Factor Xa inhibitors: next-generation antithrombotic agents

DJP Pinto, JM Smallheer, DL Cheney… - Journal of medicinal …, 2010 - ACS Publications
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 …

Contemporary developments in the discovery of selective factor Xa inhibitors: A review

NR Patel, DV Patel, PR Murumkar, MR Yadav - European journal of …, 2016 - Elsevier
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 …

Accurate modeling of scaffold hopping transformations in drug discovery

L Wang, Y Deng, Y Wu, B Kim, DN LeBard… - Journal of chemical …, 2017 - ACS Publications
The accurate prediction of protein–ligand binding free energies remains a significant
challenge of central importance in computational biophysics and structure-based drug …

Biocatalytic approaches towards the stereoselective synthesis of vicinal amino alcohols

P Gupta, N Mahajan - New Journal of Chemistry, 2018 - pubs.rsc.org
The global need for clean manufacturing technologies and the management of hazardous
chemicals and waste present new research challenges to both chemistry and biotechnology …

Chiral magnesium (II)-catalyzed asymmetric ring-opening of meso-aziridines with primary alcohols

J Li, Y Liao, Y Zhang, X Liu, L Lin, X Feng - Chemical communications, 2014 - pubs.rsc.org
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 …

Design, synthesis, and pharmacological characterization of a neutral, non-prodrug thrombin inhibitor with good oral pharmacokinetics

A Hillisch, KM Gericke, S Allerheiligen… - Journal of Medicinal …, 2020 - ACS Publications
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 …

Design, synthesis, and biological activity of piperidine diamine derivatives as factor Xa inhibitor

A Mochizuki, Y Nakamoto, H Naito, K Uoto… - Bioorganic & medicinal …, 2008 - Elsevier
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 …

Biocatalytic asymmetric ring-opening of meso-epoxides to enantiopure cyclic trans-β-amino alcohols involving a key amine transaminase

J Zhang, H Gao, L Gao, M Chen, S Huang, J Zhang - Green Chemistry, 2024 - pubs.rsc.org
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 …

Developments in factor Xa inhibitors for the treatment of thromboembolic disorders

YK Lee, MR Player - Medicinal Research Reviews, 2011 - Wiley Online Library
Thromboembolic diseases are the leading causes of morbidity and mortality in the
developed world. Anticoagulants provide effective treatment for venous or arterial …

Discovery of N-[(1R, 2S, 5S)-2-{[(5-chloroindol-2-yl) carbonyl] amino}-5-(dimethylcarbamoyl) cyclohexyl]-5-methyl-4, 5, 6, 7-tetrahydrothiazolo [5, 4-c] pyridine-2 …

T Nagata, T Yoshino, N Haginoya, K Yoshikawa… - Bioorganic & medicinal …, 2009 - Elsevier
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 …