MK-0249 is a potent H3 receptor inverse agonist patented by Abbott Laboratories for treatment of cognitive deficits. MK-0249 demonstrates promising results in preclinical models of cognitive disorders. MK0249 has been used in trials studying the treatment of Hypopnea Syndrome, Alzheimer's Disease, Paranoid Schizophrenia ets. Unfortunately, MK-0249 failed to demonstrate efficacy in schizophrenia, mild-to-moderate Alzheimer's Disease, attention-deficit/hyperactivity disorder, and future development has been discontinued.

DICHLORISONE is a synthetic corticosteroid used topically for its glucocorticoid activity in the treatment of various skin disorders.

CP 724714 is an orally bioavailable, quinazoline-based, selective small molecule inhibitor of the HER2/erbB2 receptor tyrosine kinase. The compound could have particular potential in the treatment of women with metastatic breast cancer, of which 25-30% over express HER2/erbB2. CP 724714 was in preclinical development with Pfizer.

Otsuka Pharmaceutical was developing URACIL C-13, 2- ([2-13C]uracil) breath test for diagnosis of cancer and gastric emptying disorders. Dihydropyrimidine dehydrogenase (DPD) deficiency is critical in the predisposition to 5-fluorouracil dose-related toxicity. The phenotypic [2-(13)C]uracil breath test (UraBT) demonstrated 96% specificity and 100% sensitivity for identification of DPD deficiency. Phase II development of the breath test was ongoing. As phase II clinical study didn't exploit performance as diagnostic medicines, the development of [2-13C]uracil was discontinued.

Kirax Corporation (formerly Tigris Pharmaceuticals) was developing AFP-464, a lysyl prodrug of aminoflavone for the treatment of solid tumours. AFP-464 is an antitumor agent which was in phase II clinical trials, acts against estrogen-positive breast cancer (ER+). AFP-464, has a unique mechanism of action by activating aryl hydrocarbon receptor (AhR) signaling pathway. Preclinical studies into AFP-464's mechanism of action have shown that AFP-464 is converted to metabolites, which bind covalently to DNA, resulting in p53 activation and apoptosis. AFP-464 has shown a unique pattern of growth inhibitory activity in the NCI's 60 tumor cell line screen, with breast, ovarian, lung and renal tumor cell lines exhibiting particular sensitivity to the compound. In vivo anti-tumor activity of AFP-464 has been demonstrated in several xenograft studies in mice bearing renal and breast cancer. Preclinical studies have shown that tumors (breast, ovarian, pancreatic and renal) with AhR localized in the cytoplasm are very sensitive to AFP-464 while those with AhR localized in the nucleus are more resistant. AFP-464 was being studied by Tigris Pharmaceuticals in a randomized Phase 2 clinical trial with ER-positive breast cancer patients. However, AFP-464 development was discontinued.

GSK-256066 is a PDE4B inhibitor which was developed by GlaxoSmithKline and tested in phase II of clinical trials for the treatment of COPD, Asthma and Seasonal allergic rhinitis. According to the GSK pipeline, development of GSK-256066 was terminated. There are studies that describes the possibility of repurposing of the drug as antitrypanosomal agents, because it inhibits PDEB1 of Trypanosoma brucei.

3-Pyridinecarboxylic acid, 1-(4-methylphenyl)ethyl ester is an choleretic agent.

Hyoscyamine methylbromide, a muscarinic acetylcholine receptor antagonist, was studied as an antispasmodic.