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Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors

Journal of medicinal chemistry, 2016-09, Vol.59 (17), p.7818-7839

2016

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Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

Journal of medicinal chemistry, 2017-07, Vol.60 (14), p.5990-6017

2017

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Species difference in glucuronidation formation kinetics with a selective mTOR inhibitor

Drug metabolism and disposition, 2014-04, Vol.42 (4), p.707

2014

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Applications of parallel synthetic lead hopping and pharmacophore-based virtual screening in the discovery of efficient glycine receptor potentiators

European journal of medicinal chemistry, 2017-09, Vol.137, p.63-75

2017

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Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity

BMC pharmacology, 2012-05, Vol.12 (1), p.5-5, Article 5

2012

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Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase

Journal of medicinal chemistry, 2008-05, Vol.51 (10), p.2879-2882

2008

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Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

Journal of medicinal chemistry, 2017-07, Vol.60 (14), p.5990-6017

2017

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Relationship between passive permeability, efflux, and predictability of clearance from in vitro metabolic intrinsic clearance

Drug metabolism and disposition, 2010-02, Vol.38 (2), p.223

2010

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Impact of hydrolysis-mediated clearance on the pharmacokinetics of novel anaplastic lymphoma kinase inhibitors

Drug metabolism and disposition, 2013-01, Vol.41 (1), p.238

2013

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Pharmacokinetics and metabolism of [14C]eplerenone after oral administration to humans

Drug metabolism and disposition, 2003-11, Vol.31 (11), p.1448

2003

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Involvement of CYP3A in the metabolism of eplerenone in humans and dogs: differential metabolism by CYP3A4 and CYP3A5

Drug metabolism and disposition, 2002-12, Vol.30 (12), p.1344

2002

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Decomposition of monazite concentrate in sulphuric acid

Canadian metallurgical quarterly, 2018-10, Vol.57 (4), p.422-433

2018

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Sex Differences in Sensitivity to the Depressive-like Effects of the Kappa Opioid Receptor Agonist U-50488 in Rats

Biological psychiatry (1969), 2014-08, Vol.76 (3), p.213-222

2014

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Use of Cryopreserved Hepatocytes as Part of an Integrated Strategy to Characterize In Vivo Clearance for Peptide-Antibody Conjugate Inhibitors of Nav1.7 in Preclinical Species

Drug metabolism and disposition, 2019-10, Vol.47 (10), p.1111-1121

2019

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Discovery of a Potent, Selective, and Orally Bioavailable c-Met Inhibitor: 1-(2-Hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458)

Journal of medicinal chemistry, 2008-07, Vol.51 (13), p.3688-3691

2008

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Identification of a Potent, State-Dependent Inhibitor of Nav1.7 with Oral Efficacy in the Formalin Model of Persistent Pain

Journal of medicinal chemistry, 2011-07, Vol.54 (13), p.4427-4445

2011

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Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective Na V 1.7 Inhibitors

Journal of medicinal chemistry, 2016-09, Vol.59 (17), p.7818-7839

2016

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Use of uptake intrinsic clearance from attached rat hepatocytes to predict hepatic clearance for poorly permeable compounds

Xenobiotica, 2012-09, Vol.42 (9), p.830-840

2012

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Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors

Bioorganic & medicinal chemistry letters, 2009-11, Vol.19 (22), p.6307-6312

2009

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Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors

Bioorganic & medicinal chemistry letters, 2012-06, Vol.22 (12), p.4089-4093

2012

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Abstract 2663: Preclinical pharmacokinetic characterizations and human pharmacokinetic prediction of AMG 900, an orally available small molecule inhibitor of aurora kinases

Cancer research (Chicago, Ill.), 2010-04, Vol.70 (8_Supplement), p.2663-2663

2010

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Species differences in distribution and prediction of human V(ss) from preclinical data

Drug metabolism and disposition, 2011-11, Vol.39 (11), p.2103

2011

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In vitro and in vivo pharmacokinetic characterizations of AMG 900, an orally bioavailable small molecule inhibitor of aurora kinases

Xenobiotica, 2011-05, Vol.41 (5), p.400-408

2011

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N-methylacetamide analog of salvinorin A: a highly potent and selective kappa-opioid receptor agonist with oral efficacy

The Journal of pharmacology and experimental therapeutics, 2008-01, Vol.324 (1), p.188

2008

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Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

Species difference in glucuronidation formation kinetics with a selective mTOR inhibitor

Applications of parallel synthetic lead hopping and pharmacophore-based virtual screening in the discovery of efficient glycine receptor potentiators

Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity

Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase

Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity

Relationship between passive permeability, efflux, and predictability of clearance from in vitro metabolic intrinsic clearance

Impact of hydrolysis-mediated clearance on the pharmacokinetics of novel anaplastic lymphoma kinase inhibitors

Pharmacokinetics and metabolism of [14C]eplerenone after oral administration to humans

Involvement of CYP3A in the metabolism of eplerenone in humans and dogs: differential metabolism by CYP3A4 and CYP3A5

Decomposition of monazite concentrate in sulphuric acid

Sex Differences in Sensitivity to the Depressive-like Effects of the Kappa Opioid Receptor Agonist U-50488 in Rats

Use of Cryopreserved Hepatocytes as Part of an Integrated Strategy to Characterize In Vivo Clearance for Peptide-Antibody Conjugate Inhibitors of Nav1.7 in Preclinical Species

Discovery of a Potent, Selective, and Orally Bioavailable c-Met Inhibitor: 1-(2-Hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458)

Identification of a Potent, State-Dependent Inhibitor of Nav1.7 with Oral Efficacy in the Formalin Model of Persistent Pain

Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective Na V 1.7 Inhibitors

Use of uptake intrinsic clearance from attached rat hepatocytes to predict hepatic clearance for poorly permeable compounds

Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors

Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors

Abstract 2663: Preclinical pharmacokinetic characterizations and human pharmacokinetic prediction of AMG 900, an orally available small molecule inhibitor of aurora kinases

Species differences in distribution and prediction of human V(ss) from preclinical data

Evaluation of a Series of Naphthamides as Potent, Orally Active Vascular Endothelial Growth Factor Receptor-2 Tyrosine Kinase Inhibitors

In vitro and in vivo pharmacokinetic characterizations of AMG 900, an orally bioavailable small molecule inhibitor of aurora kinases

N-methylacetamide analog of salvinorin A: a highly potent and selective kappa-opioid receptor agonist with oral efficacy

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