Hexaprofen, a potent anti-inflammatory agent, is an inhibitor of platelet aggregation. Experiments on mice have shown that hexaprofen could reduce the quantity and size of Lewis lung carcinoma (LLC) tumor nodules.

Oxarbazole was developed as an antiasthmatic agent that inhibited the only bronchoconstriction induced by immune complexes. This drug has never been marketed.

Acevaltrate is an iridoid found in variable amounts in Valerianaceae and might be among the bioactive compounds which confer anxiolytic properties to the Valeriana species. Acevaltrate inhibited total H⁺/K⁺-ATPase activity (60.7 ± 7.3 %) from rat gastric epithelium. Acevaltrate inhibited Na⁺/K⁺-ATPase with IC₅₀ value of 22.8 uM. Na⁺/K⁺-ATPase might be one of their molecular targets of Acevaltrate in vivo.

Sobetirome (3,5-dimethyl-4[(4'-hydroxy-3'-isopropylbenzyl)-phenoxy] acetic acid, also known as GC-1 and QRX-431, is a member of a class of compounds known as selective thyromimetics. It was firstly developed by Thomas Scanlan’s group at the University of California-San Francisco (UCSF) in 1995. Sobetirome binds selectively to the main hepatic form of thyroid hormone (TH) receptor, TRβ1, compared to TRα1, which is principally responsible for thyrotoxic effects on heart, muscle and bone. Sobetirome also preferentially accumulates in liver. It was originally envisaged that sobetirome could be used to stimulate hepatic pathways that lower cholesterol without harmful side effects and might be used in conjunction with statins. Indeed, sobetirome progressed through preclinical animal studies and Phase I human clinical trials with excellent results and without obvious harmful side effects. Sobetirome had been in phase I clinical trials for the treatment of lipid metabolism disorders and obesity. However, this research has been discontinued.

Metaglycodol is a tranquilizer.

Niravoline [RU 49679, RU 51599, niravolin], a novel aqueous diuretic with κ-opioid agonistic action. The drug was originally being developed by Hoechst Marion Roussel. Niravoline is a selective agonist of kappa-opioid receptors having potent aquaretic activity. Niravoline was studied with respect to the treatment of brain oedema, heart failure and liver cirrhosis. Niravoline, administered at moderate doses, safely induced a powerful aquaretic effect in patients with cirrhosis and ascites. Moderate doses of niravoline appeared to be a promising pharmacological tool in the treatment of water retention in patients with cirrhosis. The development of niravoline as an aquaretic for the treatment of cirrhosis with ascites and other hyponatraemic disorders has also been halted.

Melogliptin (EMD 675992 or GRC 8200) is an orally bioavailable dipeptidyl peptidase IV (DPP IV) inhibitor. Melogliptin was undergoing phase II clinical trials at Glenmark Pharmaceuticals and Merck KGaA for the treatment of type 2 diabetes. The completed 12 week Phase IIb clinical trial in 494 patients with type 2 diabetes melogliptin improved glycemic control in patients with type 2 diabetes mellitus and exhibited excellent safety and tolerability profile.

Sampatrilat (also known as UK 81252) was developed as a dual inhibitor of both angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP). This drug was studied for the treatment of hypertension and congestive heart failure.

Batelapine (or CGS 13429), an antipsychotic drug, that was undergoing preclinical development, but the further studied were discontinued