M. Norman

发表

Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.

N. Chen, J. Treanor, C. Dominguez, 2007, Journal of medicinal chemistry.

Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.

N. Chen, J. Treanor, V. Viswanadhan, 2007, Journal of medicinal chemistry.

Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).

K. Rex, Matthew R. Lee, C. Dominguez, 2008, Journal of Medicinal Chemistry.

Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.

D. Whittington, Matthew R. Lee, C. Dominguez, 2012, Journal of medicinal chemistry.

Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.

J. Treanor, C. Dominguez, C. Fotsch, 2006, Journal of medicinal chemistry.

4-Aminopyrimidine tetrahydronaphthols: a series of novel vanilloid receptor-1 antagonists with improved solubility properties.

J. Treanor, E. Doherty, N. Gavva, 2008, Bioorganic & medicinal chemistry letters.

Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.

J. Treanor, N. Gavva, Rami Tamir, 2007, Bioorganic & medicinal chemistry letters.

Structure-activity relationships of a series of pyrrolo[3,2-d]pyrimidine derivatives and related compounds as neuropeptide Y5 receptor antagonists.

N. Chen, Z. Chen, V. Santora, 2000, Journal of medicinal chemistry.

Synthesis and structure-activity relationships of trisubstituted phenyl urea derivatives as neuropeptide Y5 receptor antagonists.

N. Chen, C. Fotsch, M. Norman, 2001, Journal of medicinal chemistry.

Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.

Kristin L. Andrews, Jiandong Zhang, S. Chmait, 2015, Journal of medicinal chemistry.

Nonthermal Activation of Transient Receptor Potential Vanilloid-1 Channels in Abdominal Viscera Tonically Inhibits Autonomic Cold-Defense Effectors

A. A. Romanovsky, Andrej A Romanovsky, J. Treanor, 2007, The Journal of Neuroscience.

Antihyperalgesic Effects of (R,E)-N-(2-Hydroxy-2,3-dihydro-1H-inden-4-yl)-3-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenyl)-acrylamide (AMG8562), a Novel Transient Receptor Potential Vanilloid Type 1 Modulator That Does Not Cause Hyperthermia in Rats

J. Louis, B. H. Manning, N. Gavva, 2008, Journal of Pharmacology and Experimental Therapeutics.

Delayed administration of a potent cyclin dependent kinase and glycogen synthase kinase 3 β inhibitor produces long-term neuroprotection in a hypoxia-ischemia model of brain injury

G. Robertson, M. Norman, E. Magal, 2008, Neuroscience.

Discovery of AMG 458: A Potent, Selective, and Orally Bioavailable c-Met Inhibitor

K. Rex, Matthew R. Lee, S. Bellon, 2008 .

Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.

N. Chen, C. Fotsch, A. Bannon, 2005, Bioorganic & medicinal chemistry letters.

Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK).

Kristin L. Andrews, D. Powers, R. Kendall, 2015, Journal of medicinal chemistry.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket.

S. Chmait, M. Bartberger, S. Jordan, 2014, Journal of medicinal chemistry.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.

R. Kunz, Jiandong Zhang, S. Chmait, 2014, Journal of medicinal chemistry.

Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.

J. Treanor, C. Dominguez, J. Katon, 2007, Journal of medicinal chemistry.

Structure-activity relationship (SAR) investigations of tetrahydroquinolines as BKCa agonists.

E. Doherty, M. Norman, J. Ligutti, 2010, Bioorganic & medicinal chemistry letters.

Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.

G. Rigdon, M. Norman, J. Thompson, 1996, Journal of medicinal chemistry.

Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.

Jiandong Zhang, T. Osslund, C. Henley, 2007, Bioorganic & medicinal chemistry letters.

A general method for the facile synthesis of optically active 2-substituted piperazines via functionalized 2,5-diketopiperazines

M. Norman, Mitchell Denti, K. Ashton, 2014 .

Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists.

J. Treanor, P. Chakrabarti, Yunxin Y Bo, 2008, Bioorganic & medicinal chemistry letters.

Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists.

M. Bartberger, Yunxin Y Bo, N. Gavva, 2012, Journal of medicinal chemistry.

Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling.

