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 …
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
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 …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
deficient or excessive coagulation have serious health consequences. Insufficient clotting …