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Prodrugs for colon-restricted delivery: Design, synthesis, and in vivo evaluation of colony stimulating factor 1 receptor (CSF1R) inhibitors

PloS one, 2018-09, Vol.13 (9), p.e0203567

2018

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Cheminformatic Tools for Medicinal Chemists

Journal of medicinal chemistry, 2010-07, Vol.53 (13), p.4830-4841

2010

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Design, Synthesis, and Biological Activity of Potent and Selective Inhibitors of Blood Coagulation Factor Xa

Journal of medicinal chemistry, 2004-07, Vol.47 (16), p.4089-4099

2004

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Discovery of Selective and Orally Bioavailable Protein Kinase Cθ (PKCθ) Inhibitors from a Fragment Hit

Journal of medicinal chemistry, 2015-01, Vol.58 (1), p.222-236

2015

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Optimized Protein Kinase Cθ (PKCθ) Inhibitors Reveal Only Modest Anti-inflammatory Efficacy in a Rodent Model of Arthritis

Journal of medicinal chemistry, 2015-01, Vol.58 (1), p.333-346

2015

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Discovery of a Series of Imidazo[4,5-b]pyridines with Dual Activity at Angiotensin II Type 1 Receptor and Peroxisome Proliferator-Activated Receptor-γ

Journal of medicinal chemistry, 2011-06, Vol.54 (12), p.4219-4233

2011

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Rational Design, Synthesis, and Biological Activity of Benzoxazinones as Novel Factor Xa Inhibitors

Journal of medicinal chemistry, 2000-11, Vol.43 (22), p.4063-4070

2000

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Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase

Bioorganic & medicinal chemistry letters, 2013-02, Vol.23 (4), p.1051-1055

2013

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Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase

Bioorganic & medicinal chemistry letters, 2013-02, Vol.23 (4), p.1046-1050

2013

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Discovery of a Novel Series of Orally Active Non-Peptide Endothelin-A (ETA) Receptor-Selective Antagonists

Journal of medicinal chemistry, 1995-04, Vol.38 (8), p.1259-1263

1995

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Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors

Bioorganic & medicinal chemistry, 2007-09, Vol.15 (17), p.5912-5949

2007

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Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors

Bioorganic & medicinal chemistry letters, 2007-07, Vol.17 (13), p.3575-3580

2007

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The Discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an Orally Efficacious Factor Xa Inhibitor

Chemical biology & drug design, 2007-08, Vol.70 (2), p.100-112

2007

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Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action

Bioorganic & medicinal chemistry, 2009-03, Vol.17 (6), p.2501-2511

2009

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Ketopiperazine-based renin inhibitors: Optimization of the “C” ring

Bioorganic & medicinal chemistry letters, 2006-05, Vol.16 (9), p.2500-2504

2006

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Fluorination of sulfanyl amides using difluoroiodoarene reagents

Perkin 1 : an international journal of organic and bio-organic chemistry, 2002-12 (24), p.2816-2826

2002

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The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors

Bioorganic & medicinal chemistry, 2005-01, Vol.13 (1), p.59-68

2005

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Discovery of novel non-peptidic ketopiperazine-based renin inhibitors

Bioorganic & medicinal chemistry, 2005-04, Vol.13 (7), p.2657-2664

2005

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Progress in the discovery of Factor Xa inhibitors

Expert opinion on therapeutic patents, 2006-02, Vol.16 (2), p.119-145

2006

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Benzyl ether structure–activity relationships in a series of ketopiperazine-based renin inhibitors

Bioorganic & medicinal chemistry letters, 2005-11, Vol.15 (21), p.4713-4716

2005

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Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors

Bioorganic & medicinal chemistry letters, 2005-05, Vol.15 (9), p.2371-2374

2005

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The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex—Part 2

Bioorganic & medicinal chemistry letters, 2006-02, Vol.16 (4), p.1060-1064

2006

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The discovery of glycine and related amino acid-based factor Xa inhibitors

Bioorganic & medicinal chemistry, 2006-07, Vol.14 (13), p.4379-4392

2006

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The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex

Bioorganic & medicinal chemistry letters, 2005-11, Vol.15 (21), p.4752-4756

2005

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Practical Synthesis of 1-Aryl-6-(hydroxymethyl)-2-ketopiperazines via a 6-exo Amide−Epoxide Cyclization

Organic letters, 2004-10, Vol.6 (22), p.4069-4072

2004

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Prodrugs for colon-restricted delivery: Design, synthesis, and in vivo evaluation of colony stimulating factor 1 receptor (CSF1R) inhibitors

Cheminformatic Tools for Medicinal Chemists

Design, Synthesis, and Biological Activity of Potent and Selective Inhibitors of Blood Coagulation Factor Xa

Discovery of Selective and Orally Bioavailable Protein Kinase Cθ (PKCθ) Inhibitors from a Fragment Hit

Optimized Protein Kinase Cθ (PKCθ) Inhibitors Reveal Only Modest Anti-inflammatory Efficacy in a Rodent Model of Arthritis

Discovery of a Series of Imidazo[4,5-b]pyridines with Dual Activity at Angiotensin II Type 1 Receptor and Peroxisome Proliferator-Activated Receptor-γ

Rational Design, Synthesis, and Biological Activity of Benzoxazinones as Novel Factor Xa Inhibitors

Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase

Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase

Discovery of a Novel Series of Orally Active Non-Peptide Endothelin-A (ETA) Receptor-Selective Antagonists

Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors

Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors

The Discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an Orally Efficacious Factor Xa Inhibitor

Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action

Ketopiperazine-based renin inhibitors: Optimization of the “C” ring

Fluorination of sulfanyl amides using difluoroiodoarene reagents

The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors

Discovery of novel non-peptidic ketopiperazine-based renin inhibitors

Progress in the discovery of Factor Xa inhibitors

Benzyl ether structure–activity relationships in a series of ketopiperazine-based renin inhibitors

Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors

The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex—Part 2

The discovery of glycine and related amino acid-based factor Xa inhibitors

The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex

Practical Synthesis of 1-Aryl-6-(hydroxymethyl)-2-ketopiperazines via a 6-exo Amide−Epoxide Cyclization

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