Tricyclic pyridyl-vinyl pyrroles as PAR1 inhibitors

摘要

This disclosure relates to compounds of formula I:;
wherein R1, R2, R3, R4, X and Y have the meanings denoted in the disclosure. The compounds of formula I have antithrombotic activity and in particular inhibit the protease-activated receptor 1 (PAR1). The disclosure further relates to a method for producing the compound of formula I and to the use thereof as a pharmaceutical product.

主权项

1. A compound of formula I or a physiologically acceptable salt of the compound of formula I, where R1 and R2 are identical or different and are independently of one another hydrogen, —(C1-C6)-alkyl, —O—(C1-C6)-alkyl, aryl, halogen or hetaryl, where alkyl, aryl and hetaryl are in each case unsubstituted or mono-, di- or trisubstituted independently of one another by F, Cl, Br, CN, —(C1-C4)-alkyl, —NH—(C1-C4)-alkyl, —N((C1-C4)-alkyl)2, —NH2, —OH, —O—CF3, —S—CF3 or —CF3, or R3 and R4 together with the ring atoms to which they are respectively attached form a saturated or unsaturated 5-membered to 7-membered ring, where the ring consists only of carbon atoms except for the nitrogen atom which carries the group R3, or 1 or 2 of these carbon atoms are replaced by 0, S, SO, SO2 or N—R5, where the ring is unsubstituted or mono-, di- or trisubstituted independently of one another by F, Cl, —OH, —NH—R7, —(C1-C4)-alkyl, —O—(C1-C4)-alkyl, C(O)—O—(C1-C4)-alkyl, aryl or hetaryl; X is N—R6; Y is C(O), CH2, CH—CH3 or C(CH3)2; R5 is hydrogen, —C(O)—(C1-C4)-alkyl, —C(O)—O—(C1-C4)-alkyl, —(C1-C6)-alkyl, —(C2-C4)-alkyl-O—(C1-C4)-alkyl, —(C2-C4)-alkyl-OH, aryl or hetaryl; R7 is hydrogen, —C(O)—(C1-C4)-alkyl, —C(O)—O—(C1-C4)-alkyl, —(C1-C6)-alkyl, —(C2-C4)-alkyl-O—(C1-C4)-alkyl, —(C2-C4)-alkyl-OH, aryl or hetaryl; and R6 is hydrogen, —(C1-C6)-alkyl, —(C3-C7)-cycloalkyl, —(C1-C4)-alkylene-aryl or C(O)—O—(C1-C4)-alkyl.