Patent RU-2529484-C2 (RU)
Inventor: SHEFER MATTIAS
IPC: C07D333/80
Filed: 2009-04-22
Granted: 2014-09-27
Abstract: FIELD: medicine, pharmaceutics. 
     SUBSTANCE: invention relates to compound of formula (I)  , where ring A is cycloalkane ring with number of members from 3 to 7, benzene ring or monocyclic 5-member or 6-member aromatic heterocyclic ring, containing 1 heteromember of ring, selected from the group, containing N and S, and benzene and heterocyclic rings can optionally have one or two similar or different substituents, selected from the group, containing halogen, HO-, R 1 -O-, H 2 N-C(O)- and NC-; Y is selected from the group, containing S, C(R 12 )=C(R 13 ) and C(R 15 )=N; Z is selected from the group, containing C(R 16 ); R 1 , R 30 , R 33 , R 35 , R 54  and R 55  independently on each other group R 1 , R 30 , R 33 , R 35 , R 54  and R 55  are selected from the group, containing (C 1 -C 6 )-alkyl, (C 2 -C 6 )-alkenyl, (C 3 -C 7 )-cycloalkyl and (C 3 -C 7 )-cycloalkyl-(C 1 -C 4 )-alkyl-, and all of them can optionally have one or more similar or different substituents R 70 ; R 3  and R 5  represent hydrogen; R 4  and R 6  are selected independently on each other, from the group, containing hydrogen and , (C 1 -C 4 )-alkyl; R 12 , R 13 , R 15  and R 16  are selected independently on each other, from the group, containing hydrogen, halogen and O 2 N-; R 20  is selected from the group, containing hydrogen and (C 1 -C 4 )-alkyl; one of the groups R 21  and R 22  is group of formula II: R 24 -R 23 -, and the other of groups R 21  and R 22  is selected from the group, containing hydrogen, halogen, R 30 , HO-, R 30 -O-, R 30 -S(O) m -, H 2 N-, R 30 -NH-, R 30 -N(R 30 )-, R 30 -C(O)- and NC-; R 23  is chain, containing from 1 to 5 chain members of which 0 or 1 chain member is heteromember of chain, selected from the group, containing N(R 25 ), O, S, with other chain members being similar or different groups C(R 26 )(R 26 ), where two adjacent groups can be bound to each other by double bond; R 24  is selected from the group, containing hydrogen, R 31 , R 31 -O-, R 31 -NH-, R 31 -N(R 31 )-, R 31 -C(O)-NH-, HO-C(O)- and monocyclic, bicyclic or tricyclic ring with number of members from 5 to 10, which is saturated or non-saturated and contains 0, 1, 2 or 3 similar or different ring heteromembers, selected from the group, containing N, N(R 32 ), O, S, and ring can optionally have on ring carbon atoms one or 2-3 similar or different substituents, selected from the group, containing halogen, R 33 , R 33 -O-, R 33 -S(O) m -, R 33 -C(O)-NH-, R 33 -S(O) 2 -NH-, R 33 -C(O)-, HO-C(O)-, H 2 N-C(O)-, R 33 -NH-C(O)-, R 33 -N(R 33 )-S(O) 2 -, NC-, oxo, phenyl and Het; on condition that total number of C, N, O and S atoms, present in two groups R 23  and R 24 , constitutes not less than 5; R 25  is selected from the group, containing hydrogen and (C 1 -C 4 )-alkyl; R 26 , independently on each other group R 26 , is selected from the group, containing hydrogen, fluorine, (C 1 -C 4 )-alkyl and HO-, or two groups R 26 , together with included into them chain members, form monocyclic ring with number of members 4, which is saturated and contains 1 ring heteromember, selected from the group, containing O; R 31  is selected from the group, containing (C 1 -C 6 )-alkyl, which can optionally have one substituent R 70 ; R 32  is selected independently on each other, from the group, containing hydrogen, R 35  and phenyl; R 50  is selected from the group, containing R 51 -O- and R 52 -N(R 53 )-; R 51  is selected from the group, containing hydrogen and R 54 ; R 52  is selected from the group, containing hydrogen; R 53  is selected from the group, containing hydrogen; R 70  is selected from the group, containing HO-, R 71 -O-, H 2 N-, R 71 -NH-, R 71 -N(R 71 )-, R 71 -C(O)-NH-, HO-C(O)-, H 2 N-C(O)- and phenyl; R 71 , independently on each other group R 71 , is selected from the group, containing (C 1 -C 4 )-alkyl; Het, independently on each other group Het, is monocyclic heterocyclic ring with number of members 5, which contains 1 or 2 similar or different ring heteromembers, selected from the group, containing N and S, and ring is saturated or non-saturated and optionally substituted with one or more similar or different substituents, selected from the group, containing (C 1 -C 4 )-alkyl; m, independently on each other number m, is integer number, selected from the group, containing 0, 1 and 2; phenyl, independently on each other phenyl group, can optionally have one or more similar or different substituents, selected from the group, containing halogen and (C 1 -C 4 )-alkyl. 
     EFFECT: invention also relates to method of obtaining compound of formula (I) and its application for manufacturing pharmaceutical for inhibiting receptor Edg-2. 
     17 cl, 14 tbl, 362 ex