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Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9331-9345

2012

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Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV‑1 Protease Inhibitors

ACS medicinal chemistry letters, 2017-12, Vol.8 (12), p.1292-1297

2017

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Potent, selective, and orally active adenosine A2A receptor antagonists : Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1 ,5-c]pyrimidines

Bioorganic & medicinal chemistry letters, 2007-03, Vol.17 (5), p.1376-1380

2007

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The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients

Science translational medicine, 2016-11, Vol.8 (363), p.363ra150

2016

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Structure–function analysis of the SHOC2–MRAS–PP1C holophosphatase complex

Nature (London), 2022-09, Vol.609 (7926), p.408-415

2022

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Discovery of a 3‑(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity

Journal of medicinal chemistry, 2017-04, Vol.60 (7), p.2983-2992

2017

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Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells

Bioorganic & medicinal chemistry letters, 2019-09, Vol.29 (17), p.2503-2510

2019

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Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules

Cancer research (Chicago, Ill.), 2021-04, Vol.81 (8), p.2002-2014

2021

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Small-Molecule Inhibition of the Acyl-Lysine Reader ENL as a Strategy against Acute Myeloid Leukemia

Cancer discovery, 2022-11, Vol.12 (11), p.2684-2709

2022

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Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor

Bioorganic & medicinal chemistry letters, 2012-04, Vol.22 (7), p.2444-2449

2012

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Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055

ACS medicinal chemistry letters, 2024-04, Vol.15 (4), p.524-532

2024

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A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors

ACS medicinal chemistry letters, 2022-03, Vol.13 (3), p.377-387

2022

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Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety

Journal of medicinal chemistry, 2018-12, Vol.61 (23), p.10700-10708

2018

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Preladenant, a selective A2A receptor antagonist, is active in primate models of movement disorders

Experimental neurology, 2010-10, Vol.225 (2), p.384-390

2010

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Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders

Experimental neurology, 2010-10, Vol.225 (2), p.384

2010

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CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition

The Journal of neuroscience, 2014-06, Vol.34 (24), p.8336-8346

2014

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A Novel Method for the Preparation of 4‑Arylimidazolones

Organic letters, 2013-06, Vol.15 (11), p.2830-2833

2013

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Application of Fragment-Based NMR Screening, X-ray Crystallography, Structure-Based Design, and Focused Chemical Library Design to Identify Novel μM Leads for the Development of nM BACE-1 (β-Site APP Cleaving Enzyme 1) Inhibitors

Journal of medicinal chemistry, 2010-02, Vol.53 (3), p.942-950

2010

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Formal Olefination and Acylaziridination of Imidazolones

Organic letters, 2010-06, Vol.12 (12), p.2718-2721

2010

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Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction

ACS medicinal chemistry letters, 2012-11, Vol.3 (11), p.897-902

2012

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Discovery of MK-8282 as a Potent G‑Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes

ACS medicinal chemistry letters, 2018-05, Vol.9 (5), p.457-461

2018

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Characterization of a novel vasopressin V1b receptor antagonist, V1B-30N, in animal models of anxiety-like and depression-like behavior

European journal of pharmacology, 2014-05, Vol.730, p.157-163

2014

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Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation

Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV‑1 Protease Inhibitors

Potent, selective, and orally active adenosine A2A receptor antagonists : Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1 ,5-c]pyrimidines

The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients

Discovery of the 3‑Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)–A β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer’s Disease

Structure–function analysis of the SHOC2–MRAS–PP1C holophosphatase complex

Discovery of a 3‑(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity

Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells

Targeting eIF4A-Dependent Translation of KRAS Signaling Molecules

Small-Molecule Inhibition of the Acyl-Lysine Reader ENL as a Strategy against Acute Myeloid Leukemia

Recruitment of FBXO22 for targeted degradation of NSD2

Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor

Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055

A Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors

Structure-Based Design of an Iminoheterocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates

Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety

Preladenant, a selective A2A receptor antagonist, is active in primate models of movement disorders

Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders

CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition

A Novel Method for the Preparation of 4‑Arylimidazolones

Application of Fragment-Based NMR Screening, X-ray Crystallography, Structure-Based Design, and Focused Chemical Library Design to Identify Novel μM Leads for the Development of nM BACE-1 (β-Site APP Cleaving Enzyme 1) Inhibitors

Formal Olefination and Acylaziridination of Imidazolones

Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction

Discovery of MK-8282 as a Potent G‑Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes

Characterization of a novel vasopressin V1b receptor antagonist, V1B-30N, in animal models of anxiety-like and depression-like behavior

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