Journal of Medicinal Chemistry p. 2952 - 2960 (2011)
Update date:2022-07-29
Topics:
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
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.
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