Oxiniacic Acid is a nicotinic acid derivative, that shows potent hypolipidemic activity.

Pumaprazole is imidazopyridine derivative patented by Byk Gulden Lomberg Chemische Fabrik GmbH for the treatment of gastrointestinal diseases. Pumaprazole acts as a reversibly binding acid pump antagonist. Pumaprazole differs from covalently binding proton pump inhibitors (PPIs), such as omeprazole, both with respect to chemical structure and mode of interaction with the gastric H(+)/K(+)-ATPase. In preclinical models, the single dose of Pumaprazole is able to elevate intragastric pH in the dog with gastric fistula under pentagastrin or carbachol stimulation from pH 1 to about pH 7 while still displaying a dose-dependent, well-controllable duration of action of a few hours.

Tifenazoxide is a thiadiazine derivative patented by Novo Nordisk A/S as the opener of the KATP-regulated potassium channels useful in the treatment of the endocrine system diseases. Tifenazoxide is a selective opener of the beta-cell type (SUR1 / Kir6.2) KATP channel that characterized as competitive inhibitors of glibenclamide binding to membranes of HEK293 cells expressing human SUR1/Kir6.2and as potent inhibitors of insulin release in isolated rat islets. In clinical trials, Tifenazoxide administration leads to a decrease in insulin concentrations 1 h post-dose. This was accompanied by an increase in glucose and growth hormone concentrations (NS), but not of glucagon. During the OGTT a dose-dependent reduction in the 2 h glucose value was observed.

Ingliforib, aka CP-368296, is a glycogen phosphorylase inhibitor with antihyperglycemic and cardioprotective properties. It has been implicated for use in the treatment of diabetes and for myocardial ischemic protection. Ingliforib was in phase II clinical trials for diabetes, but these efforts have been discontinued.

Tolpyrramide is a sulfonamide derivative with antihyperglycemic properties. It was used as an oral antidiabetic drug.

Plafibride is an acyl derivative of morpholinomethylurea (MMU) with clofibric acid. Plafibride is hypolipemic, platelet aggregation inhibiting agent. Plafibride did not act on the arachidonic acid metabolism. Plafibride inhibited the activity of 3',5'-cyclic AMP-phosphodiesterase, which is one of the principal mechanisms of inhibition of platelet aggregation. In the rat, plafibride inhibited significantly the spontaneously formed circulating platelet aggregates. In vitro plafibride appeared as an effective antiaggregant agent although less powerful than morpholinomethylurea, one of its presumed metabolites. The most evident secondary effects of plafibride were: a certain sedation, as a light tranquilizing agent, a hypothermic effect when it was administered at high doses, a certain beta-blocking and antiarrhythmic activity probably due to its local anesthetic action. All the side effects appeared at high doses, much higher than the therapeutic ones.

Donetidine is a potent and long acting histamine H2-receptor antagonist with no H1-receptor antagonist activity. It is a highly basic drug with several amine groups. Donetidine stimulates the release of histamine when given by rapid intravenous infusion to dogs. Symptoms such as vasodilation, watering eye and nose, salivation and collapse, well known indicators of histamine release seen after administration of donetidine.

Sufotidine is a triazolamine derivative patented by Glaxo Group Ltd. as long-acting histamine H2-blocker useful for the treatment of peptic ulceration and oesophagitis. In phase II clinical treatment with sufotidine decreases median integrated 24-hour intragastric acidity by 95% compared with placebo. Twice daily sufotidine maintained the pH above 3 throughout the 24 h. Unfortunately, no further development report has been published and it seems, that Sufotidine development currently discontinued.

Spizofurone (also known as AG-629) is a spirobenzofuranone derivative patented by Japan's largest pharmaceutical company Takeda Chemical Industries, Ltd. as the anti-ulcer agent. In preclinical models Spizofurone dose-dependently increase in gastric mucosal blood flow in anesthetized dogs. The reduction in the gastric mucosal blood flow as induced by indomethacin was markedly improved by spizofurone. The topical action of spizofurone was confirmed in an in situ experiment using a stomach flap fixed to a lucite chamber. Spizofurone given orally or i.p. in a dose range of 25-200 mg/kg inhibited indomethacin-induced gastric antral ulcers in rats. Furthermore, spizofurone potentiated the inhibitory effect of prostaglandin E2 on indomethacin-induced gastric antral ulcers. The increase in alkaline secretion in bullfrog duodenal mucosa seen in the presence of spizofurone is mediated, at least in part, by stimulation of endogenous prostaglandins synthesis.