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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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Muscarinic receptor agonists and antagonists in the treatment of Alzheimer's disease

Current pharmaceutical design, 2005-10, Vol.11 (26), p.3353-3361

2005

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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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Substituted 4-morpholine N-arylsulfonamides as γ-secretase inhibitors

European journal of medicinal chemistry, 2016-11, Vol.124, p.36-48

2016

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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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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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Synthesis and SAR study of tricyclic sulfones as γ-secretase inhibitors: C-6 and C-8 positions

Bioorganic & medicinal chemistry letters, 2011-06, Vol.21 (11), p.3447-3451

2011

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Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active γ-secretase inhibitors

Bioorganic & medicinal chemistry, 2008-01, Vol.18 (1), p.215-219

2008

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Novel orally active morpholine N-arylsulfonamides γ-secretase inhibitors with low CYP 3A4 liability

Bioorganic & medicinal chemistry letters, 2009-11, Vol.19 (21), p.6032-6037

2009

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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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Small conformationally restricted piperidine N-arylsulfonamides as orally active γ-secretase inhibitors

Bioorganic & medicinal chemistry letters, 2007-10, Vol.17 (19), p.5330-5335

2007

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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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Discovery of γ-secretase inhibitors efficacious in a transgenic animal model of Alzheimer’s disease

Bioorganic & medicinal chemistry letters, 2007-01, Vol.17 (2), p.511-516

2007

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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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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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The Discovery of Ezetimibe: A View from Outside the Receptor

Muscarinic receptor agonists and antagonists in the treatment of Alzheimer's disease

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

Substituted 4-morpholine N-arylsulfonamides as γ-secretase 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

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

Synthesis and SAR study of tricyclic sulfones as γ-secretase inhibitors: C-6 and C-8 positions

Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active γ-secretase inhibitors

Novel orally active morpholine N-arylsulfonamides γ-secretase inhibitors with low CYP 3A4 liability

2-Azetidinones as Inhibitors of Cholesterol Absorption

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

Small conformationally restricted piperidine N-arylsulfonamides as orally active γ-secretase inhibitors

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

Discovery of γ-secretase inhibitors efficacious in a transgenic animal model of Alzheimer’s disease

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

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

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