyclopropane; (C 6 )aryl optionally substituted by halogen or -O(C 1 -C 4 )alkyl; and R e : a bond, (C 1 -C 4 )alkylene or (C 3 )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