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.

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

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.

Neflumozide is an antipsychotic.

Ethoxazene (2,4-diamino-4-ethoxyazobenzene) is an analgesic compound. It may be used as an indicator of acidity in an examination of gastric function.

Balamapimod, also known as MKI 833, a mitogen-activated protein kinase (Ras/Raf/MEK) inhibitor with potential anti-tumor activity. This compound can be used for the treatment of diseases that are results of deregulation of Ras/Raf/MEK kinases.

Tiflucarbine is a thieno[3,2-e]indole derivative patented by Troponwerke G.m.b.H. und Co. K.-G. as antidepressant. Tiflucarbine acts as a potent inhibitor of the 5-hydroxytryptamine (5-HT) uptake and has no effect on 5-HT2 postsynaptic receptors. In preclinical models, Tiflucarbine down-regulates the noradrenaline responses of the cAMP system in rats cerebral cortex. Tiflucarbine treatment increased the specific activity of soluble calmodulin (CaM)-dependent phosphodiesterase in rat brain. Tiflucarbine bound to CaM and inhibited its interaction with the phosphodiesterase. Adrenergic denervation by 6-hydroxydopamine injection prevented both the beta-adrenoceptor down-regulation and the increase in the specific activity of the phosphodiesterase. Tiflucarbine exerted no effect on the reserpine hypothermia, attenuated the apomorphine hypothermia and enhanced the TRH-induced hyperthermia. It did not prevent tryptamine convulsions or the fenfluramine-induced hyperthermia and inhibited the L-5-hydroxytryptophan-induced head twitches. Tiflucarbine administered repeatedly enhanced the D-amphetamine-induced locomotor hyperactivity and inhibited the clonidine-induced aggressiveness.

Desglugastrin is a gastric acid secretion stimulator. It dose dependently stimulated gastric acid secretion in anaesthetized rats. In view of the trophic action of gastrointestinal hormones on the exocrine pancreas, the effects of desglugastrin on the growth of hamster pancreatic well differentiated adenocarcinoma were investigated in vitro. Desglugastrin exhibited the greatest effect on thymidine incorporation into these cells after a lag period of 96 h. Doses of desglugastrin caused a significant and dose-dependent increase in thymidine incorporation.

Flunoprost is a prostaglandin analog. Flunoprost has been used to treat platelet-activating factor-induced shock and to prolong skin allograft survival in mouse models.

Enpiroline (WR 180,409) is an antimalarial compound. It demonstrates activity against Plasmodium falciparum both in vitro and in non-immune infected subjects. Additionally, it exerts antischistosomal activity.