Piridoxilate is a conjugation product of pyridoxine and glyoxylic acid in which pyridoxine is supposed to facilitate in vivo transformation of glyoxylic acid to glycine rather than to oxalic acid. The protective action of piridoxilate against hypoxia and metabolic inhibition of the myocardium was confirmed in the experiments on the canine heart-lung preparation using the redox potential of the myocardium and the pyridine nucleotide fluorescence of the heart as indices of cellular energy metabolism. The protective action of piridoxilate against hypoxia which may be attributable to rearrangement of the myocardial metabolism. Piridoxilate did not induce any significant changes in objective and subjective sleep variables. Long-term treatment with piridoxilate may result in overproduction of oxalic acid and in calcium oxalate nephrolithiasis. Piridoxilate should be added to the list of chemicals responsible for chronic oxalate nephropathy.

Peliglitazar (also known as BMS 426707-01), a dual α/γ peroxisome proliferator-activated receptor agonist, has been studied in phase I/II clinical trial in patients with type 2 diabetes mellitus. However, this study was discontinued.

Brequinar is a synthetic quinolinecarboxylic acid analogue with antineoplastic properties. Brequinar inhibits the enzyme dihydroorotate dehydrogenase, thereby blocking de novo pyrimidine biosynthesis. This agent may also enhance the in vivo antitumor effect of antineoplastic agents such as 5-FU. Brequinar had been in phase II clinical trials by Bristol-Myers Squibb for the treatment of cancer and transplant rejection. However, this research has been discontinued. Brequinar had been also in preclinical studys for the treatment of cytomegalovirus infections. However, this research has been discontinued.

Dersalazine is a locally-acting compound. It is a potent platelet activating factor (PAF)-antagonist. Dersalazine inhibited IL-1beta or TNF-alpha production in THP-1 or U937 cells, respectively. Dersalazine sodium reduced colonic proinflammatory cytokines IL-1b, IL-6, and IL-17 in dextran sodium sulphate (DSS)–induced colitis. After oral administration, dersalazine sodium is mostly unabsorbed until it reaches the large bowel where the azo bond is reduced by bacteria releasing the active compound. Dersalazine had been in phase I clinical trial for the treatment of ulcerative colitis. No serious adverse reactions were detected in clinical trial. However, no recent development has been reported.

Brocrinat is an ethacrynic acid derivative with diuretic activity. Chronic dosing with Brocrinat does not increase plasma uric acid suggests that therapeutically, Brocrinat as a diuretic may be useful in patients where control of plasma uric acid is desirable..

Ertiprotafib was originally developed as an inhibitor of PTP1B. Multiple targets of ertiprotafib, in addition to PTP1B inhibition, have been suggested including dual PPARalpha/PPARgamma agonism and IKK-beta inhibition. It normalized the plasma glucose and insulin levels in diabetic animal models and progressed to a phase II clinical trial for the treatment of Type 2 diabetes mellitus. Ertiprotafib development has been discontinued.

Cyclobutoic acid is a synthetic analog of mevalonic acid, developed by the Italian company Farmitalia Carlo Erba SPA. The compound inhibited the incorporation of [14C] into CO2, fatty acids and cholesterol, and was used for the treatment of hepatic deficiency.

Sulfaloxic acid is a benzamide derivative patented by Chemische Fabrik von Heyden A.-G. as an antibacterial agent.