Bertosamil was developed as an anti-ischemic and anti-arrhythmic drug that inhibits the atrial potassium channels Kv1.2, Kv1.4 and Kv1.5. However, the development of this drug has been discontinued.

Endixaprine (SR 41378 or 3-(4-hydroxy-1-piperidinyl)-6-(2,4-dichlorophenyl)-pyridazine) is a aminopyridazine derivative. Endixaprine is a nonbenzodiazepine compound with a pharmacological profile similar to barbiturates and benzodiazepines. It possesses anticonflict, anticonvulsant, antianxiety and hypnotic activities in rodents.

Emitefur or BOF-A2 is a fluorinated pyrimidine antimetabolite exerting antineoplastic properties. It is a compound composed of 5-fluorouracil (5-FU) and 3-cyano-2,6-dihydroxypyridine (CNDP), an inhibitor of 5-FU degradation by dihydrouracil dehydrogenase in order to prolong the blood 5-FU level as well as increase selective toxicity to a tumor. Emitefur demonstrated clinical activity in preliminary studies in Japan. Emitefur development for the treatment of solid tumors has been discontinued.

Salmefamol is a beta2-adrenoceptor agonist that was studied in asthmatic patients. In clinical trials, the drug had shown marked efficacy with low toxicity and was generally well tolerated. However, information about the further development of salmefamol as a bronchodilator drug is not available.

Metrifudil (previously known as Y-341) is a synthetic adenosine analog that is acid stable and has a prolonged duration of action. Metrifudil is a selective adenosine A2 receptor agonist and has anticonvulsant activity against seizures. The drug is also studied for the treatment of glomerulonephritis. However, no recent development has been reported.

(4-AMINO-5-CHLORO-2-METHOXYPHENYL)[4-(1,3-BENZODIOXOL-5-YLMETHYL)-1-PIPERAZINYL]METHANONE (peralopride) is a tranquilliser, antidepressant.

Danitracen (WA 335) is an antidepressant compound developed in the 1970s. Danitracen acts by blocking central and peripheral 5-HT receptors: it potentiates testosterone-induced sexual behavior in rats and abolishes the 5-hydroxytryptophan (5-HTP) induced hypermotility in mice. In amphetamine-treated rats, administration of danitracen lowered whole brain serotonin and norepinephrine levels. Danitracen investigated in clinical trials in depressed patients. At 3 mg/day, danitracen was equipotent to 150 mg/day amitriptyline.

Lisofylline [1-(5R-hydroxyhexyl)-3,7-dimethylxanthine] is a unique metabolite of pentoxifylline. Lisofylline inhibited the generation of phosphatidic acid and free fatty acids. Lisofylline blocked the release of pro-inflammatory cytokines in oxidative tissue injury, in response to cancer chemotherapy and in experimental sepsis. Lisofylline regulates immune cell function and autoimmune response by inhibition of IL-12 signalling and cytokine production. Lisofylline may have therapeutic value in the prevention of autoimmune disorders, including Type 1 diabetes, autoimmune recurrence following islet transplantation, and in preservation of beta cell functional mass during islet isolation.

Succinobucol (also known as AGI-1067) is a probucol derivative patented by American pharmaceutical company Atherogenics, Inc as vascular protectant with antioxidant, anti-inflammatory and antiplatelet activities. In vitro, succinobucol inhibits the TNF-α induced expression of VCAM-1 and MCP-1 with little effect on intercellular adhesion molecule (ICAM)-1. In addition, succinobucol inhibits lipopolysaccharide (LPS)-induced expression of tissue factor in human monocytic cells and endothelial cells, an effect thought to be mediated independently from the nuclear factor κB pathway. Preclinical studies have shown reduced total cholesterol and low-density lipoprotein cholesterol concentrations, increased high-density lipoprotein cholesterol concentrations, decreased levels of inflammatory mediators, and reduced atheroma area with Succinobucol treatment in animal models. Unfortunately, in clinical trials, Succinobucol failed to demonstrate a strong cardioprotective effect. Undesired metabolic effects including high-density lipoprotein cholesterol-lowering have been consistently reported, and diarrhea appears to be an expected adverse effect.