Pruvanserin (EMD 281014, LY-2422347) is a selective serotonin 5-HT2A receptor antagonist. Pruvanserin was originated by Merck KGaA. Eli Lilly had been developing pruvanserin, under a global licence from Merck KGaA, for the treatment of primary insomnia and major depressive disorder. Phase II trials were completed in the US, Hungary and Spain. However, development appears to have been discontinued.

Pyridarone is a 2-Pyridylbenzofuran derivative patented by Societe Belge de l'Azote et des Produits Chimiques du Marly S.A. as anxiolytic useful for the treatment of fear in emotions of psychogenic origin.

Pumosetrag is a novel, orally active and selective 5-HT 3 agonist. It is a partial agonist in rats and guinea-pig and a full agonist in the mouse, suggesting important species differences in 5-HT3 receptor structure. Pumosetrag had been in phase II clinical trials for the treatment of gastroesophageal reflux disease and irritable bowel syndrome. No serious adverse events were reported. Diarrhea was not more common on the drug and only one subject experienced pruritus. All researches on this drug candidate are discontinued.

Senazodan (previously known as MCI 154), a positive inotropic agent that inhibits phosphodiesterase III and possesses a vasodilating property. Senazodan was studied in the phase II clinical trial in Japan in patients with acute heart failure. However, this study was discontinued.

Sepimostat (also known as FUT-187) was developed as a serine protease inhibitor including Clr, Cls, kallikrein, trypsin, plasmin, and thrombin. Sepimostat participated in early phase II clinical study on patients with reflux esophagitis. As a result, sepimostat could be used for postgastrectomy reflux esophagitis at the dose level of 300 mg/day or less. Experiments on rodents have shown that the drug could be also useful in the therapy of alcohol-induced pancreatitis. However, all these studies were discontinued.

Serfibrate, a clofibrate derivative, is a peroxisome proliferator activated receptor-α (PPAR-α) agonist. It is a hypolipidemic agent.

Nicocortonide is an anti-inflammatory corticosteroid for topical use.

Ioprocemic Acid is hydrocinnamic acid derivative patented by Schering-Kahlbaum A.-G. as radiographic contrast medium for liver imaging

Inogatran is a low molecular weight dipeptide and competitive thrombin inhibitor developed by Aktiebolaget Astra for the potential treatment of arterial and venous thrombotic diseases. lnogatran reversibly binds to the catalytic site of the thrombin molecule, thereby in a stoichiometric fashion inhibiting both clot-bound thrombin. Its biological half-life in plasma is about 1 h and it is evenly eliminated in the urine and bile. lnogatran has shown promising antithrombotic effects in a porcine model of coronary thrombosis. Unfortunately, Inogatran failed to demonstrate superior efficacy and safety to unfractionated heparin as antithrombotic agent and clinical development was discontinued.

MK-0686 is a bradykinin B1 receptor antagonist patented by American multinational pharmaceutical company Merck & Co for the treatment of neuropathic pain and inflammation. MK-0686 demonstrates significantly reduced susceptibility to human P-gp mediated efflux and shows good potential for human CNS penetration based on brain levels in CF-1 mice and monkeys. Additionally, MK-0686 also exhibited good CNS bradykinin B1 receptor occupancy in the transgenic rat expressing the human B1 receptor and showed oral efficacy in reducing CFA-induced hyperalgesia in a humanized mouse. Unfortunately, in phase II clinical trials MK-0686 failed to demonstrate efficacy in phase II clinical trials.