GSK-1614235 (mizagliflozin) is a sodium glucose co-transporter type 1 (SGLT1) inhibitor that has been investigated for treatment in type 2 diabetes. It is thought to suppress glucose absorption from the intestine in a way that is different from conventional type 2 diabetes drugs, thereby improving postprandial hyperglycemia. Phase 1 studies have been completed.

Icopezil (previously known as CP-118,954) was developed as a selective acetylcholinesterase inhibitor for the treatment of cognitive disorders. Phase II trials of icopezil were underway in Japan and in the USA for the treatment of patients with Alzheimer's disease. However, Pfizer has discontinued these studies.

Propoxycarbazone-Sodium (also known as BAY MKH 6561) is asulfonylaminocarbonyltriazolinone derivative patented by German multinational pharmaceutical and life sciences company Bayer A.-G. as herbicide Propoxycarbazone inhibits acetolactate synthase (ALS), and has selectivity on spring, winter, and durum varieties. The spectrum of control includes several species of monocot and dicot weeds at the application rates of 30 to 45 g/ha. Bromus control is the primary target since existing herbicides have limited timing, selectivity, and use patterns which reduce usefulness. Propoxycarbazone applied postemergence between the 1- to 2-leaf stage and shoot elongation has provided economic control of the following Bromus species: B. tectorum, B. secalinus, B. mollis, B. rigidus, and B. japonicus. Side effects, and sometimes control, was also noted on Aegilops tauschii for which there is no selective control outside genetically altered wheat cultivars. Broadleaf control was obtained primarily on the mustard family, including species in the genera Sisymbrium, Brassica, Descurainia, Chorispora, Camelina, Capsella, and Thlaspi. Propoxycarbazone provides control for adequate weed spectrum, however, considerations of resistance management, difficult and diverse weed pressure, and extended growing seasons will sometimes necessitate the use of sequential herbicides or mix partners.

Nebracetam (WEB1881FU) is a pyrrolidinone nootropic. Like other racetams, it is an aminomethyl pyrrolidinone derivative of piracetam. It was first synthesized in Germany in the late 1980s, where it was manufactured by Boehringer Ingelheim. Nebracetam is a M1-muscarinic agonist. In Jurkat cells Nebracetam induced a rise of [Ca2+]i in the medium with 1 mM Ca2+ and without Ca2+ (plus 1 mM EGTA). The nebracetam-induced [Ca2+]i rise was blocked by atropine greater than pirenzepine greater than AF-DX 116. Nebracetam facilitates the ganglionic muscarinic transmission through acting on presynaptic sites. Nebracetam has been investigated as a cognition-enhancing drug, but most of the studies have taken place in animal models. It has been shown to protect neurons in animals exposed to low levels of oxygen and low blood sugar. Nebracetam is also protective against glutamate toxicity, presumably via its modulation of calcium entry. In animal models of Alzheimer’s disease, nebracetam improved memory in a dose-dependent manner. It also protected against ischemia- (lack of oxygen) induced neuronal death in a rat model of stroke. The compound has also been tested as a possible antidepressant, presumably because its mechanism of action (reducing dopaminergic and serotonergic uptake) is similar to other commonly used antidepressants. Some studies have taken place in humans. A single dose was shown to alter brain waves in healthy volunteers, who showed increased alpha activity and an associated decrease of slow activity and of fast activity in the frontal cortex. These results imply that nebracetam might improve linguistic learning and memory processing. A trial in dementia patients reported that significant clinical improvement occurred after 8 weeks. However, other studies did not replicate this finding.

Oxadimedine, an antihistamine that was developed as a local anesthetic. Information about the current use of this compound is not available.

Giripladib (PLA 695) is a Cytosolic phospholipase A2 (cPLA2) inhibitor. cPLA2 is associated with tumor progression and radioresistance in mouse tumor models. In these models, treatment with giripladib attenuates radiation induced increases of phospho-ERK and phospho-Akt in endothelial cells. Combined with irradiation, giripladib reduces migration and proliferation in endothelial cells (HUVEC & bEND3) and induces cell death and attenuated invasion by tumor cells (LLC &A549). The combination treatment of giripladib and irradiation also delayes growth in both LLC and A549 tumors and results in reduced tumor vasculature. Phase I studies have been conducted to test the gastrointestinal safety of giripladib, and potential pharmacokinetic interaction with other compounds. A phase II study was terminated.

Oxifentorex was developed as a CNS stimulant and anorectic agent. However, information about the current use of this compound is not available.

Sulfinalol is a hydroxyphenylalkanolamine derivative patented by Sterling Drug Inc. as the antiarrhythmic, antihypertensive, vasodilating, and adrenergic agent. Oral administration of sulfinalol reduces the pressure of conscious spontaneously hypertensive rats. Antihypertensive action of sulfinalol was inhibited by propranolol pretreatment. Sulfinalol demonstrates effective beta-adrenergic blockade at the antihypertensive dose tested as judged by inhibition of the chronotropic responses to sympathetic stimulation and isoproterenol in pithed rats. In the renal hypertensive dog. sulfinalol lowered both systolic and diastolic blood pressure to normal values with an only slight change in heart rate.

Cizolirtine is a potent analgesic in mice and rats, with an efficacy superior to that of aspirin and other nonsteroid anti-inflammatory drugs. Recent studies have shown that the analgesic effect of cizolirtine could be related, at least partially, to an inhibition of spinal substance P and calcitonin gene-related peptide release. Cizolirtine has been in clinical trials for the treatment of pain and overactive bladder. Reported adverse events are: dry mouth, dizziness, nausea, vomiting, blurred vision.