abstract |
REFERS TO FORMULA I TRICYCLIC COMPOUNDS, WHERE THE SIMPLE DOTTED LINE REPRESENTS AN OPTIONAL SINGLE LINK; ......... REPRESENTS AN OPTIONAL DOUBLE LINK; n IS 0 A 2; Q IS (a), (b), AMONG OTHERS; R1 AND R2 ARE H, ALKYL (C1-C6), MONO, DI, OR TRI-FLUOROALKYL- (C1-C6 -) -, ALKENYL (C2-C6), CYCLOALKYL (C3-C6), AMONG OTHERS; R3 IS H, OH, (C1-C6) ALKYL, (C1-C6) ALCOXY, HALOGEN, -S0R16, AMONG OTHERS; Het IS A MONO OR BI-CYCLIC HETEROARYL OF 5 TO 10 ATOMS WITH 1 TO 4 HETEROATOMS OF N, OYS, WHERE AN N OF THE RING CAN FORM AN N-OXIDE OR QUATERNARY GROUP WITH AN ALKYL (C1-C4) AND Het CAN BE UNITED TO AB THROUGH A C OF THE RING, WHERE Het IS REPLACED BY W; R8, R10 AND R11 ARE R1 AND -OR1, AS LONG AS THE DOUBLE LINK IS PRESENT, R10 IS ABSENT; B IS - (CH2) n3, CIS OR TRANS - (CH2) n4CR12 = CR12a (CH2) n5- O - (CH2) n4C ° C (CH2) n5-, WHERE n3 IS O A 5; n4 AND n5 ARE O A 2; X IS -O- OR -NR6- WHEN THE LINE REPRESENTS A SIMPLE LINK OR IS -OH OR -NHR20 IF THE LINK IS ABSENT; AND IS = O, = S, (H, HO OH) O (H, ALCOXI (C1-C6)), IF THE DOTTED LINE IS A SIMPLE LINK, OR IF IT IS ABSENT AND IS = O, AMONG OTHER SUBSTITUTES. THESE COMPOUNDS ARE ANTAGONISTS OF THROMBIN RECEPTORS AND MAY BE USEFUL FOR THE TREATMENT OF THROMBOTIC, INFLAMMATORY, ATHEROSCLEROTIC AND FIBROPROLIFERATIVE DISORDERS. ALSO REFERS TO PHARMACEUTICAL COMPOSITIONS IN COMBINATION WITH AN ADDITIONAL CARDIOVASCULAR AGENT SUCH AS ASPIRIN OR CLOPRIDROGEL |