Panomifene (also known as GYKI-13504 or EGIS-5660), a triphenyl-alkene derivative that was studied as an antiestrogen. This drug binds to specific estrogen receptors and exhibits inhibitory effects on experimental mammary tumors both in vitro and in vivo. Panomifene reached phase II clinical trials for the treatment of breast cancer before development was terminated.

Ritobegron (KUC 7483) is a selective β3-adrenoceptor agonist that was developed for oral treatment of overactive bladder. It is the prodrug of the active compound KUC-7322. Phase I studies have investigated the pharmacodynamic and pharmacokinetic effects of ritobegron in healthy individuals and patients with spinal cord injury. Ritobegron exhibits a high selectivity for the bladder versus other organs, and decreased intravesical pressure with minimal effects on the cardiovascular system in rats. When administered in combination with organic anion transporter (OAT) inhibitors such as probenecid (primarily used in treating gout and hyperuricemia), the plasma concentration of the active compound KUC-7322 may increase.

Carvotroline [WY 47791] is a novel γ-carboline derivative with a preclinical profile suggestive of antipsychotic activity. Carvotroline has an affinity for the dopamine D2 receptor and cortical 5-HT2 receptor that is ten times greater than serotonin. Carvotroline administration to rats leads to a decrease of plasma corticosterone levels and demonstrated a moderating effect on the rotational-stress induced rise in plasma corticosterone levels.

Dimetipirium is a spasmolytic, antineoplastic and anticholinergic agent.

ITROCAINIDE is an antiarrhythmic agent.

Dexlofexidine is an isomer “+“ of lofexidine, which is agonist of alpha 2-adrenoceptor, but in 10 times less potent than the other isomer, levlofexidine.

Almorexant (ACT-078573) is an orally active dual orexin receptor antagonist that is being developed by Actelion Ltd, in collaboration with GlaxoSmithKline plc, for the treatment of primary insomnia. Almorexant is a first-in-class compound that targets the orexin system, which plays a key role in wake promotion and stabilization; In January 2011, GlaxoSmithKline (GSK) and Actelion Ltd announced that clinical development of Phase III of almorexant has been discontinued. This decision follows a review of data from additional clinical studies, which were conducted to further establish the clinical profile of almorexant, including the tolerability profile.

Carbazeran is a potent PDE-II and PDE-III inhibitor. Potently inhibits cAMP hydrolysis. Shows chronotropic and inotropic effect in vivo (EC50 = 100 μM, ionotropic effects, independent of adrenergic mechanisms). Carbazeran is a potent cardiac stimulant. Phosphodiesterase inhibition and elevation of intracellular cyclic AMP concentration may be involved, at least in part, in carbazeran`s cardiac effect.

Verilopam is a potent analgesic.

FENIMIDE, a succinimide derivative, is an antipsychotic drug. It is not found in any pharmaceutical preparations sold in the US. It was found that FENIMIDE produced a sedative effect prior to deeper central nervous system depression.