Flutroline, an antipsychotic drug that was studied to treat patients with schizophrenia. Clinical trials have shown that the drug was a safe, effective, and 20 mg and above offered the best potential for optimal clinical effectiveness. However, information about the further development of this drug is not available.

Ezutromid (SMTC-1100) is a small molecule utrophin upregulator. Ezutromid was identified from an iterative analoging approach from initial hits identified using a human muscle-specific utrophin A promoter cell-based assay. It increases both utrophin RNA and protein resulting in a significant reduction in dystrophic symptoms and increased muscle function in dystrophin-deficient mdx mice ( a mouse model of Duchenne muscular dystrophy (DMD)). Ezutromid was deemed safe and well tolerated in a Phase 1a healthy volunteer study and successfully completed a Phase 1b study in DMD boys. Summit Therapeutics is developing Ezutromid for the treatment of Duchenne muscular dystrophy.

Semotiadil (also known as sesamodil or SD 3211) is a (+)-(R)-stereoisomer, the corresponding (−)-(S)-stereoisomer is called levosemotiadil. Semotiadil, a benzothiazine derivative was developed as a novel Ca2+ channel blocker with antiplatelet activity. Experiments on rodents have revealed that the drug had an advantage in the treatment of angina with regard to long-lasting action and selectivity for coronary artery and myocardium. In addition, semotiadil improved survival of rats with monocrotaline-induced pulmonary hypertension: comparison with diltiazem. Semotiadil was studied in phase II clinical trials for the treatment of angina pectoris and hypertension in Europe, and in Japan for the treatment of arrhythmias. However, the further development of semotiadil has now been discontinued.

Sulazepam is a desmethylbenzodiazepine. It is the thioamide derivative of diazepam. It has sedative, muscle relaxant, hypnotic, anticonvulsant and anxiolytic properties like those of other benzodiazepines. Sulazepam in vivo in experimental animals undergoes enzymic desulfonation, demethylation, and [3C] hydroxylation, with the formation of basic metabolites: diazepam, desmethyldiazepam, and oxazepam.

Indocate is indole derivative and monoamine oxidase inhibitor with peripheral antiserotonin properties.

Epelsiban (GSK557296), a pyridyl-2,5-diketopiperazine, is a potent, highly selective, and orally bioavailable non-peptide oxytocin receptor antagonist. GlaxoSmithKline was developing epelsiban for the treatment of women infertility due to adenomyosis and premature ejaculation.

Refametinib (RDEA-119, BAY- 869766) is a highly potent and selective inhibitor of mitogen-activated ERK kinase (MEK1/2) activity, Refametinib binds to an allosteric pocket adjacent to the ATP binding site, locking the enzyme in a catalytically inactive conformation. This compound is highly efficacious at inhibiting cell proliferation in several tumor cell lines in vitro. In vivo, Refametinib exhibits potent activity in xenograft models of cancers. Ardea Biosciences (a subsidiary of AstraZeneca) and Bayer HealthCare are developing refametinib for the treatment of cancer. The sulfonamide agent was originally developed by Valeant Pharmaceuticals International. Refametinib is in phase II development for hepatocellular carcinoma, and phase I/II development for pancreatic cancer and other solid tumours.

Raxofelast (IRFI 016) is a hydrophilic vitamin E-like antioxidant, that was developed to maximize the antioxidant potency of phenols related to vitamin E. It has been investigated as a mucoactive drug, a type of drug that is used for treatment of respiratory diseases. Also, in diabetic mice, raxofelast was shown to improve wound healing to a level close to that seen in healthy mice, and in another study it improved clinical outcomes in experimental burn wounds. In a rat model of myocardial damage, raxofelast was found to be a useful drug to reduce heart attacks. This compound has good bioavailability and physicochemical properties. No clinical trials have been conducted.

Ralimetinib (LY2228820), a trisubstituted imidazole derivative, is a potent and selective, ATP-competitive inhibitor of the α- and β-isoforms of p38 mitogen-activated protein kinase. LY2228820 produced significant tumor growth delay in multiple in vivo cancer models (melanoma, non-small cell lung cancer, ovarian, glioma, myeloma, breast). Eli Lilly is developing ralimetinib for the treatment of cancer.

Ralitoline is thiazolidinylidene derivative patented by Goedecke A.-G. as an anticonvulsant. In preclinical models, ralitoline blocks sustained repetitive firing of sodium action potentials with effects on firing activity triggered by spontaneous excitatory postsynaptic potentials at higher concentrations. No effects on iontophoretic GABA and glutamate responses were noted. Ralitoline inhibit the binding of tritiated batrachotoxinin A 20-alpha-benzoate ([3H]BTX-b) to rat brain synaptosomes. In healthy volunteers with single and multiple doses (50-200 mg). ralitoline is well absorbed by oral ingestion, with peak plasma concentrations occurring approximately 2-3 hr postdose. Approximately 2 weeks of administration of ralitoline had no effect on the steady-state kinetics of phenytoin or phenobarbitone in healthy volunteers.