Clogestone Acetate (AY-11440) is a steroidal progestin that was synthesized in 1964 and was investigated as a progestin-only contraceptive but was never marketed.

Crisnatol is a derivative of arylmethylaminopropanediol with significant antineoplastic activity in a variety of murine and human tumor models. Crisnatol functions as a DNA intercalator, with the presence of additional basic amine groups in the sidechain enhancing binding to DNA due to electrostatic interactions. Crisnatol did not show antitumor efficacy in patients with ovarian carcinoma. In another clinical study, 2 of 26 patients with glioma showed complete long-lasting responses to the drug. The dose-limiting side effect was neurotoxicity.

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.