Naphthonone is an antitussive agent.

Vicriviroc or SCH 417690 is a potent and selective antagonist of the CCR5 receptor. vicriviroc binds specifically to the CCR5 receptor and prevents infection of target cells by CCR5-tropic HIV-1 isolates. In antiviral assays, vicriviroc showed potent, broad-spectrum activity against genetically diverse and drug-resistant HIV-1 isolates and was consistently more active than SCH-C in inhibiting viral replication. This compound demonstrated synergistic anti-HIV activity in combination with drugs from all other classes of approved antiretrovirals. Competition binding assays revealed that vicriviroc binds with higher affinity to CCR5 than SCH-C. Functional assays, including inhibition of calcium flux, guanosine 5'-[35S]triphosphate exchange, and chemotaxis, confirmed that vicriviroc acts as a receptor antagonist by inhibiting signaling of CCR5 by chemokines. Finally, vicriviroc demonstrated diminished affinity for the human ether a-go-go related gene transcript ion channel compared to SCH-C, suggesting a reduced potential for cardiac effects. Vicriviroc represented a promising new candidate for the treatment of HIV-1 infection. Vicriviroc for HIV treatment was previously in Phase III studies but has since been discontinued.

Etalocib (LY-293111 or VML 295) is a potent and orally active leukotriene B4 receptor antagonist of the biphenylphenol class. It efficiently blocks neutrophil activation and subsequent inflammation. Additionally, it exerts antineoplastic properties through induction of cell cycle arrest and apoptosis in tumor cells. Etalocib was being developed for the treatment of inflammatory diseases and solid tumors.

Cyprodenate is a stimulant drug, developed by the French company Les Laboratoires Albert Rolland. Cyprodenate was used in the clinical practice to correct the tranquilizing action of benzodiazepine drugs. Upon administration, cyprodenate is hydrolyzed to produce dimethylethanolamine (deanol), which is a precursor of choline, and may enhance central acetylcholine formation.

Denotivir is an organic chemical compound with antiviral activity. In vitro antiviral activity of denotivir has been demonstrated against human HSV types 1 and 2, and varicella zoster virus (VZV). Clinical trials with vratizolin have given impressive results in the patients with local HSV infections and very good results in VZV infections. Genital herpes, a sexually transmitted HSV infection, whose incidence is increasing and whose treatment has never been adequate, appears to respond well to the treatment with vratizolin with very good results. Very good therapeutic results were also obtained by applying vratizolin to the patients with an ophthalmic HSV infection. Vratizolin exerted strong immunosuppressive actions. Vratizolin inhibited to some degree LPS-induced cytokine production in human peripheral blood cultures. The activities of TNF-alpha, IL-1 and IL-6 were inhibited on average by 37, 26 and 35%, respectively.

Besonprodil (also known as CI-1041), an NR2B subunit specific NMDA receptor antagonist, has been developed for the treatment of certain inflammatory and neuropathic pain, however, these studies were discontinued. Besides, besonprodil was investigated as a supplemental medication for Parkinson's disease. Experiments on animals have shown that this drug could be effective in counteracting the dyskinesia associated with long-term treatment with levodopa and related drugs.

Bromofenofos is an anthelminthic agent used in veterinary medicine to treat common liver fluke (Fasciola hepatica) infections in cattle and sheep.

Piragliatin is a nonessential, mixed-type (i.e. increases maximal velocity and affinity of glucokinase for glucose) small-molecule activators of glucokinase. Preclinical pharmacology studies confirmed that piragliatin had activity in both pancreatic beta-cell and hepatic cell glucose metabolism. Piragliatin augmented glucose-stimulated insulin secretion (GSIS) in human islets from both normal individuals and patients with type 2 diabetes, primarily by left-shifting the glucose dependency curve of GSIS. In healthy volunteers a single administration of piragliatin showed dose-dependent reduction of fasting plasma glucose. The glucokinase activator piragliatin has an acute glucose-lowering action in patients with mild type 2 diabetes, mainly mediated through a generalized enhancement of beta-cell function and through fasting restricted changes in glucose turnover. Headache and mild hypoglycemia were the most frequent adverse events associated with piragliatin treatment. The effect of piragliatin treatment on the QTc interval was dose/exposure dependent following short-term multiple doses. Piragliatin had been in phase II clinical trial for the treatment of Type 2 diabetes mellitus. However, this development was discontinued.

Valategrast (R-411) is a dual-acting α4/β1 - α4/β7 integrin antagonist which underwent clinical development with Roche for the treatment of multiple sclerosis (MS) and asthma. Phase I and II studies have been conducted. It had shown good efficacy in animal disease models. Following oral administration, R-411 was rapidly and completely biotransformed into its active metabolite, RO-0270608, most of which was eliminated by biliary excretion. R-411 had shown acceptable pharmacokinetics and good safety in healthy volunteers. R-411 inhibited eosinophil and T H 2 cell excitation and survival, and inhibited eosinophil migration from blood to pulmonary tissues. The idea of combining R-411 with montelukast (leukotriene antagonist) in the pharmaceutical dosage forms, therefore, provided a therapeutic treatment that had the combined effect of reducing circulating eosinophil counts and reducing eosinophil egress into pulmonary tissues, thereby providing an early onset of bronchodilation as well as sustained anti-inflammatory effects. Valategrast had been in phase II clinical trials by Roche for the treatment of asthma and in phase I clinical trials for the treatment of multiple sclerosis (MS). However, the study had been discontinued. Development of Valategrast was discontinued for the treatment of asthma after clarification of the regulatory framework for that class of compounds.

Lemildipine is a 1,4-dihydropyridine calcium channel blocker which is under phase III development by Banyu (Merck and Co), in Japan, for its potential to treat hypertension and cerebrovascular ischemia. In one study, involving five patients with essential hypertension accompanied by cerebrovascular disorder, lemildipine, administered orally at doses of 5 to 20 mg/day, significantly lowered blood pressure and increased cerebral blood flow. Another study in 31 patients with essential hypertension demonstrated that lemildipine has significant pressure lowering effects without affecting serum lipids. Worldwide rights to market the drug have been assigned to Kowa in Japan.