Scopoletin is a coumarin that can be isolated from plants of the genus Scopolia. It has been identified as a natural antifungal compound. Scopoletin was also demonstrated to be an MAO inhibitor capable of increasing dopamine levels in mice and is therefore of potential interest for developing treatments for neurodegenerative diseases.

Granotapide (JTT-130) has been studied for use in treatment of diabetes mellitus type II. This intestine-specific microsomal transfer protein inhibitor has hypoglycemic effects. Granotapide is thought to block fat absorption, which results in enhanced glucose-stimulated insulin secretion and enhanced insulin sensitivity. In an animal study, granotapide improved hyperglycemia and dyslipidemia via a mechanism independent of suppression of food intake. Granotapide enhances glucagon-like peptide-1 secretion and reduces lipotoxicity. A phase 2 study has been conducted to evaluate the effect of JTT-130 on diabetes as well as the safety and tolerability of JTT-130 in obese Type 2 diabetic patients.

Ravatirelin is a thiazolyl-alanine derivative patented by Japanese pharmaceutical company Shionogi & Co., Ltd. as a thyrotropin-releasing compound with improved central nerve activating effects such as sustained acetylcholine-releasing effect, and spontaneous motility increasing effect. Rovatirelin binds to the human thyrotropin-releasing hormone receptor with nanomolar affinity and increases the spontaneous firing of action potentials in the acutely isolated noradrenergic neurons of rat locus coeruleus. In in vivo studies, oral administration of Ravatirelin increased both c-Fos expression in the LC and extracellular levels of noradrenaline in the medial prefrontal cortex of rats. Furthermore, Ravatirelin increased locomotor activity. The increase in noradrenaline level and locomotor activity by Ravatirelin was more potent and longer acting than those by taltirelin. In phase I studies in healthy adult males, Ravatirelin exhibited linear pharmacokinetics in a single-ascending dose (0.1 to 10 mg) and a benign safety profile supportive of once-daily oral administration. From results of Phase II and III studies to evaluate the efficacy and safety of Ravatirelin in spinocerebellar degeneration patients, a daily dose of 1.6 to 3.2 mg of Ravatirelin has been considered to be dosage level intended for clinical use as once-daily oral administration.

Burixafor is an orally bioavailable inhibitor of CXC chemokine receptor 4 (CXCR4) with receptor binding and hematopoietic stem cell-mobilization activities. Burixafor binds to the chemokine receptor CXCR4, thereby preventing the binding of stromal derived factor-1 (SDF-1 or CXCL12) to the CXCR4 receptor and subsequent receptor activation; this may induce the mobilization of hematopoietic stem and progenitor cells from the bone marrow into the blood. CXC motif chemokine receptor 4 (CXCR4) blockade is pursued as an alternative to mesenchymal stem cell treatment after heart transplantation. The augmentation of conventional mycophenolate mofetil plus corticosteroids with a CXCR4 antagonist is potentially effective in improving outcomes after heart transplantation in humans

Ordopidine (also known as ACR-325) is a dopaminergic stabilizer that acts as dopamine D2 receptor antagonists with low affinity. Ordopidine under the development of NeuroSearch participated in phase I trials for the treatment of Parkinson's disease and bipolar disorder. Information about the current study of this drug is not available.

Saniona was developing seridopidine (also known as ACR343), a modulator of dopaminergic activity, as an orally administered therapy for schizophrenia, Tourette's syndrome and parkinson's disease. Seridopidine is a modulator of dopaminergic activity.

Cenisertib (also known as R763) is water-soluble, synthetic small molecule aurora kinase inhibitor with potential antineoplastic activity. Cenisertib is a potent adenine triphosphate-competitive inhibitor of Aurora kinase isoforms A–C, disrupting mitotic spindle activity, blocking cell separation, and leading to polyploidy and cell death. At low nanomolar concentrations, Cenisertib also inhibits other kinases involved in cell survival and proliferation including FLT3, BCR-ABL1, and BCR-ABL1 with T315I mutation. It also inhibits JAK2 kinase, but at higher concentrations. Preclinically, Cenisertib has demonstrated potent antitumor activity as a single agent and in combination treatment in leukemia cell lines, freshly isolated leukemia cells, and leukemia xenograft models. Toxicities appear to be related mainly to the gastrointestinal and hematopoietic systems. In animal models, activity and toxicity depend not only on dose but also on the schedule of administration.