Etazolate (EHT-0202) is a selective, positive GABAA receptor modulator has completed phase II clinical trials in patients with Alzheimer's disease. It is also a selective phosphodiesterase-4 inhibitor that is specific for cAMP. Etazolate showed anxiolytic and antidepressant activity and could be useful in managing post-traumatic stress disorder.

Cefazaflur (INN) is a semisynthetic first-generation cephalosporin antibiotic patented by Smithkline Corp. For treatment of bacterial infections.

Tiacrilast (also known as Ro 22-3747) is a quinazolinyl-propenoic acid derivative patented by Hoffmann-La Roche, Inc. as an antihypertensive useful for anaphylaxis management. Tiacrilast acts as a potent mast cell degranulation inhibitor in vitro and inhibits of antigen-induced histamine release from passively sensitized rat peritoneal cells in vitro. In preclinical models, Tiacrilast shows marked activity in rat passive cutaneous anaphylaxis assay, rat anaphylactic bronchospasm assay. In vitro studies have confirmed that the mechanism of action of Tiacrilast in the in vivo models is through allergic mediator release inhibition. Clinical evaluations of Tiacrilast in patients with ragweed sensitive allergic asthma, Tiacrilast demonstrates significant inhibitory activity relative to placebo in reducing acute airway responses to inhaled pollen extracts

Picenadol is a 4-phenylpiperidine derivative and a racemic mixture whose mixed agonist-antagonist properties are a consequence of the d-isomer being a potent opiate agonist, whereas the I-isomer is an opioid antagonist. In the mouse writhing and rat tail heat tests, the analgesic potency of picenadol is estimated to be 1/3 that of morphine. Picenadol itself has weak antagonist activity, whereas the antagonist potency of the l-isomer is approx. 1/10 that of nalorphine. Picenadol has high affinity for both the mu and delta receptors but a markedly lower affinity for the kappa receptor. Extensive pharmacological investigations show picenadol to have a low potential to produce opiate-like side effects, including a low liability for abuse and physical dependence. Antinociceptive properties of picenadol arise from mu agonist actions of the dextrorotatory isomer and that the levorotatory isomer acts to limit the efficacy of the racemate.

Serazapine (CGS15040) is an anxiolytic agent. It is structurally novel 5-HT2 receptor antagonist. Preliminary preclinical findings indicated an anticonflict effect in a behavioral suppression test, and two preliminary investigations in volunteers also suggested anxiolytic potential. In the first of these studies serazapine resembled diazepam, a reference anxiolytic drug, electroencephalographically. Additionally, in a test of psychogenic stress in volunteers it reduced cardiac output.

SPK-843 is a water-soluble partricin derivative patented by SPA Societa Prodotti Antibiotici S.p.A. and developed by Aparts and Kaken for the potential treatment of systemic fungal infections. In preclinical models, SPK-843 shows in vitro inhibitory activity comparable to or better than that of Amphotericin B against Candida spp., Cryptococcus neoformans, and Aspergillus spp. SPK-843 exhibits dose-dependent efficacy on murine pulmonary aspergillosis models. SPK-843 doses of higher than 1.0 mg/kg of body weight exhibit no renal toxicities and a tendency toward better survival prolongation than the estimated maximum tolerated doses of amphotericin B (Fungizone) and liposomal amphotericin B.

Dazopride is an antagonist of the 5-HT3 receptor and agonist of the 5-HT4 receptor, structurally related to metoclopramide. Dazopride was developed by A. H. Robins Company as an antiemetic and gastroprokinetic drug. Dazoptide demonstrated an antiemetic effect in the clinic after i.v. infusion to patients, receiving anticancer therapy.

GSK-2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. GSK-2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines. On April 1 2016 GlaxoSmithKine completes a phase-I/II trial for Solid tumours (Late-stage disease) in USA, United Kingdom and South Korea (NCT01458067).

Metethoheptazine (WY-535) is an analgesic agent.