Indacrinone is an orally active, indanone-based loop diuretic patented by American pharmaceutical company Merck and Co as mixture of two enantiomers. In healthy volunteers, the racernic mixture of indacrinone exhibited greater natriuretic potency than furosemide, with a slower onset and longer duration of action. Furthermore, single doses of indacrinone decreased serum uric acid concentrations and increased uric acid clearance, while similar doses of furosemide generally had the opposite effects. Differences in the pharmacologic effects of the resolved enantiomers of indacrinone were initially studied in animals and confirmed in a series of studies we conducted in healthy human volunteer. The S( + ) form is a potent uricosuric agent that produces mild natriuresis only at higher doses, while the R( - ) form is a potent loop diuretic with only transient uricosuric effects. The (-) enantiomer and its active metabolite appear to be primarily responsible for the natriuretic effects of the racemic mixture; the ( + ) enantiomer is 20-40 times less potent a natriuretic agent.

FLORDIPINE is a calcium channel blocker with a structure similar to that of nifedipine, and with similar cardiovascular effects. However, unlike nifedipine, FLORDIPINE requires hepatic metabolism for its activation.

FLUMINOREX is an anorexic agent.

Tomelukast (previously known as LY171883), an orally active antagonist of the CysLT1 receptor (leukotriene D4), which was investigated to treat asthma, but this study was discontinued because of adverse gastrointestinal effect.

Medroxalol is a competitive antagonist at alpha1-adrenergic receptors and beta1-adrenergic receptors. Medroxalol also an agonist at beta2-adrenergic receptors. Medroxalol exerts antihypertensive and vasodilating effects. It was concluded that the principal action of medroxalol was to produce a fall in blood pressure by decreasing peripheral vascular resistance more than cardiac output.

GSK-2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. GSK-2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines. On April 1 2016 GlaxoSmithKine completes a phase-I/II trial for Solid tumours (Late-stage disease) in USA, United Kingdom and South Korea (NCT01458067).

FLUMECINOL, a benzhydrol derivative, is a hepatic microsomal drug-metabolizing enzyme inducer. It was in clinical development for the treatment of pruritus associated with primary biliary cirrhosis.

Etoxadrol is an NMDA receptor antagonist. It exerts phencyclidine-like properties. Etoxadrol has anticonvulsant and anesthetic activity. Intravenous etoxadrol was clinically tested as an anesthetic.

CE-224535 is a potent, highly selective, orally bioavailable, non-competitive antagonist of the human P2X7 receptor. Pre-clinical pharmacokinetic studies with CE-224535 indicate limited CNS penetration. In clinical trials, CE-224535 failed to demonstrate efficacy in a 2-week study of knee pain in osteoarthritis or a 12-week study in patients with rheumatoid arthritis. CE-224535 is safe and well tolerated after administration of up to 1600 mg as a single dose or 600 mg every 12 hours for 14 days in healthy subjects and 500 mg every 12 hours for 2 weeks in subjects with osteoarthritis of the knee and 12 weeks in rheumatoid arthritis patients with an inadequate response to methotrexate.