Ciclazindol is an indole derivative and monoamine uptake inhibitor patented by pharmaceutical company John Wyeth and Brother Ltd. as an antidepressant. Besides that, Ciclazindol is effective anorectic agent, inducing weight loss in rats and man. Ciclazindol was shown to inhibit ATP-sensitive K+ (K(ATP)) channel currents and stimulate insulin secretion from CRI-G1 insulin-secreting cells. The inhibition of KATP channel currents by ciclazindol is unaffected by the removal of intracellular Mg2+ ions and after trypsinization of the cytoplasmic surface of excised patches, treatments known to abolish sulphonylurea sensitivity.

Miroprofen, an imidazopyridine derivative, possesses anti-inflammatory properties. It was shown that this compound could be effective in suppressing pain responses and acute inflammation accompanied by increased vascular permeability. Analgesic effect of this compound was studied in post-extraction pain. However, information about the current study of this agent is not available.

Diacetamate (Acetaminophen Acetate, Acetaminophen Impurity, diacetyl-p-aminophenol) is a acetaminophen synthetic impurity. Acetaminophen-aspirin mixtures have lower stability due to acetylation of the former by the latter, producing diacetyl-p-aminophenol.

Deximafen is antidepressant drug developed by Abbot Laboratories Inc.

GTS-21 (also known as DMBX-A), a selective alpha-7 nicotinic acetylcholine receptor agonist that has demonstrated memory and cognition enhancement activity in human clinical trials. GTS-21 has been studied in Phase II in patients with schizophrenia and in patients with Alzheimer disease. However, these studies were discontinued. GTS-21 was also involved in phase II to reduce negative affect, improve cognition and/or reduce smoking relapse in healthy adult men and women who are chronic cigarette smokers. However, this study was withdrawn. Besides, GTS-21 has participated in phase II to investigate safety and efficacy in adults with attention-deficit hyperactivity disorder.

Bepafant (also known as WEB-2170), an inverse agonist of platelet-activating factor receptor that has been preclinical studied in asthma, Ischemic heart disorder and in reperfusion injury after orthotopic liver transplantation. However, these studies were discontinued. Besides, several experiments have shown that bepafant induced apoptosis in human acute myelogenous leukemia and thus could be the powerful antileukemic agent.

Berubicin, an anthracycline derivative, is a DNA binding agent and potent topoisomerase II poison. Reata Pharmaceuticals were developing it as a treatment for brain cancer as it can breach the blood-brain barrier. It had also been in early clinical trials for the treatment of lung cancer and malignant gliomas. However, studies have been terminated. In October 2006, it was granted orphan drug designation from the FDA for the treatment of malignant gliomas. According to a CNS Pharmaceuticals media release in April 2018, berubicin will be studied for glioblastoma patients, these investigations will be funded in part by an equity crowdfunding campaign.

Ciluprevir (BILN-2061) is a selective inhibitor of the HCV NS3 serine protease, which was developed by Boehringer Ingelheim for the treatment of hepatitis C infection. The drug was discontinued in phase II due to adverse events such as cardiac toxicity (demonstrated in animals). In the cell-based replicon assay, ciluprevir inhibited HCV RNA replication at low nanomolar levels. It had inhibitory rate constant (Ki) values of 0.3 and 0.66 nM for the NS3 proteases of HCV genotypes 1a and -1b, respectively.

Siratiazem [LRA 113] is a calcium channel antagonist that is structurally similar to diltiazem but has a branched alkyl group on the basic nitrogen. Siratiazem has been developed in an attempt to limit the in vivo N-demethylation that is known to occur with diltiazem. Preliminary binding and functional studies in cardiac and vascular tissues indicate that it not only binds to diltiazem binding sites but also exhibits Ca2+ channel blocking properties comparable to diltiazem. Siratiazem has a similar profile of activity to its parent compound, diltiazem, in that it blocks calcium channels in vascular, intestinal smooth muscle and cardiac tissue, and is least potent in cardiac muscle. At higher concentrations, siratiazem may also block cardiac sodium channels.

Fosbretabulin (Combretastatin A4 phosphate, CA4P) is the lead compound of a relatively new class of agents termed vascular disrupting agents that target existing tumor blood vessels. Rapid tumor blood flow shutdown has been demonstrated in preclinical models and patients by various techniques such as dynamic contrast-enhanced MRI, perfusion computed tomography and PET scans following CA4P infusion. CA4P typically induces rapid tumor necrosis in the center of the tumor and leaves a rim of viable cells in the periphery. In oncology, CA4P does not appear to be that active by itself, but may be more efficacious when combined with chemotherapy, antiangiogenic therapy and radiation therapy. Combretastatin was initially isolated from the root bark of the South African Bush willow Combretum caffrum in 1982 by Pettit and colleagues at the Arizona State University (AZ, USA). Combretastatin A4 phosphate binds avidly to tubulin at the colchicine-binding site to inhibit microtubule assembly and destabilize the cytoskeleton. CA4P is a tubulin-binding agent that binds at or near the colchicine binding site of β-tubulin (Kd = 0.40 uM), inhibits tubulin assembly with IC50 of 2.4 uM. Fosbretabulin has orphan drug status in the EU and the US for the treatment of ATC (Anaplastic Thyroid Cancer). Later the development of this drug was discontinued.