THIOINOSINE (Methylmercaptopurine riboside, NSC- 40774) is a purine derivative with antineoplastic and anti-angiogenic properties. THIOINOSINE is readily converted in cells to its active form, 6-methylmercaptopurine ribonucleoside 5'- monophosphate (MMPR-P), by the enzyme adenosine kinase. THIOINOSINE inhibits amidophosphoribosyltransferase, the first committed step in de novo purine synthesis, and inhibits fibroblast growth factor-2 (FGF2)-induced cell proliferation. It has been used similarly to Mercaptopurine in the treatment of Leukemia. It has being tested in clinical trials for advanced pancreatic cancer.

Noreximide, a sedative, is generally contaminated to some extent with its endo-isomer, norendimide, which produces excitation. Noreximide is an investigational drug which displays a peculiar activity on the central nervous system in laboratory animals and in humans. The compound was selected as the most promising member from a series of analogous dicarboxylic acid imides, after a Hansch correlation analysis of the biological activities to some physicochemical properties. The preceding pharmacological and toxicological screening yielded satisfactory results and the compound was undergoing extensive clinical trials in psychiatric patients.

Daxalipram is a selective inhibitor of phosphodiesterase (PDE) 4B.This compound is an R-isomer of mesopram and is known as (R)-mesopram. Mesopram is known to trigger ovulation and exhibits efficacy against experimental autoimmune encephalomyelitis and murine colitis in vivo. Moreover, is used in compositions for the treatment or prevention of respiratory inflammation.

Cypothrin is a synthetic pyrethroid insecticide, developed by American Cyanamide for the control of ticks and marketed under the tradename Panecto. The compound exhibited systemic insecticidal activity in the model of flies infestation in mice and ixodicidal activity in against larvae of Boophilus microplus.

Dagapamil is a calcium-channel blocker, discovered by BASF. The compound is claimed to have antihypertensive, antiarrhythmic, cardioprotective, antiallergic and platelet aggregation-inhibiting action in animal models.

Viprostol (also known as CL115,347), a prostaglandin E2 congener that was studied as an antihypertensive agent. Viprostol has a potent and prolonged blood pressure lowering effect in many models of hypertension. In clinical studies, viprostol has been demonstrated to lower arterial blood pressure significantly in man following transdermal and/or intravenous administration. The antihypertensive action of viprostol has been suggested to be the result of peripheral vasodilatation. In addition, the drug participated in a clinical trial in normal subjects and in patients with Raynaud's phenomenon. It was found the optimal dosage was 1000 ug; the effect could last for 84 hours; higher dosage may be associated with a "steal" phenomenon.

Amicus Therapeutics was investigating afegostat (isofagomine; Plicera; HGT-3410; AT-2101), an orally available pharmacological chaperone molecule, which binds to glucocerebrosidase (Gba) and stimulates proper folding and trafficking of the enzyme, for the potential treatment of Parkinsons disease(PD) and Gaucher disease. Afegostat specifically and reversibly binds GCase in the ER with highaffinity; this stabilizes the active form of the enzyme in the ER and increases trafficking of GCase to lysosomes. In 2006, Orphan Drug designations were granted in the U.S. and E.U. in 2006 and 2007, respectively. However, this research has been discontinued.

Cuproxoline is a copper complex used in a veterinary as a copper supplement. Cuproxoline was also used for the treatment of rheumatoid arthritis, where it was administered by intravenous or intramuscular injections. Clinical studies has shown that cuproxoline therapy gave good results for the treatment of rheumatoid arthritis which had been active for less than a year, even if the patient had become resistant to gold therapy.

Levomequitazine is the L-enantiomer of mequitazine. The antihistaminergic activity mainly resides in the S-enantiomer, L-mequitazine, whereas the anticholinergic activity mainly resides in the D-enantiomer. It was shown, that L-enantiomer of mequitazine is less potent antagonist of human M3 muscarinic acetylcholine receptors than D-enantiomer. In vitro binding studies have shown that the affinity of L-mequitazine for H1 receptors is approximately ten times higher and to muscarinic receptors ten times lower, compared to d-mequitazine. Memory impairment was observed after administration of L-mequitazine 10 mg alone on delayed recall. This could be due to indirect effects of H1 receptor blockade. L-mequitazine 10 mg produced mild driving impairment, whereas L-mequitazine 2.5 and 5.0 mg show no effects on driving. Levomequitazine had been in phase III clinical trials by Pierre Fabre for the treatment of perennial allergic rhinitis and seasonal allergic rhinitis.