期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 8, 页码 2952-2960出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm200049r
关键词
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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 rat; 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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