Pirbenicillin is a broad-spectrum semisynthetic penicillin with activity against both gram-positive cocci and gram-negative bacilli. Pirbenicillin is less active than either carbenicillin or ticarcillin against Proteus spp. It is as active as carbenicillin against Serratia spp. and Enterobacter spp. Pirbenicillin demonstrated eight- and fourfold better minimal bactericidal concentration values towards Pseudomonas isolates than those of carbenicillin and ticarcillin, respectively. Pirbenicillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. The drug is somewhat more stable in serum than carbenicillin. Pirbenicillin does not appear to inactivate gentamicin as rapidly as carbenicillin.

Indoxole is phenylindene derivative patented by Mead Johnson & Co. as antidepressants. Indoxole have potent activity in the prevention of reserpine-induced ptosis in mice.

Ralimetinib (LY2228820), a trisubstituted imidazole derivative, is a potent and selective, ATP-competitive inhibitor of the α- and β-isoforms of p38 mitogen-activated protein kinase. LY2228820 produced significant tumor growth delay in multiple in vivo cancer models (melanoma, non-small cell lung cancer, ovarian, glioma, myeloma, breast). Eli Lilly is developing ralimetinib for the treatment of cancer.

Doxpicomine is the hydrochloride salt of l-3[(dimethylamino)-(m-dioxan-5-yl)methyl]pyridine, a derivative of substituted 1,3 dioxanes. Its analgesic effect appears to be mediated centrally through opiate-like receptors. Preclinical animal studies revealed analgesic activity and duration of action of the same order as that of meperidine and codeine when administered subcutaneously and of codeine but of shorter duration when administered orally. The analgesic effects were reversed by naloxone. The drug did not reduce or antagonize the analgesic effect of morphine. Drowsiness is an expected response to effective analgesics. It was the foremost side effect observed but was of short duration and minimal intensity and did not interfere with the postoperative regimen of coughing, deep breathing, and early ambulation. Nausea and vomiting were not reported after doxpicomine.

FEZOLAMINE is a nontricyclic antidepressant. It acts as a serotonin, norepinephrine, and dopamine reuptake inhibitor, with a preference for the former neurotransmitter. It was found to be effective and well tolerated in clinical trials but was never marketed.

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.

Tampramine (also known as AHR-9377) is a potent and selective, noncompetitive inhibitor of norepinephrine reuptake possesses antidepressant activity. This drug was studied for the treatment of the major depressive disorder; however, this study was discontinued.

Daledalin is a norepinephrine reuptake inhibitor, developed in the 1970s by Pfizer. In animal models, daledalin potentiates the action of catecholamines, reverses the hypothermia induced by noradrenaline or noradnamine injected into the cerebral ventricles of mice. Daledalin potentiates amphetamine-induced excitation in rats and antagonizes reserpine-hypothermia in mice, tetrabenazine-sedation in rats and reserpine- and tetrabenazine-induced ptosis in mice. It inhibits noradrenaline and 5-hydroxytryptamine uptake by rat brain slices in vitro. In a clinical trial on patients with a depressive illness, no difference in efficacy between daledalin and amitriptyline was found.

Metethoheptazine (WY-535) is an analgesic agent.

Clociguanil (BRL 50216, WR 38839) is an antimalarial compound, a derivative of N-benzyloxydihydrotriazine, developed by Beecham Pharmaceuticals. Mode of action studies indicated that clociguanil is a dihydrofolate reductase inhibitor of Plasmodium and is capable of marked potentiation with a selected sulphonamide against both the sensitive N strain and the cycloguanil-resistant B line of P. berghei. A combination of clociguanil and sulphadiazine prevented the development of parasitemia caused by P. falciparum in humans. The subsequent development of clociguanil was discontinued because of a relatively short half-life in man and lack of suppression of pre-erythrocytic schizogony of a strain of P. falciparum resistant to chloroquine, pyrimethamine, and proguanil.