Quadazocine is a substituted hexahydro-2,6-methano-3-benzazocine patented by Sterling Drug Inc. as analgesics and narcotic antagonist. Quadazocine is a potent antagonist of μ opioid receptor, less potent antagonist of κ and δ opioid receptors. In monkeys for whom responding was reinforced by food delivery, quadazocine blocks the rate-decreasing effects of the µ-agonists alfentanil and fentanyl with greater potency than it blocked the rate-decreasing effects of the κ-agonists U69,593

Eniporide belongs to the new class of drugs that specifically inhibit the Sodium/hydrogen exchanger 1 (NHE-1) isoform, which is the predominant isoform in the cardiac myocytes. Extensive preclinical studies, in vitro and in animals, have suggested that NHE inhibition with eniporide before the onset of ischemia is a very effective and reproducible means of limiting the extent of infarction and that this agent provides protective benefit even when given just before reperfusion. Eniporide had been in phase II clinical trial for the treatment of myocardial infarction. Administration of the eniporide, before reperfusion therapy in patients with acute ST-elevation myocardial infarction, did not limit infarct size or improve clinical outcome.

Fanetizole is a derivative of 2-aminothiazole. It is an anti-inflammatory agent. This drug is reported to have some cyclooxygenase inhibiting activity. Production of superoxide in response to the chemotactic factor formyl-methionyl-leucyl-phenylalanine (f-Met-Leu-Phe) was markedly inhibited by fanetizole. Suppression of neutrophil production of toxic oxygen metabolites may partially explain the antiarthritic effect of fanetizole. Fanetizole was shown to restore depressed E-rosetting activity in adult thymectomized mice, as well as enhance in in vitro proliferation of murine thymic cells to mitogen and synergistically acted with the monokine interleukin-1. It displays anti-arthritic activity in viva in the rat adjuvant arthritis model, inhibiting the development of disease in the non-infected foot. This drug has less side effects than levamisole in animals.

Deditonium is an antibacterial compound developed by the French company Centre de Recherches des Laboratoires Diamant. Deditonium is a quaternary ammonium derivative and has a bacteriostatic action at concentrations ranging from 1x10-6 to 5x10-4 M. Gram-positive cocci were found to be the most sensitive as well as many enterobacteria.

Proligestone is a pregnane derivative patented by Koninklijke Nederlandsche Gist-en Spiritusfabriek N. V. As a progestin medication for veterinary medicine. Proligestone is used to control estrus in dogs and cats and has also been used to treat hypersexuality in dogs and cats. Administration of progestins in the dog may result in overproduction of growth hormone, suppression of the hypothalamic-pituitary-adrenocortical axis, and insulin resistance.

Darenzepine is an antagonist of muscarinic receptors, developed by at Knoll/BASF Pharma. It is claimed to have antiulcer effect superior to pirenzepine and to have less anticholinergic adverse effects.

Bamnidazole was developed as an antiprotozoal agent against Tryhomonas, however, has never been marketed.

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

Apadoline [RP 60180, RP 60180A, RPR 60180] is a κ-opioid receptor agonist which was undergoing phase II clinical trials with Aventis Pharma for the treatment of pain.

Broclepride is dopamine antagonist developed be Almirall for treatment of gastrointestinal diseases