TRICYCLIC ANTAGONISTS OF THROMBIN RECEPTORS Russian patent published in 2008 - IPC C07D405/06 C07D405/14 A61K31/443 A61P7/02 A61P9/00 A61P35/00 

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=CR^12a(CH₂)_n5 or -(CH₂)_n4C=C(CH₂)_n5, where n₃ denotes 0-5, n₄ and n₅ independently denote 0-2, and R¹² and R^12a 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)OR^16b, -(CH₂)_n6NHC(O)R^16b, -(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)OR^16b, -(CH₂)_n6NHC(O)R^16b, -(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)OR^16b, -(CH₂)_n6NHC(O)R^16b, -(CH₂)_n6NHC(O)NR⁴R⁵, -(CH₂)_n6NHSO₂R¹⁶ and -(CH₂)_n6C(O)NR²⁸R²⁹, where n₆ denotes 0, R¹⁶ represents an alkyl with 1-6 carbon atoms, R^16b 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