K. Lyons

发表

(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

G. Scapin, N. Thornberry, R. S. Roy, 2005, Journal of medicinal chemistry.

Utility of unbound plasma drug levels and P-glycoprotein transport data in prediction of central nervous system exposure

K. Lyons, L. Cohen, G. Salituro, 2009, Xenobiotica; the fate of foreign compounds in biological systems.

Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.

You-Jung Park, N. Thornberry, B. Leiting, 2004, Bioorganic & medicinal chemistry letters.

Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.

Joseph L Duffy, Aleksandr Petrov, N. Thornberry, 2005, Bioorganic & medicinal chemistry letters.

Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors.

G. Scapin, N. Thornberry, B. Leiting, 2008, Bioorganic & medicinal chemistry letters.

Potent and selective proline derived dipeptidyl peptidase IV inhibitors.

N. Thornberry, B. Leiting, Sanjeev Kumar, 2004, Bioorganic & medicinal chemistry letters.

Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

Ping Chen, N. Thornberry, B. Leiting, 2004, Bioorganic & medicinal chemistry letters.

4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.

Aleksandr Petrov, N. Thornberry, B. Leiting, 2004, Bioorganic & medicinal chemistry letters.

Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors.

Aleksandr Petrov, N. Thornberry, B. Leiting, 2006, Bioorganic & medicinal chemistry letters.

(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

G. Scapin, N. Thornberry, R. S. Roy, 2006, Journal of medicinal chemistry.

Imidazopyridines: a novel class of hNav1.7 channel blockers.

V. Warren, K. Lyons, G. Kaczorowski, 2008, Bioorganic & medicinal chemistry letters.

Synthesis and SAR of 1,2-trans-(1-hydroxy-3-phenylprop-1-yl)cyclopentane carboxamide derivatives, a new class of sodium channel blockers.

M. Fisher, K. Lyons, M. Wyvratt, 2006, 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.

The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.

M. Maccoss, S. D. de Laszlo, J. Fenyk-Melody, 2002, Bioorganic & medicinal chemistry letters.

A single-run liquid chromatography mass spectrometry method to quantify neuroactive kynurenine pathway metabolites in rat plasma.

C. Dominguez, Laura Orsatti, F. Bonelli, 2015, Journal of pharmaceutical and biomedical analysis.

Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole.

N. Thornberry, B. Leiting, Huaibing He, 2005, Bioorganic & medicinal chemistry letters.

Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).

N. Thornberry, B. Leiting, Dooseop Kim, 2007, Bioorganic & medicinal chemistry letters.

Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.

Youwei Yan, Ping Chen, J. Metzger, 2015, Bioorganic & medicinal chemistry letters.

A novel benzazepinone sodium channel blocker with oral efficacy in a rat model of neuropathic pain.

V. Warren, K. Lyons, G. Kaczorowski, 2013, Bioorganic & medicinal chemistry letters.

Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.

Jun Liang, J. W. Tarpley, M. Fisher, 2005, Bioorganic & medicinal chemistry letters.

Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

Ping Chen, N. Thornberry, B. Leiting, 2004, Bioorganic & medicinal chemistry letters.

Improved Cav2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide.

O. McManus, A. Swensen, J. Herrington, 2013, ACS medicinal chemistry letters.

A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.

O. McManus, A. Swensen, J. Herrington, 2011, Bioorganic & medicinal chemistry letters.

Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain.

K. Lyons, A. Weber, G. Kaczorowski, 2009, Bioorganic & medicinal chemistry letters.

A Peripherally Acting Nav1.7 Sodium Channel Blocker Reverses Hyperalgesia and Allodynia on Rat Models of Inflammatory and Neuropathic Pain

Xiaohua Li, K. Lyons, C. Abbadie, 2009, Anesthesia and analgesia.

Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.

V. Warren, Sanjeev Kumar, M. Fisher, 2010, Bioorganic & medicinal chemistry letters.

Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.

Jun Liang, J. W. Tarpley, M. Fisher, 2005, Bioorganic & medicinal chemistry letters.

Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.

Ping Chen, N. Thornberry, B. Leiting, 2007, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors.

Ping Chen, N. Thornberry, Huaibing He, 2011, Bioorganic & medicinal chemistry letters.

Pyridinesulfonylureas and pyridinesulfonamides as selective bombesin receptor subtype-3 (BRS-3) agonists.

M. Reitman, O. Palyha, R. Nargund, 2011, Bioorganic & medicinal chemistry letters.

Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.

D. Macintyre, V. Warren, K. Lyons, 2007, Bioorganic & medicinal chemistry letters.

The discovery of small molecule carbamates as potent dual α4β1/α4β7 integrin antagonists

M. Maccoss, W. Hagmann, K. Lyons, 2002 .

2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.

K. Lyons, M. Wyvratt, M. Goulet, 2002, Bioorganic & medicinal chemistry letters.

Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.

N. Thornberry, B. Leiting, S. Xu, 2007, Bioorganic & medicinal chemistry letters.

Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.

