Atopaxar, also known as E 5555 is a novel reversible protease-activated receptor-1 (PAR-1) thrombin receptor antagonist. The inhibition of thrombin-mediated platelet activation by means of protease-activated receptor-1 inhibitors represents an attractive therapeutic option for patients with atherothrombotic disease processes. In preclinical studies, atopaxar demonstrated inhibition of thrombin receptor-activating peptides (TRAP)- and thrombin-induced platelet aggregation. Atopaxar was being developed by Eisai for acute coronary syndromes (ACS) and coronary disorders, including atherothrombosis, unstable angina pectoris and myocardial infarction. Atopaxar was in phase II clinical development in the US, EU and Japan. However, development was discontinued in May 2012.

Quinetolate is a quinolone derivative patented by The Geschickter Fund for Medical Research, Inc. for the treatment of bronchial asthma. In preclinical studies, Quinetolate antagonized the effect of histamine on the lung in rabbits and blocked arrhythmias induced by chloroform in mice. Quinetholate shows potent antiarrhythmic activities on ouabain-induced tachycardia. Quinetholate caused the longest lasting reversions of ouabain-induced tachycardia, i.e. usually lasting at least 30 min after infusion was stopped.

Onapristone is a type I progesterone receptor (PR) antagonist that prevents PR- mediated DNA transcription and was studied as an antitumor agent. This drug possessed activity in breast cancer and is participating in phase II clinical trials to test any good and bad effect for the treatment of endometrial cancer, ovarian cancer, peritoneal cancer, and prostate cancer.

Quinelorane is an octahydropyrimido[4,5-g]quinolone derivative patented by American pharmaceutical company Eli Lilly and Co. as for the treatment anxiety, Parkinson's syndrome, depression, and hypertension. Quinelorane acts as an agonist of dopamine agonist for the D2 and D3 receptors. In preclinical studies Quinelorane (IM) treatment produced dose-dependent effects on male sexual responding. Penile erections and masturbation were markedly facilitated following treatment with either 2.5 or 5 micrograms/kg quinelorane. Higher doses of quinelorane (10 and 25 micrograms/kg) generally did not further augment sexual responding but rather resulted in a return in sexual responding to control vehicle levels. Quinelorane had a biphasic effect on yawning behavior of the monkeys with low doses (2.5 and 5 micrograms/kg) facilitating yawning and high doses (25 micrograms/kg) inhibiting yawning.

Trenizine is a diphenylmethyl piperazine derivative. It is a vasodilator, antiemetic, antihistamine and anti-anaphylactic agent.

Perfluamine is an oxygen-carrying agent (blood substitute).

Buthalital is a barbiturate derivative which was under development as a short-acting anesthetic. However, development was discontinued, perhaps due to its extremely rapid elimination rate] and buthalital sodium was never marketed.

Prodilidine is an arylpyrrolidine derivative patented by Mead Johnson & Co.as moderately potent analgesic. By comparison with other drugs, including morphine, Prodilidine has a prompt and unusually sustained antinociceptive action in rodents by all routes. Prodilidine substantially lacks antipyretic, anti-inflammatory, antitussive, constipating, respiratory depressant, and cardiovascular effects. Prodilidine resembles meperidine in excitatory properties and body-temperature lowering action at high dosage. The d-isomer is about twice as potent and toxic as the l-isomer parenterally; by the gastric route, the difference is markedly less.