Patent RU-2278115-C2 (RU)
Inventor: MAVUNKEL BABU DZH
IPC: C07D403/06
Filed: 2000-05-19
Granted: 2006-06-20
Abstract: FIELD: organic chemistry, biochemistry, medicine, pharmacy. 
     SUBSTANCE: invention relates to new derivatives of indole of the formula (1):   and their pharmaceutically acceptable salts wherein   represents a double bond; Z 1  represents nitrogen atom (N), -CR 5  wherein R 5  represents hydrogen atom (H), (C 1 -C 6 )-alkyl, hydroxy-group (OH),(C 1 -C 6 )-alkoxy-group or halogen atom; Z 2  at position 2 represents CR 1  and at position it represents CA wherein each R 1  means independently (C 1 -C 6 )-alkyl; A represents -W i -COX j Y wherein Y means -COR 2  wherein R 2  means -OR, -NR 2,  -NRNR 2  or -NROR wherein each R represents independently hydrogen atom (H), (C 1 -C 6 )-alkyl, or (C 5- C 6 )-heteroaryl comprising one or two heteroatoms in ring chosen from atoms N, O and S wherein each of them is substituted with one or some groups chosen from -NR' 2 , -OR', -COOR', (C 1 -C 6 )-alkyl, -CN, =O, and -SR' wherein each R' represents hydrogen atom (H) or (C 1 -C 6 )-alkyl and wherein two R or R' jointed to the same nitrogen atom (N) can form 3-8-membered ring chosen from the group comprising piperazine ring, morpholine ring, thiazolidine ring, oxazolidine ring, pyrrolidine ring, piperidine ring, azacyclopropane ring, azacyclobutane ring and azacyclooctane ring and wherein indicated ring can be substituted additionally with (C 1 -C 6 )-alkyl or -COO-(C 1 -C 6 )-alkyl; X represents unsubstituted (C 1 -C 6 )-alkylene, or Y means imidazole substituted with methyl group; i = 0; j = 0 or 1; R 7  means hydrogen atom (H) or (C 1 -C 6 )-alkyl, -SOR, -SO 2 R, -RCO, -COOR, (C 1 -C 6 )-alkyl-COR, -CONR 2 , -SO 2 NR 2 ,-CN, -OR, (C 1 -C 6 )-alkyl-SR, (C 1 -C 6 )-alkyl-OCOR, (C 1 -C 6 )-alkyl-COOR, (C 1 -C 6 )-alkyl-CN, or (C 1 -C 6 )-alkyl-CONR 2  wherein each R represent independently hydrogen atom (H), (C 1 -C 6 )-alkyl or aryl that is substituted optionally with halogen atom, (C 1 -C 4 )-alkyl or (C 1 -C 4 )-alkoxy-group; or R 7  represents methoxymethyl, methoxyethyl, ethoxymethyl, benzyloxymethyl or 2-methoxyethyloxymethyl; each R 3  represent independently halogen atom, (C 1 -C 6 )-alkyl, -OR, -SR or -NR 2  wherein R represents hydrogen atom (H) or (C 1 -C 6 )-alkyl; n = 0-3; L 1  means -CO; L 2  means (C 1 -C 4 )-alkylene optionally substituted with one or two groups of (C 1 -C 4 )-alkyl; each R 4  is chosen independently from the group comprising (C 1 -C 6 )-alkyl, halogen atom, -OR, -NR 2 , -SR, -SOR, -SO 2 R, -RCO, -COOR, -CONR 2 , -SO 2 NR 2  wherein each R represents independently hydrogen atom (H) or (C 1 -C 6 )-alkyl; or R 4  represents =O; m = 0-4; Ar means aryl group substituted with from 0 to 5 substitutes chosen from the group comprising (C 1 -C 6 )-alkyl, halogen atom, -OR, -NR 2 , -SR, -SOR, -SO 2 R, -RCO, -COOR, -CONR 2  and -SO 2 NR 2  wherein each R represents independently hydrogen atom (H) or (C 1 -C 6 )-alkyl. Compounds of the formula (I) possess the inhibitory activity with respect to p38-α kinase that allows their using as components of the pharmaceutical composition. 
     EFFECT: valuable medicinal and biochemical properties of compounds and pharmaceutical composition. 
     63 cl, 3 tbl, 9 sch, 16 ex