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Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (nN → σS–X) Interaction for Conformational Constraint

Journal of medicinal chemistry, 2015-12, Vol.58 (24), p.9663-9679

2015

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2-(S)-Phenethylaminothiazolones as Potent, Orally Efficacious Inhibitors of 11β-Hydroxysteriod Dehydrogenase Type 1

Journal of medicinal chemistry, 2007-02, Vol.50 (3), p.429-432

2007

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Discovery of dihydroquinoxalinone acetamides containing bicyclic amines as potent Bradykinin B1 receptor antagonists

Bioorganic & medicinal chemistry, 2008-08, Vol.18 (16), p.4477-4481

2008

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Discovery of Novel, Potent Benzamide Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Exhibiting Oral Activity in an Enzyme Inhibition ex Vivo Model

Journal of medicinal chemistry, 2008-07, Vol.51 (13), p.3953-3960

2008

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The discovery of 2-anilinothiazolones as 11β-HSD1 inhibitors

Bioorganic & medicinal chemistry, 2007-11, Vol.17 (22), p.6056-6061

2007

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Synthesis and Initial SAR Studies of 3,6-Disubstituted Pyrazolo[1,5- a]pyrimidines: A New Class of KDR Kinase Inhibitors

Bioorganic & medicinal chemistry letters, 2002-10, Vol.12 (19), p.2767-2770

2002

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Discovery of novel hydroxy-thiazoles as HIF-α prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation

Bioorganic & medicinal chemistry, 2008-07, Vol.18 (14), p.3925-3928

2008

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Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11β-HSD1 inhibitors

Bioorganic & medicinal chemistry letters, 2009-03, Vol.19 (6), p.1797-1801

2009

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Discovery of dehydro-oxopiperazine acetamides as novel bradykinin B1 receptor antagonists with enhanced in vitro potency

Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (2), p.1061-1067

2012

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Further Studies with the 2-Amino-1,3-thiazol-4(5H)-one Class of 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Reducing Pregnane X Receptor Activity and Exploring Activity in a Monkey Pharmacodynamic Model

Journal of medicinal chemistry, 2008-12, Vol.51 (24), p.7953-7967

2008

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Vascular Endothelial Growth Factor Receptor KDR Tyrosine Kinase Activity Is Increased by Autophosphorylation of Two Activation Loop Tyrosine Residues

The Journal of biological chemistry, 1999-03, Vol.274 (10), p.6453-6460

1999

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3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation

Bioorganic & medicinal chemistry letters, 2011-06, Vol.21 (11), p.3384-3389

2011

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An Efficient and Scalable One-Pot Double Michael Addition-Dieckmann Condensation for the Synthesis of 4,4-Disubstituted Cyclohexane β-Keto Esters

Journal of organic chemistry, 2007-09, Vol.72 (19), p.7455-7458

2007

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Optimization of a pyrazolo[1,5- a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics

Bioorganic & medicinal chemistry letters, 2002-12, Vol.12 (24), p.3537-3541

2002

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Aryl sulfones as novel Bradykinin B1 receptor antagonists for treatment of chronic pain

Bioorganic & medicinal chemistry, 2008-09, Vol.18 (17), p.4764-4769

2008

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Aryl sulfonamides containing tetralin allylic amines as potent and selective bradykinin B1 receptor antagonists

Bioorganic & medicinal chemistry letters, 2010-08, Vol.20 (15), p.4593-4597

2010

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Potent Nonpeptide Antagonists of the Bradykinin B1 Receptor: Structure−Activity Relationship Studies with Novel Diaminochroman Carboxamides

Journal of medicinal chemistry, 2007-05, Vol.50 (9), p.2200-2212

2007

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Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists

Bioorganic & medicinal chemistry letters, 2005-12, Vol.15 (23), p.5211-5217

2005

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The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase

Bioorganic & medicinal chemistry letters, 2004-06, Vol.14 (11), p.2941-2945

2004

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Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR

Bioorganic & medicinal chemistry letters, 2003-08, Vol.13 (15), p.2485-2488

2003

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Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors

Bioorganic & medicinal chemistry letters, 2003-09, Vol.13 (18), p.2973-2976

2003

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Dipeptidyl-Quinolone Derivatives Inhibit Hypoxia Inducible Factor-1α Prolyl Hydroxylases-1, -2, and -3 with Altered Selectivity

Journal of combinatorial chemistry, 2010-09, Vol.12 (5), p.676-686

2010

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An efficient synthesis of 1,6- and 1,7-dibromo-3-aminoisoquinolines: versatile templates for the preparation of functionalized isoquinolines

Tetrahedron letters, 2007-01, Vol.48 (3), p.487-489

2007

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Regio-controlled synthesis of N-substituted imidazoles

Tetrahedron letters, 2005-10, Vol.46 (43), p.7315-7319

2005

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Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (nN → σS–X) Interaction for Conformational Constraint

Discovery of a Potent, Orally Active 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor for Clinical Study: Identification of (S)-2-((1S,2S,4R)-Bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221)

2-(S)-Phenethylaminothiazolones as Potent, Orally Efficacious Inhibitors of 11β-Hydroxysteriod Dehydrogenase Type 1

Discovery of dihydroquinoxalinone acetamides containing bicyclic amines as potent Bradykinin B1 receptor antagonists

Discovery of Novel, Potent Benzamide Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Exhibiting Oral Activity in an Enzyme Inhibition ex Vivo Model

The discovery of 2-anilinothiazolones as 11β-HSD1 inhibitors

Synthesis and Initial SAR Studies of 3,6-Disubstituted Pyrazolo[1,5- a]pyrimidines: A New Class of KDR Kinase Inhibitors

Discovery of novel hydroxy-thiazoles as HIF-α prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation

Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11β-HSD1 inhibitors

Discovery of dehydro-oxopiperazine acetamides as novel bradykinin B1 receptor antagonists with enhanced in vitro potency

Further Studies with the 2-Amino-1,3-thiazol-4(5H)-one Class of 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Reducing Pregnane X Receptor Activity and Exploring Activity in a Monkey Pharmacodynamic Model

Vascular Endothelial Growth Factor Receptor KDR Tyrosine Kinase Activity Is Increased by Autophosphorylation of Two Activation Loop Tyrosine Residues

3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation

An Efficient and Scalable One-Pot Double Michael Addition-Dieckmann Condensation for the Synthesis of 4,4-Disubstituted Cyclohexane β-Keto Esters

Optimization of a pyrazolo[1,5- a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics

Aryl sulfones as novel Bradykinin B1 receptor antagonists for treatment of chronic pain

Aryl sulfonamides containing tetralin allylic amines as potent and selective bradykinin B1 receptor antagonists

Potent Nonpeptide Antagonists of the Bradykinin B1 Receptor: Structure−Activity Relationship Studies with Novel Diaminochroman Carboxamides

Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists

The discovery of N-(1,3-thiazol-2-yl)pyridin-2-amines as potent inhibitors of KDR kinase

Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR

Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors

Dipeptidyl-Quinolone Derivatives Inhibit Hypoxia Inducible Factor-1α Prolyl Hydroxylases-1, -2, and -3 with Altered Selectivity

An efficient synthesis of 1,6- and 1,7-dibromo-3-aminoisoquinolines: versatile templates for the preparation of functionalized isoquinolines

Regio-controlled synthesis of N-substituted imidazoles

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