| 摘要 |
In formula I: X is S, or an NR3 group, wherein R3 is H, (C1-6)alkyl, (C1-6)acyl, aryl, aryl-(C1-6)alkyl or heteroaryl-(C1-6)alkyl group; Y is O, T is CH or N when the bond that links it is a single bond, or a carbon atom if the bond is a double bond; A is a single bond or an optionally substituted (C1-6)alkylene, arylene, cycloalkylene, heterocycloalkylene, heteroarylene or an SO2R4 group, where R4 is (C1-6)alkylene, arylene, aryl-(C1-6)alkylene, cycloalkylene, heterocycloalkylene and heteroarylene; W is hydroxy, (C1-6)alkyoxy, aryloxy, aryl-(C1-6)alkyoxy, cycloalkoxy, heterocyloalkyoxy, heteraryloxy, amino and hydroxyamino; U1 is O, S or optionally substituted (C1-6)alkylene, wherein one or more of the carbon atoms may be optionally replaced by one or more hetero atoms selected from O, N and S; V1 is arylene, heteroarylene or heterocycloalkylene, U2 is a single bond, SO2, O, N or S, or an optionally substituted (C1-6)alkylene, wherein one or more of the carbon atoms may be optionally replaced by one or more hetero atoms selected from O, N and S; V2 is aryl, heteoaryl or heterocycloalkyl group; Ra, Rb and Rc are identical or different and represent a group selected from: - H, halogen; - hydroxy, cyano, nitro; - (C1-6)alkyl, (C1-6)alkoxy, (C1-6)acyl, carboxy, (C1-6)alkoxycarbonyl, (C1-6)trihaloalkyl; - optionally substituted amino; - aryloxy, aryl-(C1-6)alkoxy, heteroaryloxy, heteroaryl-(C1-6)alkoxy; - -U1-V1-U2-V2 (where U1, U2, V1 and V2 are as defined above); or - two of Ra, Rb and Rc together form an optionally substituted methylenedioxy or ethylenedioxy group, R1 is an optionally substituted phenyl, quinolyl or pridyl; and R2 is H, aryl or heteroaryl. The compounds of formula I may be used in pharmaceutical compositions for use as inhibitors of PAI-1, and to treat thrombosis and associated pathologies.
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