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The Discovery of Ezetimibe: A View from Outside the Receptor

Journal of medicinal chemistry, 2004-01, Vol.47 (1), p.1-9

Clader, John W

2004

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HIV-1 Escape from a Small Molecule, CCR5-Specific Entry Inhibitor Does Not Involve CXCR4 Use

Proceedings of the National Academy of Sciences - PNAS, 2002-01, Vol.99 (1), p.395-400

2002

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Analysis of the Mechanism by Which the Small-Molecule CCR5 Antagonists SCH-351125 and SCH-350581 Inhibit Human Immunodeficiency Virus Type 1 Entry

Journal of Virology, 2003-05, Vol.77 (9), p.5201-5208

2003

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Discovery of a Novel, Potent Spirocyclic Series of γ‑Secretase Inhibitors

Journal of medicinal chemistry, 2015-11, Vol.58 (22), p.8806-8817

2015

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Ezetimibe and other azetidinone cholesterol absorption inhibitors

Current topics in medicinal chemistry, 2005-01, Vol.5 (3), p.243-256

Clader, John W

2005

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Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors

Bioorganic & medicinal chemistry, 2016-11, Vol.24 (21), p.5534-5545

2016

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Discovery of 1-(4-Fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)- hydroxypropyl]-(4S)-(4-hydroxyphenyl)-2-azetidinone (SCH 58235): A Designed, Potent, Orally Active Inhibitor of Cholesterol Absorption

Journal of medicinal chemistry, 1998-03, Vol.41 (6), p.973-980

1998

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Interaction of small molecule inhibitors of HIV-1 entry with CCR5

Virology (New York, N.Y.), 2006-05, Vol.349 (1), p.41-54

2006

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Discovery of Orally Efficacious Melanin-Concentrating Hormone Receptor-1 Antagonists as Antiobesity Agents. Synthesis, SAR, and Biological Evaluation of Bicyclo[3.1.0]hexyl Ureas

Journal of medicinal chemistry, 2006-04, Vol.49 (7), p.2294-2310

2006

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Discovery of 4-[(Z)-(4-Bromophenyl)- (ethoxyimino)methyl]-1‘-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4‘-methyl-1,4‘- bipiperidine N-Oxide (SCH 351125): An Orally Bioavailable Human CCR5 Antagonist for the Treatment of HIV Infection

Journal of medicinal chemistry, 2001-10, Vol.44 (21), p.3339-3342

2001

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Discovery of Bicycloalkyl Urea Melanin Concentrating Hormone Receptor Antagonists: Orally Efficacious Antiobesity Therapeutics

Journal of medicinal chemistry, 2005-04, Vol.48 (7), p.2274-2277

2005

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Synthesis, SAR, and Biological Evaluation of Oximino-Piperidino-Piperidine Amides. 1. Orally Bioavailable CCR5 Receptor Antagonists with Potent Anti-HIV Activity

Journal of medicinal chemistry, 2002-07, Vol.45 (14), p.3143-3160

2002

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SCH-C (SCH 351125), An Orally Bioavailable, Small Molecule Antagonist of the Chemokine Receptor CCR5, is a Potent Inhibitor of HIV-1 Infection in vitro and in vivo

Proceedings of the National Academy of Sciences - PNAS, 2001-10, Vol.98 (22), p.12718-12723

2001

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Biaryl Ureas as Potent and Orally Efficacious Melanin Concentrating Hormone Receptor 1 Antagonists for the Treatment of Obesity

Journal of medicinal chemistry, 2005-07, Vol.48 (15), p.4746-4749

2005

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2-Azetidinones as Inhibitors of Cholesterol Absorption

Journal of medicinal chemistry, 1994-06, Vol.37 (12), p.1733-1736

1994

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Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists

Bioorganic & medicinal chemistry letters, 2000-10, Vol.10 (20), p.2247-2250

2000

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Bicyclic[4.1.0]heptanes as phenyl replacements for melanin concentrating hormone receptor antagonists

Bioorganic & medicinal chemistry, 2006-05, Vol.14 (10), p.3285-3299

2006

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Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides

