Discovery of AZD8165 – a clinical candidate from a novel series of neutral thrombin inhibitors
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U. Bredberg | J. Bergman | S. Pehrsson | I. Nilsson | U. Eriksson | D. Gustafsson | M. Strimfors | A. Egnell | P. Andersson | S. Nielsen | M. Polla | T. Skjaeret | C. Wern | J. Bran̊alt | K. Abrahamsson | M. Ölwegård-Halvarsson | K.-J. Hoffman | Y. Örtengren | Joakim Bergman | J. Brånalt
[1] Staffan Karlsson,et al. A One-Pot Asymmetric Synthesis of a N-Acylated 4,5-Dihydropyrazole, A Key Intermediate of Thrombin Inhibitor AZD8165 , 2014 .
[2] H. Zachrisson,et al. Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations. , 2014, Bioorganic & medicinal chemistry letters.
[3] Alexander Parkhomenko,et al. Comparison of the efficacy and safety of new oral anticoagulants with warfarin in patients with atrial fibrillation: a meta-analysis of randomised trials , 2014, The Lancet.
[4] Alexander Hillisch,et al. Oral, direct thrombin and factor Xa inhibitors: the replacement for warfarin, leeches, and pig intestines? , 2011, Angewandte Chemie.
[5] S. Pehrsson,et al. Evaluation of AR-H067637, the active metabolite of the new direct thrombin inhibitor AZD0837, in models of venous and arterial thrombosis and bleeding in anaesthetised rats , 2010, Thrombosis and Haemostasis.
[6] B. Tomczuk,et al. Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif. , 2010, Journal of medicinal chemistry.
[7] Bengt I Eriksson,et al. Population pharmacokinetics and pharmacodynamics of once and twice-daily rivaroxaban for the prevention of venous thromboembolism in patients undergoing total hip replacement , 2008, Thrombosis and Haemostasis.
[8] V. Matassa,et al. Design and Discovery of Novel, Potent Pyrazinone-Based Thrombin Inhibitors with a Solubilizing P1-P2-Linker , 2006 .
[9] Udo E W Lange,et al. Orally active thrombin inhibitors. Part 2: optimization of the P2-moiety. , 2006, Bioorganic & medicinal chemistry letters.
[10] B. Eriksson,et al. Pharmacokinetic Profile of the Oral Direct Thrombin Inhibitor Dabigatran Etexilate in Healthy Volunteers and Patients Undergoing Total Hip Replacement , 2005, Journal of clinical pharmacology.
[11] Lawrence C Kuo,et al. Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors. , 2004, Journal of medicinal chemistry.
[12] C. Lindemann,et al. Influence of physicochemical properties and intestinal region on the absorption of 3-fluoro-2-pyrimidylmethyl 3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide, a water insoluble thrombin inhibitor, in dogs. , 2004, International journal of pharmaceutics.
[13] N. Bunnett,et al. Protease-activated receptors: contribution to physiology and disease. , 2004, Physiological reviews.
[14] Youwei Yan,et al. Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides. , 2003, Bioorganic & medicinal chemistry letters.
[15] U. Bredberg,et al. Absorption, distribution, metabolism, and excretion of ximelagatran, an oral direct thrombin inhibitor, in rats, dogs, and humans. , 2003, Drug metabolism and disposition: the biological fate of chemicals.
[16] Youwei Yan,et al. Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'. , 2003, Bioorganic & medicinal chemistry letters.
[17] H. Nar,et al. Structure-based design of novel potent nonpeptide thrombin inhibitors. , 2002, Journal of medicinal chemistry.
[18] M. Nishida,et al. The protease-activated receptor-2 agonist induces gastric mucus secretion and mucosal cytoprotection. , 2001, The Journal of clinical investigation.
[19] C. Masimirembwa,et al. In vitro high throughput screening of compounds for favorable metabolic properties in drug discovery. , 2001, Combinatorial chemistry & high throughput screening.
[20] A Abrahamsson,et al. The direct thrombin inhibitor melagatran and its oral prodrug H 376/95: intestinal absorption properties, biochemical and pharmacodynamic effects. , 2001, Thrombosis research.
[21] C. Masimirembwa,et al. Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. , 2001, Drug metabolism and disposition: the biological fate of chemicals.
[22] S. Lee,et al. Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption. , 1999, Bioorganic & medicinal chemistry letters.
[23] S. Brady,et al. Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position. , 1998, Journal of medicinal chemistry.
[24] S. Brady,et al. Design of novel, potent, noncovalent inhibitors of thrombin with nonbasic P-1 substructures: rapid structure-activity studies by solid-phase synthesis. , 1998, Journal of medicinal chemistry.