Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor. Aloxistatin was developed for treating muscular dystrophy. Open trials on 73 Duchene’s muscular dystrophy patients were conducted for 3 years at four Japanese national sanatoriums and resulted in some muscle strength improvement but the results were inconclusive and final double-blind studies did not confirm the results. Taisho has discontinued development of aloxistatin for the potential treatment of muscular dystrophy. The  trials completed through Phase 3. In animal models Aloxistatin (100 mg/kg, p.o.) strongly inhibits the cathepsin B&L activities in the skeletal muscle, heart and liver of hamsters. In spinal cord injury (SCI) rats, Aloxistatin provides neuroprotection in SCI lesion and penumbra.Aloxistatin reduces brain amyloid-β and improves memory deficits in Alzheimer's disease animal models by inhibiting cathepsin B activity.

Alphameprodine (ACSCN 9604) is an opioid analgesic classified by the United States Drug Enforcement Administration under Schedule I of illegal substances. The stereoisomer betameprodine is similarly classified, however alphameprodine is more widely used (both are referred to as Meprodine). Alphameprodine is a structural analogue of meperidine. It exerts physiological effects characteristic of opioids, such as analgesia, euphoria and sedation, as well as itching, nausea, and respiratory depression.

Dimenoxadol is an opioid analgesic which produces typical opioid effects such as analgesia and sedation. It is structurally similar to methadone and is a benzilic acid derivative. In the United States it is classified as a Schedule I controlled drug.

UK-432097 is a selective adenosine A2a agonist which was in development with Pfizer as an inhaled treatment for asthma and chronic obstructive pulmonary disease. UK-432097 had been in phase II clinical trials by Pfizer for the treatment of chronic obstructive pulmonary disease (COPD). However, this study was terminated prematurely due to futility based on results of interim analysis.

Primidolol (also known as UK-11,443) is an imidazolidinone derivative patented by American pharmaceutical corporation Pfizer Corp as a specific β-adrenergic blocker. In clinical trials, Primidolol shows some antihypertensive activity but the overall change in the cardiovascular parameters failed to demonstrate a significant difference compared to placebo.

Dexetozoline is a safe and effective diuretic agent in the treatment of acute cardiac failure. In isolated rings of guinea-pig aorta not responding to acetylcholine, the diuretic dexetozoline did not influence basal vascular tone but inhibited noradrenaline- and histamine-induced contractions. Dexetozoline has a very high bioavailability after oral administration and is fairly lipohilic. The half-life of etozolin is 2.5 h. Dexetozoline accumulates in cirrhosis.

Detanosal is antipyretic, analgesic and anti-inflammatory agent.