842153-79-1

Upstream product

• 32469-28-6 (3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one 
• 19094-56-5 2-chloro-5-iodobenzoic acid 
• 281652-58-2 2-chloro-5-iodobenzoylchloride 
• 1450738-14-3 2-chloro-5-(1-methoxy-2,3,4,6-tetra-O-acetyl-D-glucopyranosyl)benzoyl chloride 
• 842134-05-8 2-chloro-5-(1-methoxy-2,3,4,6-tetra-O-acetyl-D-glucopyranosyl)benzoic acid 
• 866605-85-8 2-chloro-5-(1-methoxy-2,3,4,6-tetra-O-acetyl-D-glucopyranosyl)phenyl 5-bromo-2-thienyl ketone 
• 842134-04-7 tert-butyl 2-chloro-5-(1-methoxy-2,3,4,6-tetra-O-acetyl-D-glucopyranosyl)benzoate 
• 842134-03-6 tert-butyl 2-chloro-5-(1-methoxy-D-glucopyranosyl)benzoate 
• 503555-23-5 tert-butyl 5-bromo-2-chloro-benzoate 

Downstream Products

• 842134-46-7 4-chloro-1-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)-3-((5-(6-fluoro-3-pyridyl)-2-thienyl)methyl)benzene 
• 866605-84-7 4-chloro-1-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl)-3-[(5-(3-pyridyl)-2-thienyl)methyl]benzene 

Relevant academic research and scientific papers

GLUCOPYRANOSE DERIVATIVES USEFUL AS SGLT2 INHIBITORS

The present invention is directed to glucopyranose derivatives of formula (I), pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT2 activity. More particularly, the compounds of the present invention are useful in the treatment of for example, Type II diabetes mellitus, Syndrome X, and complications and symptoms associated with said disorders.

GLUCOPYRANOSE DERIVATIVES USEFUL AS SGLT2 INHIBITORS

The present invention is directed to glucopyranose derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT2 activity. More particularly, the compounds of the present invention are useful in the treatment of for example, Type II diabetes mellitus, Syndrome X, and complications and symptoms associated with said disorders.

C-Glucosides with heteroaryl thiophene as novel sodium-dependent glucose cotransporter 2 inhibitors

Canagliflozin (1), a novel inhibitor for sodium-dependent glucose cotransporter 2 (SGLT2), has been developed for the treatment of type 2 diabetes. To investigate the effect of replacement of the phenyl ring in 1 with heteroaromatics, C-glucosides 2 were designed, synthesized, and evaluated for their inhibitory activities against SGLT2. Of these, 3-pyridyl, 2-pyrimidyl or 5-membered heteroaryl substituted derivatives showed highly potent inhibitory activity against SGLT2, while 5-pyrimidyl substitution was associated with slightly reduced activity. In particular, 2g (TA-3404) had remarkable anti-hyperglycemic effects in high-fat diet fed KK (HF-KK) mice.