Celivarone is a benzofuran derivative with a multifactorial mode of action including class IV Vaughan Williams’ electrophysiological as well as anti-adrenergic properties. It has no iodine and has a limited tissue accumulation compared with amiodarone. Celivarone exhibits effective anti-arrhythmic properties in several ventricular ischemia- or reperfusioninduced arrhythmia models as well as in in vitro and in vivo atrial fibrillation (AF) models. Its electrophysiological properties are similar to amiodarone (multifactorial mode of action) but with different relative effects on the ion channels. At the ventricular level, celivarone shows anti-arrhythmic activities by suppressing reperfusion-induced arrhythmias (i.v. and oral routes) and reducing the early mortality due to myocardial infarction (oral route) in rats models. At the atrial level, celivarone is effective in atrial fibrillation models with restoration of sinus rhythm or prevention of AF induction and AF recurrence.

Benzobarbital (under the brand name Benzona), a barbiturate derivative developed in Russia that is used to treat convulsive forms of epilepsy, newborn hemolytic disease, and insomnia.

Mazapertine (RWJ-37796) is an arylpiperazine antipsychotic with high affinity to dopamine D2 and D3, serotonin 5-HT1A and alpha 1A-adrenergic receptors. It was being studied in the treatment of schizophrenia.

Lometrexol, formerly known as DDATHF; LY 264618; T-64 was the first glycinamide ribonucleotide formyl transferase (GARFT) inhibitor to be investigated clinically. Lometrexol had been in phase II clinical trial for the treatment non-small cell lung cancer (NSCLC). However, the studies have been discontinued by Tularik Inc, because Company had suggested, that drug would face competition from other companies in the indication

Delmetacin is a non-steroidal anti-inflammatory agent related to indomethacin. It has analgesic, antipyretic and anti-inflammatory properties.

Cariporide is a selective sodium-hydrogen antiporter inhibitor patented by a pharmaceutical company Hoechst A.-G. for treatment myocardial ischemia-reperfusion injury. The sodium-hydrogen exchanger is an important player in the pathophysiology of myocardial ischemia-reperfusion injury. The accumulation of hydrogen ions in the myocyte cytosol; during ischemia creates a proton gradient that promotes the efflux of hydrogen ions in exchange for the influx of sodium ions. This sodium buildup can secondary activates the sodium-calcium exchanger to operate in the reverse mode, resulting in a net calcium accumulation in myocyte cytosol, which leads to dysfunction and cell death. By inhibiting sodium-hydrogen exchange, Cariporide can prevent the accumulation of calcium in the cytosol, therefore reduce the infarct size. In clinical trials, Cariporide shows a statistically significant decline in myocardial infarction but increases mortality. Due to the increase in mortality, cariporide did not pass clinical trials.

Salmisteine was studied as an antipyretic and mucolytic agent. Information about the current use of this compound is not available.

Tifurac is a benzofuranacetic acid derivative patented by Syntex, Inc. as an analgesic, anti-inflammatory, and antipyretic agent. In preclinical models, Tifurac can exert anti-inflammatory and analgesic activity in rat paw edema assay and mouse writhing assay.

Otamixaban is a synthetically derived parenteral fXa inhibitor currently in late stage clinical development at Sanofi-Aventis for the management of acute coronary syndrome. Otamixaban is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa. Factor Xa (fXa) is a critical serine protease situated at the confluence of the intrinsic and extrinsic pathways of the blood coagulation cascade. FXa catalyzes the conversion of prothrombin to thrombin via the prothrombinase complex. Its singular role in thrombin generation, coupled with its potentiating effects on clot formation render it an attractive target for therapeutic intervention. In vivo experiments have demonstrated that Otamixaban is highly efficacious in rodent, canine and porcine models of thrombosis. In addition, recent clinical findings indicate that Otamixaban is efficacious, safe and well tolerated in humans and therefore has considerable potential for the treatment of acute coronary syndrome. Following the results of the Treatment of non-ST elevation Acute coronary syndrome with otamixaban, Sanofi has decided to discontinue the investigational programme with otamixaban, due to efficacy lower than expected. Otamixaban did not show superior benefit/risk to the combination of unfractionated heparin.

Boehringer Ingelheim is developing BI-671800, an orally administered treatment for seasonal allergic rhinitis and asthma. BI-671800 is an antagonist of the PGD2 receptor, CRTH2. PGD2 stimulates bronchoconstriction and allergic airway inflammation in animal models. Inhibition of CRTH2 may reduce airway inflammatory cells, IL -4, -5, -13 production, serum IgE and airway hyper reactivity. Treatment with BI-671800 in poorly controlled asthmatic patients receiving FP was associated with a significant improvement in FEV1. BI-671800 was well tolerated at a total daily dose of 800 mg for 6 weeks.