G. Scapin, N. Thornberry, B. Leiting, 2007, Bioorganic & medicinal chemistry letters.

Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.

D. Macintyre, V. Warren, M. Fisher, 2007, Bioorganic & medicinal chemistry letters.

Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.

K. Lyons, Y. Yang, M. Goulet, 2001, Bioorganic & medicinal chemistry letters.

Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9.

A. Woods, D. Zaller, N. Thornberry, 2005, Diabetes.

Block of Peripheral Nerve Sodium Channels Selectively Inhibits Features of Neuropathic Pain in Rats

O. McManus, J. W. Tarpley, Z. Ali, 2006, Molecular Pharmacology.

Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines.

G. Scapin, N. Thornberry, R. S. Roy, 2008, Journal of medicinal chemistry.

Pharmacokinetics of memantine in rats and mice

C. Dominguez, D. Howland, M. Beconi, 2011, PLoS currents.

The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors.

J. Metzger, G. Scapin, S. Xu, 2016, Bioorganic & medicinal chemistry letters.

Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.

M. Reitman, J. Metzger, O. Palyha, 2011, ACS medicinal chemistry letters.

Synthesis of 7-benzyl-5-(piperidin-1-yl)-6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c][2,7]naphthyridin-1-ylamine and its analogs as bombesin receptor subtype-3 agonists.

J. Metzger, Mark Hadden, O. Palyha, 2010, Bioorganic & Medicinal Chemistry Letters.

Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.

N. Thornberry, B. Leiting, Huaibing He, 2004, Bioorganic & medicinal chemistry letters.

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.

Highly constrained bicyclic VLA-4 antagonists.

M. Maccoss, Gail Forrest, W. Hagmann, 2007, 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.

Analgesic Effects of a Substituted N-Triazole Oxindole (TROX-1), a State-Dependent, Voltage-Gated Calcium Channel 2 Blocker

Clare London, Joseph L Duffy, Owen B McManus, 2010, Journal of Pharmacology and Experimental Therapeutics.

Fosmetpantotenate (RE-024), a phosphopantothenate replacement therapy for pantothenate kinase-associated neurodegeneration: Mechanism of action and efficacy in nonclinical models

S. Harper, D. Elbaum, M. Beconi, 2018, PloS one.

Metabolism and Pharmacokinetics of JM6 in Mice: JM6 Is Not a Prodrug for Ro-61-8048

C. Dominguez, D. Winkler, M. Beconi, 2012, Drug Metabolism and Disposition.

4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.

Joseph L Duffy, G. Scapin, N. Thornberry, 2007, Bioorganic & medicinal chemistry letters.

Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.

G. Scapin, N. Thornberry, B. Leiting, 2006, Bioorganic & medicinal chemistry letters.

Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.

G. Scapin, N. Thornberry, R. S. Roy, 2009, Bioorganic & medicinal chemistry letters.

4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV.

Joseph L Duffy, G. Scapin, N. Thornberry, 2007, Bioorganic & medicinal chemistry letters.

Potent and selective proline derived dipeptidyl peptidase IV inhibitors.

N. Thornberry, B. Leiting, Sanjeev Kumar, 2004, Bioorganic & Medicinal Chemistry Letters.

Prodrug for Ro-61-8048

C. Dominguez, D. Winkler, M. Beconi, 2012 .

Microsoft Word-75872698-file00.docx

D. Winkler, M. Beconi, K. Lyons, 2012 .

Metabolism and Pharmacokinetics of JM6 in Mice: JM6 Is Not a Prodrug for Ro-61-8048

C. Dominguez, D. Winkler, M. Beconi, 2012, Drug Metabolism and Disposition.

Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain.

K. Lyons, A. Weber, G. Kaczorowski, 2009, Bioorganic & medicinal chemistry letters.

Discovery of a novel class of isoxazoline voltage gated sodium channel blockers.

K. Lyons, A. Weber, G. Kaczorowski, 2009, Bioorganic & medicinal chemistry letters.

3-Amino-1,5-benzodiazepinones: potent, state-dependent sodium channel blockers with anti-epileptic activity.

V. Warren, M. Fisher, K. Lyons, 2008, Bioorganic & medicinal chemistry letters.

Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain.

M. Fisher, K. Lyons, M. Wyvratt, 2005, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors.

Ping Chen, N. Thornberry, Huaibing He, 2011, Bioorganic & medicinal chemistry letters.

Analgesic Effects of a Substituted N-Triazole Oxindole (TROX-1), a State-Dependent, Voltage-Gated Calcium Channel 2 Blocker

O. McManus, S. Arneric, A. Swensen, 2010, Journal of Pharmacology and Experimental Therapeutics.

Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.

O. McManus, A. Swensen, J. Herrington, 2012, Journal of medicinal chemistry.

Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines.

G. Scapin, N. Thornberry, R. S. Roy, 2008, Journal of medicinal chemistry.