1210344-25-4Relevant academic research and scientific papers
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane Class of sodium-dependent glucose cotransporter 2 inhibitors
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
, p. 2952 - 2960 (2011)
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.
DIOXA-BICYCLO[3.2.1.]OCTANE-2,3,4-TRIOL DERIVATIVES
-
Page/Page column 38-39, (2010/04/06)
Compounds of Formula (I) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).The compounds disclosed herein are useful for the prevention and treatment of obesity and its associated co-morbidities, inn particular type Il (type 2) diabetes.
