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3 results on '"Carpenter, Andrew J."'

1. Development of Large-Scale Routes to Potent GPR119 Receptor Agonists

Author

Matthew Jude Sharp, Will L. Canoy, Kae M. Bullock, Eric Eugene Boros, Xiao-ming M. Zhou, Richard T. Matsuoka, Greg A. Erickson, Vassil I. Elitzin, Mark B. Mitchell, Matthew C. Salmon, David H. Igo, Nicole M. Deschamps, Daniel W. Reynolds, Andrew D. Brown, Gregory E. Peckham, Istvan Kaldor, Jennifer F. Toczko, Shannon Condon, Carpenter Andrew J, Elie Amine Tabet, Jing M. Fang, Biren K. Joshi, Lianming Michael Wu, and Jeremy D. Cobb

Subjects
0301 basic medicine, 03 medical and health sciences, 030104 developmental biology, 0302 clinical medicine, GPR119, Chemistry, 030220 oncology & carcinogenesis, Organic Chemistry, Physical and Theoretical Chemistry, Receptor, Combinatorial chemistry
Abstract

Practical and scalable syntheses were developed that were used to prepare multikilogram batches of GSK1292263A (1) and GSK2041706A (15), two potent G protein-coupled receptor 119 (GPR119) agonists. Both syntheses employed relatively cheap and readily available starting materials, and both took advantage of an SNAr synthetic strategy.

Published
2016
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2. Discovery Process and Characterization of Novel Carbohydrazide Derivatives as Potent and Selective GHSR1a Antagonists

Author

Claudia Mundi, Sebastien Guery, Alberto Buson, Romano Di Fabio, Sergio Melotto, Federico Faggioni, Chiara Savoia, Michela Tessari, Lucilla D'Adamo, Fabio Maria Sabbatini, Carla Di Francesco, Benedetta Perini, Paolo Cavanni, Giovanna Dal Forno, Steve M. Bromidge, Yves St-Denis, Stefania Contini, Mauro Corsi, Elisabetta Perdona, Francesca Pavone, Marilisa Rinaldi, Carpenter Andrew J, and Mario Mattioli

Subjects
Pharmacology, Chemistry, Organic Chemistry, Drug Evaluation, Preclinical, Carbohydrazide, Biochemistry, Cell Line, Feeding and Eating Disorders, Structure-Activity Relationship, chemistry.chemical_compound, Hydrazines, Drug Discovery, Humans, Molecular Medicine, Structure–activity relationship, Ghrelin, General Pharmacology, Toxicology and Pharmaceutics, Receptors, Ghrelin, Receptor
Published
2010
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3. Discovery of Potent, Nonsystemic Apical Sodium-Codependent Bile Acid Transporter Inhibitors (Part 2)

Author

Miller Raymond E, Wei Huang, Horng-Chih Huang, Jay S. Trivedi, Scott R. Both, Nigam P. Rath, David B. Reitz, Deborah A. Mischke, Len F. Lee, Samuel J. Tremont, Steve R. Rapp, Danny J. Garland, Claude Jones, Banerjee Shyamal C, Matthew W. Mahoney, Theresa Fletcher, Michael B. Tollefson, Karen Regina, Emily J. Reinhard, Grace M. Wagner, Mark E. Smith, Judy Beaudry, J.-H Li, Kevin C. Glenn, Bradley T. Keller, Robert E. Manning, Kevin J. Koeller, Joe R. Schuh, Kolodziej Steve A, William F. Vernier, Carpenter Andrew J, and Ching-Cheng Wang

Subjects
Male, Taurocholic Acid, medicine.drug_class, medicine.medical_treatment, Sodium, Organic Anion Transporters, Sodium-Dependent, chemistry.chemical_element, Benzothiepins, Chemical synthesis, Absorption, Cell Line, Steroid, Bile Acids and Salts, Structure-Activity Relationship, chemistry.chemical_compound, X-Ray Diffraction, Cricetinae, Drug Discovery, medicine, Animals, Humans, Structure–activity relationship, Rats, Wistar, Mesocricetus, Symporters, Bile acid, Chemistry, Reabsorption, Anticholesteremic Agents, Humidity, Stereoisomerism, Taurocholic acid, Rats, Biochemistry, Symporter, Molecular Medicine, Crystallization
Abstract

In the preceding paper several compounds were reported as potent apical sodium-codependent bile acid transporter (ASBT) inhibitors. Since the primary site for active bile acid reabsorption is via ASBT, which is localized on the luminal surface of the distal ileum, we reasoned that a nonsystemic inhibitor would be desirable to minimize or eliminate potential systemic side effects of an absorbed drug. To ensure bioequivalency and product stability, it was also essential that we identify a nonhygroscopic inhibitor in its most stable crystalline form. A series of benzothiepines were prepared to refine the structure-activity relationship of the substituted phenyl ring at the 5-position of benzothiepine ring and to identify potent, crystalline, nonhygroscopic, and efficacious ASBT inhibitors with low systemic exposure.

Published
2005
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