Discovery of two novel antiplatelet clinical candidates (BMS-986120 and BMS-986141) that antagonize protease-activated receptor 4

ES Priestley, J Banville, D Deon, L Dubé… - Journal of Medicinal …, 2022 - ACS Publications
Protease-activated receptor 4 (PAR4) is a G-protein coupled receptor that is expressed on
human platelets and activated by the coagulation enzyme thrombin. PAR4 plays a key role …

Development of apixaban: a novel anticoagulant for prevention of stroke in patients with atrial fibrillation

MS Hanna, P Mohan, R Knabb, E Gupta… - Annals of the New …, 2014 - Wiley Online Library
The factor Xa inhibitor apixaban is one of the novel anticoagulants to emerge as alternatives
to long‐standing standards of care that include low‐molecular‐weight heparin and warfarin …

Berotralstat (BCX7353): structure-guided design of a potent, selective, and oral plasma kallikrein inhibitor to prevent attacks of hereditary angioedema (HAE)

PL Kotian, M Wu, S Vadlakonda… - Journal of Medicinal …, 2021 - ACS Publications
Hereditary angioedema (HAE) is a rare and potentially life-threatening disease that affects
an estimated 1 in 50 000 individuals worldwide. Until recently, prophylactic HAE treatment …

Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors

ML Quan, PC Wong, C Wang, F Woerner… - Journal of Medicinal …, 2014 - ACS Publications
Antithrombotic agents that are inhibitors of factor XIa (FXIa) have the potential to
demonstrate robust efficacy with a low bleeding risk profile. Herein, we describe a series of …

Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2′ Moiety

Z Hu, PC Wong, PJ Gilligan, W Han… - ACS Medicinal …, 2015 - ACS Publications
Structure–activity relationship optimization of phenylalanine P1′ and P2′ regions with a
phenylimidazole core resulted in a series of potent FXIa inhibitors. Introducing 4 …

From basic science to life-saving therapy: the rationale, and drug discovery efforts that led to the direct factor Xa inhibitor eliquis

RM Knabb, RR Wexler - Journal of Thrombosis and Thrombolysis, 2021 - Springer
Over the past few decades, drug discovery directed at the treatment and prevention of
thromboembolic diseases has been challenged by the need to balance robust efficacy with …

Palladium-Catalyzed C–N Coupling of Pyrazole Amides with Triazolo-and Imidazopyridine Bromides in Ethanol

F Bliss, S Fantasia, E Le Coz… - … Process Research & …, 2021 - ACS Publications
An efficient palladium-catalyzed coupling between a pyrazole amide and a heteroaryl
bromide was developed to enable the streamlined synthesis of a lead candidate for …

[PDF][PDF] Bitter Pills: Why the NHS can't swallow big pharma's profiteering

A Angelis - globaljustice.org.uk
The strain on Britain's National Health Service is plain for all to see. Serious under-
investment, under-staffing, ill-conceived part-privatisation schemes and strategic failure in …

Anticoagulants

ML Quan, PW Glunz… - … Medicinal Chemistry and …, 2003 - Wiley Online Library
Although blood circulation is highly regulated, dysfunctional activities resulting from either
deficient or excessive coagulation have serious health consequences. Insufficient clotting …

[引用][C] Advances in Anticoagulants

ML Quan, PW Glunz, JM Smallheer - 2017 - Elsevier