J. Clader

发表

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.

W. Greenlee, Mark D. McBriar, H. Guzik, 2006, Journal of medicinal chemistry.

Identification of presenilin 1-selective γ-secretase inhibitors with reconstituted γ-secretase complexes.

J. Clader, D. Burnett, E. Parker, 2011, Biochemistry.

HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use

A. Trkola, John P. Moore, T. Ketas, 2002, Proceedings of the National Academy of Sciences of the United States of America.

Studies to Investigate the in Vivo Therapeutic Window of the γ-Secretase Inhibitor N2-[(2S)-2-(3,5-Difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-l-alaninamide (LY411,575) in the CRND8 Mouse

Lynn A. Hyde, G. Higgins, J. Clader, 2006, Journal of Pharmacology and Experimental Therapeutics.

Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity.

W. Greenlee, S. Shapiro, A. Palani, 2002, Journal of medicinal chemistry.

Solution-phase parallel synthesis of carbamates as gamma-secretase inhibitors.

J. Clader, Lixin Song, G. Terracina, 2008, Journal of combinatorial chemistry.

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.

J. Clader, T. Huynh, H. Davis, 1998 .

2-Azetidinones as inhibitors of cholesterol absorption.

R. Burrier, J. Clader, H. Davis, 1994, Journal of medicinal chemistry.

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

W. Greenlee, A. Stamford, H. Guzik, 2005, Bioorganic & medicinal chemistry letters.

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

Lynn A. Hyde, W. Greenlee, Mark D. McBriar, 2008, Bioorganic & medicinal chemistry letters.

Tricyclic sulfones as orally active gamma-secretase inhibitors: synthesis and structure-activity relationship studies.

Lynn A. Hyde, W. Greenlee, R. Xu, 2010, Bioorganic & medicinal chemistry letters.

Tetracyclic sulfones as potent gamma-secretase inhibitors: synthesis and structure-activity relationship studies.

Lynn A. Hyde, W. Greenlee, R. Xu, 2010, Bioorganic & medicinal chemistry letters.

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

W. Greenlee, J. Lachowicz, J. Clader, 2000, Bioorganic & medicinal chemistry letters.

Facilitation of acetylcholine release and improvement in cognition by a selective M2 muscarinic antagonist, SCH 72788.

C. Strader, J. Lachowicz, J. Clader, 2001, Life sciences.

2,6-Disubstituted N-arylsulfonyl piperidines as γ-secretase inhibitors

W. Greenlee, H. Guzik, J. Clader, 2007 .

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

J. Clader, G. Scapin, J. Voigt, 2016, Bioorganic & medicinal chemistry.

SCH 57790: a novel M2 receptor selective antagonist.

C. Strader, J. Lachowicz, J. Clader, 1999, Life sciences.

Identification and characterization of an acyl-CoA:triterpene acyltransferase activity in rabbit and human tissues.

J. Clader, I. Tabas, L. L. Chen, 1991, Journal of lipid research.

Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors.

Lynn A. Hyde, W. Greenlee, Mark D. McBriar, 2013, Bioorganic & medicinal chemistry letters.

SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.

W. Greenlee, A. Stamford, R. Xu, 2004, Bioorganic & medicinal chemistry letters.

Inhibitors of acyl CoA:cholesterol acyltransferase.

R. Burrier, J. Clader, J. Berger, 1996, Journal of medicinal chemistry.

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.

J. Clader, T. Huynh, H. Davis, 1998, Journal of medicinal chemistry.

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

W. Greenlee, S. Shapiro, A. Palani, 2003, Bioorganic & medicinal chemistry letters.

Muscarinic M2 antagonists: anthranilamide derivatives with exceptional selectivity and in vivo activity.

W. Greenlee, J. Lachowicz, J. Clader, 2004, Bioorganic & medicinal chemistry.

2-Azetidinone cholesterol absorption inhibitors: structure-activity relationships on the heterocyclic nucleus.

R. Burrier, J. Clader, H. Zhao, 1996, Journal of medicinal chemistry.

The discovery of ezetimibe: a view from outside the receptor.

J. Clader, 2004, Journal of medicinal chemistry.

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

J. Clader, S. Altmann, H. Davis, 2002, Bioorganic & medicinal chemistry letters.

Metabolism and structure activity data based drug design: discovery of (−) SCH 53079 an analog of the potent cholesterol absorption inhibitor (−) SCH 48461

J. Clader, H. Davis, N. Yumibe, 1996 .

New Alcohol Protecting Groups. β,β,β-Trichloroethoxymethyl Ethers

J. Clader, R. M. Jacobson, 1979 .

Synthesis of novel bicyclo[4.1.0]heptane and bicyclo[3.1.0]hexane derivatives as melanin-concentrating hormone receptor R1 antagonists.

