S. Mills

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Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.

Karen Holmes, Kathy Lyons, Joseph Kessler, 2004, Bioorganic & medicinal chemistry letters.

Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists.

M. Struthers, J. Demartino, S. Mills, 2008, Bioorganic & medicinal chemistry letters.

The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.

M. Maccoss, S. D. de Laszlo, J. Fenyk-Melody, 2001, Bioorganic & medicinal chemistry letters.

Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.

M. Maccoss, W. Hagmann, K. Lyons, 2002, Bioorganic & medicinal chemistry letters.

Selective Small-Molecule Agonists of G Protein–Coupled Receptor 40 Promote Glucose-Dependent Insulin Secretion and Reduce Blood Glucose in Mice

Yun-ping Zhou, J. Berger, N. Thornberry, 2008, Diabetes.

CCR 5 Blockade Modulates Inflammation and Alloimmunity in Primates 1

Miller, R. Pierson, J. Šál, 2007 .

CCR5 Blockade Modulates Inflammation and Alloimmunity in Primates1

R. Pierson, J. Mudgett, J. Demartino, 2007, The Journal of Immunology.

Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist.

Margaret S. Wu, Yun-ping Zhou, A. Howard, 2012, ACS medicinal chemistry letters.

Characterization of a novel and selective cannabinoid CB1 receptor inverse agonist, Imidazole 24b, in rodents.

D. Macneil, J. Metzger, D. Macintyre, 2008, European journal of pharmacology.

Expression and characterization of the chemokine receptor CCR2B from rhesus monkey.

M. Struthers, W. Hanlon, J. Demartino, 2003, Biochemical pharmacology.

An expeditious synthesis of 3-(difluoromethoxy)- and 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridines

M. Maccoss, D. Guiadeen, S. Kothandaraman, 2008 .

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.

D. Hazuda, W. Schleif, E. Emini, 2002, Bioorganic & medicinal chemistry letters.

Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.

Yun-ping Zhou, J. Berger, N. Thornberry, 2010, Bioorganic & medicinal chemistry letters.

3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.

A. Howard, Carina P. Tan, G. Eiermann, 2011, Bioorganic & medicinal chemistry letters.

Chemistry of FK 506

W. Parsons, M. Goulet, S. Mills, 1994 .

2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.

L. Gantert, R. DeVita, R. Hargreaves, 2013, Journal of medicinal chemistry.

Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.

J. Metzger, M. Maccoss, D. Macintyre, 1998, Journal of medicinal chemistry.

Phosphinic acid inhibitors of matrix metalloproteinases

W. Hagmann, R. Stein, S. Mills, 1996 .

Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists.

M. Tota, A. Howard, S. Feighner, 2009, Bioorganic & medicinal chemistry letters.

Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor.

D. Hazuda, W. Schleif, E. Emini, 2004, Bioorganic & Medicinal Chemistry Letters.

Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.

D. Hazuda, Ping Chen, W. Schleif, 2004, Bioorganic & medicinal chemistry letters.

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.

D. Hazuda, W. Schleif, E. Emini, 2004, Bioorganic & medicinal chemistry letters.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.

D. Hazuda, Ping Chen, W. Schleif, 2003, Bioorganic & medicinal chemistry letters.

CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.

D. Hazuda, W. Schleif, E. Emini, 2002, Bioorganic & medicinal chemistry letters.

Development of aprepitant, the first neurokinin‐1 receptor antagonist for the prevention of chemotherapy‐induced nausea and vomiting

R. Hargreaves, J. Brands, J. Hale, 2011, Annals of the New York Academy of Sciences.

Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.

G. Chrebet, M. Forrest, H. Rosen, 2004, Bioorganic & medicinal chemistry letters.

Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.

G. Chrebet, H. Rosen, J. Hale, 2004, Bioorganic & medicinal chemistry letters.

Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.

J. Chen, L. V. D. van der Ploeg, L. Shearman, 2005, Bioorganic & medicinal chemistry letters.

Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.

M. Struthers, M. Maccoss, J. Demartino, 2009, Bioorganic & medicinal chemistry letters.

Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities.

Margaret S. Wu, Michael E. Lassman, J. Berger, 2010, Bioorganic & medicinal chemistry letters.

Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics.

