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

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

2005

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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

Clader, John W

2005

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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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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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Design, synthesis, and structure–activity relationship studies of N-arylsulfonyl morpholines as γ-secretase inhibitors

Bioorganic & medicinal chemistry letters, 2010-11, Vol.20 (22), p.6606-6609

2010

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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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Design, synthesis, and evaluation of tetrahydroquinoline and pyrrolidine sulfonamide carbamates as γ-secretase inhibitors

Bioorganic & medicinal chemistry letters, 2007-06, Vol.17 (11), p.3010-3013

2007

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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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Tetrahydroquinoline sulfonamides as γ-secretase inhibitors

Bioorganic & medicinal chemistry letters, 2007, Vol.17 (1), p.205-207

2007

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In Vivo Characterization of a Novel γ-Secretase Inhibitor SCH 697466 in Rodents and Investigation of Strategies for Managing Notch-Related Side Effects

Interdisciplinary perspectives on infectious diseases, 2013, Vol.2013, p.823528-823528

2013

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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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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

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

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

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

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

Design, synthesis, and structure–activity relationship studies of N-arylsulfonyl morpholines as γ-secretase inhibitors

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

Design, synthesis, and evaluation of tetrahydroquinoline and pyrrolidine sulfonamide carbamates as γ-secretase inhibitors

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

2-Azetidinones as Inhibitors of Cholesterol Absorption

Tetrahydroquinoline sulfonamides as γ-secretase inhibitors

In Vivo Characterization of a Novel γ-Secretase Inhibitor SCH 697466 in Rodents and Investigation of Strategies for Managing Notch-Related Side Effects

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

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