W. Greenlee, J. Clader, B. Hawes, 2007, Bioorganic & medicinal chemistry letters.

Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency.

J. Lachowicz, J. Clader, S. Dugar, 2000, Bioorganic & medicinal chemistry letters.

Substituted 2-azaspiro[5.3]nonan-1-ones as potent cholesterol absorption inhibitors: defining a binding conformation for SCH 48461.

J. Clader, H. Davis, S. Dugar, 1995, Journal of medicinal chemistry.

Synthesis of an optically pure 3-unsubstituted β-lactam using an asymmetric Reformatsky reaction and its conversion to cholesterol absorption inhibitors

J. Clader, A. Ganguly, B. Shankar, 1996 .

Trans diastereoselective synthesis of 3-alkyl substituted β-lactams via the acid chloride-imine reaction of nonactivated acid chlorides

J. Clader, D. Burnett, S. Dugar, 1995 .

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

Ruo Xu, William J Greenlee, Daniel J Weston, 2006, Bioorganic & medicinal chemistry.

Ezetimibe and other azetidinone cholesterol absorption inhibitors.

J. Clader, 2005, Current topics in medicinal chemistry.

Synthesis of Fluorescent Biochemical Tools Related to the 2‐Azetidinone Class of Cholesterol Absorption Inhibitors.

J. Clader, H. Davis, D. Burnett, 2002 .

Stereoselective synthesis and biological activity of cis azetidinones as cholesterol absorption inhibitors

J. Clader, A. McPhail, H. Davis, 1996 .

Metabolism and Structure Activity Data Based Drug Design: Discovery of (‐)SCH 53079 (Ia), an Analogue of the Potent Cholesterol Absorption Inhibitor (‐)SCH 48461 (Ib).

J. Clader, H. Davis, N. Yumibe, 1996 .

Three-carbon annelations. Regiocontrolled reactivity of trimethylsilyl- and ethoxyethyl-protected cyanohydrins. Versatile homoenolate and acyl anion equivalents

J. Clader, G. Lahm, R. M. Jacobson, 1980 .

Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease.

Lynn A. Hyde, W. Greenlee, Wei Zhou, 2012, ACS medicinal chemistry letters.

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

Lynn A. Hyde, W. Greenlee, J. Clader, 2009, Bioorganic & medicinal chemistry letters.

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

W. Greenlee, J. Clader, A. Nomeir, 2007 .

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

W. Greenlee, R. Xu, J. Clader, 2010, Bioorganic & medicinal chemistry letters.

Editorial [Hot Topic:Lipid Lowering Agents (Guest Editor: John W. Clader)]

J. Clader, 2005 .

Discovery of SCH 900229, a Potent Presenilin 1 Selective γ-Secretase Inhibitor for the Treatment of Alzheimer's Disease.

W. Greenlee, R. Xu, J. Clader, 2012, ACS medicinal chemistry letters.

Substituted (1,2-diarylethyl)amide acyl-CoA:cholesterol acyltransferase inhibitors: effect of polar groups on in vitro and in vivo activity.

R. Burrier, J. Clader, H. Davis, 1995, Journal of medicinal chemistry.

Inhibitors of platelet-derived growth factor

J. Clader, J. Weinstein, H. Davis, 1994 .

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

Thomas P. Sakmar, Christoph Seibert, A. Trkola, 2003, Journal of Virology.

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.

W. Greenlee, M. Endres, S. Shapiro, 2001, Journal of medicinal chemistry.

Rabbit and human liver contain a novel pentacyclic triterpene ester with acyl-CoA: cholesterol acyltransferase inhibitory activity.

J. Clader, A. McPhail, I. Tabas, 1990, The Journal of biological chemistry.

Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as γ-secretase inhibitors

Ruo Xu, Zhiqiang Zhao, Murali Rajagopalan, 2007 .

Tetrahydroquinoline sulfonamides as γ-secretase inhibitors

Zhiqiang Zhao, Wei Li, William J. Greenlee, 2007 .

Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution.

W. Greenlee, J. Lachowicz, J. Clader, 2001, Bioorganic & medicinal chemistry letters.

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

C. Strader, J. Lachowicz, J. Clader, 2001, Farmaco.

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

Anandan Palani, Christoph Seibert, John P. Moore, 2006, Virology.

