ADX 10059 is a first-in-class reflux inhibitor that works by reducing activation of the metabotropic glutamate receptor 5 (mGluR5) through negative allosteric modulation (NAM). This approach may lead to a new class of drugs that addresses the causes of GERD rather than just the symptoms. ADX 10059 is a potent selective NAM of the mGluR5, with an IC50 of 17.1 nM on hmGluR5 showing good selectivity compared with > 65 other receptors, transporters, ion channels and enzymes. ADX 10059 completed Phase IIb testing in gastroesophageal reflux disease (GERD) and migraine prevention, demonstrated significant potential in a non-human primate model of Parkinson's disease levodopa induced dyskinesia (PD-LID). However, Addex Pharmaceuticals announced the discontinuation of development of ADX 10059 in December 2009 due to liver enzyme changes.

Barasertib (AZD1152) is a dihydrogen phosphate prodrug of a pyrazoloquinazoline Aurora kinase inhibitor [AZD1152–hydroxyquinazoline pyrazol anilide (HQPA)] and is converted rapidly to the active AZD1152-HQPA in plasma. AstraZeneca was developing the aurora kinase inhibitor, barasertib (AZD 1152) as a therapeutic for cancer. AZD1152-HQPA is a highly potent and selective inhibitor of Aurora B (Ki, 0.36nmol/L) compared with Aurora A (Ki, 1,369nmol/L) and has a high specificity versus a panel of 50 other kinases. Consistent with inhibition of Aurora B kinase, addition of AZD1152-HQPA to tumour cells in vitro induces chromosome misalignment, prevents cell division, and consequently reduces cell viability and induces apoptosis. Barasertib (AZD1152) potently inhibited the growth of human colon, lung, and haematologic tumour xenografts (mean tumour growth inhibition range, 55% to ≥100%; P < 0.05) in immunodeficient mice. Detailed pharmacodynamic analysis in colorectal SW620 tumour-bearing athymic rats treated i.v. with Barasertib (AZD1152) revealed a temporal sequence of phenotypic events in tumours: transient suppression of histone H3 phosphorylation followed by accumulation of 4N DNA in cells (2.4-fold higher compared with controls) and then an increased proportion of polyploid cells (>4N DNA, 2.3-fold higher compared with controls). Histologic analysis showed aberrant cell division that was concurrent with an increase in apoptosis in AZD1152-treated tumours. Bone marrow analyses revealed transient myelosuppression with the drug that was fully reversible following cessation of Barasertib (AZD1152) treatment. Barasertib (AZD1152) was in phase III for the treatment of Acute myeloid leukaemia, but later these studies were discontinued.

Gamfexine (WIN 1344) was introduced in the literature in 1966 as an anti-depressant. Although it was reported to be effective in the treatment of withdrawal in schizophrenia, it worsened psychotic symptoms.

Acridorex (BS 7573a) is an anorectic agent.

Medorubicin is an antineoplastic agent.

Mecloxamine is an anticholinergic exerting sedative and hypnotic activity.

Pyrophenindane is pyrrolidylmethyl-substituted arylindan patented by Mead Johnson & Co. as antispasmodic agent. Pyrophenindane have potent activity in the prevention of reserpine-induced ptosis in mice, a test for antidepressant activity.

Troxolamide is a targeted ultrasound contrast diagnostic agent.

Algestone acetonide is a cyclic ketal that is the 16α,17α-acetonide derivative of algestone. It is a steroidal progestin used as a contraceptive drug and anti-inflammatory agent (topical).

Ristianol (Ristianol phosphate) is a bioactive chemical that is registered as an anti-inflammatory agent and immunoregulator (in Europe), but no further information is available.