| Literature DB >> 21449606 |
Vincent Mascitti1, Tristan S Maurer, Ralph P Robinson, Jianwei Bian, Carine M Boustany-Kari, Thomas Brandt, Benjamin M Collman, Amit S Kalgutkar, Michelle K Klenotic, Michael T Leininger, André Lowe, Robert J Maguire, Victoria M Masterson, Zhuang Miao, Emi Mukaiyama, Jigna D Patel, John C Pettersen, Cathy Préville, Brian Samas, Li She, Zhanna Sobol, Claire M Steppan, Benjamin D Stevens, Benjamin A Thuma, Meera Tugnait, Dongxiang Zeng, Tong Zhu.
Abstract
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 predictions related to 4. This compound demonstrated robust urinary glucose excretion in rats and an excellent preclinical safety profile. It is currently in phase 2 clinical trials and is being evaluated for the treatment of type 2 diabetes.Entities:
Mesh：
Substances：
Year: 2011 PMID： 21449606 DOI： 10.1021/jm200049r
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446