L-MTX is a second-generation tau protein aggregation inhibitor. It acts by reducing levels of aggregated or misfolded tau proteins, which are associated with the progressive neurodegeneration. It is currently under development for the treatment of Alzheimer’s disease.

Rumenic acid is the major conjugated linoleic acid (CLA), probably because of successive desaturation and chain elongation and can be considered as the principal dietary form. In experiments on rodents was shown that rumenic acid possessed the protective effect against colitis, which was associated with the activation of the Nrf2 pathway.

Mitolactol is a synthetic derivative of hexitol with antineoplastic and radiosensitizing properties. Mitolactol alkylates DNA via actual or derived epoxide groups, resulting in inhibition of DNA and RNA synthesis.

(E)-Tetrachlorovinphos is an (E)- isomer of Tetrachlorovinphos. Tetrachlorovinphos is an organophosphate cholinesterase inhibitor that is used as an insecticide. Tetrachlorvinphos was introduced and first used commercially in 1966 in the USA. Tetrachlorvinphos was originally registered for use on various food crops, livestock, pet animals. Tetrachlorvinphos is applied dermally to livestock to control flies and mites. It is used as an oral larvicide in cattle, hog, goats and horses; in cattle ear tags to control flies; in cattle feedlots; in poultry dust boxes to control poultry mites; and in poultry houses. Tetrachlorvinphos also is used in pet sleeping areas and pet flea collars and to control flies around refuse sites, recreational areas, and for general outdoor treatment. Tetrachlorvinphos can cause cholinesterase inhibition in humans; that is, it can overstimulate the nervous system causing nausea, dizziness, confusion, and at very high exposures (e.g., accidents or major spills), respiratory paralysis and death. In 2014, the Natural Resources Defense Council (NRDC) filed a lawsuit against the United States Environmental Protection Agency (EPA) seeking EPA to respond to NRDC’s 2009 petition to ban tetrachlorvinphos in common pet flea treatment products. Tetrachlorvinphos is reportedly registered for use in Canada, South Africa, and Australia.

Tanomastat (previously known as BAY 12-9566) is an inhibitor of angiogenesis and a biphenyl matrix metalloprotease (MMP). The drug was selective towards MMPs 2,3, and 9 and no activity against MMP1. Tanomastat was developed for the treatment of cancer and arthritis. Tanomastat participated in phase III clinical trials as maintenance therapy in patients with advanced ovarian cancer, and in patients with pancreatic, lung cancers. However, all studied were discontinued after the recommendation of the independent data safety monitoring board.

Sibopirdine (EXP921) is a cognition enhancing agent structurally related to linopirdine that was in preclinical development with Bristol-Myers Squibb in the USA as a treatment of Alzheimer's disease. EXP921 was a potential drug candidate for the improvement of cognitive performance in patients with Alzheimer's-type dementia. It has been shown to improve cognitive performance in rodent and primate models of learning and memory. EXP921 was observed to increase the depolarization induced release of acetylcholine, dopamine, and, to a lesser extent, serotonin using slices from the rat cerebral cortex, hippocampus, and caudate nucleus.

Camiglibose is a glucopyranoside and inhibitor of alpha-glucosidase with antihyperglycemic activity patented by Merrell Dow Pharmaceuticals. In rats, a single oral dose of Camiglibose administered simultaneously with 2 g/kg body wt sucrose resulted in a dose dependent reduction in the area under the 0- to 3-h glycemic response curve, A reduction in the glycemic response to sucrose was accompanied by reduced insulin secretion. Camiglibose was more effective against a sucrose load in streptozocin-administered rats than in control rats and was as effective after 16 daily doses as after a single dose. Doses that reduced the glycemic response to carbohydrate did not inhibit liver lysosomal a-glucosidase activity or cause lysosomal glycogen accumulation. In cynomolgus monkeys, an oral dose of 1 mg/kg Camiglibose reduced the glycemic and insulin responses to sucrose

Midesteine (previously known as MR 889), a thiolactic acid derivative was developed as an inhibitor of the chymotrypsin and elastolytic activity of leukocyte elastase. Midesteine participated in clinical trials for patients with chronic obstructive pulmonary disease. The drug is also studied to treat asthma, cystic fibrosis, and emphysema. However, all these studies were discontinued.