Synthesis and Evaluation of 1-Arylsulfonyl-3-piperazinone Derivatives as Factor Xa Inhibitors^<1-4)> V. A Series of New Derivatives Containing a Spiro [imidazo [1,2-a] pyrazine-2(3H),4'-piperidin]-5(1H)-one Scaffold

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We have already reported unique compounds containing a N,O-spiro acetal structure as an orally active factor Xa (FXa) inhibitor. This time, we described a N,N-spiro acetal structure as an analogue of the N,O-spiro acetal structure for an orally active FXa inhibitor. The synthesis of these analogues could be achieved in a similar fashion to the N,O-spiro acetal synthesis. Consequently, FXa inhibitory activity was increased and more active compounds could be found (M58163: IC_<50>=0.61nM, M58169: IC_<50>=0.58nM). Additionally, the absolute configuration could be determined by X-ray crystallography analysis (M58169: (R)-config.).
2006-11-01