449756-95-0Relevant articles and documents
PLASMA KALLIKREIN INHIBITORS AND USES THEREOF
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Paragraph 0692; 0696, (2021/03/19)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
A one-pot asymmetric synthesis of a N-acylated 4,5-dihydropyrazole, a key intermediate of thrombin inhibitor AZD8165
Karlsson, Staffan,Branalt, Jonas,Oelwegard Halvarsson, Maria,Bergman, Joakim
, p. 969 - 975 (2014/11/08)
A short, chromatography-free, and scalable synthetic route to thrombin inhibitor 1, the active metabolite of the propionic ester prodrug AZD8165, has been developed. The key synthetic step involved cycloaddition of TMS-diazomethane and ethyl acrylate to give an intermediate racemic dihydropyrazole which was reacted with enantiomerically pure 4-fluoro mandelic acid chloride in a one-pot dynamic kinetic resolution (DKR) process.
Thrombin inhibitors
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, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: wherein R1 is, for example, hydrogen, Cl, or cyano, and R2 is, for example, hydrogen,