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Discovery of N‑(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro‑1H‑pyrrolo[2,3‑c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor

Journal of medicinal chemistry, 2017-10, Vol.60 (20), p.8369-8384

2017

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Enabling, Decagram-Scale Synthesis of Macrocyclic MCL‑1 Inhibitor ABBV-467

Journal of organic chemistry, 2023-11, Vol.88 (22), p.15562-15568

2023

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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

Bioorganic & medicinal chemistry letters, 2018-06, Vol.28 (10), p.1804-1810

2018

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Methylpyrrole inhibitors of BET bromodomains

Bioorganic & medicinal chemistry letters, 2017-05, Vol.27 (10), p.2225-2233

2017

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Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases

Bioorganic & medicinal chemistry letters, 2010-10, Vol.20 (20), p.6067-6071

2010

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1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyano- pyrazi-2-yl)ureas as Potent and Selective Inhibitors of Chk1 Kinase: Synthesis, Preliminary SAR, and Biological Activities

Journal of medicinal chemistry, 2005-05, Vol.48 (9), p.3118-3121

2005

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Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids

Bioorganic & medicinal chemistry letters, 2007-05, Vol.17 (10), p.2817-2822

2007

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2,4-Diarylpyrrolidine-3-carboxylic AcidsPotent ETA Selective Endothelin Receptor Antagonists. 1. Discovery of A-127722

Journal of medicinal chemistry, 1996-03, Vol.39 (5), p.1039-1048

1996

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Methylpyrrole inhibitors of BET bromodomains

Bioorganic & medicinal chemistry letters, 2017-05, Vol.27 (10)

2017

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Discovery of a series of pyrrolidine-based endothelin receptor antagonists with enhanced ET A receptor selectivity

Bioorganic & medicinal chemistry, 1999-06, Vol.7 (6), p.991-1002

1999

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Nonpeptide Renin Inhibitors with Good Intraduodenal Bioavailability and Efficacy in Dog

Journal of medicinal chemistry, 1994-09, Vol.37 (19), p.2991-3007

1994

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C-Terminal modifications of nonpeptide renin inhibitors: improved oral bioavailability via modification of physicochemical properties

Journal of medicinal chemistry, 1992-05, Vol.35 (10), p.1735-1746

1992

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Pyridone-Containing farnesyltransferase inhibitors: synthesis and biological evaluation

Bioorganic & medicinal chemistry letters, 2003-11, Vol.13 (22), p.4001-4005

2003

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Abstract A248: Substituted 4-amino-1 H -pyrazolo[3,4- d ]pyrimidines as multitargeted inhibitors targeting insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor tyrosine kinases

Molecular cancer therapeutics, 2009-12, Vol.8 (12_Supplement), p.A248-A248

2009

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Substituted 4-amino-1 H-pyrazolo[3,4- d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases

Bioorganic & medicinal chemistry letters, 2010, Vol.20 (20), p.6067-6071

2010

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Stereoselective syntheses of hydroxyethylene dipeptide isosteres

Journal of organic chemistry, 1991-01, Vol.56 (1), p.438-442

1991

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Abstract A245: Imidazo[2,1-b]thiazole and imidazo[1,2-a]pyridine amides as novel inhibitors of the insulin-like growth factor (IGF1R) and members of the epidermal growth factor family of tyrosine kinases

Molecular cancer therapeutics, 2009-12, Vol.8 (12_Supplement), p.A245-A245

2009

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Effects of High Doses of A-74273, a Novel Nonpeptidic and Orally Bioavailable Renin Inhibitor

Journal of cardiovascular pharmacology, 1993-01, Vol.21 (1), p.149-155

1993

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1-(5-chloro-2-alkoxyphenyl)-3-(5-cyano-pyrazi-2-yl)ureas as potent and selective inhibitors of chkl kinase : Synthesis, preliminary SAR, and biological activities

Journal of medicinal chemistry, 2005, Vol.48 (9), p.3118-3121

2005

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Discovery of a series of pyrrolidine-based endothelin receptor antagonists with enhanced ETA receptor selectivity

Bioorganic & medicinal chemistry, 1999-06, Vol.7 (6), p.991-1002

1999

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2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists

Journal of medicinal chemistry, 1993-09, Vol.36 (18), p.2676-2688

1993

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A stereoselective synthesis of hydroxyethylene and erythro-dihydroxyethylene dipeptide isosteres: a facial selective anti-Aldol reaction

Tetrahedron letters, 1991-11, Vol.32 (45), p.6507-6508

1991

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2,4-Diarylpyrrolidine-3-carboxylic AcidsPotent ET A Selective Endothelin Receptor Antagonists. 1. Discovery of A-127722

Journal of medicinal chemistry, 1996-01, Vol.39 (5), p.1039-1048

1996

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Discovery of N‑(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro‑1H‑pyrrolo[2,3‑c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor

Enabling, Decagram-Scale Synthesis of Macrocyclic MCL‑1 Inhibitor ABBV-467

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

Methylpyrrole inhibitors of BET bromodomains

Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases

Discovery and Optimization of Anthranilic Acid Sulfonamides as Inhibitors of Methionine Aminopeptidase-2: A Structural Basis for the Reduction of Albumin Binding

1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyano- pyrazi-2-yl)ureas as Potent and Selective Inhibitors of Chk1 Kinase: Synthesis, Preliminary SAR, and Biological Activities

Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids

2,4-Diarylpyrrolidine-3-carboxylic AcidsPotent ETA Selective Endothelin Receptor Antagonists. 1. Discovery of A-127722

Methylpyrrole inhibitors of BET bromodomains

Discovery of a series of pyrrolidine-based endothelin receptor antagonists with enhanced ET A receptor selectivity

Nonpeptide Renin Inhibitors with Good Intraduodenal Bioavailability and Efficacy in Dog

C-Terminal modifications of nonpeptide renin inhibitors: improved oral bioavailability via modification of physicochemical properties

Pyridone-Containing farnesyltransferase inhibitors: synthesis and biological evaluation

Abstract A248: Substituted 4-amino-1 H -pyrazolo[3,4- d ]pyrimidines as multitargeted inhibitors targeting insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor tyrosine kinases

Substituted 4-amino-1 H-pyrazolo[3,4- d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases

Stereoselective syntheses of hydroxyethylene dipeptide isosteres

Abstract A245: Imidazo[2,1-b]thiazole and imidazo[1,2-a]pyridine amides as novel inhibitors of the insulin-like growth factor (IGF1R) and members of the epidermal growth factor family of tyrosine kinases

Effects of High Doses of A-74273, a Novel Nonpeptidic and Orally Bioavailable Renin Inhibitor

1-(5-chloro-2-alkoxyphenyl)-3-(5-cyano-pyrazi-2-yl)ureas as potent and selective inhibitors of chkl kinase : Synthesis, preliminary SAR, and biological activities

Discovery of a series of pyrrolidine-based endothelin receptor antagonists with enhanced ETA receptor selectivity

2-(Alkylamino)nicotinic acid and analogs. Potent angiotensin II antagonists

A stereoselective synthesis of hydroxyethylene and erythro-dihydroxyethylene dipeptide isosteres: a facial selective anti-Aldol reaction

2,4-Diarylpyrrolidine-3-carboxylic AcidsPotent ET A Selective Endothelin Receptor Antagonists. 1. Discovery of A-127722

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