Serfibrate, a clofibrate derivative, is a peroxisome proliferator activated receptor-α (PPAR-α) agonist. It is a hypolipidemic agent.

Ioprocemic Acid is hydrocinnamic acid derivative patented by Schering-Kahlbaum A.-G. as radiographic contrast medium for liver imaging

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.

CGP-36742 (3-Aminopropyl-n-butyl-phosphinic acid) is one of the first GABAB receptor antagonists that can penetrate the blood-brain barrier after peripheral administration. Although its affinity for GABA B binding sites labeled with a tritiated agonist is modest, being in the low micromolar range, it displays significant pharmacological activity when administered either orally or parenterally. CGP 36742 was effective in the learned helplessness paradigm in rats, dose-dependently improving the escape failures induced by the inescapable shocks, suggesting that it may have an antidepressant profile. CGP36742 displays pronounced cognition enhancing effects in Rhesus monkeys in active and passive avoidance paradigms, in an eight-arm radial maze and a Morris water maze and in a social learning task. CGP36742 blocks the late inhibitory postsynaptic potential and the paired-pulse inhibition of population spikes recorded from CA1 pyramidal neurons of the hippocampus of rats in vitro and in vivo. CGP36742 significantly enhances the release of glutamate, aspartate, glycine and somatostatin in vivo. Chronic administration of CGP36742 causes an up-regulation of GABA(B) receptors in the frontal cortex of rats. The effects of CGP36742 on cognition were investigated in a double-blind, placebo-controlled study undertaken as the first assessment of the efficacy of CGP36742 in 110 patients age 59–85 years with Mild cognitive impairment. The results showed significant improvement in working memory, psychomotor speed and attention with SGS742 as compared with placebo. SGS742 appeared to be safe and well tolerated in this study.

Fosfocreatinine, a cardioprotectant that was used for the treatment of cardiac disorders. Information about the current use of this drug is not available.

Nicoclonate is a nicotinic acid derivative. It is an antilipidemic drug.

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.

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

FLUMEXADOL is a non-opioid analgesic. Its prodrug OXAFLOZANE was used as an antidepressant in France till 2004.

Ragaglitazar (DRF 2725, NNC 61-0029) is phenoxazine analog of phenyl propanoic acid having dual (PPARα and PPARγ) agonist property intended to restore insulin sensitivity and correct diabetic dyslipidemia. PPAR-α is highly expressed in liver and muscle and upon activation leads to decreases in plasma triglycerides and increases in HDL cholesterol levels. PPAR-γ activation leads to enhancement of glucose uptake in skeletal muscles and adipose tissue. Ragaglitazar provided the glycemic control that was comparable with that of pioglitazone and, compared with placebo, provided a significant improvement in the lipid profile.