THIALBARBITAL is a barbiturate derivative with sedative effects. Barbiturates have hypnotic properties and are used as active moiety on central nervous system. Thialbarbital was synthesized in the 1960s. It was used primarily as a surgical anesthesia. Thialbarbital causes marked depression of the activity of the reticular formation and only slight depression of cortical activity. Thialbarbital is short acting and has less of a tendency to induce respiratory depression than other barbiturate derivatives such as pentobarbital.

Telupidine (GR53992B), a dihydropyridine derivative is a calcium channel blocker. This is an antihypertensive and cardiovascular agent. Information about the current use of this compound is not available.

Octapinol, a substance with a low antibacterial activity that was studied to use in gingivitis and in stomatitis. Information about the current use of this compound is not available.

Nonapyrimine is an anticonvulsant, vasodilator.

Nonabine is a chromenol structurally related to the cannabinoids which has shown antiemetic efficacy in clinical trials. Nonabine also produced sedative clinical effects, but with an EEG profile which resembled that reportedly caused by cannabinoids. In contrast to cannabinoids, nonabine did not cause changes of mood or perception, suggesting that nonabine lacks the potential for social abuse at antiemetic doses. Nonabine was studied in the 1980s for the prevention of nausea and vomiting associated with cancer chemotherapy.

Irsogladine, a mucosal protective drug, was developed in Japan for the treatment of peptic ulcer disease and acute gastritis. Irsogladine increases intracellular cyclic adenosine 3',5'-monophosphate content via non-selective inhibition of phosphodiesterase isozymes and exhibits gastric cytoprotection partly mediated by endogenous nitric oxide. These effects may account for a variety of actions of irsogladine in the gastrointestinal tract, including facilitation of gap junctional intercellular communication, inhibition of the reduced gastric mucosal blood flow response, suppression of reactive oxygen generation and so on.

IPROZILAMINE, a member of 4-piperazinopyrimidines, has powerful antiemetic activity. It also exhibits a relaxant effect on smooth muscle fiber.

Ipatasertib, an investigational Akt inhibitor, is currently in clinical development based on its potential to specifically target Akt in tumors with activated Akt signaling. Preclinical data have shown that ipatasertib selectively decreased cell viability and increased apoptosis in tumor cell lines characterized by activated Akt. Ipatasertib is advancing in clinical development including three Phase 2 trials in patients with breast cancer, gastric cancer and prostate cancer. The most commonly reported adverse events associated with Ipatasertib were Grade 1-2 diarrhea, nausea, fatigue, vomiting, decreased appetite and rash.

Indorenate (TR3369, INDO) is a serotonin-like compound with high affinity for 5- HT1A receptors and a lower affinity for 5-HT1C and 5-HT1B receptors. Indorenate possesses antihypertensive and anxiolytic activity in animal behaviour tests. Similar to other serotonin receptor agonists, Indorenate also has anorectic activity; this effect was blocked by the administration of the 5-HT2A/2C receptor antagonists cinanserin, cyproheptadine, metergoline and methysergide. A unpublished clinical trial confirmed its antihypertensive activity in men.

Imisopasem Manganese is a manganese-based non-peptidyl mimetic of the human mitochondrial manganese superoxide dismutase (MnSOD), with potential antioxidant and radioprotective activities. Metaphore Pharmaceuticals Inc. is developing Imisopasem Manganese for the potential treatment of pain, dermatological disease and inflammation. Upon administration, imisopasem manganese mimics the activity of MnSOD and scavenges reactive oxygen species (ROS), such as superoxide anion, which prevents oxygen free radical damage to macromolecules such as DNA. This reduces ROS-mediated lipid peroxidation, prevents apoptosis and protects against oxygen free radical-induced toxicity in normal tissues.