Fenmetozole is an alpha-2 adrenergic receptor antagonist which was developed for the treatment of schizophrenic and/or depressed patients, however never reached the market. It was also shown that the drug may reduce symptoms of minimal brain dysfunction in children and antagonize the effect of barbiturates and ethanol.

Ciaftalan Zinc (also known as Zinc(II)-phthalocyanine) is phthalocyanine and photosensitizers which showed a high activity in photodynamic therapy studies on a variety of animal tumors. Ciaftalan Zinc belongs to second generation photosensitizers that have a more intense long wavelength absorption and greater extinction coefficient compare to the first generation. The greater the extinction coefficient value associated with greater efficacy, smaller drug dosage required to induce a cytotoxic response and diminished risk of provoking systemic toxic reactions. The long absorption wavelength correlates with higher penetration depth and it is, therefore, Ciaftalan Zinc causes deep tumor necrosis in animal models. Currently, Tetra-triethyleneoxysulfonyl substituted Ciaftalan Zinc derivatives are studied as novel photodynamic therapy of cancer.

Ciladopa, is a troponylpiperazine derivative and dopamine agonist that has been shown to influence dopaminergic mechanisms in animals. Preclinical pharmacological studies have suggested that it has antiparkinsonian activity similar to that of bromocriptine but without many of the troublesome side effects. Unfortunately in some clinical trials no significant differences was found among the treatment groups and placebo.

Berupipam (also known as NNC 22-0010), a dopamine antagonist with a high affinity and selectivity for D1 receptor has been studied for patients with psychotic disorders. Berupipam participated in phase I clinical trials; however, further development of this drug was discontinued

Cinoctramide a derivative of cinnamic acid. It was patented in 1967, and was claimed to act on a central nervous system as a harmonious tranquilizer, and possess anti-convulsive properties in the case of chemically or electrically induced cramps. No clinical development of cinoctramide was reported.

The nitrofuran derivative, nifurprazine, is a topical antibacterial agent used mainly for the treatment of animal diseases. It is a trypanocidal drug. Nifurprazine proved to be the most promising derivative since it was redox-cycled by both T. cruzi LipDH and TR and had pronounced antiparasitic effects in cultures of T. cruzi and Trypanosoma brucei.

Etriciguat is a novel potent, selective, orally available soluble guanylate cyclase (sGC) stimulator.

Lorpiprazole (brand name Normarex) is a marketed anxiolytic drug of the phenylpiperazine group. It has been described as a serotonin antagonist and reuptake inhibitor (SARI) in the same group as trazodone, nefazodone, and etoperidone.

Leucinocaine is the local anaesthetic with actions similar to lignocaine. It has been used by topical application for local pain relief.

Ritobegron (KUC 7483) is a selective β3-adrenoceptor agonist that was developed for oral treatment of overactive bladder. It is the prodrug of the active compound KUC-7322. Phase I studies have investigated the pharmacodynamic and pharmacokinetic effects of ritobegron in healthy individuals and patients with spinal cord injury. Ritobegron exhibits a high selectivity for the bladder versus other organs, and decreased intravesical pressure with minimal effects on the cardiovascular system in rats. When administered in combination with organic anion transporter (OAT) inhibitors such as probenecid (primarily used in treating gout and hyperuricemia), the plasma concentration of the active compound KUC-7322 may increase.