Spirilene is an antipsychotic agent. In rabbit caudate nucleus (CN) spirilene exhibited Ki value of 3.5 uM at the 5-HT1R site, but produced less than 50% inhibition of [3H]5-HT binding to the 5-HT1D site even at concentrations as high as 100 uM.

Stearylsulfamide is a sulfanilamide derivative patented by American Cyanamid Co. for the treatment of bacterial infections. Stearylsulfamide was never marketed.

Lodinixil is antilipidaemic and anti-atherosclerotic agent. It had been in the preclinical phase for the hyperlipidemia treatment but this development was discontinued.

Sulfasuccinamide is a sulfonamide antibacterial with properties similar to those of sulfamethoxazole. It has been applied topically in the treatment of local infections of the ear, nose, and throat. It has also been given as the sodium salt. Sulfasuccinamide is a carbonic anhydrase inhibitor.

Dezinamide is a potential antiepileptic drug that binds to the voltage-sensitive sodium channel. It is a metabolite of fluzinamide. It was active in preventing maximal seizures induced in mice or rats by electroshock and threshold seizures induced in mice by metrazol, bicuculline, and picrotoxin. It was predominantly active against tonic-clonic seizures. Adverse experiences included headache, ataxia, blurred vision, diplopia, dizziness, lightheadedness, and mild confusion. Dezinamide development was discontinued because of toxicity problems not observed with the metabolite.

Libenzapril is a long-acting, small polar angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Libenzapril competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Libenzapril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow. Both libenzapril and water transport was found to be significantly higher (about two- to five-fold) in six of the seven different brain regions in hypertensive rats as compared to the normotensive controls.

Adipiplon is an oral, partial agonist of the GABAA alpha-3 (α3) receptor that was being developed by Neurogen Corporation for the treatment of insomnia, anxiety disorders and schizophrenia. Adipiplon has been tested in Phase 1 and 2 studies in over 600 subjects for the treatment of insomnia, demonstrating statistical significance compared to placebo on primary endpoints for sleep initiation and maintenance in patients with chronic insomnia. Adipiplon has also demonstrated statistical significance compared to placebo for self-reported quality of sleep in all completed Phase 2 studies to date. Additionally, in studies completed to date it has been well tolerated at all doses tested. Development of adipiplon was discontinued during 2008.

Vercirnon (GSK-1605786, CCX-282, nTraficet-EN) is a selective, and potent antagonist of human CCR9. Vercirnon binds to the intracellular side of the receptor, exerting allosteric antagonism and preventing G-protein coupling. CCR9 is a tissue-specific lymphocyte trafficking molecule that selectively attracts both B- and T-cells to the small gut. Inhibition of CCR9 by GSK-1605786 may inhibit B- and T-cell entry to the small gut and ameliorate inflammation while leaving immune function at other anatomical sites unaffected. Vercirnon is an orally bioavailable, anti-inflammatory agent that is being developed by ChemoCentryx for treatment of inflammatory bowel disease with an initial focus in Crohn's disease. A pivotal phase III programme of vercirnon was initiated in patients with moderate-to-severe Crohn's disease, however, the programme was suspended when the first pivotal trial failed to meet its primary endpoint. Phase II trials for ulcerative colitis and celiac disease were conducted, however investigations for ulcerative colitis were suspended while no further development has been reported for celiac disease.

Galunisertib is a potent inhibitor of TGF beta type 1 receptor. The drug is under clinical development for the treatment of different cancers: pancreatic, hepatocellular, breast, rectal, prostate etc. and reached phase 2/3 in patients with myelodysplastic syndromes.