D. Whittington, H. Bregman, Matthew R. Lee, 2016, Bioorganic & medicinal chemistry.

Structure-activity relationships of a series of substituted benzamides: potent D2/5-HT2 antagonists and 5-HT1a agonists as neuroleptic agents.

G. Rigdon, M. Norman, W. Hall, 1996, Journal of medicinal chemistry.

Effect of linking bridge modifications on the antipsychotic profile of some phthalimide and isoindolinone derivatives.

G. Rigdon, M. Norman, D. Minick, 1996, Journal of medicinal chemistry.

Cyclic benzamides as mixed dopamine D2/serotonin 5-HT2 receptor antagonists: potential atypical antipsychotic agents.

B. Cooper, G. Rigdon, M. Norman, 1994, Journal of medicinal chemistry.

Acyclic stereoselection. 29. Stereoselection in the Michael addition reaction. 1. The Mukaiyama-Michael reaction

D. Uehling, M. Norman, C. Heathcock, 1985 .

Improved synthesis of N-benzyl-5-ethyl-1,2,3,4-tetrahydropyridine

M. Norman, C. Heathcock, 1988 .

Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis.

S. Chmait, M. Bartberger, S. Jordan, 2015, Journal of medicinal chemistry.

Acyclic stereoselection. 29. Stereoselection in the Michael addition reaction. 1. The Mukaiyama-Michael reaction

D. Uehling, M. Norman, C. Heathcock, 1985 .

Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.

J. Treanor, P. Chakrabarti, N. Gavva, 2007, Bioorganic & medicinal chemistry letters.

A short, facile synthesis of 5-substituted 3-amino-1H-pyrrole-2-carboxylates.

Y. Lu, C. Fotsch, M. Norman, 2000, The Journal of organic chemistry.

Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.

Daniel J. Freeman, R. Wahl, J. McCarter, 2011, Journal of medicinal chemistry.

Conformationally restricted analogues of remoxipride as potential antipsychotic agents.

E. Hollingsworth, M. Norman, J. Kelley, 1993, Journal of medicinal chemistry.

Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.

Ming Huang, Hong Sun, Eileen Johnson, 2007, Journal of medicinal chemistry.

Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.

H. Monenschein, M. Bartberger, Yunxin Y Bo, 2014, Journal of medicinal chemistry.

AMG 9810 [(E)-3-(4-t-Butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a Novel Vanilloid Receptor 1 (TRPV1) Antagonist with Antihyperalgesic Properties

Mark H. Norman, J. Treanor, T. Vanderah, 2005, Journal of Pharmacology and Experimental Therapeutics.

The Vanilloid Receptor TRPV1 Is Tonically Activated In Vivo and Involved in Body Temperature Regulation

J. Treanor, T. Juan, J. Louis, 2007, The Journal of Neuroscience.

Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists.

J. Treanor, R. Hungate, E. Doherty, 2005, Bioorganic & medicinal chemistry letters.

Proton Activation Does Not Alter Antagonist Interaction with the Capsaicin-Binding Pocket of TRPV1

J. Treanor, J. Louis, N. Gavva, 2005, Molecular Pharmacology.

Novel Synthesis of (+/−)-cis-4-Amino-2-cyclopentene-1-methanol, a Key Intermediate in the Preparation of Carbocyclic 2′,3′-Didehydro-2′,3′-dideoxy Nucleosides

M. Norman, M. Almond, B. Reitter, 1992 .

Analogues of the potential antipsychotic agent 1192U90: amide modifications.

M. Norman, L. T. Schaller, F. Navas, 1998, Bioorganic & medicinal chemistry.

Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).

Michael G Kelly, J. Cheetham, M. Jarosinski, 2003, Bioorganic & medicinal chemistry letters.

TOTAL SYNTHESIS OF ()-VALLESAMIDINE

M. Norman, C. Heathcock, D. Dickman, 1990 .

Novel transformations leading to 3-benzylindolizidin-2-ones

M. Norman, C. Heathcock, M. H. Norman, 1987 .

Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.

K. Rex, Matthew R. Lee, C. Dominguez, 2012, Journal of medicinal chemistry.

Structural elucidation of an oxazolo[5,4-b]pyridine : an alternative cyclization product related to nevirapine

M. Norman, G. Martin, D. Minick, 1993 .