Discovery of a Clinical Candidate from the Structurally Unique Dioxa-bicyclo[3.2.1]octane Class of Sodium-Dependent Glucose Cotransporter 2 Inhibitors

Compound 4 (PF-04971729) belongs to a new class of potent and selective sodium-dependent glucose cotransporter 2 inhibitors incorporating a unique dioxa-bicyclo[3.2.1]octane (bridged ketal) ring system. In this paper we present the design, synthesis, preclinical evaluation, and human dose prediction...

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Bibliographic Details
Published in:	Journal of medicinal chemistry 2011-04, Vol.54 (8), p.2952-2960
Main Authors:	Mascitti, Vincent, Maurer, Tristan S, Robinson, Ralph P, Bian, Jianwei, Boustany-Kari, Carine M, Brandt, Thomas, Collman, Benjamin M, Kalgutkar, Amit S, Klenotic, Michelle K, Leininger, Michael T, Lowe, André, Maguire, Robert J, Masterson, Victoria M, Miao, Zhuang, Mukaiyama, Emi, Patel, Jigna D, Pettersen, John C, Préville, Cathy, Samas, Brian, She, Li, Sobol, Zhanna, Steppan, Claire M, Stevens, Benjamin D, Thuma, Benjamin A, Tugnait, Meera, Zeng, Dongxiang, Zhu, Tong
Format:	Article
Language:	English
Subjects:	Animals Area Under Curve Bridged Bicyclo Compounds, Heterocyclic - chemistry Bridged Bicyclo Compounds, Heterocyclic - pharmacokinetics Bridged Bicyclo Compounds, Heterocyclic - pharmacology Crystallography, X-Ray Drug Discovery Drug Evaluation, Preclinical Humans Magnetic Resonance Spectroscopy Mass Spectrometry Models, Molecular Rats Sodium-Glucose Transporter 2 - antagonists & inhibitors
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