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

Zhiqiang Zhao, William J Greenlee, Murali Rajagopalan, 2007, Bioorganic & medicinal chemistry letters.

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

W. Greenlee, R. Xu, J. Clader, 2011, Bioorganic & medicinal chemistry letters.

SAR of tricyclic sulfones as γ-secretase inhibitors

Lynn A. Hyde, W. Greenlee, Mark D. McBriar, 2011 .

Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.

W. Greenlee, Mark D. McBriar, R. Xu, 2010, Bioorganic & medicinal chemistry letters.

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

William J Greenlee, Anandan Palani, W. Greenlee, 2003, Bioorganic & medicinal chemistry letters.

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

Serena Xu, Anandan Palani, William J. Greenlee, 2001, Proceedings of the National Academy of Sciences of the United States of America.

Synthesis and receptor affinities of some conformationally restricted analogues of the dopamine D1 selective ligand (5R)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl- 1H-3-benzazepin-7-ol.

J. Clader, A. McPhail, D. Hou, 1989, Journal of medicinal chemistry.

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

W. Greenlee, J. Clader, B. Hawes, 2007, Bioorganic & medicinal chemistry.

Effects of a selective melanin-concentrating hormone 1 receptor antagonist on food intake and energy homeostasis in diet-induced obese mice.

Mark D. McBriar, H. Guzik, J. Clader, 2006, European journal of pharmacology.

Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.

Walter A. Korfmacher, W. Greenlee, J. Clader, 2015, Bioorganic & medicinal chemistry letters.

Three carbon annelation reagents: unsaturated alpha aminonitriles as homoenolate equivalents

J. Clader, R. M. Jacobson, 1980 .

Biaryl ureas as potent and orally efficacious melanin concentrating hormone receptor 1 antagonists for the treatment of obesity.

William J Greenlee, Anandan Palani, Brian Hawes, 2005, Journal of medicinal chemistry.

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

J. Clader, Y. Wang, John W Clader, 2005, Current pharmaceutical design.

Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo.

Lynn A. Hyde, W. Greenlee, Xiaohong Zhu, 2012, Journal of medicinal chemistry.

Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists.

William J Greenlee, Anandan Palani, Brian Hawes, 2005, Bioorganic & medicinal chemistry letters.

Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics.

Ruo Xu, William J Greenlee, Anandan Palani, 2005, Journal of medicinal chemistry.

Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.

Lynn A. Hyde, R. Xu, J. Clader, 2015, Journal of medicinal chemistry.

New Alcohol Protecting Groups. β,β,β-Trichloroethoxymethyl Ethers

J. Clader, R. M. Jacobson, 1979 .

Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.

W. Greenlee, J. Lachowicz, J. Clader, 2002, Journal of Medicinal Chemistry.

Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists.

W. Greenlee, J. Lachowicz, A. Palani, 2004, Bioorganic & medicinal chemistry letters.

The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease.

Lynn A. Hyde, W. Greenlee, Wei Zhou, 2013, Bioorganic & medicinal chemistry letters.

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

Lynn A. Hyde, G. Higgins, J. Clader, 2013, International journal of Alzheimer's disease.

Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators.

Lynn A. Hyde, W. Greenlee, A. Palani, 2011, Bioorganic & medicinal chemistry letters.

METABOLITES OF CIBENZOLINE: SYNTHESIS OF HYDROXYLATED 1,1‐DIPHENYL‐2‐IMIDAZOLYLCYCLOPROPANES AND 5,5‐DIPHENYL‐2H‐PYRROLO(1,2‐A)IMIDAZOLINES

J. Clader, J. Blount, M. Wirkus, 1985 .

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

John P. Moore, A. Palani, J. Clader, 2006, Virology.

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

Lynn A. Hyde, W. Greenlee, R. Xu, 2011, Bioorganic & medicinal chemistry letters.

Hypocholesterolemic activity of a novel inhibitor of cholesterol absorption, SCH 48461.

R. Burrier, J. Clader, H. Davis, 1995, Atherosclerosis.

SCH 48461, a novel inhibitor of cholesterol absorption

R. Burrier, J. Clader, H. Davis, 1994 .

(‐)‐SCH 57939: Synthesis and Pharmacological Properties of a Potent, Metabolically Stable Cholesterol Absorption Inhibitor.

J. Clader, A. McPhail, H. Davis, 1996 .

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

Mark D. McBriar, H. Guzik, S. Shapiro, 2006, Bioorganic & medicinal chemistry letters.