G. Kaczorowski, B. Priest, Haifeng Tang, 2012, ACS medicinal chemistry letters.

Conformational studies of 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists leading to new spirocyclic antagonists.

M. Struthers, J. Demartino, G. Butora, 2008, Bioorganic & medicinal chemistry letters.

Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor.

S. Boyce, R. DeVita, J. Demartino, 2010, Bioorganic & medicinal chemistry letters.

Substituted fused bicyclic pyrrolizinones as potent, orally bioavailable hNK1 antagonists.

P. Davies, S. Boyce, M. Reibarkh, 2010, Bioorganic & medicinal chemistry letters.

Fused bicyclic pyrrolizinones as new scaffolds for human NK1 antagonists.

S. Boyce, R. DeVita, J. Demartino, 2008, Bioorganic & medicinal chemistry.

Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.

R. DeVita, K. Tsao, S. Mills, 2007, Bioorganic & medicinal chemistry letters.

Characterization of the binding and activity of a high affinity, pseudoirreversible morpholino tachykinin NK1 receptor antagonist.

C. Strader, M. Tota, M. Maccoss, 1997, European journal of pharmacology.

Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.

G. Chrebet, H. Rosen, J. Hale, 2004, Bioorganic & medicinal chemistry letters.

The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.

R. DeVita, H. Burns, R. Hargreaves, 2007, Bioorganic & medicinal chemistry letters.

1,2,4-Triacylpiperidine substance p antagonists: Separation of affinities for the NK-1 receptor and the L-type calcium channel

M. Maccoss, P. Hutson, Smita Patel, 1995 .

1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists.

C. Strader, W. Greenlee, M. Maccoss, 1993 .

Comparison of the functional blockade of rat substance P (NK1) receptors by GR205171, RP67580, SR140333 and NKP-608

G. Bentley, K. Tsao, R. Kilburn, 2003, Neuropharmacology.

Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes.

G. Chrebet, J. Hale, S. Mills, 2006, Bioorganic & medicinal chemistry letters.

Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.

J. Chen, L. V. D. van der Ploeg, L. Shearman, 2005, Bioorganic & medicinal chemistry letters.

Discovery of 3,5-bis(trifluoromethyl)benzyl L-arylglycinamide based potent CCR2 antagonists.

M. Maccoss, W. Hanlon, G. Butora, 2006, Bioorganic & medicinal chemistry letters.

Distinct mechanism for antidepressant activity by blockade of central substance P receptors.

R G Hill, David J. Smith, J. Feighner, 1998, Science.

Total synthesis of (.+-.)-methyl homodaphniphyllate

S. Davidsen, C. Heathcock, S. Mills, 1986 .

Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane.

D. Hazuda, W. Schleif, E. Emini, 2005, Bioorganic & medicinal chemistry letters.

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains.

Karen Holmes, Joseph Kessler, Anthony Carella, 2004, Bioorganic & medicinal chemistry letters.

Design, synthesis, and biological evaluation of aminopyrazine derivatives as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).

K. Chapman, James E. Thompson, J. Hale, 2015, Bioorganic & medicinal chemistry letters.

Disubstituted pyrimidines as Lck inhibitors.

A. Woods, D. Zaller, J. Hermes, 2009, Bioorganic & Medicinal Chemistry Letters.

Chemistry of tricarbonyl hemiketals and application of Evans technology to the total synthesis of the immunosuppressant (-)-FK-506

R. Reamer, S. Mills, T. K. Jones, 1990 .

Discovery of 3-piperidinyl-1-cyclopentanecarboxamide as a novel scaffold for highly potent CC chemokine receptor 2 antagonists.

M. Maccoss, G. Butora, W. Parsons, 2007, Journal of medicinal chemistry.

A comparison of secondary and tertiary amides as directors of ortho and adjacent benzylic lithiation and of asymmetric induction in ortho lithiated benzamides

S. Mills, C. Chen, P. Beak, 1983 .

Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.

J. Metzger, M. Maccoss, D. Macintyre, 2000, Journal of medicinal chemistry.

2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.

