Patent RU-2619463-C2 (RU)
Inventor: ESHVELL MARK A
IPC: A61K31/437
Filed: 2010-12-29
Granted: 2017-05-16
Abstract: FIELD: chemistry. 
     SUBSTANCE: invention relates to a heterocyclic compound of formula (I) or a pharmaceutically acceptable salt or ester, wherein X 1 : N and X 2 : CR x ; R x , R 1  and R 3 : H, halogen, nitro, C 1 -C 6 alkyl, C 1 -C 6 alkyl, substituted by three halogen atoms, C 1 -C 6 alkoxy, amino, C 6 -C 10 -aryl, C 6 -C 10 -aryl substituted by 1-2 substituents selected from hydroxyl, halogen, cyano, amino, di-C 1 -C 6 alkilamino, C 1 -C 6 alkyl, C 1 -C 6 alkyl substituted by hydroxyl or amino, C 1 -C 6 alkoxy, C 1 -C 6 alkoxy substituted by three halogen atoms, C 1 -C 6 alkilkarbonyl, C 1 -C 6 alkoxykarbonyl, carboxyl, aminocarbonyl, C 1 -C 6 alkilaminokarbonyl, C 1 -C 6 alkilkarbonylamino, C 1 -C 6 alkilsulfinyl, 5-x heteroaryl containing 2 atom of N, and 5-x or 6-x heterocycle Containing 1-2 heteroatoms selected from N and O, Heteroaryl containing one or two 5-x or 6-x rings and 1-2 heteroatoms selected from N, O and S, heteroaryl containing one or two 5-x or 6-x rings and 1-2 heteroatoms selected from N and O, substituted by 1 or more substituents selected from hydroxyl, halogen, amino, C 1 -C 6 alkylcarbonyl, carboxyl, C 1 -C 6 alkyl and a 6-x heterocycle containing 2 heteroatoms selected from N and O, C 3 -C 6  saturated carbocycle or 6-membered A heterocycle containing 1 N atom; X or y is 0 or 1; R p1 : halogen; R p2 : C 1 -C 6 alkyl or 5-x heteroaryl containing 2 heteroatoms selected from N and O; R n5  and R n6 : H or S(O)2R 8 ; R 8 : H or C 1 -C 6 alkyl; R: H, halogen, C 1 -C 6 alkyl, C 1 -C 6 alkyl, substituted by amino, C 1 -C 6 alkoxy, amino, 5-x heteroaryl containing 2-3 heteroatoms selected from N, C 3 -C 6 saturated carbocycle, C 3 -C 6  saturated carbocycle substituted by one A substituent selected from amino, C 1 -C 6 alkoxycarbonyl, C 1 -C 6 alkylaminocarbonyl, carboxyl, and aminocarbonyl, a heterocycle containing one 4-x or 6-x ring and 1-2 heteroatoms selected from N, A heterocycle containing one 4-, 5-x or 6-x ring and 1-2 heteroatoms selected from N, O and S substituted with one substituent selected from methyl and amino or Q-T; Q: connection or C 1 -C 6 alkyl linker; T: NR n1 R n2 , C(O)R o , or S(O)2R s ; R n1 : H; R n2 : H, C 1 -C 6 alkyl, C 1 -C 6 alkyl substituted by C 6 -C 10 aryl, C(O)R 4 , C(O)OR 4 , C(O)NR 4 'R 4 , or S(O)2R 5  or R n1  and R n2 , together with the nitrogen atom to which they are attached form a 6-x ring, which optionally contains 1 additional O atom; R 4 , R 4 ', and R 5 : H, C 1 -C 6 alkyl, C 1 -C 6 alkyl substituted by 1-2 substituents independently selected from C 6 -C 10 aryl, 5-x or 6-x heteroaryl containing 1 to 4 N atoms and C 3  to C 6  saturated carbocycle, C 6 -C 10 aryl, C 6 -C 10 aryl substituted by 1-2 substituents independently selected from halo, cyano, C 1 -C 6 alkyl, C 1 -C 6 alkyl substituted with three halogen atoms or with one phenyl, C 1 -C 6 alkoxy, C 1 -C 6 alkoxy substituted with three atoms of halogen, C 1 -C 6 alkilamino, di-C 1 -C 6 alkilamino, C 6 -C 10 arilkarbonyl wherein aryl is substituted by halogen, C 1 -C 6 alkoksikarbonyl, C 1 -C 6 alkilkarbonylamine, C 6 -C 10 -aryl and 5-h ennogo heteroaryl containing 1 or 2 N atoms, heteroaryl containing one or two 5-x or 6-x rings and 1-2 heteroatoms selected from N, O and S, heteroaryl containing one or two 5- or 6-membered rings and 1-2 heteroatoms selected from N, O and S, substituted with 1 or 2 substituents independently selected from halogen and C 1 -C 6  alkyl, or C 3 -C 6  saturated carbocycle; R o : C 6 -C 10 aryl, NR o1 R o2 , or OR o3 ; R s : a 6-x heterocycle containing 1 N atom, or NR s 1R s2 ; R o1  and R o2 : H, C 1 -C 6 alkyl, C 1 -C 6 alkyl substituted by 1 substituent selected from C 3 -C 8  saturated carbocycle, C 6 -C 10  aryl, and C 1 -C 6 alkylcarbonylamino, C 6 -C 10 aryl, C 6 -C 10 aryl substituted by one or two substituents, Independently selected from halogen, cyano, C 1 -C 6 alkyl, C 1 -C 6 alkoxy and C 1 -C 6 alkylcarbonylamino, heteroaryl containing one or two 5-x or 6-x rings and 1 heteroatom selected from N or O, heteroaryl containing one or two 5-x or 6-x rings and 1-2 heteroatoms selected from N and S substituted with one substituent selected from halogen and C 1 -C 6 alkyl or C 3 -C 6  A saturated carbocycle; R o3 : H or C 1 -C 6 alkyl; And R s1  and R s 2: H or C 1 -C 6 alkyl. The invention also relates to specific compounds, pharmaceutical compositions based on compounds of formula (I) 
     
       
     
     a method of treating a cell proliferative disorder. 
     EFFECT: obtaining novel heterocyclic compounds, useful in the treatment of bacterial infections. 
     21 cl, 4 tbl, 134 ex