Suxemerid is a succinic acid derivative patented by Warner-Lambert Pharmaceutical Co. as an antihypertensive agent.

Napamezole [WIN 51181] is a potent alpha-2 adrenergic receptor antagonist and a selective inhibitor of 5-hydroxytryptamine re-uptake in vitro. Napamezole was at the phase I stage of development with Sanofi Winthrop (formerly known as Sterling Drug before it was purchased by Sanofi) in the USA as a treatment for depression. The alpha adrenergic antagonist activity of napamezole was determined in vitro in rat brain receptor binding assay using [3H]clonidine and [3H]prazosin for alpha-2 and alpha-1 receptors, respectively. The Ki values for napamezole were 28 nM (alpha-2) and 93 nM (alpha-1).

FIGOPITANT is a tachykinin NK1 receptor antagonist. It can inhibit scratching behavior in an atopic dermatitis model. It is under investigation in clinical trials to obtain preliminary pharmacokinetics data and information about FIGOPITANT safety and tolerability in healthy volunteers.

Myrophine is an opiate analog and long-acting prodrug for morphine with a slow onset of effects. It is weaker than morphine as an analgesic but longer-lasting in effects and was thought to have a more local anesthetic effect than morphine, though with a somewhat greater tendency to cause histamine reactions like itching and rash. In addiction studies conducted in human subjects in the 1950s, myrophine did not substitute for morphine in withdrawal, did not produce notable morphine-like effects, and did not produce addiction or dependence regardless of dose or how it was administered.

Capravirine (S-1153, AG1549) is a 1,2,4,5-tetrasubstituted imidazole derivative patented by pharmaceutical company Shionogi as specific inhibitors of HIV-​1 reverse transcriptase. However, safety and efficacy studies showed that Capravirine had no specific advantages over currently used NNRTIs. Consequently, clinical trials were discontinued after phase IIb.

1,4-Butanediol diglycidyl ether (BDDE) is a viscous liquid, which is hygroscopic in nature. BDDE is the most commonly used homobifunctional epoxide compound. BDDE may react with amines, hydroxyls, sulfhydryl groups to produce secondary amines, ether or thioether bonds respectively. BDDE is a cross linking agent used • for preparing amylose, xylan and hydroxyethyl-cellulose • to cross link polyethylenimine which also serves as a hole-blocking layer in organic solar cells • to cross link hyaluronic acid (HA) into hydrogels • for the activation of soluble dextran polymers. • Amine or hydroxyl containing bis-epoxy supports are reacted with BDDE to form particles containing terminal epoxide group for immobilization reactions. In most commercial products, HA is crosslinked to increase its longevity, and the crosslinking agent used has an important effect on the properties of the final product; BDDE is the crosslinking agent used in the majority of the market-leading HA fillers, and its stability, biodegradability, and long safety record spanning more than 15 years are what make it the industry standard, ahead of other crosslinkers such as divinyl sulfone and 2,7,8-diepoxyoctane. Its ability to crosslink is attributed to the reactivity of the epoxide groups present at the two ends of the molecule. Under basic (pH > 7) conditions, these epoxide groups preferentially react with the most accessible primary alcohol in the HA backbone, forming an ether bond connection. The superior stability of the ether bond (relative to the ester or amide bond) is one of the reasons that BDDE-crosslinked HA fillers have a clinical duration that can reach or exceed 1 year. In addition, BDDE has a significantly lower toxicity than other ether-bond crosslinking chemistry based agents (e.g., divinyl sulfone), is biodegradable, and has been well studied.

Clentiazem is a chloride derivative of diltiazem, originated in Tanabe Seiyaku. It works as a blocker of calcium channels. The drug was investigated in the clinical trials for the treatment of stable angina, and essential hypertension. Despite the positive results of clinical trials, no development of the drug was reported.

Clofenamic acid is a derivative of anthranilic acid, discovered by Parke-Davis. It possesses anti-inflammatory activity in the carrageenan-induced rat foot edema test.

Cinanserin is a 5-hydroxytryptamine receptor antagonist; it shows a low affinity to 5-HT2b binding sites and a 4-to 10-fold lower affinity to 5-HT2c receptor binding sites than for 5-HT2a sites. Nevertheless, at concentrations normally used 5-HT2c receptor blocking effects are still likely. Experiments on animal have shown that intravenous administration of cinanserin significantly reduces systemic burn edema and leukocyte-endothelial interactions.

Ciladopa, is a troponylpiperazine derivative and dopamine agonist that has been shown to influence dopaminergic mechanisms in animals. Preclinical pharmacological studies have suggested that it has antiparkinsonian activity similar to that of bromocriptine but without many of the troublesome side effects. Unfortunately in some clinical trials no significant differences was found among the treatment groups and placebo.