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 …

Novel factor Xa inhibitors: a patent review

M De Candia, G Lopopolo… - Expert opinion on …, 2009 - Taylor & Francis
Importance of the field. New oral anticoagulants with favorable safety profiles and fixed
doses are required for the management of thromboembolism and stroke prevention in …

3,4-Dihydro-2H-1,4-benzoxazine Derivatives Combining Thrombin Inhibitory and Glycoprotein IIb/IIIa Receptor Antagonistic Activity as a Novel Class of …

J Ilaš, Z Jakopin, T Borštnar… - Journal of medicinal …, 2008 - ACS Publications
3, 4-Dihydro-2 H-1, 4-benzoxazine derivatives possessing both thrombin inhibitory and
glycoprotein IIb/IIIa (GPIIb/IIIa) receptor antagonistic activities were obtained by combining …

Discovery of a Tetrahydropyrimidin-2(1H)-one Derivative (TAK-442) as a Potent, Selective, and Orally Active Factor Xa Inhibitor

T Fujimoto, Y Imaeda, N Konishi, K Hiroe… - Journal of medicinal …, 2010 - ACS Publications
Coagulation enzyme factor Xa (FXa) is a particularly promising target for the development of
new anticoagulant agents. We previously reported the imidazo [1, 5-c] imidazol-3-one …

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 …

Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit

KG Zbinden, L Anselm, DW Banner, J Benz… - European journal of …, 2009 - Elsevier
Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit - ScienceDirect
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Design, synthesis, and SAR of cis-1, 2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part II: Exploration of 6–6 fused rings as alternative S1 moieties

K Yoshikawa, S Kobayashi, Y Nakamoto… - Bioorganic & medicinal …, 2009 - Elsevier
A series of cis-1, 2-diaminocyclohexane derivatives possessing a 6–6 fused ring for the S1
moiety were synthesized as novel factor Xa (fXa) inhibitors. The synthesis, structure–activity …

The Discovery of (2R,4R)‐N‐(4‐chlorophenyl)‐N‐ (2‐fluoro‐4‐(2‐oxopyridin‐1(2H)‐yl)phenyl)‐4‐methoxypyrrolidine‐1,2‐dicarboxamide (PD 0348292), an Orally …

JT Kohrt, CF Bigge, JW Bryant… - Chemical Biology & …, 2007 - Wiley Online Library
Herein, we report the discovery of novel, proline‐based factor Xa inhibitors containing a
neutral P1 chlorophenyl pharmacophore. Through the additional incorporation of 1‐(4 …

Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores

U Trstenjak, J Ilaš, D Kikelj - European Journal of Medicinal Chemistry, 2013 - Elsevier
Dual antithrombotic agents acting as anticoagulants and aggregation inhibitors could have
substantial advantages over currently prescribed combinations of antithrombotic drugs …

Design, synthesis, and SAR of cis-1, 2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part I: Exploration of 5–6 fused rings as alternative S1 moieties

K Yoshikawa, A Yokomizo, H Naito, N Haginoya… - Bioorganic & medicinal …, 2009 - Elsevier
A series of cis-1, 2-diaminocyclohexane derivatives were synthesized with the aim of
optimizing previously disclosed factor Xa (fXa) inhibitors. The exploration of 5–6 fused rings …