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Drug Annotations Series Change in Guidelines

Journal of medicinal chemistry, 2019-03, Vol.62 (5), p.2217-2217

2019

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Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine

Bioorganic & medicinal chemistry letters, 2016-07, Vol.26 (13), p.3207-3211

2016

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Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine

Bioorganic & medicinal chemistry letters, 2016-07, Vol.26 (13), p.3202-3206

2016

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Novel short-acting A2A adenosine receptor agonists for coronary vasodilation: inverse relationship between affinity and duration of action of A2A agonists

The Journal of pharmacology and experimental therapeutics, 2001-07, Vol.298 (1), p.209

2001

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CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability

Bioorganic & medicinal chemistry letters, 2004-12, Vol.14 (24), p.6017-6021

2004

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Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor

Bioorganic & medicinal chemistry letters, 2002-10, Vol.12 (20), p.2935-2939

2002

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Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents

Bioorganic & medicinal chemistry letters, 2004-07, Vol.14 (14), p.3793-3797

2004

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Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor: efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)

Bioorganic & medicinal chemistry letters, 2004-01, Vol.14 (2), p.535-539

2004

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Partial A(1) adenosine receptor agonists from a molecular perspective and their potential use as chronic ventricular rate control agents during atrial fibrillation (AF)

Current topics in medicinal chemistry, 2004, Vol.4 (8), p.839

2004

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A1 adenosine receptor agonists and their potential therapeutic applications

Expert opinion on investigational drugs, 2008-12, Vol.17 (12), p.1901-1910

2008

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A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias

The Journal of pharmacology and experimental therapeutics, 2013-01, Vol.344 (1), p.23

2013

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Discovery of the pan-genotypic hepatitis C virus NS3/4A protease inhibitor voxilaprevir (GS-9857): A component of Vosevi

Bioorganic & medicinal chemistry letters, 2019-08, Vol.29 (16), p.2428-2436

2019

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Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B

Journal of medicinal chemistry, 2020-09, Vol.63 (18), p.10188-10203

2020

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The Drug Annotations Series

Journal of medicinal chemistry, 2013-09, Vol.56 (17), p.6541-6541

2013

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Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency

Bioorganic & medicinal chemistry letters, 2016-12, Vol.26 (24), p.5926-5930

2016

Volltextzugriff (PDF)

A1 adenosine receptor antagonists, agonists, and allosteric enhancers

Handbook of experimental pharmacology, 2009 (193), p.25

2009

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The novel late Na+ current inhibitor, GS‐6615 (eleclazine) and its anti‐arrhythmic effects in rabbit isolated heart preparations

British journal of pharmacology, 2016-11, Vol.173 (21), p.3088-3098

2016

Volltextzugriff (PDF)

How Can Rates of Prostate-Specific Antigen Screening Be Reduced in Men Aged 80 and Older?

Journal of the American Geriatrics Society (JAGS), 2010-04, Vol.58 (4), p.757-759

2010

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Inhibition of aldehyde dehydrogenase-2 suppresses cocaine seeking by generating THP, a cocaine use-dependent inhibitor of dopamine synthesis

Nature Medicine, 2010-09, Vol.16 (9), p.1024-1028

2010

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Discovery of a Novel A2B Adenosine Receptor Antagonist as a Clinical Candidate for Chronic Inflammatory Airway Diseases

Journal of medicinal chemistry, 2008-04, Vol.51 (7), p.2267-2278

2008

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Marked difference in saxitoxin and tetrodotoxin affinity for the human nociceptive voltage-gated sodium channel (Nav1.7)

Proceedings of the National Academy of Sciences - PNAS, 2012-10, Vol.109 (44), p.18102-18107

2012

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Suppression of Heavy Drinking and Alcohol Seeking by a Selective ALDH-2 Inhibitor

Alcoholism, clinical and experimental research, 2009-11, Vol.33 (11), p.1935-1944

2009

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Characterization of the potency, selectivity, and pharmacokinetic profile for six adenosine A2A receptor antagonists

Naunyn-Schmiedeberg's archives of pharmacology, 2007-04, Vol.375 (2), p.133-144

2007

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Selective, high affinity A(2B) adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines

Bioorganic & medicinal chemistry letters, 2008-02, Vol.18 (4), p.1397-1401

2008

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Drug Annotations Series Change in Guidelines

Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine

Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine

Novel short-acting A2A adenosine receptor agonists for coronary vasodilation: inverse relationship between affinity and duration of action of A2A agonists

CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability

Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor

Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents

Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor: efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)

Partial A(1) adenosine receptor agonists from a molecular perspective and their potential use as chronic ventricular rate control agents during atrial fibrillation (AF)

A1 adenosine receptor agonists and their potential therapeutic applications

A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias

Discovery of the pan-genotypic hepatitis C virus NS3/4A protease inhibitor voxilaprevir (GS-9857): A component of Vosevi

Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B

The Drug Annotations Series

Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency

A1 adenosine receptor antagonists, agonists, and allosteric enhancers

The novel late Na+ current inhibitor, GS‐6615 (eleclazine) and its anti‐arrhythmic effects in rabbit isolated heart preparations

How Can Rates of Prostate-Specific Antigen Screening Be Reduced in Men Aged 80 and Older?

Inhibition of aldehyde dehydrogenase-2 suppresses cocaine seeking by generating THP, a cocaine use-dependent inhibitor of dopamine synthesis

Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor

Discovery of a Novel A2B Adenosine Receptor Antagonist as a Clinical Candidate for Chronic Inflammatory Airway Diseases

Marked difference in saxitoxin and tetrodotoxin affinity for the human nociceptive voltage-gated sodium channel (Nav1.7)

Suppression of Heavy Drinking and Alcohol Seeking by a Selective ALDH-2 Inhibitor

Characterization of the potency, selectivity, and pharmacokinetic profile for six adenosine A2A receptor antagonists

Selective, high affinity A(2B) adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines

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