Millennium Pharmaceuticals Inc's tandutinib (MLN-518), a piperazinyl derivative of quinazoline, is an orally active inhibitor of FLT3 kinase and family members PDGFR beta and c-Kit. Tandutinib inhibited FLT3 phosphorylation, downstream signaling and malignant growth in vitro and in animal models. The drug exhibited limited activity as a single agent in phase I and II clinical trials in patients with AML and myelodysplastic syndrome, but displayed promising antileukemic activity (90% complete remissions) in a phase I/II trial in patients with newly diagnosed AML when administered in combination with cytarabine and daunorubicin. Phase II clinical trials for tandutinib in patients with Glioblastoma have being discontinued. The use of tandutinib to treat AML has been granted fast-track status by the U.S. Food and Drug Administration. Phase II trials were underway., but later withwrawn.

PNU-96391A (known as OSU6162) is a weak dopamine (DA) D(2) receptor antagonist with behavioral stabilizing properties. OSU6162 seem to act as stabilizers not only on dopaminergic, but also on serotonergic brain signaling (partial agonist on 5-HT2A receptor). OSU6162 in a phase II European clinical trial in treatment of Myalgic Encephalomyelitis/Chronic Fatigue Syndrome. One of the isomer of OSU 6162, has promise for treating Parkinson's disease, Huntington's disease and schizophrenia, but both enantiomers of OSU 6162 had dual effects on behavior, stimulating locomotor activity in 'low activity' animals and inhibiting locomotor activity in 'high activity' animals.

Edonentan (BMS 207940) is a highly selective biphenylsulfonamide endothelin A receptor antagonist. (11)C- and (18)F-labeled analogs of edonentan were evaluated of novel PET radioligands for imaging the endothelin-A receptor. Edonentan was in clinical trials for the treatment of heart failure however its development has been discontinued.

Prizidilol (also known as SKF 92657) is arylpyridazinylhydrazine derivative patented by Smith Kline and French Laboratories Ltd. as an antihypertensive agent. In clinical trials, Supine and standing blood pressure measured 24--27 h after drug intake was reduced Slight but significant decreases in heart rate were seen after moderate doses of prizidilol. A more pronounced blood pressure reduction was noticed 2--7 h after drug administration. Prizidilol was well tolerated, although dizziness and tiredness were reported by four patients and edema by two.

Pelanserin is an antagonist of the serotonin 5-HT2 receptor and blocks alpha 1-adrenoceptor. Experiments on dogs have revealed that pelanserin showed adequate pharmacokinetic and pharmacodynamics profiles as an antihypertensive agent that is why the drug possessed potential therapeutic usefulness in the treatment of hypertension. Pelanserin was undergoing phase II clinical trials by Cinvestav in Mexico; however, these studied were discontinued.

Atrasentan (ABT-627, A-127722) is a selective endothelin A receptor antagonist. Atrasentan is being developed by AbbVie as an oral treatment for diabetic nephropathies.Abbott Laboratories was conducting clinical development of atrasentan for the treatment of certain cancers, including phase II trials for prostate cancer. However, no recent development has been reported for cancer indications and development is presumed to be discontinued.

Piperamide is substituted piperazine with a tertiary amine group. It was used as an anthelmintic agent. Initially, it was investigated because of its effectiveness against Trypanosoma. Piperamide distorts choroid plexus epithelial ultrastructure by engendering hydropic vacuoles.

Remogliflozin is the active component of the pro-drug remogliflozin etabonate, which is used the treatment of non-alcoholic steatohepatitis ("NASH") and type 2 diabetes. Remogliflozin inhibits the sodium-glucose transport proteins (SGLT), is selective for SGLT2, which is responsible for glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine.

Edaglitazone have a clear PPAR-gamma agonist profile, with predominant PPAR-gamma activity and little PPAR-alpha activity. Edaglitazone was reported to significantly improve insulin sensitivity and enhance the rate of glucose oxidation in both the presence and absence of insulin. Additional studies have shown that edaglitazone affects muscle glucose metabolism by additional mechanisms other than PPAR-gamma activation. Phase I clinical studies have revealed that edaglitazone is well-tolerated and capable of significantly improving glucose homeostasis. Edaglitazone had been in phase II clinical trials for the treatment if type 2 diabetes. However, this research has been discontinued.