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REMOGLIFLOZIN

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REMOGLIFLOZIN ETABONATE

5-methyl-4-[4-(1-methylethoxy)benzyl]-1-(1-methylethyl)-1H-pyrazol-3-yl 6-O-(ethoxycarbonyl)-β-D-glucopyranoside, CAS 442201-24-3

189075  BHV-091009  GSK-189075  GSK-189075A  KGT-1681 

 

BHV Pharma  Kissei (Originator)  , GlaxoSmithKline

Remogliflozin etabonate (INN/USAN)[1] is a proposed drug for the treatment of type 2diabetes being investigated by GlaxoSmithKline.[2] Remogliflozin is now being developed by BHV Pharma.

Figure imgf000004_0002

Remogliflozin inhibits the sodium-glucose transport proteins, which are responsible for glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine.[3]

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  1. Statement on a nonproprietory name adopted by the USAN council
  2.  Fujimori Y, Katsuno K, Nakashima I, Ishikawa-Takemura Y, Fujikura H, Isaji M (June 2008). “Remogliflozin etabonate, in a Novel Category of Selective Low-Affinity / High-Capacity Sodium Glucose Cotransporter (SGLT2) Inhibitors, Exhibits Antidiabetic Efficacy in Rodent Models”. J. Pharmacol. Exp. Ther. 327 (1): 268–276.doi:10.1124/jpet.108.140210PMID 18583547.
  3.  Prous Science: Molecule of the Month November 2007

DPP IV inhibitors represent a novel class of agents that are being developed for the treatment or improvement in glycemic control in patients with type 2 diabetes. For example, DPP IV inhibitors and their uses are disclosed in WO 2002/068420, WO 2004/018467, WO 2004/018468, WO 2004/018469, WO 2004/041820, WO 2004/046148, WO 2005/051950, WO 2005/082906, WO 2005/063750, WO 2005/085246, WO 2006/027204, WO 2006/029769, WO2007/014886; WO 2004/050658, WO 2004/1 1 1051 , WO 2005/058901 , WO 2005/097798; WO 2006/068163, WO 2007/071738, WO 2008/017670; WO 2007/054201 or WO 2007/128761.

 

 

Chemical structures of remogliflozin etabonate (A), remogliflozin (B), sergliflozin (C), phlorizin (D), and T-1095 (E). Remogliflozin etabonate is metabolized to remogliflozin, its active form.

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