Thiazosulfone (also known as Promizole) is a phenylsulfonylthiazole derivative patented by Parke, Davis & Co. as the anti-tuberculosis agent. In preclinical models, Thiazosulfone exerts a definitely favorable influence on the course of experimental tuberculosis previously established in the highly susceptible guinea pig. In clinical trials Thiazosulfone and Streptomycin combined therapy exerts favor influences on tuberculous meningitis. Thiazosulfone seems to have an inhibitory action on hematogenous tuberculosis. Its toxicity is very low and it can, therefore, be administered for a prolonged period.

Pirinixic acid is a PPARα ligand that can affect atherogenesis by modulating hepatic lipid metabolism and by acting directly on vascular tissue. PPARα activation is generally assumed to be the primary means by which Pirinixic acid produces its biological effects. Nevertheless, there is increasing evidence to suggest that Pirinixic acid is also capable of affecting cellular processes directly. It is under experimental investigation for prevention of severe cardiac dysfunction, cardiomyopathy and heart failure as a result of lipid accumulation within cardiac myocytes. Treatment is primarily aimed at individuals with an adipose triglyceride lipase (ATGL) enzyme deficiency or mutation. For example, cardiac contractility was improved by treating ATGL(-/-) mice with the Pirinixic acid.

The BET-bromodomain inhibitor OTX015 (MK-8628) was initially developed by Mitsubishi Tanabe Pharma Corporation, but then was licensed by OncoEthix, privately held biotechnology company. OTX015 is a selective bromodomains: BRD2, BRD3, and BRD4 inhibitor and inhibits their binding to AcH4. Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and differentiation to energy homeostasis and neurological processes. OTX015 has potent antiproliferative activity accompanied by c-MYC down-regulation in several tumor types, and has demonstrated synergism with the mTOR inhibitor everolimus in different models. Oral administration of OTX-015 markedly inhibited tumor growth and reduced tumor volume. OTX015 is currently in Phase 1b studies for the treatment of hematological malignancies and advanced solid tumors such as Triple Negative Breast Cancer, Non-small Cell Lung Cancer, Castrate-resistant Prostate Cancer (CRPC) and Pancreatic Ductal Adenocarcinoma. In addition, OTX015 was in phase II for the treatment of Glioblastoma Multiforme, but there were not detected clinical activity of the drug in the treatment populations and trial was closed.

Duoperone is a neuroleptic agent. Duoperone blocked d-amphetamine lethality in mice under aggregated conditions when the pretreatment interval was between one hour and seven days. Conditioned avoidance responding in mice and cats was suppressed by duoperone in doses that did not impair escape behavior. Duoperone produced catalepsy in rats. The onset of this effect was delayed and the duration was prolonged when compared with that of chlorpromazine. It was a potent antiemetic agent in dogs, with a delayed onset and prolonged duration of action.

Dicarbine is an orally active drug approved in Russia under the trade name Карбидин, is used for the treatment patients with schizophrenia and alcoholic psychosis. This drug blocks dopamine receptors in various brain parts, which leads to a reduction in the productive symptoms of psychosis: delusions and hallucinations.

Tiazuril is a triazinedione derivative patented by American multinational pharmaceutical corporation Pfizer Inc. as the coccidiostatic agent. Tiazuril controlled all the major species of poultry coccidia at low concentrations but elicited toxicological symptoms suggesting interference with nucleic acid synthesis.

Azeliragon is an orally bioavailable small molecule that inhibits the receptor for advanced glycation endproducts (RAGE). RAGE has been proposed to contribute to Alzheimer's disease pathology by promoting vascular leakage, promoting influx of peripheral amyloid beta into brain, mediating amyloid beta induced oxidative stress, mediating AGE induced hyperphosphorylation of tau and amyloid beta mediated neuronal death. Azeliragon is in Phase III clinical trial for the treatment of mild Alzheimer's disease.

Tarenflurbil (Flurizan or R-flurbiprofen) is the single enantiomer of the racemate NSAID flurbiprofen. Tarenflurbil is a first in class, selective amyloid-beta42 (A42) lowering agent (SALA), which acts by modulating the activity of gamma-secretase, an enzyme that converts amyloid precursor protein to amyloid-beta. The reduction of A42 may prevent the development of the amyloid plaques thought to be a key pathological process associated with Alzheimer’s disease. For several years, research and trials for the drug were conducted by Myriad Genetics, to investigate its potential as a treatment for Alzheimer's disease. In a brief statement issued June 30, Myriad Genetics reports that tarenflurbil (Flurizan) failed to have a significant effect in a phase 3 trial of patients with mild Alzheimer's disease (AD). The failure of Flurizan™ is generally attributed to its insufficient pharmacodynamics, i.e., inadequate ability to penetrate the brain and engage its target protein at doses sufficient to yield an effect. Two additional Phase 3 trials were terminated and further development of Flurizan™ was discontinued. Separate clinical development of Flurizan™ for prostate cancer has also been discontinued following negative Phase 2 results. Tarenflurbil activates c-Jun N terminal kinase, increases AP-1 binding to DNA, and downregulates cyclin D1 expression, resulting in the arrest of tumour cells in the G1 phase of the cell cycle and apoptosis. This agent also affects the expression of nuclear factor kappa B, a rapid response transcription factor that stimulates the immune response to tumour cells. Tarenflurbil does not inhibit the enzyme cyclooxygenase. The Fraunhofer Institute for Molecular Biology and Applied Ecology is currently developing tarenflurbil for the treatment of relapsing, remitting multiple sclerosis.

Esculamine is a hemostatic, vasodilator and anti-inflammatory agent.

Neflumozide is an antipsychotic.