AST-1306, also known as Allitinib, is an orally active potent, selective, irreversible inhibitor of the HER family of receptor tyrosine kinases. AST-1306 inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems. AST1306 potently suppressed tumor growth in ErbB2-overexpressing adenocarcinoma xenograft and FVB-2/N(neu) transgenic breast cancer mouse models. Allitinib is in Phase I clinical trial for the treatment of advanced solid tumors. Serious adverse effects detected were: diarrhea, dehydration and hyperbilirubinemia.

Tinazoline is an imidazole derivative patented by Ciba-Geigy A.-G. as vasoconstrictors, particularly as nasal decongestants in the treatment of common cold. Tinazoline showing potent and long-acting vasoconstrictor activity on several vascular beds in dogs, guinea-pigs, cats, and rabbits. The vasoconstrictor effect has been shown in animals to be due to a stimulation of the 1-adrenoceptors and the compound does not exhibit any B-adrenoceptor agonist activity.

Nonaperone, a butyrophenone, is a neuroleptic agent. It is antipsychotic in schizophrenics at doses which do not elicit extrapyridal side effects.

Alazanine triclofenate is a mixture of one molecule of 3-ethyl-2-(3-(3-ethyl-2-benzothiazolinylidene)propenyl)benzothiazolium 2,4,5-trichlorophenate and two molecules of 2,4,5-trichlorophenol. It is an antiparasitic agent. It is antimalarial drug, highly active against multiple Plasmodium falciparum isolates with IC50 value of 2.36E-07 M.

AE-37 (ANAVEX2-73, Tetrahydro-N, N-dimethyl-2, 2-diphenyl-3-furanemethanamine) is an orally available drug candidate developed to potentially modify Alzheimer’s disease rather than temporarily address its symptoms. It has a clean Phase 1 data profile and shows a reversal of memory loss (anti-amnesic properties) and neuroprotection in several models of Alzheimer’s disease. This drug is in Phase II trials for Alzheimer's disease, phase I trials for epilepsy, and in preclinical trials for amyotrophic lateral sclerosis, Parkinson's disease, Rett syndrome, stroke. AE-37 may function as a pro-drug for ANAVEX19-144 and acts as a muscarinic receptor and a moderate sigma1 receptor agonist.

Dioxifedrine is the putative metabolite of 3,4-methylenedioxymethamphetamine. It is the sympathomimetic agent and beta-2 -adrenergic agonist with bronchodilator activity. Dioxifedrine selectively binds to and activates beta-2 adrenergic receptors in bronchiolar smooth muscle, thereby causing stimulation of adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased intracellular cAMP levels cause relaxation of bronchial smooth muscle. In stimulatory studies dioxifedrine increased locomotor activity from 15 to 30 min following the drug administration. Following intracerebroventricular injection dioxifedrine rapidly reduced blood pressure and heart rate.

Nuclomedone (TEI-3096), a thiazolopyrimidine compound has been shown to suppress adjuvant arthritis in rats without any effect on conventional inflammation. TEI-3096 also enhanced the delayed type hypersensitivity in mice and rats. These results suggests that TEI-3096 restores the abnormal immune response. Nuclomedone was discovered by Teijin and investigated as a potential treatment for rheumatoid arthritis and inflammatory disorders.