Balaglitazone, also known as DRF-2593; NNC-61-0645; NNC-61-2344; NN-2344; NNC-610645; NNC-612344, is an agonist of peroxisome proliferator-activated receptor (PPAR)γ. Balaglitazone plays an important role in the regulation of insulin, triglycerides and lipid metabolism. It is an attractive target for the therapy of Type II Diabetes. Balaglitazone is a partial agonist of PPARγ. It has showed potent effects on lowering blood glucose in various animal models. Balaglitazone passed phase III clinical trial for the treatment of type 2 diabetes. However, Dr. Reddy's Laboratories decided to terminate further clinical development of balaglitazone. Balaglitazone exists as two enantiomers: BALAGLITAZONE, (S)- and BALAGLITAZONE, (R)-. A capillary electrophoresis method for separation of a racemic mixture of glitazone compounds has being used. The method separated the R and S enantiomers of balaglitazone, and showed that the samples contained an equal (50:50) quantity of the enantiomers as a mixture. The Rs for the separations were 3.5 for balaglitazone enantiomers.

PSN632408 is an optimized agonist of GPR119 receptors. Systemic administration of PSN632408 suppresses food intake, reduces weight gain and white adipose tissue deposition in rats. PSN632408 treatment improved the function and/or mass of β-cells, significantly increased both human α- and β-cell areas in islet grafts and stimulated α- and β-cell replication. PSN632408 may be useful as a therapeutic agent for the treatment of obesity, diabetes and related metabolic disorders.

Lyxose, an analog of riboflavin, isolated from human myocardium.

GS-9851 (formerly PSI 7851) is an orally available, second generation uridine nucleoside analog polymerase inhibitor of hepatitis C treatment. GS-9851 is a nucleotide prodrug of the nucleoside analog GS-331007 (formerly PSI-6206). GS-9851 potently inhibits HCV NS5B polymerase and has demonstrated pan-genotypic activity in vitro. Preclinical studies of GS-9851 demonstrated a favorable profile in terms of antiviral potency, distribution, and metabolism. GS-9851 is first hydrolyzed to the intermediate GS-566500 (formerly PSI-352707), which is then metabolized to either the inactive metabolite, GS-331007, or the monophosphate GS-606965 (formerly PSI-7411). Inside the hepatocyte, GS-606965 is further phosphorylated by a series of enzymatic steps to an active triphosphate metabolite, GS-461203 (formerly PSI-7409), that selectively inhibits recombinant NS5B. A first-time-in-human study demonstrated that GS-9851 (25 to 800 mg) is generally safe and well tolerated in patients chronically infected with HCV. GS-9851 has a pharmacokinetic profile consistent with once-daily dosing. Administration of GS-9851 led to significant reductions in plasma HCV RNA levels without the evolution of known resistance mutations.