Sprodiamide is a nonionic paramagnetic dysprosium chelate agent patented by Salutar, Inc.as diagnostic imaging contrast media. Compare with gadolinium-based agents Sprodiamide shows a stronger T2 effect and negligible T1 effect. This property makes Sprodiamide useful for blood volume imaging. In a preclinical model of reperfused ischemia of the rat intestine administration of Sprodiamide improved the contrast between the normal and ischemic intestine on T2-weighted images, and administration of both gadodiamide and Sprodiamide improved the contrast on T1- and T2-weighted images.

Binodenoson, a selective adenosine A(2A) receptor agonist, was being developed as a short-acting coronary vasodilator as an adjunct to radiotracers for use in myocardial stress imaging. Binodenoson for injection under the brand name CorVue was developed for use in patients with or at risk for coronary artery disease (CAD) who are unable to perform a cardiac exercise stress test. CorVue was designed to minimize side effects such as dyspnea, flushing, heart block, and chest pain. Binodenoson did not achieve FDA approval in 2009 due to concerns over equivalence of its efficacy with adenosine.

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.

Sarmazenil (previously known as RO 153505) was developed as a weak inverse agonist at the omega modulatory sites (benzodiazepine receptors). This compound is used in veterinary medicine in order to rapidly re-awake anesthetized animals. In addition, this compound was studied in the treatment of a moxidectin intoxication in foals. Sarmazenil was also involved in preclinical development for Alzheimer's disease in the USA. However, the information about the further development of the drug is not available.

Brifentanii, a potent narcotic analgesic structurally similar to alfentanil, that was studied in clinical trials in the early 1990s. The effects of brifentanil are very similar to those of alfentanil, with strong but short lasting analgesia and sedation, and particularly notable itching and respiratory depression. Side effects of Brifentanii are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening.

Xyloxemine is an antitussive agent that has never been marketed. Information about the current use of this compound is not available.

Xylocoumarol is an anticoagulant that has never been marketed. Information about the current use of this compound is not available.

AT-406 (DEBIO-1143, SM-406), is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). AT-406 inhibits cancer cell growth in various human cancer cell lines. It has good oral bioavailability in mice, rats, non-human primates, and dogs, is highly effective in induction of apoptosis in xenograft tumors, and is capable of complete inhibition of tumor growth. Debiopharm under a licence from Ascenta Therapeutics is developing AT-406 for the treatment of cancers.