Binospirone (MDL-73,005-EF) acts as a potent, highly selective 5-HT1A ligand: as an antagonist at postsynaptic 5-HT1A receptors and also acts as a highly efficacious partial agonist at somatodendritic autoreceptors. Experiments on rodents have shown, that it also possesses anxiolytic properties.

Nafetolol (K5407) is a beta-blocking agent.

Omiloxetine, a serotonin uptake inhibitor was developed in Spain for the treatment of depression. However, in 2005, it was abandoned.

Benhepazone (also known as RCH-314) possessed potent analgesic and anti-inflammatory activities. Information about the nowadays use of this compound is not available.

Iosimenol, is a synthetic non-ionic dimeric contrast medium with lower molecular weight patented by Schering A.-G. In clinical trials Iosimenol was not metabolized, had a distribution volume corresponding to the extracellular space, and was rapidly excreted through the kidneys by glomerular filtration. The area under the plasma concentration curve and the peak plasma concentration was proportional to dose, while clearance was independent of dose. Iosimenol upon intravenous as well as upon intra-arterial injection exhibits a safety profile and shows an efficacy similar to that of iodixanol.

Catramilast is imidazolone derivative patented by Janssen Pharmaceutica N.V. as PDE IV inhibitor for the treatment of allergic, atopic, and inflammatory diseases.

Vatalanib a potent oral tyrosine kinase inhibitor with a selective range of molecular targets, has been extensively investigated and has shown promising results in patients with solid tumors in early trials. Vatalanib selectively inhibits the tyrosine kinase domains of vascular endothelial growth factor (VEGF) receptor tyrosine kinases (important enzymes in the formation of new blood vessels that contribute to tumor growth and metastasis), platelet-derived growth factor (PDGF) receptor, and c-KIT. The adverse effects of vatalanib appear similar to those of other VEGF inhibitors. In the CONFIRM trials, the most common side effects were high blood pressure, gastrointestinal upset (diarrhea, nausea, and vomiting), fatigue, and dizziness.

ISOSULPRIDE, a benzamide derivative, is an atypical neuroleptic.

Lidorestat is a highly potent and selective aldose reductase inhibitor with good oral bioavailability that is reported to improve nerve conduction and reduce cataract formation. Lidorestat reduced mortality rates in hAR transgenic mice. Mice receiving lidorestat had similar survival rates as nonhAR-expressing diabetic mice. Lidorestat treatment did not affect plasma lipids, glucose, or weights of diabetic mice. Drugs such as lidorestat will improve human health by reducing the production of toxic products of the polyol pathway. Lidorestat was developed for the treatment of diabetic complications, including neuropathy, retinopathy, cataracts, nephropathy.