Carbenzide is hydrazine derivative with the high antidepressant activity and low toxicity patented by pharmaceutical company Warner-Lambert Pharmaceutical Co. Carbenzide acts via monoamine oxidase (MAO) inhibition and increase the level of brain serotonin.

Avagacestat (BMS-708163) is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta (Aβ) synthesis. Avagacestat was in development by Bristol-Myers Squibb for the treatment of Alzheimer's disease (AD). Avagacestat is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. In November 2012, Bristol-Myers Squibb terminated clinical trials of the drug and announced its decision to end further development of avagacestat

RTI-336 was developed as a selective dopamine transporter (DAT) inhibitor. It is known that DAT inhibitors have been developed as a promising treatment approach for cocaine dependence. RTI-336 can be a useful adjunct in the treatment of cocaine dependence because preclinical data has shown that this drug inhibits DAT with a slower onset and offset rate than cocaine and with less abuse potential and psychomotor stimulant activity. RTI-336 participated in phase I clinical trial where it showed the excellent safety and tolerability, and thus further studies in humans are warranted.

RGB-286638 is a multi-targeted protein kinase inhibitor currently in Phase 1 clinical testing. In vitro cell-free kinase assays indicated that RGB-286638 inhibits CDK1, 2, 3, 4, 5, and 9 and is less active against CDK6 and 7. The RGB-286638 compound has been shown to inhibit the processes controlling cell division in cancer cells by targeting multiple cyclin-dependent kinase proteins involved in regulating the cell cycle. RGB-286638 has also been shown to induce apoptosis (programmed cell death) and to inhibit other important protein kinases involved in the proliferation of cancer cells. RGB-286638 treatment results in tumor regression and increased survival in a number of pre-clinical models of solid and hematological tumors.

Recoflavone (DA-6034) is a synthetic derivative of eupatillen (flavone derivative). It has antioxidant properties, and anti-inflammatory effects in inflammatory bowel disease (IBD). Although the exact mechanism is still unknown, recoflavone may decrease intestinal permeability in an indomethacin-induced intestinal injury model via the extracellular signal-regulated kinase pathway. In a phase I clinical trial, recoflavone was well tolerated and minimally absorbed in healthy volunteers. In other (phase II and III) clinical trials, the drug has been evaluated for use in treatment of gastritis (phase III), dry eyes, and Crohn’s disease (discontinued).

Olvanil, a structural analog of capsaicin, is an agonist of the transient receptor potential vanilloid type-1 (TRPV1) channel. This compound was developed as a potential analgesic compound. Olvanil has potent anti-hyperalgesic effects in several experimental models of chronic pain.

Iogulamide is triiodobenzenedicarboxamide derivative patented by Mallinckrodt, Inc. as nonionic X-ray contrast agent for intrathecal use. Comparative preclinical animal studies demonstrated an acute safety profile significantly superior to that of metrizamide. Improved safety was unrelated to low osmolality. Intrathecally administered iogulamide produced no evidence of epileptogenic activity.

Pridefine (AHR-1118) is a pyrrolidine derivative with clinically established antidepressant efficacy. Pridefine acted predominantly as a reuptake blocker of norepinephrine, dopamine, and 5-hydroxytryptamine, although some releasing activity was also present. Several clinical studies have demonstrated that pridefine is clinically as efficacious as imipramine and, perhaps more importantly, less toxic than standard antidepressants used.

Synthetic compound Erteberel (LY500307) is a highly potent and selective ERβ agonist; it has a 12-fold higher affinity for ERβ than ERα and exhibits 32-fold more functional potency. LY500307 was well tolerated in benign prostatic hypertrophy (BPH) patients with no side effects and it is currently being tested in phase 2 clinical trials for improving negative symptoms and cognitive impairment associated with Schizophrenia. In BPH clinical trial incidence of adverse events was comparable between treatment groups, and no clinically meaningful changes in laboratory tests were observed.

Mitsubishi Tanabe Pharma was developing Sofigatran, a thrombin inhibitor, for the treatment of deep vein thrombosis. Sofigatran, is a direct oral thrombin inhibitor with a competitive binding mechanism. It has been assessed in a phase II trial for the treatment of deep vein thrombosis The compound was in phase II clinical trial for the treatment of DVT. Results of this trial have not been published and the clinical development of sofigatran has been discontinued by Mitsubishi Tanabe Pharma in 2007.