Bioorganic & medicinal chemistry letters, 2003-02, Vol.13 (4), p.709-712

2003

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2-Azetidinone Cholesterol Absorption Inhibitors: Structure−Activity Relationships on the Heterocyclic Nucleus

Journal of medicinal chemistry, 1996-09, Vol.39 (19), p.3684-3693

1996

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Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists

Bioorganic & medicinal chemistry letters, 2005-12, Vol.15 (23), p.5234-5236

2005

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Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: Impacting hERG liability via aryl modifications

Bioorganic & medicinal chemistry letters, 2006-08, Vol.16 (16), p.4262-4265

2006

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SAR study of bicyclo[4.1.0]heptanes as melanin-concentrating hormone receptor R1 antagonists: Taming hERG

Bioorganic & medicinal chemistry, 2007-08, Vol.15 (16), p.5369-5385

2007

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Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors

Bioorganic & medicinal chemistry letters, 2002-02, Vol.12 (3), p.311-314

2002

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Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED

Bioorganic & medicinal chemistry letters, 2005-05, Vol.15 (9), p.2365-2369

2005

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Biological evaluation and interconversion studies of rotamers of SCH 351125, an orally bioavailable CCR5 antagonist

Bioorganic & medicinal chemistry letters, 2003-02, Vol.13 (4), p.705-708

2003

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The Discovery of Ezetimibe: A View from Outside the Receptor

HIV-1 Escape from a Small Molecule, CCR5-Specific Entry Inhibitor Does Not Involve CXCR4 Use

Analysis of the Mechanism by Which the Small-Molecule CCR5 Antagonists SCH-351125 and SCH-350581 Inhibit Human Immunodeficiency Virus Type 1 Entry

Discovery of a Novel, Potent Spirocyclic Series of γ‑Secretase Inhibitors

Ezetimibe and other azetidinone cholesterol absorption inhibitors

Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors

Discovery of 1-(4-Fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)- hydroxypropyl]-(4S)-(4-hydroxyphenyl)-2-azetidinone (SCH 58235): A Designed, Potent, Orally Active Inhibitor of Cholesterol Absorption

Interaction of small molecule inhibitors of HIV-1 entry with CCR5

Discovery of Orally Efficacious Melanin-Concentrating Hormone Receptor-1 Antagonists as Antiobesity Agents. Synthesis, SAR, and Biological Evaluation of Bicyclo[3.1.0]hexyl Ureas

Discovery of 4-[(Z)-(4-Bromophenyl)- (ethoxyimino)methyl]-1‘-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4‘-methyl-1,4‘- bipiperidine N-Oxide (SCH 351125): An Orally Bioavailable Human CCR5 Antagonist for the Treatment of HIV Infection

Discovery of Bicycloalkyl Urea Melanin Concentrating Hormone Receptor Antagonists: Orally Efficacious Antiobesity Therapeutics

Synthesis, SAR, and Biological Evaluation of Oximino-Piperidino-Piperidine Amides. 1. Orally Bioavailable CCR5 Receptor Antagonists with Potent Anti-HIV Activity

SCH-C (SCH 351125), An Orally Bioavailable, Small Molecule Antagonist of the Chemokine Receptor CCR5, is a Potent Inhibitor of HIV-1 Infection in vitro and in vivo

Biaryl Ureas as Potent and Orally Efficacious Melanin Concentrating Hormone Receptor 1 Antagonists for the Treatment of Obesity

2-Azetidinones as Inhibitors of Cholesterol Absorption

Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists

Bicyclic[4.1.0]heptanes as phenyl replacements for melanin concentrating hormone receptor antagonists

Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides

2-Azetidinone Cholesterol Absorption Inhibitors: Structure−Activity Relationships on the Heterocyclic Nucleus

Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists

Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: Impacting hERG liability via aryl modifications

SAR study of bicyclo[4.1.0]heptanes as melanin-concentrating hormone receptor R1 antagonists: Taming hERG

Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors

Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED

Biological evaluation and interconversion studies of rotamers of SCH 351125, an orally bioavailable CCR5 antagonist

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