Tiafibrate is a dithiahexadecanediol derivative patented by Juste S. A. Quimico-Farmaceutica as a hypocholesteremic agent. In rats, Tiafibrate at 125 mg/kg day orally for 14 days gave a 38.8% decrease in blood lipids and a 33.7% decrease in blood cholesterol.

Nepicastat (SYN-117) is a potent and selective inhibitor of dopamine-β-hydroxylase. This compound in Phase 2 of clinical trial for the treatment cocaine addiction and posttraumatic stress disorder.

Modithromycin (EDP-420, EP-013420, S-013420) is 6-11-bicyclic erythromycin derivative patented by Enanta Pharmaceuticals, Inc as an antibacterial agent. In preclinical studies, Modithromycin exhibited high levels of in vitro activities against N. gonorrhea, including isolates resistant to azithromycin, cefixime, ceftriaxone, spectinomycin, ampicillin, tetracycline, and ciprofloxacin. Modithromycin also has the good in vivo efficacy against S. pneumoniae and H. influenzae, which might be due to its lasting intracellular activity. In healthy adults, clinical trials Modithromycin shows long half-life and its high systemic exposure. Modithromycin was well tolerated, with no serious or severe adverse events reported, and no subject was discontinued from the study due to an adverse event. In 2005 Modithromycin was studied in phase II clinical trials but no further development reports were published.

Fluorescein Lisicol (NRL972) is a fluorescent-labelled bile acid analog that is used as an investigational marker for liver function, specifically hepatic biliary transporter function. Fluorescein Lisicol has been used in trials investigating the pharmacokinetics of hepatic cirrhosis, viral hepatitis, non-alcoholic steatohepatitis and non-alcoholic fatty liver disease.

Cyclexanone is an antitussive drug developed by the Swiss pharmaceutical company Ciba. The compound is claimed to have an analgesic action and an action on central respiratory control.

NeuroSearch was developing brasofensine (or NS 2214), an oral dopamine reuptake inhibitor for the treatment of Parkinson's disease. Brasofensine successfully passed phase II clinical trial in patients with Parkinson's disease, The drug was safe and well tolerated. However, NeuroSearch discontinued the development of the drug because of the cis-anti isomerization of the 2α-methyloxime group of brasofensine in favor of NS 2230.

Dexsecoverine ia an antimuscarinic drug.

Fenaperone exerts tranquilizing and neuroleptic properties.

Tolgabide is a gabamimetic agent. It exhibits antiepileptic, anticonvulsant and antidyskinetic activity. Tolgabide has a very similar structure and biological properties to those of progabide.