Nitromiphene (NIT; CI 628) is a triarylethylene antiestrogen shown to be effective in treatment of experimental breast cancer. Nitromiphene is one of the earliest nonsteroidal selective estrogen receptor modulators (SERMs). It is an anti-estrogen capable to translocate the estrogen receptor to the nucleus and to induce the replenishment of the cytosol receptor. Nitromiphene inhibited the uptake of [3H]-estradiol in rat whole homogenates and isolated cell nuclei tissues and the pituitary, and inhibited estradiol-induced female sexual behavior. Nitromiphene has thus been shown to suppress the growth of chemically induced and ransplantedmammary tumors in rodents. Also, Nitromiphene was shown to have potent, prolonged antiuterotropic effects in immature rats. Nitromiphene has been shown to undergo conversion to demethyl Nitromiphene (CI628M), a phenolic metabolite which had greater affinity for estrogen receptors and greater biological potency in vitro than did Nitromiphene. However, the in vivo antiestrogenic effects of Nitromiphene and demethyl Nitromiphene were similar, possibly due to facile O-demethylation of the former compound after administration.

Maleylsulfathiazole is a sulphonamide antibacterial. It was used in the treatment of diarrhea.

Sodelglitazar is an oral insulin sensitiser, a peroxisome proliferator-activated receptor (PPAR) pan agonist that was under development with GlaxoSmithKline for the treatment of hyperlipidaemia, type 2 diabetes mellitus and metabolic syndrome. Sodelglitazar exerts higher binding affinity for the delta subtype as compared to gamma and alpha subtypes. Sodelglitazar was being investigated in Phase II clinical trials for the treatment of T2DM and its complications, but this research has been discontinued.

Paranyline was used in dispersible formulations of anti-inflammatory agents. Information about the current use of this drug is not available.

There is no much information related to the pharmacological and/or biological properties of parapropamol. However, the analgesic properties of this compound had been studied in dentistry.

Nitraquazone (TVX 2706) is an phosphodiesterase inhibitor with antiinflammatory action. It strongly enhances the increase in intracellular levels of cyclic AMP caused by appropriate effectors in all systems tested so far. EC50 values are in the submicromolar range. The effect is apparently neither due to an increased responsiveness of the hybrid cells for an effector like prostaglandin E1 nor to an increased activity of adenylate cyclase, but to an inhibition of both low and high affinity cyclic AMP phosphodiesterases. Half-maximal inhibition of enzyme activity is obtained at 10 uM TVX 2706. TVX 2706 does not interfere with the calmodulin activation of phosphodiesterase. Nitraquazone affected cytokine production by PHA-stimulated human blood cells. Nitraquazone was active in reducing the production of IL-5 (IC50 = 0.8 uM), while its potency against IL-2, GM-CSF and IFN-gamma was 3-6 times lower.

Org 25935 (SCH 900435) is a synthetic drug developed by Organon International, which acts as a selective inhibitor of the glycine transporter GlyT-1. In human trial for prevention of relapse in alcohol-dependent patients in Org 25935 demonstrated no benefit over placebo in preventing alcohol relapse. Org 25935 was tested as an adjunctive treatment to atypical antipsychotics in predominant persistent negative symptoms of schizophrenia, where it did not differ significantly from placebo in reducing negative symptoms or improving cognitive functioning. Clinical trials against panic disorder did not show any benefit compared to placebo.

Bristol-Myers Squibb developed BMS-275183 for cancer indications. BMS 275183 is an inhibitor of tubulin polymerization. The drug participated in phase II clinical trials for patients with non-small cell lung cancer and in phase I for patients with advanced cancer. However, further development has been discontinued.