C. Strader, J. Metzger, M. Maccoss, 1996, Journal of medicinal chemistry.

Chapter 6. Recent Advances in Neurokinin Receptor Antagonists

S. Mills, 1997 .

1,2,3-Trisubstituted cyclohexyl substance P antagonists: Significance of the ring nitrogen in piperidine-based NK-1 receptor antagonists

C. Strader, D. Underwood, M. Maccoss, 1995 .

Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.

Joseph Kessler, Anthony Carella, D. Hazuda, 2005, Bioorganic & medicinal chemistry letters.

Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).

K. Chapman, James E. Thompson, J. Hale, 2009, Bioorganic & medicinal chemistry letters.

α-Aminothiazole-γ-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists

M. Maccoss, W. Parsons, Changyou Zhou, 2007 .

An Efficient Procedure for the Synthesis of p-Anisidine Phenylglyoxal Imine from Acetophenone

R. Volante, S. Mills, Richard A Desmond, 1989 .

Daphniphyllum alkaloids. 10. Classical total synthesis of methyl homodaphniphyllate

S. Davidsen, C. Heathcock, S. Mills, 1992 .

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements.

M. Maccoss, J. Demartino, L. Malkowitz, 2001, Bioorganic & medicinal chemistry letters.

Discovery of a Potent and Orally Bioavailable CCR2 and CCR5 Dual Antagonist

M. Struthers, J. Demartino, R. Kilburn, 2010 .

Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.

S. A. Parent, G. Chrebet, M. Forrest, 2005, Journal of medicinal chemistry.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity.

D. Hazuda, W. Schleif, E. Emini, 2002, Bioorganic & medicinal chemistry letters.

Dipole-stabilized carbanions: evidence for a complex in the .alpha.'-lithiation of N,N-dimethyl-2,4,6-triisopropylbenzamide

Stanley G. Smith, D. Kempf, S. Mills, 1983 .

Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.

G. Chrebet, H. Rosen, C. L. Lynch, 2004, Bioorganic & medicinal chemistry letters.

Solvent effects on keto-enol equilibria: tests of quantitative models

S. Mills, P. Beak, 1985 .

Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: a molecular modeling-guided mutagenesis study of the binding pocket.

M. Maccoss, J. Demartino, C. L. Lynch, 2003, Biochemistry.

In vitro and in vivo predictors of the anti-emetic activity of tachykinin NK1 receptor antagonists.

M. Maccoss, R. Hargreaves, C. Swain, 1997, European journal of pharmacology.

Tetrahydroindolizinone NK1 antagonists.

R. DeVita, K. Tsao, G. Morriello, 2010, Bioorganic & medicinal chemistry letters.

Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.

J. Metzger, M. Maccoss, D. Macintyre, 2006, Bioorganic & medicinal chemistry letters.

The novel NK1 receptor antagonist MK–0869 (L–754,030) and its water soluble phosphoryl prodrug, L–758,298, inhibit acute and delayed cisplatin-induced emesis in ferrets

S. Tye, R. Hargreaves, F. D. Tattersall, 2000, Neuropharmacology.

Concise preparation of 8-trifluoromethyltetrahydro-6H-pyrido [1,2-a] pyrazine-6-one

M. Maccoss, G. Butora, D. Guiadeen, 2009 .

Diastereospecific, non-racemic synthesis of the C.20–C.34 segment of the novel immunosuppressant FK-506

R. Volante, R. Reamer, S. Mills, 1988 .

Novel, Orally Bioavailable γ-Aminoamide CC Chemokine Receptor 2 (CCR2) Antagonists

M. Maccoss, W. Parsons, S. Mills, 2006 .

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes.

E A Emini, D. Hazuda, W. Schleif, 2001, Bioorganic & medicinal chemistry letters.

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 3: a proposed pharmacophore model for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-[4-(substituted)piperidin-1-yl]butanes.

M. Maccoss, J. Demartino, P E Finke, 2001, Bioorganic & medicinal chemistry letters.

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes.

E A Emini, D. Hazuda, W. Schleif, 2001, Bioorganic & medicinal chemistry letters.

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes.

E A Emini, D. Hazuda, W. Schleif, 2001, Bioorganic & medicinal chemistry letters.

SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.

G. Chrebet, J. Hale, S. Mills, 2007, Bioorganic & medicinal chemistry letters.

Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.

