Ramciclane is a bicycloheptyloxyethanamine derivative that acts with sedative activity.

Varespladib (LY315920; A-001) is a potent and selective inhibitor of IIa, V, and X isoforms of human non-pancreatic secretory phospholipase A2 with nM IC50. The molecule acts as an anti-inflammatory agent by disrupting the first step of the arachidonic acid pathway of inflammation. Varespladib methyl is being developed by Anthera Pharmaceuticals Inc for the potential treatment of coronary artery disease, acute coronary syndrome and inflammation. Varespladib methyl is a prodrug that is rapidly metabolized to varespladib, and both compounds are able to potently inhibit the enzymes of the human secretory phospholipase groups. Phase II clinical trials of varespladib methyl in patients with coronary artery disease, rheumatoid arthritis, asthma and ulcerative colitis revealed that the drug was well tolerated. Varespladib methyl did not demonstrate a good efficacy profile in patients with rheumatoid arthritis, asthma and ulcerative colitis; whereas in patients with coronary artery disease, varespladib methyl consistently reduced LDL-cholesterol levels, (elevated LDL-cholesterol levels are a marker of increased cardiovascular risk). Varespladib methyl could represent a novel therapy for the treatment of cardiovascular disease, although the efficacy, safety profile and advantages of this drug compared with existing therapeutic options would need to be established in upcoming phase III trials.

Dexpemedolac is long-acting non-narcotic analgesic. Dexpemedolac exhibited potent analgesic effects against chemically induced pain in rats and mice and against inflammatory pain in rats. Dexpemedolac differed from standard nonsteroidal anti-inflammatory drugs (NSAIDs) in that the doses, which produced analgesia were much lower than those required for either anti-inflammatory or gastric irritant effects. The common to the NCAIDs class actions are antipyresis and inhibitory effects on platelet aggregation. In yeast-induced hyperthermic rats, dexpemedolac exhibited antipyretic actions, whereas the drug did not affect body temperature in normothermic animals. Aggregation of human platelets was inhibited by high concentrations of dexpemedolac.

Nitralamine is an antifungal agent.

Midaglizole (also known as DG 5128) is a α2 adrenoceptor antagonist. Daiichi Pharmaceutical developed this drug as an oral antidiabetic agent and to treat asthma. However, further study of this drug was discontinued.

Emapunil acts as a selective agonist at the peripheral benzodiazepine receptor (TSPO). At the cellular level, the selective TSPO ligand XBD173 potentiated the amplitude and duration of GABA-mediated inhibitory postsynaptic currents in mouse medial prefrontal cortical neurons, which was prevented by finasteride. In animal and human trials, XBD173 produced rapid anxiolytic and anti-panic effects probably via newly synthesized neurosteroids, without producing sedation or withdrawal symptoms, and may represent a promising target for the development of fast-acting anxiolytics with a more favourable side-effect profile than benzodiazepines.

Ambasilide, a class III antiarrhythmic, has been shown to block multiple cardiac channels in a variety of animals including humans. Ambasilide is a potassium channel antagonist. Ambasilide has multichannel blocking properties including beta-adrenergic antagonism.

Amiterol, a phenethylamine derivative, is an oral anti-asthma drug (bronchodilator).

Telinavir (previously known as SC-52151) was developed as an anti-HIV aspartyl protease inhibitor for the treatment of HIV Infections. Telinavir participated in Phase I/II clinical study. In spite of the drug was well tolerated no antiviral activity was produced and further development of the drug was discontinued.

Milfasartan is an inhibitor of angiotensin II receptor type 1 was used in phase II clinical trial for the treatment of hypertension. However, these studies were discontinued.