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Your search keyword '"Perry Leung"' showing total 3 results
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3 results on '"Perry Leung"'

1. Characterization of JNJ-2482272 [4-(4-Methyl-2-(4-(Trifluoromethyl)Phenyl)Thiazole-5-yl) Pyrimidine-2-Amine] As a Strong Aryl Hydrocarbon Receptor Activator in Rat and Human

Author

Kevin J. Coe, Mark Feinstein, J. William Higgins, Perry Leung, Brian P. Scott, Judy Skaptason, Yuen Tam, Laurie P. Volak, Jennifer Kinong, Anton Bittner, Heather McAllister, Nathan M. Lim, Michael Hack, and Tatiana Koudriakova

Subjects
Pharmacology, Thiazoles, Pyrimidines, Receptors, Aryl Hydrocarbon, Cytochrome P-450 CYP1A1, Pharmaceutical Science, Animals, Humans, Amines, Rats
Abstract

[4-(4-Methyl-2-(4-(trifluoromethyl)phenyl)thiazole-5-yl)pyrimidine-2-amine] (JNJ-2482272), under investigation as an anti-inflammatory agent, was orally administered to rats once daily at 60 mg/kg for 6 consecutive days. Despite high plasma exposure after single administration (C

Published
2021

2. Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: Identification of candidates for clinical development

Author

Pascal Bonaventure, Anita M. Everson, S. Timothy Motley, Brian Lord, Jonathan Shelton, Raymond Rynberg, Ian Fraser, Christine Dugovic, Diane Nepomuceno, Leah Aluisio, Michael A. Letavic, John M. Keith, Perry Leung, Michele C. Rizzolio, John R. Atack, Tatiana Koudriakova, Kia Sepassi, Timothy W. Lovenberg, Mark A. Feinstein, Kiev S. Ly, Nicholas I. Carruthers, Kirsten L. Morton, Xiaohui Jiang, and Kenway Hoey

Subjects
Pyridines, medicine.drug_class, Clinical Biochemistry, Drug Evaluation, Preclinical, Pharmaceutical Science, Carboxamide, Biochemistry, Chemical synthesis, chemistry.chemical_compound, In vivo, Drug Discovery, medicine, Animals, Molecular Biology, Organic Chemistry, Antagonist, Azepines, Rat brain, Amides, In vitro, Rats, chemistry, Molecular Medicine, Histamine H3 receptor, Histamine, Histamine H3 Antagonists
Abstract

The pre-clinical characterization of novel aryloxypyridine amides that are histamine H(3) receptor antagonists is described. These compounds are high affinity histamine H(3) ligands that penetrate the CNS and occupy the histamine H(3) receptor in rat brain. Several compounds were extensively profiled pre-clinically leading to the identification of two compounds suitable for nomination as development candidates.

Published
2010
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3. Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists

Author

John R. Atack, Kirsten L. Morton, Emily M. Stocking, Christine Dugovic, Akinola Soyode-Johnson, Anita M. Everson, Ian Fraser, Xiaohui Jiang, Brian Lord, Jonathan Shelton, Chandravadan R. Shah, Leah Aluisio, Pascal Bonaventure, Perry Leung, Kiev S. Ly, Nicholas I. Carruthers, Diane Nepomuceno, and Michael A. Letavic

Subjects
Pyrrolidines, Stereochemistry, Clinical Biochemistry, Drug Evaluation, Preclinical, Administration, Oral, Pharmaceutical Science, Pharmacology, Biochemistry, Mice, Structure-Activity Relationship, Histamine receptor, Dogs, Oral administration, Drug Discovery, Animals, Humans, Receptors, Histamine H3, Molecular Biology, Chemistry, Organic Chemistry, Brain, Azepines, Rat brain, Rats, Molecular Medicine, Histamine H3 receptor, Histamine H3 Antagonists
Abstract

Pre-clinical characterization of novel substituted pyrrolidines that are high affinity histamine H(3) receptor antagonists is described. These compounds efficiently penetrate the CNS and occupy the histamine H(3) receptor in rat brain following oral administration. One compound, (2S,4R)-1-[2-(4-cyclobutyl-[1,4]diazepane-1-carbonyl)-4-(3-fluoro-phenoxy)-pyrrolidin-1-yl]-ethanone, was extensively profiled and shows promise as a potential clinical candidate.

Published
2010
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