Nepicastat (SYN-117) is a potent and selective inhibitor of dopamine-β-hydroxylase. This compound in Phase 2 of clinical trial for the treatment cocaine addiction and posttraumatic stress disorder.

Soraprazan (remofuscin), a potassium-competitive acid blocker (P-CAB; formerly called an acid pump antagonist [APA]), is being developed by Katairo GmbH for the treatment of Stargardt's disease and dry age-related macular degeneration (AMD). Clinical development is underway for Stargardt's disease and dry age-related macular degeneration in the Netherlands and Germany. On 13 November 2013, orphan designation was granted by the European Commission to Katairo GmbH, Germany, for soraprazan for the treatment of Stargardt’s disease. Soraprazan is a a highly potent reversible, and fast-acting inhibitor of gastric H,K-ATPase. Soraprazan shows immediate inhibition of acid secretion in various in vitro models and in vivo and was found to be more than 2000-fold selective for H,K-ATPase over Na,K- and Ca-ATPases.

Furethidine, a pethidine analog was studied as an analgesic agent. This compound is not currently used in medicine and is listed in schedules of the single convention on narcotic drugs of 1961 as amended by the 1972 protocol.

Methyldesorphine is a synthetic narcotic analgesic derived from morphine. It has no medicinal value in the US. This compound is listed as a Schedule I Narcotic controlled substance under the Controlled Substances Act 1970.

RGH-896 (radiprodi) is orally active and selective NMDA NR2B antagonist, a potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions. It blocks pain signaling without interacting with other NMDA receptor subtypes thus potentially improving therapeutic index and side effect profile. RGH-896 is the first of this group and is currently in early clinical development. Forest and Richter initiated a Phase IIb study in neuropathic pain in the United Stated in the second half of 2006. The drug did not produce significant reductions in patient-reported pain scores for all the dosages tested. Forest says that it and Gedeon Richter will review the findings before making a decision about the further development of radiprodil. In addition to neuropathic pain, the companies intend to investigate various other pain conditions and possibly CNS indications not related to pain. Forest will pay Richter undisclosed upfront and milestone payments in addition to royalties and will have exclusive rights in the U.S. and Canada. The two companies will jointly fund the development program. RGH-896 has patent applications that provide patent protection until at least 2022.

Camobucol is a novel, orally active, phenolic antioxidant and anti-inflammatory compound with antirheumatic properties. Camobucol exhibited potent antioxidant activity toward lipid peroxides in vitro and displayed enhanced cellular uptake relative to a structurally related drug, probucol. This resulted in potent inhibition of cellular levels of reactive oxygen species in multiple cell types. Camobucol selectively inhibited tumor necrosis factor (TNF)-alpha-inducible levels of the redox-sensitive genes, vascular cell adhesion molecule-1 and monocyte chemoattractant protein-1, with less inhibition of E-selectin, and no effect on intracellular adhesion molecule-1 expression in endothelial cells. In addition, Camobucol inhibited cytokine-induced levels of monocyte chemoattractant protein-1, interleukin (IL)-6, and IL-8 from endothelial cells and human fibroblast-like synoviocytes as well as lipopolysaccharide-induced release of TNF-alpha, IL-1beta, and IL-6 from human peripheral blood mononuclear cells. Camobucol did not inhibit TNF-alpha-induced nuclear translocation of nuclear factor of the kappa-enhancer in B cells (NF-kappaB), suggesting that the mechanism of action is independent of this redox-sensitive transcription factor.

Naronapride (ATI-7505), an orally administered, cisapride analogue and serotonin4 (5HT4) receptor agonist, is being developed by Renexxion for the treatment of multiple gastrointestinal disorders. Sinovant is initially developing naronapride for the treatment of irritable bowel syndrome – constipation (IBS-C), a disease that affects millions of Chinese patients and for which few effective treatment options are available. Naronapride has been evaluated in over 900 subjects in multiple randomized controlled clinical studies and has demonstrated promising results in patients with gastroesophageal reflux disease (GERD), erosive esophagitis (EE), and chronic idiopathic constipation (CIC). Naronapride’s low systemic absorption and high specificity for 5HT4 and D2 receptors is thought to improve its safety and tolerability profile relative to other members of the class.

Levophenacylmorphan is the synthetic narcotic analgesic and sedative agent. Levophenacylmorphan have been used as pre-anaesthetic medication. Phenazocine and levophenacylmorphan have similar pharmacologic properties and similar analgesic potency. Levophenacylmorphan is under international control according to the UN Single Convention 1961 and its amendments. It is not found in any pharmaceutical preparations sold in the United States.

Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure (in Phase 2 of development). Omecamtiv mecarbil is an inotropic agent that prolongs systolic ejection time and increases ejection fraction through myosin ATPase activation.