Tebufelone (formerly NE-11740) is a member of the di-tert-butyl-phenol anti-inflammatory agents. Tebufelone is a dual cyclooxygenase (CO)/5-lipoxygenase (LO) inhibitor that has potent analgesic, antipyretic, and anti-inflammatory effects. This drug was studied for the treatment of rheumatic disorders; however, this study was discontinued.

Bemitradine (SC-33643), a diuretic antihypertensive agent that was dropped from the development. Experiments on rodents have revealed this drug was a carcinogen and acted by a hormonally modulated promotional activity in inducing tumors in the liver and mammary glands.

(S)-baclofen (or L-baclofen) is an enantiomer of baclofen, a direct GABA-B receptor mimetic. L-baclofen represents a significant improvement over racemic baclofen in the treatment of trigeminal neuralgia.

Deramciclane is camphor derivative. It is an anxiolytic agent that binds with high affinity to 5-HT2A/2C receptor. Deramciclane showed significant evidence of efficacy for the treatment of generalized anxiety disorder in adult patients. A single dose of deramciclane was rapidly absorbed with peak plasma concentrations being reached after about 3 h. Deramciclane has a half-life of around 27 h. The most commonly reported adverse event was headache. In the in vitro studies deramciclane concentration-dependently inhibited NMDA evoked spreading depression.

Ortataxel (previously known as IDN 5109 or BAY59-8862), a second-generation taxane derivative that was developed as an antitumor agent. Ortataxel binds to and stabilizes tubulin molecules, thereby interfering with the dynamics of microtubule assembly/disassembly. This results in the inhibition of cell division and cellular proliferation. In addition, ortataxel modulates multi-drug resistance mechanisms and may be useful for treating multi-drug resistant tumors that express Pgp, MRP-1, and BCRP. This drug participated in phase II clinical trials in patients with advanced renal cell carcinoma and in patients with Non-Hodgkin's lymphoma. However, these studies were discontinued. Ortataxel was also involved in phase II clinical trials for patients with glioblastoma; however, in a limited number of patients, the drug produced a benefit that lasted for a long time. Besides, ortataxel successfully completed phase II trials in taxane-resistant metastatic breast cancer patients and in taxane-resistant non-small cell lung cancer patients.

MK 0777 is a selective GABAA α2/3 receptor partial agonist, for potential use in the treatment of Schizophrenia, Anxiety Disorder, and Generalized Anxiety Disorder. MK-0777 is functionally selective for the α2 and α3 subunits, with virtually no activity for the α1 and α5 subunits. Therefore, MK-0777 cause less sedation, interact less with alcohol, and exhibit less abuse potential and physical dependence than benzodiazepines. Unfortunately, in clinical trials, MK-0777 has little benefit for cognitive impairments in people with schizophrenia and anxiety disorder.

Tuclazepam, a benzodiazepine derivative, is a tranquilizer.

Utibapril (FPL 63547) is an ester prodrug of a novel thiadiazoline ACE inhibitor. Utibapril was undergoing phase II clinical studies in the United Kingdom for the treatment of heart failure and hypertension. Utibapril is an angiotensin-converting enzyme (ACE) inhibitor with a proposed tissue-specific inhibitory profile. This implies that at a certain dose, utibapril should be able to inhibit tissue ACE activity without affecting plasma ACE.