Sufugolix (TAK-013 or 5-(N-benzyl-N-methylaminomethyl)-1-(2,6-difluorobenzyl)-6-[4-(3-methoxyureido)phenyl]-3-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione) is a highly potent and orally active non-peptide antagonist of luteinizing hormone-releasing hormone (LHRH) receptor. Sufugolix by oral administration suppresses a pituitary-ovarian axis continuously and reversibly in cynomolgus monkeys. Takeda studied Sufugolix in the trials for the treatment of endometriosis and uterine leiomyoma however development was discontinued.

Bemoradan (RWJ-22867), a potent positive inotropic agent, inhibits cardiac phosphodiesterase fraction III. This compound was developed for the management of congestive heart failure. However, the information about the nowadays study of bemoradan is not available.

Nicofibrate is an antilipidemic drug. Treatment of diabetics led to a significant reduction in plasma cholesterol and triglycerides and brought the lipoprotein picture back within the norm. Nicofibrate did not lead to significant increases in uricaemia nor to any worsening in carbohydrate tolerance. Nicofibrate may also lead to a significant drop in plasma prothrombinic activity.

Semorphone (previously known as Mr 2264), a partial opiate receptor agonist that was in two times more potent than morphine. Semorphone has a ceiling effect on both analgesia and respiratory depression; it means that these effects stop becoming any stronger after a certain maximum dose.

Iomeglamic Acid is an iodinated aryldicarboxylic acid monoamide used as insoluble X-ray contrast media. Iomeglamic acid has been successfully applied for radioscopy of the gall-bladder since 1972 but currently discontinued.

Losigamone possesses an unique anticonvulsant activity profile and has an excellent tolerability. Losigamone causes dose-dependent inhibition of the tonic hind leg extension produced by electric shock, pentylenetetrazole, bicuculline, nicotine and 4-aminopyridine. Losigamone also inhibits clonic seizures induced by pentylenetetrazole, bicuculline and picrotoxin, whereas it has no effect on the hind leg extension caused by strychnine and picrotoxin or the clonic seizures induced by NMDA. Losigamone had been in phase III clinical trial for the treatment of partial epilepsies. However, this development was discontinued.

FENFLUMIZOLE, an imidazole derivative, is a nonsteroidal, anti-inflammatory agent. It is a potent cyclooxygenase inhibitor with anti-phlogistic potency equalling that of indomethacin.

Piconol (2-Pyridinemethanol) is a pyridylalcohol devivative with hypoglycemic activity.

KRN-5500, a spicamycin derivative, is a nucleoside-like antibiotic with a broad spectrum of antitumor activity against human cancer cell lines. It also may have value in the treatment of neuropathic pain.