ARUNDIC ACID (ONO-2506) is an enantiomeric, three carbon atom homolog of valproic acid under development by ONO Pharmaceutical for the potential treatment of stroke, as well as Amyotrophic Lateral Sclerosis and Parkinson's disease. The injectable formulation (Proglia) is finished phase III trials for acute-phase cerebral infarction, and the oral formulation (Cereact) is finished phase II trials in the UK for Alzheimer's disease (AD) and Parkinson's disease (PD). ARUNDIC ACID restores normal astrocyte functions after brain damage by preventing reactive astrocytosis, by activating astrocytic GABAA receptors and suppressing GABA transferase. ARUNDIC ACID inhibits S-100β synthesis in activated cultured astrocytes. This agent has additional antiglutamate and antiinflammatory COX-2 inhibitor properties

Propatylnitrate (or propatyl nitrate), a coronary vasodilator that has been studied for the relief of acute attacks of angina pectoris. However, was revealed that this drug didn’t abolish or diminish the frequency of attacks of angina pectoris.

Aminothiazole is a heterocyclic amine, commonly used as a starting point for synthesis of many compounds. In 1940s aminothiazole was used for the treatment of thyrotoxicosis. It has a direct action on the thyroid and acts by inhibiting T4 synthesis and accelerating its deiodination. Aminothiazole is an inhibitor of inducible NO synthetase (IC50 18 uM).

Fendiline or Sensit (N-(3,3-diphenylpropyl)-(1-phenylethyl)-amine), is a diphenylalkylamine blocker of L-type calcium channels. Fendiline is an anti-anginal agent for the treatment of coronary heart disease. Pharmaco-dynamically, it exerts the typical calcium as well as calmodulin antagonistic actions: inhibition of the transmembrane calcium current, smooth muscle relaxation, negative inotropism, cardioprotection, inhibition of calmodulin-activated myosin light-chain kinase and phosphodiesterase. Pharmacokinetics reveal slow onset of action and a long half-life. The anti-anginal and anti-ischaemic efficacy of fendiline has been proven in several placebo-controlled, double-blind trials. Fendiline is an FDA-approved, albeit now clinically obsolete. Additionally, fendiline is a specific inhibitor of K-Ras plasma membrane localization that also inhibits K-Ras signal output and blocks the proliferation of K-Ras-transformed tumor cells.

Fazadinium (used as a bromide salt) is a muscle relaxant, which was applied in anesthesia under the name Fazadon. The current marketing status is unknown and the drug is supposed to be discontinued.

Timiperone is a neuroleptic agent that was developed in Japan. Timiperone has a potent antipsychotic activity, which is comparable to other butyrophenones such as haloperidol (HAL). Timiperone has a five-eight-times higher affinity to dopamine receptors and a 15-times higher affinity to serotonin receptors than those of HAL. Clinical trials have suggested that TIM has a specific action against negative symptoms such as lack of initiative or blunted affect as well as positive symptoms such as delusions and hallucinations in schizophrenics.

Vapiprost is a potent dicyclopentadiene thromboxane receptor antagonist that was being developed by Glaxo Wellcome in Japan. Vapiprost has been shown to be a potent and specific thromboxane (Tx)A2 receptor blocking drug in vitro using platelets and both vascular and airways smooth muscle preparations from different species. The drug is active in various experimental models of thrombosis. The potential clinical applications for a thromboxane receptor blocking drug include the treatment of thrombotic events and occlusive vascular disease. Phase III trials were underway in Japan for the treatment of deep vein thrombosis, which later were discontinued.

Candoxatril is the orally-active prodrug of candoxatrilat (UK-73967), a potent neutral endopeptidase (NEP) inhibitor. Neutral endopeptidase inhibitors such as Candoxatril have a dual mechanism of action. They inhibit two metalloprotease enzymes, neutral endopeptidase, and ACE, resulting in an increased availability of natriuretic peptides that exhibit vasodilatory effects and, possibly, tissue protective effects. Candoxatril is the first drug of its kind to be released for clinical trials regarding heart failure. This is because Candoxatril produces favorable hemodynamic effects in patients with chronic heart failure. It has been demonstrated that Candoxatril is associated with a beneficial hemodynamic effect that is useful both for rest and exercise. In several different studies, candoxatril has been shown to improve performance in people with heart failure. In one study, 12 different patients were selected, all with moderately severe heart failure. On day one of this study, the candoxatril had increased plasma ANP levels, suppressed aldosterone and decreased right atrial and pulmonary capillary wedge pressures. After treatment for 10 days, patients health had improved with an increase of basal ANP and a decrease of aldosterone, along with a reduced body weight that could be a reflection of chronic natriuretic, diuretic effects, or both. It was decided that on day 10 of the study, the effects of candoxatril were similar to that on day one.

Levopropylhexedrine acts similar to amphetamine, at therapeutic doses has anorexigenic effect.

Gimeracil is a component of an oral fixed combination known under the name Teysuno or S-1 (tegafur, gimeracil and oteracil potassium at a molar ratio of 1:0.4:1). The formulation was approved in Asia and Europe for the treatment of a rare condition of gastric cancer. Given in combination, gimeracil enhances the efficacy of tegafur by inhibiting dihydropyrimidine dehydrogenase, an enzyme involved in metabolism of tegafur and its active metabolite 5-fluorouracil.