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Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy

Journal of medicinal chemistry, 2022-02, Vol.65 (3), p.1770-1785

2022

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Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities

Bioorganic & medicinal chemistry, 2023-05, Vol.85, p.117273-117273, Article 117273

2023

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Discovery and Optimization of Aryl Piperidinone Ureas as Selective Formyl Peptide Receptor 2 Agonists

ACS medicinal chemistry letters, 2024-09, Vol.15 (9), p.1500-1505

2024

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Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists

Journal of medicinal chemistry, 2018-02, Vol.61 (3), p.681-694

2018

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Rosuvastatin Liver Partitioning in Cynomolgus Monkeys: Measurement In Vivo and Prediction Using In Vitro Monkey Hepatocyte Uptake

Drug metabolism and disposition, 2015-11, Vol.43 (11), p.1788-1794

2015

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Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists

ACS medicinal chemistry letters, 2022-06, Vol.13 (6), p.943-948

2022

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Selective FPR2 Agonism Promotes a Proresolution Macrophage Phenotype and Improves Cardiac Structure-Function Post Myocardial Infarction

JACC. Basic to translational science, 2021-08, Vol.6 (8), p.676-689

2021

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Molecular Mechanisms of Desensitization Underlying the Differential Effects of Formyl Peptide Receptor 2 Agonists on Cardiac Structure–Function Post Myocardial Infarction

ACS pharmacology & translational science, 2022-10, Vol.5 (10), p.892-906

2022

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Application of ultrasound‐guided cholecystocentesis to the evaluation of the metabolite profiling in bile of dogs and cynomolgus monkeys

Pharmacology research & perspectives, 2019-06, Vol.7 (3), p.e00488-n/a

2019

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Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-β Receptor Type I Inhibitor as Antitumor Agent

Journal of medicinal chemistry, 2008-04, Vol.51 (7), p.2302-2306

2008

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Studies of the Heme Coordination and Ligand Binding Properties of Soluble Guanylyl Cyclase (sGC): Characterization of Fe(II)sGC and Fe(II)sGC(CO) by Electronic Absorption and Magnetic Circular Dichroism Spectroscopies and Failure of CO To Activate the Enzyme

Biochemistry (Easton), 1995-05, Vol.34 (17), p.5896-5903

1995

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Demonstration of the Role of Scission of the Proximal Histidine−Iron Bond in the Activation of Soluble Guanylyl Cyclase through Metalloporphyrin Substitution Studies

Journal of the American Chemical Society, 1997-08, Vol.119 (31), p.7316-7323

1997

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Glu-320 and Asp-323 Are Determinants of the CYP4A1 Hydroxylation Regiospecificity and Resistance to Inactivation by 1-Aminobenzotriazole

Biochemistry (Easton), 1998-02, Vol.37 (7), p.1839-1847

1998

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The Catalytic Site of Cytochrome P4504A11 (CYP4A11) and Its L131F Mutant

The Journal of biological chemistry, 1998-09, Vol.273 (36), p.23055-23061

1998

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A method for the simultaneous evaluation of the activities of seven major human drug-metabolizing cytochrome P450s using an in vitro cocktail of probe substrates and fast gradient liquid chromatography tandem mass spectrometry

Drug metabolism and disposition, 2001-01, Vol.29 (1), p.23

2001

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Abstract TMP117: Preclinical and Early Clinical Characterization of a Parenterally Administered Direct Factor XIa Inhibitor

Stroke (1970), 2017-02, Vol.48 (suppl_1)

2017

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Nitric oxide (NO •), the only nitrogen monoxide redox form capable of activating soluble guanylyl cyclase

Biochemical pharmacology, 1996-06, Vol.51 (12), p.1593-1600

1996

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The Deactivation of Soluble Guanylyl Cyclase by Redox-Active Agents

Archives of biochemistry and biophysics, 1998-03, Vol.351 (1), p.1-7

1998

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Variable forms of soluble guanylyl cyclase: protein-ligand interactions and the issue of activation by carbon monoxide

Journal of biological inorganic chemistry, 1999-12, Vol.4 (6), p.804-813

1999

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Structure-function of cytochromes P450 and flavin-containing monooxygenases: implications for drug metabolism

Drug metabolism and disposition, 1998-12, Vol.26 (12), p.1223

1998

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Preservation of Post-Infarction Cardiac Structure and Function via Long-Term Oral Formyl Peptide Receptor Agonist Treatment

JACC. Basic to translational science, 2019-12, Vol.4 (8), p.905-920

2019

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Novel Bispecific Degrader BHV-1300 Achieves Rapid, Robust, and Selective IgG Reduction in Preclinical Models Including Nonhuman Primates (S43.004)

Neurology, 2024-04, Vol.102 (17_supplement_1)

2024

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Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy

MGAT2 inhibitor decreases liver fibrosis and inflammation in murine NASH models and reduces body weight in human adults with obesity

Discovery of 12 (BMS-986172) as a Highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a Low Human Dose for the Treatment of Metabolic Disorders

Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities

Discovery and Optimization of Aryl Piperidinone Ureas as Selective Formyl Peptide Receptor 2 Agonists

Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists

Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode

Rosuvastatin Liver Partitioning in Cynomolgus Monkeys: Measurement In Vivo and Prediction Using In Vitro Monkey Hepatocyte Uptake

Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists

Selective FPR2 Agonism Promotes a Proresolution Macrophage Phenotype and Improves Cardiac Structure-Function Post Myocardial Infarction

Molecular Mechanisms of Desensitization Underlying the Differential Effects of Formyl Peptide Receptor 2 Agonists on Cardiac Structure–Function Post Myocardial Infarction

Application of ultrasound‐guided cholecystocentesis to the evaluation of the metabolite profiling in bile of dogs and cynomolgus monkeys

Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-β Receptor Type I Inhibitor as Antitumor Agent

Studies of the Heme Coordination and Ligand Binding Properties of Soluble Guanylyl Cyclase (sGC): Characterization of Fe(II)sGC and Fe(II)sGC(CO) by Electronic Absorption and Magnetic Circular Dichroism Spectroscopies and Failure of CO To Activate the Enzyme

Demonstration of the Role of Scission of the Proximal Histidine−Iron Bond in the Activation of Soluble Guanylyl Cyclase through Metalloporphyrin Substitution Studies

Glu-320 and Asp-323 Are Determinants of the CYP4A1 Hydroxylation Regiospecificity and Resistance to Inactivation by 1-Aminobenzotriazole

The Catalytic Site of Cytochrome P4504A11 (CYP4A11) and Its L131F Mutant

A method for the simultaneous evaluation of the activities of seven major human drug-metabolizing cytochrome P450s using an in vitro cocktail of probe substrates and fast gradient liquid chromatography tandem mass spectrometry

Abstract TMP117: Preclinical and Early Clinical Characterization of a Parenterally Administered Direct Factor XIa Inhibitor

Nitric oxide (NO •), the only nitrogen monoxide redox form capable of activating soluble guanylyl cyclase

The Deactivation of Soluble Guanylyl Cyclase by Redox-Active Agents

Variable forms of soluble guanylyl cyclase: protein-ligand interactions and the issue of activation by carbon monoxide

Structure-function of cytochromes P450 and flavin-containing monooxygenases: implications for drug metabolism

Preservation of Post-Infarction Cardiac Structure and Function via Long-Term Oral Formyl Peptide Receptor Agonist Treatment

Novel Bispecific Degrader BHV-1300 Achieves Rapid, Robust, and Selective IgG Reduction in Preclinical Models Including Nonhuman Primates (S43.004)

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