Indopine is indolylalkyl derivative patented by Irwin, Neisler and Co as potent analgesic.

Pirepolol is the beta-adrenergic blocking agent. It was developed as an antihypertensive agent.

Gliamilide is a high-potency sulfamylurea hypoglycemic agent. It has been found to be well tolerated in humans and displays a very short plasma half-life. Like sulfonylureas, gliamilide can lower blood glucose levels by increasing the insulin release from pancreatic beta cells.

Azepexole (or previously known as B-HT 933), a selective alpha 2-adrenoceptor agonist that was studied for the man with physiological tremor. It was shown that the drug produced sedation compared to placebo but not when compared to pre-treatment values. Some studies also have revealed the anti-tussive and antihypertensive properties of azepexole.

Atiratecan (previously known as CH4556300 or TP300), the prodrug of a topoisomerase 1 inhibitor, CH0793076. Atiratecan has been studied in phase II clinical trials to treat cancers (e.g., colorectal cancer; gastric cancer; esophageal cancer), but these studies were suspended.

Peraquinsin is an antihypertensive agent.

Cositecan (BNP1350) is semi-synthetic silicon-containing camptothecin and an inhibitor of topoisomerase I. It was engineered by BioNumerik Pharmaceuticals for superior oral bioavailability, lactone stability, and insensitivity to Pgp/MRP/LRP drug resistance. The compound shows a broad spectrum of activity in experimental human tumors. Cositecan was investigated in clinical trials in patients with malignant melanoma, relapsed or refractory non-small cell lung cancer, ovarian and peritoneal cancer, malignant glioma. The compound had little activity in recurrent glioma and ovarian cancer.