1201686-93-2Relevant articles and documents
Discovery of AZD8165 - A clinical candidate from a novel series of neutral thrombin inhibitors
Abrahamsson,Andersson,Bergman,Bredberg,Br?nalt,Egnell,Eriksson,Gustafsson,Hoffman,Nielsen,Nilsson,Pehrsson,Polla,Skjaeret,Strimfors,Wern,?lweg?rd-Halvarsson,?rtengren
, p. 272 - 281 (2016/03/01)
A novel series of neutral thrombin inhibitors has been developed using a selection process based on docking experiments and property calculations and predictions. This work resulted in the identification of the highly potent thrombin inhibitor compound 85 (Ki = 300 pM) and the corresponding propionate prodrug 5 (AZD8165) as a candidate for clinical evaluation in the treatment of thrombosis and related diseases. AZD8165 was found to be safe and well tolerated and delivered the expected pharmacological response in a phase I trial in healthy male volunteers.
Novel Compounds 148
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Page/Page column 30-31, (2009/12/28)
This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containi
