Xylocoumarol is an anticoagulant that has never been marketed. Information about the current use of this compound is not available.

AT-406 (DEBIO-1143, SM-406), is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). AT-406 inhibits cancer cell growth in various human cancer cell lines. It has good oral bioavailability in mice, rats, non-human primates, and dogs, is highly effective in induction of apoptosis in xenograft tumors, and is capable of complete inhibition of tumor growth. Debiopharm under a licence from Ascenta Therapeutics is developing AT-406 for the treatment of cancers.

Tiquinamide (Wy 24081) is a potent inhibitor of gastric secretion and gives good protection in animals against gastric and duodenal erosions induced by stress and chemical stimuli. It reduces basal as well as stimulated acid secretion but has no anticholinergic activity and is only a weak histamine H2 antagonist, since it is substantially more potent in inhibiting basal acid-secretion than the established H2-receptor antagonists, metiamide and burimamide. Since no other pharmacological effect of tiquinamide has been detected in isolated tissues, it seems unlikely that the gastric antisecretory effect of the compound results from a direct action on the peripheral autonomic nervous system. The report from Dr. Szabo on the protective effect of dopamine agonists against duodenal ulceration suggests a possible mechanism of action for tiquinamide.

Timoprazole is a substituted benzimidazole patented by Aktiebolag Hassle as an antisecretory agent that inhibits gastric acid secretion by interference with (H+-K+)-ATPase. Timoprazole given orally was found to be cytoprotective for the stomach when given 30 min prior to a challenge to boiling water, ethanol, or HCl. Timoprazole also prevented necrosis of the mucosa and acute ulcerations induced by alcohol in the rat fundus, as evaluated by histopathology.

Milverine was studied as an antibacterial agent. Information about the current use of this drug is not available.

Neboglamine is a functional modulator of the glycine site on the N-methyl-D-aspartate (NMDA) receptor. Neboglamine appeared to promote neuronal growth as measured by expression of Fos-like immunoreactivity, particularly in the prefrontal cortex, nucleus accumbens, and lateral septal nucleus. Neboglamine behaves as a potential antipsychotic. Neboglamine is in phase II clinical trials by Rottapharm for the treatment of schizophrenia and cocaine abuse.

Mecrylate (metyl 2-cyanoacrylate) ) is a clear, colorless liquid with a strong, acrid odor. In contact with hydroxide ions (liquids like blood or water, air humidity), the cyanoacrylates form long, strong and waterproof chains in an exothermic reaction. The resulting polymer leads to a stable adhesive bond. It may be used as tissue adhesive in surgery. Mecrylate is the first generation short-chain cyanoacrylate, it turned out to be histotoxic and caused distinct foreign-body reactions.

Maraciclatide (NC100692 or diamine dioxime-Lys-Cys-Arg-Gly-Asp-Cyc-Phe-Cys-polyethylene glycol) is a cyclic peptide that contains an RGD tripeptide sequence held in a specific conformation by a disulphide and one thioether bridge. The ε-amino group of the lysine residue serves as an attachment point for the technetium chelator and the C-terminal end modified with a short polyethylene glycol unit. Cyclic RGD peptides such as this have a high affinity towards vitronectin receptors. Maraciclatide radiolabelled with technetium 99m (99mTc) is being developed as an in vivo diagnostic marker of vitronectin integrin receptor expression.

Lunacalcipol (CTA-018 or MT-2832) is a vitamin D analog having a dual mechanism of action. It inhibits CYP24A1 and induced VDR expression. It was being developed for the treatment of clinical consequences of vitamin D insufficiency and secondary hyperparathyroidism associated with chronic kidney disease. Lunacalcipol development has been discontinued.