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.

LAMTIDINE is an irreversible and specific gastric histamine H2-receptor antagonist.

Becliconazole (or 1-CBCMI) is an antimycotic agent. Information about the nowadays application of this drug is not available

Tiplasinin (PAI-039) is an orally efficacious and selective plasminogen activator inhibitor-1 (PAI-1) inhibitor. Tiplasinin bound specifically to the active conformation of PAI-1 and exhibited reversible inactivation of PAI-1 in vitro. Tiplaxtinin exhibited in vivo oral efficacy in two different models of acute arterial thrombosis. The remarkable preclinical safety and metabolic stability profiles of tiplaxtinin led to advancing the compound to Phase-I clinical trial for Thrombosis, which was later discontinued.

Cliropamine (D 16427) is a positive inotropic compound.

Cetaben has been identified as an anti-atherosclerotic hypolipidaemic substance. Cetaben is a unique, PPARα-independent peroxisome proliferator with hypolipidemic activity that inhibits cholesterol synthesis in the human hepatoma Hep-G2 cells resulting in reversible changes in Golgi morphology. Cetaben represents an exceptional type of peroxisome proliferator, specifically affecting peroxisomes, without having a negative influence on the processes of peroxisome biogenesis. Cetaben raised only the peroxisomal enzymes, acyl-CoA oxidase, glycerone-phosphate acyltransferase, D-amino-acid oxidase, catalase, and urate oxidase. Cetaben sodium has being shown to be an antiatherosclerotic agent.

Sufugolix (TAK-013 or 5-(N-benzyl-N-methylaminomethyl)-1-(2,6-difluorobenzyl)-6-[4-(3-methoxyureido)phenyl]-3-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione) is a highly potent and orally active non-peptide antagonist of luteinizing hormone-releasing hormone (LHRH) receptor. Sufugolix by oral administration suppresses a pituitary-ovarian axis continuously and reversibly in cynomolgus monkeys. Takeda studied Sufugolix in the trials for the treatment of endometriosis and uterine leiomyoma however development was discontinued.