C. Davis

发表

AMG 580: A Novel Small Molecule Phosphodiesterase 10A (PDE10A) Positron Emission Tomography Tracer

N. Chen, E. Hu, R. Kunz, 2015, The Journal of Pharmacology and Experimental Therapeutics.

The identification of [2-(14)C]2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine metabolites in humans.

K. Turteltaub, K. Kulp, M. Knize, 1999, Carcinogenesis.

Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery.

J. Macor, R. Schartman, G. Thalody, 2013, Bioorganic & medicinal chemistry letters.

In vivo human metabolism of [2-14C]2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP).

K. Turteltaub, K. Kulp, M. Knize, 1999, Cancer letters.

AMG2850, a potent and selective TRPM8 antagonist, is not effective in rat models of inflammatory mechanical hypersensitivity and neuropathic tactile allodynia

C. Stucky, N. Gavva, Andy D. Weyer, 2015, Naunyn-Schmiedeberg's Archives of Pharmacology.

Discovery of a cyclopentylamine as an orally active dual NK1 receptor antagonist-serotonin reuptake transporter inhibitor.

J. Macor, R. Westphal, R. Bertekap, 2014, Bioorganic & medicinal chemistry letters.

Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.

J. Macor, R. Westphal, R. Bertekap, 2013, Bioorganic & 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.

Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A).

E. Hu, S. Chmait, J. Treanor, 2014, ACS medicinal chemistry letters.

Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and effici

Kimberly A. Widmann, J. Macor, R. Schartman, 2008, Journal of medicinal chemistry.

Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.

S. Dworetzky, Ronald J. Knox, C. Polson, 2003, Journal of medicinal chemistry.

The Role of Drug Metabolism in Toxicity

C. Davis, U. Hanumegowda, 2010 .

AMG2850, a potent and selective TRPM8 antagonist, is not effective in rat models of inflammatory mechanical hypersensitivity and neuropathic tactile allodynia

C. Stucky, N. Gavva, Andy D. Weyer, 2015, Naunyn-Schmiedeberg's Archives of Pharmacology.

An Introduction to Metabolic Reaction Phenotyping

A. D. Rodrigues, C. Davis, 2010 .

Cytochrome P450 reaction-phenotyping: an industrial perspective

A. D. Rodrigues, Hongjiang Zhang, Michael W Sinz, 2007, Expert opinion on drug metabolism & toxicology.

Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).

E. Hu, R. Kunz, Shannon Rumfelt, 2013, Journal of medicinal chemistry.

Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists.

Kimberly A. Widmann, J. Macor, R. Schartman, 2013, Bioorganic & medicinal chemistry letters.

Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).

E. Hu, R. Kunz, N. Chen, 2014, Journal of medicinal chemistry.

NK1 receptor antagonism lowers occupancy requirement for antidepressant-like effects of SSRIs in the Gerbil forced swim test

J. Macor, R. Pieschl, T. Molski, 2013, Neuropharmacology.

Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.

H. Monenschein, M. Horner, M. Bartberger, 2018, Journal of medicinal chemistry.

Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists.

Kimberly A. Widmann, Ping Chen, J. Macor, 2020, Bioorganic & medicinal chemistry letters.

Selection of a Suitable Physical Form and Development of a Crystallization Process for a PDE10A Inhibitor Exhibiting Enantiotropic Polymorphism

Jodi Liu, Christopher J. Borths, Robert E. Saw, 2015 .

Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.

V. Gribkoff, Ping Chen, S. Dworetzky, 2013, Bioorganic & medicinal chemistry letters.

Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation

N. Gavva, S. Lehto, C. Davis, 2012, Molecular pain.

Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.

E. Hu, R. Kunz, N. Chen, 2014, Bioorganic & medicinal chemistry.

Involvement of Multiple Cytochrome P450 and UDP-Glucuronosyltransferase Enzymes in the in Vitro Metabolism of Muraglitazar

W. Humphreys, Hongjiang Zhang, Donglu Zhang, 2007, Drug Metabolism and Disposition.

Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonists: Heterocyclic Modification of a Novel Azepinone Lead.

Kimberly A. Widmann, Ping Chen, J. Macor, 2021, Bioorganic & medicinal chemistry letters.

The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1.

Kimberly A. Widmann, J. Macor, R. Schartman, 2012, Bioorganic & medicinal chemistry letters.

AMG 580: A Novel Small Molecule Phosphodiesterase 10A (PDE10A) Positron Emission Tomography Tracer

N. Chen, E. Hu, R. Kunz, 2015, The Journal of Pharmacology and Experimental Therapeutics.

E. Hu, R. Kunz, N. Chen, 2014, Journal of medicinal chemistry.

Initial characterization of a PDE10A selective positron emission tomography tracer [11C]AMG 7980 in non-human primates.

D. Hwang, E. Hu, Shannon Rumfelt, 2014, Nuclear medicine and biology.

Discovery of Phosphodiesterase 10A (PDE10A) PET Tracer AMG 580 to Support Clinical Studies.

D. Hwang, E. Hu, R. Kunz, 2016, ACS medicinal chemistry letters.

Radiosynthesis and initial characterization of a PDE10A specific PET tracer [18F]AMG 580 in non-human primates.

D. Hwang, E. Hu, J. Treanor, 2015, Nuclear medicine and biology.