Dibupyrone is an analgesic agent.

Coluracetam (code name BCI-540; formerly MKC-231) is a nootropic agent of the racetam family. It was initially developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer's disease. After the drug failed to reach endpoints in its clinical trials it was in-licensed by BrainCells Inc for investigations into major depressive disorder (MDD). Like most racetam compounds, Coluracetam increases choline uptake, but it also increases uptake in damaged neurons. Specifically, Coluracetam interacts with the HACU process, which is responsible for absorbing choline into the neurons. This increased uptake occurs during the Acetylcholine synthesis process. Since Coluracetam improves choline preservation during this process, a larger amount is converted into Acetylcholine. This results in increased memory, attention and alertness. It is important to note here, that these benefits were only seen in subjects with previously impaired neurons, not in subjects with normally functioning neurons. Coluracetam is also shown to improve AMPA potentiation, which is a process that triggers cognitive function and alertness. Although Coluracetam interacts with choline transporters as well, there isn’t enough evidence to explain why or how this interaction occurs, or what occurs after the interaction. Coluracetam has been in phase II clinical trials for the treatment of major depression and anxiety. However, this research has been discontinued.

Linopristin is a chemically modified form of quinupristin. It is an antibiotic of the streptogramin B class. It is one of the components of the antibiotic combination NXL103 (XRP 2868). NXL-103 is a combination of streptogramin A:streptogramin B components, initially developed in a 70:30 dose ratio. In multiple in vitro studies, NXL-103 demonstrated potent activity against different types of bacteria, such as Staphylococcus aureus (including MRSA), Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecium, Enterococcus faecalis, Haemophilus influenzae and Haemophilus parainfluenzae. In phase I clinical trials, NXL-103 achieved bactericidal levels in plasma and was generally well tolerated, with side effects primarily on the gastrointestinal system. The first phase II trial conducted to evaluate the efficacy of NXL-103 against community-acquired pneumonia revealed that the compound was comparable with amoxicillin. NXL-103 has promise to become an important agent in the treatment of community-acquired pneumonia and complex skin and soft tissue infections, pending further development.

Nelotanserin is a potent, selective 5-HT(2A) inverse agonist. Originally called ADP-125, the compound was developed by Arena Pharmaceuticals as a treatment for insomnia, but failed efficacy measures for this indication in Phase 2. In 2015, Axovant Sciences licensed this compound for development, renamed it nelotanserin, and began evaluating it in dementia with Lewy bodies (DLB). Both radioligand binding and functional inositol phosphate accumulation assays suggest that nelotanserin has low nanomolar potency on the 5-HT(2A) receptor with at least 30- and 5000-fold selectivity compared with 5-HT(2C) and 5-HT(2B) receptors, respectively. Nelotanserin dosed orally prevented (+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI; 5-HT(2A) agonist)-induced hypolocomotion, increased sleep consolidation, and increased total nonrapid eye movement sleep time and deep sleep, the latter marked by increases in electroencephalogram (EEG) delta power. Nelotanserin has been used in trials studying the treatment of Lewy body dementia, visual hallucinations, dementia with Lewy bodies, and REM sleep behavior disorder.

Aliflurane, a halocarbon drug, is an inhalational anesthetic.

Nebicapone (BIA 3-202) is a reversible, and tight-binding peripheral inhibitor of the enzyme catechol-O-methyltransferase (COMT) being developed for use as an adjunct to levodopa/dopa decarboxylase inhibitor in the treatment of PD. Nebicapone dose dependently and significantly decreased COMT activity. Nebicapone also increased systemic exposure to levodopa and improved motor response. The tight-binding nature of the inhibition produced by BIA 3-202 was evaluated by performing an Ackermann-Potter plot. The true K(i) for BIA 3-202, derived from the nonlinear regression analysis, was 0.19+/-0.02 nM. In substrate competition studies, an increase in the concentration of adrenaline resulted in a linear increase in IC(50) values for BIA 3-202.

Spirofylline, theophylline derivative, is a bronchodilator, which can be used to treat asthma and bronchitis and emphysema.

Pirodomast is Thromboxane A (TXA2) synthetase inhibitor. Pirodomast can inhibit leukotriene (LT) D4, C4, E4 formation and Thromboxane B2 (TXB2) activities. It was weak or ineffective as an antagonist of histamine, methacholine, serotonin, LTC4 or platelet activating factor induced bronchospasms in guinea pigs. Also, pirodomast was not a bronchodilator or calcium influx blocker and had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is, therefore, a potential antiallergic agent that inhibits leukotriene (LT) release. Pirodomast inhibited tryptase proteolytic activity in-vitro. In experimental studies in vivo, pirodomast blocked antigen-induced immediate and late asthmatic responses in allergic sheep. Pirodomast inhibited antigen-induced airway hyperresponsiveness to both histamine and carbachol in allergic sheep. Pirodomast was being investigated for use in asthma and allergic rhinitis.