From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3
摘要:
Highly potent and selective substrate analogue factor Xa inhibitors were obtained by incorporation of non-basic or modestly basic PI residues known from the development of thrombin inhibitors. The modification of the P2 and P3 amino acids strongly influenced the selectivity and provided potent dual factor Xa and thrombin inhibitors without affecting the fibrinolytic enzymes. Several inhibitors demonstrated excellent anticoagulant efficacy in standard clotting assays in human plasma. (c) 2007 Elsevier Ltd. All rights reserved.
Compounds are provided which are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.
Substituted Dihydroquinazolines as Platelet ADP Receptor Inhibitors
申请人:Scarborough Robert M.
公开号:US20110098247A1
公开(公告)日:2011-04-28
Compounds of formula I are provided:
wherein Ar
1
and Ar
2
are substituted aromatic rings and L
1
and L
2
are independent divalent linking groups. The compounds are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.