Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
J Med Chem
; 54(8): 2952-60, 2011 Apr 28.
Article
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| MEDLINE
| ID: mdl-21449606
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.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Compuestos Bicíclicos Heterocíclicos con Puentes
/
Descubrimiento de Drogas
/
Inhibidores del Cotransportador de Sodio-Glucosa 2
Tipo de estudio:
Prognostic_studies
Idioma:
En
Revista:
J Med Chem
Año:
2011
Tipo del documento:
Article
País de afiliación:
Estados Unidos