Benhepazone (also known as RCH-314) possessed potent analgesic and anti-inflammatory activities. Information about the nowadays use of this compound is not available.

FEPRADINOL is an analgesic, antipyretic and anti-inflammatory agent. Its anti-inflammatory activity does not seem to be related to an inhibitory effect on prostaglandin biosynthesis.

Brecanavir (previously known as VX-385), a HIV aspartyl protease inhibitor was developed for the treatment of HIV. The inhibition of HIV viral proteinase enzyme prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. Brecanavir reached Phase II development. However, GlaxoSmithKline announced to discontinue development brecanavir. Because of the inability to develop a viable oral dosage formulation capable of delivering the desired brecanavir levels in patients with multi-drug resistant HIV.

Benzetimide, a muscarinic acetylcholine receptor antagonist that was investigated as an antiparkinson-agent and was studied in the treatment of diarrheas of cattle and calves. Benzetimide is an enantiomer of dexetimide that has been used to treat neuroleptic-induced Parkinsonism.

LEDAZEROL is a derivative of mivazerol. It was under development as an antianginal agent.

Metaterol is a beta-adrenoceptor agonist. It exerts sympathomimetic and broncholytic properties.

Berubicin, an anthracycline derivative, is a DNA binding agent and potent topoisomerase II poison. Reata Pharmaceuticals were developing it as a treatment for brain cancer as it can breach the blood-brain barrier. It had also been in early clinical trials for the treatment of lung cancer and malignant gliomas. However, studies have been terminated. In October 2006, it was granted orphan drug designation from the FDA for the treatment of malignant gliomas. According to a CNS Pharmaceuticals media release in April 2018, berubicin will be studied for glioblastoma patients, these investigations will be funded in part by an equity crowdfunding campaign.

Wyeth was developing the small molecule plasminogen activator inhibitor-1 (PAI-1) antagonist aleplasinin for the treatment of Alzheimer's disease in the US. PAZ-417 inhibits PAI-I (Plasminogen activator inhibitor-1), thereby increasing the activation of plasminogen to form plasmin. There is some evidence that plasmin can increase the cleavage of amyloid precursor protein at the alpha cleavage site, which could reduce the formation or increase the clearance of amyloid beta, a suspected culprit in Alzheimer's disease. However, it`s development for Alzheimer's disease treatment was discontinued.

Elucaine is local anesthetic and anti-ulcerative agent, acting as a gastric muscarinic acetylcholine receptor antagonist.

Torcetrapib is a CETP inhibitor which was developed by Pfizer for the treatment of diseases associated with elevated level of cholesterol. The drug was tested in phase III (in combination with atorvastatin) of clinical trials in coronary heart disease patients as well as in patients with hyperlipoproteinemia, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, however its development was terminated due to the high risk of death and heart problems.