M. H. Norman

发表

Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans

Mark J. Rose, Andrej A. Romanovsky, A. A. Romanovsky, 2008, PAIN.

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.

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.

dioxin-6-yl ) acrylamide ] , a Novel Vanilloid Receptor 1 ( TRPV 1 ) Antagonist with Antihyperalgesic Properties

J. Treanor, T. Vanderah, J. Louis, 2005 .

Novel transformations leading to 3-benzylindolizidin-2-ones

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

1192U90 in Animal Tests That Predict Antipsychotic Efficacy, Anxiolysis, and Extrapyramidal Side Effects

B. Cooper, J. L. Howard, G. Rigdon, 1996, Neuropsychopharmacology.

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 .

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

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

TOTAL SYNTHESIS OF ()-VALLESAMIDINE

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

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.

Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.

Daniel J. Freeman, J. McCarter, Nancy Zhang, 2012, Journal of medicinal chemistry.

Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: investigations of various 6,5-heterocycles to improve metabolic stability.

Daniel J. Freeman, J. McCarter, Nancy Zhang, 2011, Journal of medicinal 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.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series.

R. Kunz, S. Chmait, M. Bartberger, 2014, Journal of medicinal chemistry.

Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.

Daniel J. Freeman, J. McCarter, Nancy Zhang, 2012, Bioorganic & medicinal chemistry letters.

Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.

J. McCarter, D. Whittington, A. Tasker, 2014, Bioorganic & medicinal chemistry letters.

Behavioral characterization of neuropeptide Y knockout mice

A. Bannon, M. McCaleb, J. M. Francis, 2000, Brain Research.

The Transient Receptor Potential Vanilloid-1 Channel in Thermoregulation: A Thermosensor It Is Not

A. A. Romanovsky, S. Morrison, A. Steiner, 2009, Pharmacological Reviews.

The Transient Receptor Potential Vanilloid-1 Channel in Thermoregulation : A Thermosensor

S. Morrison, A. Steiner, A. Romanovsky, 2009 .

Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.

Daniel J. Freeman, J. McCarter, D. Whittington, 2012, Journal of 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.

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.

Is clozapine selective for the dopamine D4 receptor?

G. Rigdon, M. Durcan, P. F. Morgan, 1995, Life sciences.

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

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

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

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

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.

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.

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.

Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors

R. Wahl, Jiandong Zhang, S. Chmait, 2013, Nature.

The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors.

J. McCarter, D. Whittington, Nancy Zhang, 2015, Bioorganic & medicinal chemistry letters.

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.

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.

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.

Discovery of ( R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4- b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3 H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies.

K. Rex, J. Canon, B. Herberich, 2019, Journal of medicinal chemistry.

Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.

K. Rex, B. Herberich, Matthew R. Lee, 2016, 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.

Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists.

P. Chakrabarti, E. Doherty, A. Bannon, 2008, Journal of medicinal chemistry.

Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.

Daniel J. Freeman, Hongyu Liao, Nancy Zhang, 2011, Journal of medicinal chemistry.

4-(Heteroarylthio)-2-biphenylyltetrazoles as nonpeptide angiotensin II antagonists.

C. Cowan, R. Steffen, C. Andrews, 1995, Journal of Medicinal Chemistry.

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.

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

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

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.

Synthesis of 13C‐ and 14C‐labeled 1192U90, an ortho‐amino benzamide with a preclinical atypical antipsychotic profile

S. Gabriel, M. H. Norman, 1996 .

Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity.

L. Arik, E. Laird, V. Viswanadhan, 2007, Journal of medicinal chemistry.

Repeated Administration of Vanilloid Receptor TRPV1 Antagonists Attenuates Hyperthermia Elicited by TRPV1 Blockade

J. Treanor, L. Arik, C. Henley, 2007, Journal of Pharmacology and Experimental Therapeutics.

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.

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.

TRPV1 modulator that does not cause hyperthermia in rats

J. Louis, B. H. Manning, N. Gavva, 2008 .

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

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

Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.

N. Chen, J. Treanor, P. Chakrabarti, 2005, Journal of medicinal chemistry.

Three-dimensional quantitative structure-activity relationships and activity predictions of human TRPV1 channel antagonists: comparative molecular field analysis and comparative molecular similarity index analysis of cinnamides.

V. Viswanadhan, Yaxiong Sun, M. H. Norman, 2007, Journal of Medicinal Chemistry.

Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists.

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

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.

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

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

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.

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.

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.

Design and synthesis of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors.

C. Henley, D. Powers, R. Rzasa, 2009, Bioorganic & medicinal chemistry letters.

Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.

V. Viswanadhan, T. Osslund, D. Powers, 2007, Bioorganic & 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.

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

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

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.

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.

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

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

Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.

C. Fotsch, Markian M Stec, N. Xi, 2004, Bioorganic & medicinal chemistry letters.

Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.

J. Cheetham, K. Stark, C. Fotsch, 2003, 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.

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.

Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.

G. Rigdon, M. Norman, J. Thompson, 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.

P450-mediated O-demethylated metabolite is responsible for rat hepatobiliary toxicity of pyridyltriazine-containing PI3K inhibitors.

D. Branstetter, H. Lebrec, R. Subramanian, 2014, Toxicological sciences : an official journal of the Society of Toxicology.

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

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

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