570398-75-3Relevant academic research and scientific papers
Oxygenated analogues of UK-396082 as inhibitors of activated thrombin activatable fibrinolysis inhibitor
Owen, Dafydd R.,Bull, David J.,Bunnage, Mark E.,Glossop, Melanie S.,Maguire, Robert J.,Strang, Ross S.
scheme or table, p. 92 - 96 (2010/04/24)
A suitable inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa) has the potential to be a novel treatment for thrombosis. The TAFIa inhibitor UK-396082 (1) was used as a starting point to seek more potent analogues. With knowledge of encouraging human pharmacokinetics and toleration for the clinical candidate (1), the programme continued to seek structure-activity relationships (SAR) that could positively impact on both potency and half-life, and therefore the projected dose of any future nominated clinical agent. A series of oxygenated analogues based on compound 1 were prepared to evaluate changes in pharmacology, selectivity and pharmacokinetics.
3-(Imidazolyl)-2-alkoxypropanoic acids
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, (2008/06/13)
Compounds according to formula (I) wherein n is 0-3, R1 is optionally substituted C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl, Heterocycle, Aromatic heterocycle, Aryl or hydrogen and R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from hydrogen and optionally substituted C1-6 alkyl, or R5 and R8 are an alkylene chain, are novel. They are useful in the treatment of thrombotic conditions and other pathologies associated with fibrin deposition.
