Esafloxacin (7-(3-amino-1-pyrrolidinyl)-1-ethyl-6-fluoro-1,4 -dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid) is an antibacterial agent.

Dotefonium is the anticholinergic, spasmolytic agent.

Pruvanserin (EMD 281014, LY-2422347) is a selective serotonin 5-HT2A receptor antagonist. Pruvanserin was originated by Merck KGaA. Eli Lilly had been developing pruvanserin, under a global licence from Merck KGaA, for the treatment of primary insomnia and major depressive disorder. Phase II trials were completed in the US, Hungary and Spain. However, development appears to have been discontinued.

Inogatran is a low molecular weight dipeptide and competitive thrombin inhibitor developed by Aktiebolaget Astra for the potential treatment of arterial and venous thrombotic diseases. lnogatran reversibly binds to the catalytic site of the thrombin molecule, thereby in a stoichiometric fashion inhibiting both clot-bound thrombin. Its biological half-life in plasma is about 1 h and it is evenly eliminated in the urine and bile. lnogatran has shown promising antithrombotic effects in a porcine model of coronary thrombosis. Unfortunately, Inogatran failed to demonstrate superior efficacy and safety to unfractionated heparin as antithrombotic agent and clinical development was discontinued.

MK-0686 is a bradykinin B1 receptor antagonist patented by American multinational pharmaceutical company Merck & Co for the treatment of neuropathic pain and inflammation. MK-0686 demonstrates significantly reduced susceptibility to human P-gp mediated efflux and shows good potential for human CNS penetration based on brain levels in CF-1 mice and monkeys. Additionally, MK-0686 also exhibited good CNS bradykinin B1 receptor occupancy in the transgenic rat expressing the human B1 receptor and showed oral efficacy in reducing CFA-induced hyperalgesia in a humanized mouse. Unfortunately, in phase II clinical trials MK-0686 failed to demonstrate efficacy in phase II clinical trials.

Osmadizone was investigated as a uricosuric agent. Information about the current use of this compound is not available.

Etabenzarone is an anti-inflammatory and anticoagulant agent.

Tamethicillin is a basic ester pro-drug of methicillin (MET) which is converted in the body by non-specific esterases to MET. Tamethicillin was used as an antibacterial agent in the veterinary as a useful alternative for the treatment of mastitis in livestock, especially in mastitis due to beta-lactamase-producing Staphylococcus.

Melquinast is an antiasthmatic, antiallergic substance not acting primarily as antihistamines.

Varespladib (LY315920; A-001) is a potent and selective inhibitor of IIa, V, and X isoforms of human non-pancreatic secretory phospholipase A2 with nM IC50. The molecule acts as an anti-inflammatory agent by disrupting the first step of the arachidonic acid pathway of inflammation. Varespladib methyl is being developed by Anthera Pharmaceuticals Inc for the potential treatment of coronary artery disease, acute coronary syndrome and inflammation. Varespladib methyl is a prodrug that is rapidly metabolized to varespladib, and both compounds are able to potently inhibit the enzymes of the human secretory phospholipase groups. Phase II clinical trials of varespladib methyl in patients with coronary artery disease, rheumatoid arthritis, asthma and ulcerative colitis revealed that the drug was well tolerated. Varespladib methyl did not demonstrate a good efficacy profile in patients with rheumatoid arthritis, asthma and ulcerative colitis; whereas in patients with coronary artery disease, varespladib methyl consistently reduced LDL-cholesterol levels, (elevated LDL-cholesterol levels are a marker of increased cardiovascular risk). Varespladib methyl could represent a novel therapy for the treatment of cardiovascular disease, although the efficacy, safety profile and advantages of this drug compared with existing therapeutic options would need to be established in upcoming phase III trials.