Zonampanel (also known as YM872) was developed as selective, potent and highly water-soluble competitive alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor antagonist. Zonampanel possesses the neuroprotective effect against focal cerebral ischemia and participated in phase II clinical trials in acute stroke patients. However, because of the severe effects, including hallucinations, agitation, and catatonia the further studied were terminated.

Giripladib (PLA 695) is a Cytosolic phospholipase A2 (cPLA2) inhibitor. cPLA2 is associated with tumor progression and radioresistance in mouse tumor models. In these models, treatment with giripladib attenuates radiation induced increases of phospho-ERK and phospho-Akt in endothelial cells. Combined with irradiation, giripladib reduces migration and proliferation in endothelial cells (HUVEC & bEND3) and induces cell death and attenuated invasion by tumor cells (LLC &A549). The combination treatment of giripladib and irradiation also delayes growth in both LLC and A549 tumors and results in reduced tumor vasculature. Phase I studies have been conducted to test the gastrointestinal safety of giripladib, and potential pharmacokinetic interaction with other compounds. A phase II study was terminated.

Nifurthiazole, a 5-nitrofuran derivative, is an antibacterial and antiprotozoal agent, it is active against Trypanosoma. It was also used for controlling Salmonella choleraesuis in swine. The mode of action of 5-nitrofuran analogues is based on red-ox biotransformation.

Uredepa, a thiotepa derivative, is a antineoplastic, alkylating agent. It has also been used experimentally as an insect chemosterilant.

Iocanlidic Acid I-123 is a radiolabeled phenylfatty acid derivative studied as a diagnostic agent for myocardial imaging

Pelretin is an antikeratinizing agent that was in phase II trials for the treatment of skin disorders. However, these studies were discontinued. In addition, pelretin was studied in cosmetic as a cream to treat acne and against skin wrinkling. Information about the further development of pelretin is not available.

Tomicorat is an anti-inflammatory agent.

Methyl palmoxirate, an oral hypoglycemic agent, was studied as a selective and irreversible inhibitor of the mitochondrial enzyme carnitine palmitoyltransferase and of long-chain fatty acid oxidation to treat diabetes. In addition, this compound was used to study the brain lipid metabolism by quantitative autoradiography or positron emission tomography (PET).