Asulacrine, also known as CI-921, an inhibitor of topoisomerase II, participated in clinical trials phase II for the treatment of cancer. In spite of the positive and promising results, this drug showed the toxicity, phlebitis that blocks its implementation in the future.

Lometraline is a tranquillizer and anti-parkinsonian drug. It was developed as an antidepressant agent. Lometraline is a congener of popular antidepressant (+)-sertraline.

Limazocic is a cyclic disulfide compound newly synthesized as a hepatoprotective agent. It has a protective effect against both chronic liver injuries induced by carbon tetrachloride (CCL) and swine serum and several chemically induced acute liver injuries. The inhibitory effects of limazocic on immunologically induced liver injuries in mice have also been demonstrated and furthermore, limazocic has been shown to have immunomodulatory effects such as induction of cytotoxic cell activities and modulation of interleukin-2 and interferon-gamma production. Limazocic had a markedly inhibitory effect on ANIT-induced intrahepatic cholestasis in rats. Limazocic suppresses VEGF production and reduces vascular leakage and the growth of mouse experimental choroidal neovascularization.

Cogazocine is an opioid analgesic of the benzomorphan family, invented by the Dutch company ACF Chemiedfarma N.V. The compound was active in a tail withdrawal and writhing tests in rats and possessed nalorphine-like activity in rats after an intravenous dose of 0.04 mg/kg.

Cetohexazine is pyridazone derivative with atypical antidepressant, serotonergic and dopaminergic activities.

Bedoradrine (also known as KUR-1246 or MN-221), an ultra selective beta 2-adrenoceptor agonist, that participated in phase II clinical trials as an adjunct to standard therapy in the management of patients with acute exacerbation of asthma who did not respond to standard therapy. In addition, the drug was involved in trials for the treatment of preterm labor in obstetrical practice. Bedoradrine is also was studied in phase I of clinical trials for its use for treating chronic obstructive pulmonary disease, however, the efficacy for this disease was uncertain.

Apratastat (Tmi 005) was developed by Wyeth Research as a dual TNF-alpha-converting enzyme and matrix metalloprotease-13 inhibitor for the treatment of rheumatoid arthritis. Apratastat was in phase II clinical trials, but because of the lack of efficacy, this trial was terminated.

Rolgamidine is an antidiarrheal agent. No information on current use of this compound is available.

Lodazecar is a benzodiazepine derivative, which does not bind to the brain benzodiazepine receptor. The drug shares some similarity in tertiary structure with the cholesterol molecule. Oral administration of lodazecar in the cholesterol-fed rat is associated with significant changes in plasma lipoproteins and in key enzymes controlling hepatic cholesterol metabolism. In human the treatment reduced both the fractional and the absolute cholesterol absorption and increased fecal neutral sterol excretion by about 50%, serum plant sterol levels were reduced, most probably because of diminished sterol absorption. Biliary cholesterol secretion was unchanged.