Patent RU-2329264-C2 (RU)
Title: Tricyclic antagonists of thrombin receptors
Inventor: CHAKALAMANNIL SEHMJUEHL
IPC: A61K31/443
Filed: 2003-04-14
Granted: 2008-07-20
Abstract: 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   ,  R 1  denotes H, R 2  represents H or alkyl with 1-6 carbon atoms, R 3  represents H, hydroxy-group, -NR 22 R 23 , 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, R 21 -aryl and P 21 -heteroaryl, R 4  and R 5  are independently selected from the group containing H and alkyl with 1 - 6 carbon atoms, R 7 , R 8 , R 10  and R 11  denote R 1 , R 9  represent H, B represents -(CH 2 ) n3 -. cis- or trans -(CH 2 ) n4 CR 12 =CR 12a (CH 2 ) n5  or -(CH 2 ) n4 C=C(CH 2 ) n5 , where n 3  denotes 0-5, n 4  and n 5  independently denote 0-2, and R 12  and R 12a  denote H, X represents -O-, Y represents =O, each R 13  is independently selected from the group containing H, alkyl with 1-6 carbon atoms, -(CH 2 ) n6 NHC(O)OR 16b , -(CH 2 ) n6 NHC(O)R 16b , -(CH 2 ) n6 NHC(O)NR 4 R 5 , -(CH 2 ) n6 NHSO 2 R 16 , and -(CH 2 ) n6 C(O)NR 28 R 29 , where n 6  denotes 0, each R 14  is independently selected from the group containing H, alkyl with 1-6 carbon atoms, -(CH 2 ) n6 NHC(O)OR 16b , -(CH 2 ) n6 NHC(O)R 16b , -(CH 2 ) n6 NHC(O)NR 4 R 5 , -(CH 2 ) n6 NHSO 2 R 16  and -(CH 2 ) n6 C(O)NR 28 R 29 , where n 6  denotes 0, where, at least one of R 13  and R 14  is chosen from the group containing -(CH 2 ) n6 NHC(O)OR 16b , -(CH 2 ) n6 NHC(O)R 16b , -(CH 2 ) n6 NHC(O)NR 4 R 5 , -(CH 2 ) n6 NHSO 2 R 16  and -(CH 2 ) n6 C(O)NR 28 R 29 , where n 6  denotes 0, R 16  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)-, R 22 -O-C(O)-(an alkyl with 1 - 6 carbon atoms)-, a cycloalkyl with 3-6 carbon atoms, R 21  represents from 1 to 3 substitutes, which are independently selected from a group comprising of H, -CN, -CF 3 , halogen, alkyl with 1 - 6 carbon atoms, -OH, alkoxy- group with 1 - 6 carbon atoms, -C(O)NR 25 R 26  and -SR 13 , R 22  represents H or an alkyl with 1-6 carbon atoms, R 23  represents H, R 25  and R 26  are independently selected from a group comprising of H and an alkyl with 1 - 6 carbon atoms, and R 28  and R 29  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