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Potent and selective human beta(3)-adrenergic receptor antagonists.
TLDR
Novel and selective beta(3)-AR antagonists with high affinity for the human receptor are described and specific 3'-phenoxy substitutions are described that transform these compounds from potent agonists into selective antagonists.
Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9.
TLDR
Assessment of selectivity of potential clinical candidates may be important to an optimal safety profile for this new class of antihyperglycemic agents, according to the results of toxicity and tolerability studies.
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the
TLDR
A novel series of beta-amino amides incorporating fused heterocycles, i.e., triazolopiperazines, were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV) for the treatment of type 2 diabetes and MK-0431, the phosphate salt of compound 1, was selected for development.
Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy
TLDR
MK-8722 is developed, a potent, direct, allosteric activator of all 12 mammalian AMPK complexes that induced robust, durable, insulin-independent glucose uptake and glycogen synthesis, with resultant improvements in glycemia and no evidence of hypoglycemia in rodents and rhesus monkeys.
Discovery of JANUVIA (Sitagliptin), a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
The emergence of glucagon-like peptide 1 (GLP-1) as a well validated approach to the treatment of type 2 diabetes and preclinical validation of dipeptidyl peptidase IV (DPP-4) inhibition as an
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
  • A. Weber
  • Biology
    Journal of medicinal chemistry
  • 12 August 2004
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
TLDR
MK-3102 (omarigliptin), was identified as a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor with an excellent pharmacokinetic profile amenable for once-weekly human dosing and selected as a clinical development candidate.
Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
TLDR
The discovery of vibegron, a potent and selective human β3-AR agonist for the treatment of overactive bladder (OAB), is described, which possesses improved druglike properties and an overall superior preclinical profile compared to MK-0634.
A comparative study of the binding properties, dipeptidyl peptidase‐4 (DPP‐4) inhibitory activity and glucose‐lowering efficacy of the DPP‐4 inhibitors alogliptin, linagliptin, saxagliptin,
TLDR
Since 2006, DPP‐4 inhibitors have become established therapy for the treatment of type 2 diabetes, and considerable chemical diversity exists amongst members of the D PP‐4 inhibitor class, raising the question as to whether structural differences may result in differentiated enzyme inhibition and antihyperglycaemic activity.
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