G. Chrebet, M. Forrest, H. Rosen, 2004, Bioorganic & medicinal chemistry letters.

Total synthesis of immunosuppressant (-)-FK-506

R. Volante, R. Reamer, S. Mills, 1989 .

Total Synthesis of the Immunosuppressant (‐)‐FK‐506.

R. Volante, R. Reamer, S. Mills, 1989 .

A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.

M. Ferrer, B. Strulovici, S. A. Parent, 2004, Journal of medicinal chemistry.

Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.

G. Chrebet, P. Váchal, J. Hale, 2006, Bioorganic & Medicinal Chemistry Letters.

2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors.

G. Chrebet, C. L. Lynch, J. Hale, 2006, Bioorganic & medicinal chemistry letters.

Identification of Leu276 of the S1P1 Receptor and Phe263 of the S1P3 Receptor in Interaction with Receptor Specific Agonists by Molecular Modeling, Site-Directed Mutagenesis, and Affinity Studies

S. A. Parent, G. Chrebet, Q. Deng, 2007, Molecular Pharmacology.

The discovery of 3-(N-alkyl)aminopropylphosphonic acids as potent S1P receptor agonists.

G. Chrebet, H. Rosen, J. Hale, 2004, Bioorganic & medicinal chemistry letters.

1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.

Karen Holmes, Joseph Kessler, Anthony Carella, 2003, Bioorganic & medicinal chemistry letters.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.

D. Hazuda, W. Schleif, E. Emini, 2001, Bioorganic & medicinal chemistry letters.

Synthesis and study of alendronate derivatives as potential prodrugs of alendronate sodium for the treatment of low bone density and osteoporosis.

M. Maccoss, P. Váchal, F. Kesisoglou, 2006, Journal of medicinal chemistry.

Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.

R. DeVita, R. Hargreaves, K. Tsao, 2009, Journal of medicinal chemistry.

Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists.

M. Maccoss, W. Hagmann, K. Lyons, 2002, Bioorganic & medicinal chemistry letters.

Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.

M. Maccoss, W. Hagmann, K. Lyons, 2002, Bioorganic & Medicinal Chemistry Letters.

Spiroimidazolidinone NPC1L1 inhibitors. Part 2: structure-activity studies and in vivo efficacy.

Daniel R. McMasters, J. Lisnock, R. DeVita, 2010, Bioorganic & medicinal chemistry letters.

1,3,4-Trisubstituted Pyrrolidine CCR5 Receptor Antagonists. Part 1. Discovery of the Pyrrolidine Scaffold and Determination of Its Stereochemical Requirements.

M. Maccoss, J. Demartino, L. Malkowitz, 2001 .

2,5-Disubstituted pyrrolidine carboxylates as potent, orally active sphingosine-1-phosphate (S1P) receptor agonists.

J. Hale, S. Mills, S. Mandala, 2006, Bioorganic & medicinal chemistry letters.

Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.

D. Hazuda, W. Schleif, E. Emini, 2001, Bioorganic & medicinal chemistry letters.

Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection.

D. Hazuda, W. Schleif, E. Emini, 2001, Bioorganic & medicinal chemistry letters.

Characterization of the interaction of diacylpiperazine antagonists with the human neurokinin-1 receptor: identification of a common binding site for structurally dissimilar antagonists.

C. Strader, C. Swain, S. Mills, 1995, Molecular pharmacology.

Immune Cell Regulation and Cardiovascular Effects of Sphingosine 1-Phosphate Receptor Agonists in Rodents Are Mediated via Distinct Receptor Subtypes

R. Proia, M. Forrest, C. Meyers, 2004, Journal of Pharmacology and Experimental Therapeutics.

Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.

G. Chrebet, H. Rosen, C. L. Lynch, 2004, Bioorganic & medicinal chemistry letters.

A Highly Selective Method for the Synthesis of E‐α‐Methyl‐α,β‐Unsaturated Aldehydes.

R. Volante, S. Mills, Richard A Desmond, 1989 .

Supporting Information Synthesis and Study of Alendronate Derivatives as Potential Prodrugs of Alendronate Sodium; for the Treatment of Low Bone Density and Osteoporosis

M. Maccoss, F. Kesisoglou, J. Hale, 2006 .

Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics.

G. Kaczorowski, B. Priest, Haifeng Tang, 2012, ACS medicinal chemistry letters.