| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: tricyclic bonds are substituted with heterocyclic ones, which have the formula (I), or its pharmaceutically acceptable salt or solvate in which: n denotes 0-2; Q denotes , R1 denotes H, R2 represents H or alkyl with 1-6 carbon atoms, R3 represents H, hydroxy-group, -NR22R23, Het denotes mono- or bycyclic heteroaryl group from 5 - 10 atoms, containing from 1 to 9 carbon atoms and 1 heteroatom N, where Het bonds with B through the cyclic carbon atom, and the group Het has a substitute W. W consists of from 1 to 4 substitutes, independently selected from the group containing H, halogen, R21-aryl and P21-heteroaryl, R4 and R5 are independently selected from the group containing H and alkyl with 1 - 6 carbon atoms, R7, R8, R10 and R11 denote R1, R9 represent H, B represents -(CH2)n3-. cis- or trans -(CH2)n4CR12=CR12a(CH2)n5 or -(CH2)n4C=C(CH2)n5, where n3 denotes 0-5, n4 and n5 independently denote 0-2, and R12 and R12a denote H, X represents -O-, Y represents =O, each R13 is independently selected from the group containing H, alkyl with 1-6 carbon atoms, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16, and -(CH2)n6C(O)NR28R29, where n6 denotes 0, each R14 is independently selected from the group containing H, alkyl with 1-6 carbon atoms, -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16 and -(CH2)n6C(O)NR28R29, where n6 denotes 0, where, at least one of R13 and R14 is chosen from the group containing -(CH2)n6NHC(O)OR16b, -(CH2)n6NHC(O)R16b, -(CH2)n6NHC(O)NR4R5, -(CH2)n6NHSO2R16 and -(CH2)n6C(O)NR28R29, where n6 denotes 0, R16 represents an alkyl with 1-6 carbon atoms, R16b represents H, an alkyl with 1-6 carbonatoms, (an alkoxy with 1-6 carbon atoms)-(an alkyl with 1 - 6 carbon atoms)-, R22-O-C(O)-(an alkyl with 1 - 6 carbon atoms)-, a cycloalkyl with 3-6 carbon atoms, R21 represents from 1 to 3 substitutes, which are independently selected from a group comprising of H, -CN, -CF3, halogen, alkyl with 1 - 6 carbon atoms, -OH, alkoxy- group with 1 - 6 carbon atoms, -C(O)NR25R26 and -SR13, R22 represents H or an alkyl with 1-6 carbon atoms, R23 represents H, R25 and R26 are independently selected from a group comprising of H and an alkyl with 1 - 6 carbon atoms, and R28 and R29 are independently selected from a group comprising of H, an alkyl with 1 - 6 carbon atoms, heteroaryl, heterocyclil and also a pharmaceutical composition, containing these bonds. ^ EFFECT: application for getting medication for the treatment of diseases related to thrombosis, atherosclerosis, restenosis, hypertension, sternocardia, arrythmia, cardiac insufficiency and cancer, the way of administering is specified in the bonds Also therapy in combination with other cardiovascular agents is allowed. ^ 23 cl, 7 tbl, 92 ex |
