Thrombosis is the underlying cause of a host of common, debilitating, and often fatal
cardiovascular disorders. Formation of thrombi in the arterial circulation can lead to acute …

Thrombosis is a leading cause of death in cardiovascular diseases such as myocardial
infarction (MI), unstable angina and acute coronary syndrome (ACS) in the industrialized …

The accurate prediction of protein–ligand binding free energies remains a significant
challenge of central importance in computational biophysics and structure-based drug …

The global need for clean manufacturing technologies and the management of hazardous
chemicals and waste present new research challenges to both chemistry and biotechnology …

The asymmetric ring-opening of meso-aziridines with primary alcohols is realized using an
N, N′-dioxide–Mg (OTf) 2 complex as the catalyst. The desired vicinal trans-β-amino ethers …

Despite extensive research on small molecule thrombin inhibitors for oral application in the
past decades, only a single double prodrug with very modest oral bioavailability has …

Previously, we identified cyclohexane diamine derivative 1 as orally bioavailable factor Xa
inhibitor. We have investigated two racemic cis-piperidine diamine derivatives 2 and 3 …

Chiral cyclic β-amino alcohols are vital building blocks for the synthesis of numerous
pharmaceuticals and bioactive molecules. Asymmetric ring-opening of cyclic meso-epoxides …

Thromboembolic diseases are the leading causes of morbidity and mortality in the
developed world. Anticoagulants provide effective treatment for venous or arterial …

In the early 1990's, we reported on the low-molecular selective fXa inhibitor DX-9065a
having two amidino groups. However, it had poor oral bioavailability due to its strong basic …