Cormethasone is a topical antiinflammatory corticosteroid discovered by Du Pont.

Telupidine (GR53992B), a dihydropyridine derivative is a calcium channel blocker. This is an antihypertensive and cardiovascular agent. Information about the current use of this compound is not available.

Ensaculin is related to naturally occurring benzopyranones like scoparone. The compound is a potent functional antagonist of excitatory amino acid-induced convulsions and mortality. In receptor-binding studies, Ensaculin showed high affinity to dopaminergic (D2, D3), serotoninergic (5-HT1A, 5-HT7), and adrenergic (A1a, A1b) receptors in the nanomolar range. Ensaculin antagonizes NMDA responses in a voltage-dependent manner. Various studies support the notion that this compound could indeed have a broad range of nootropic properties. Although few patients presented postural hypotension and dizziness after receiving ensaculin in phase I clinical trials, this drug candidate was further discontinued in phase III due to potential side effects.

Levophacetoperane is a piperidine derivative. Levofacetoperane is a sympathomimetic central nervous system stimulant and is commonly used to treat depression. Levophacetoperane is also a known analeptic and is strongly linked to apnea reversal in dogs after a single intravenous injection.

Spirorenone is an androstadienone derivative patented by Schering A.-G as a highly effective aldosterone antagonist. Spirorenone is 8.6 times as potent as spironolactone, but showed a lower affinity for the mineralocorticoid receptors. In phase I clinical trials Spirorenone was absorbed with a half-life of 20-30 min, achieving maximum concentrations of about 100 ng/ml (10 mg) and 260 ng/ml (40 mg) after 1-2 h. Disposition of the parent drug was biphasic with half-lives of 50-60 min (distribution) and 5-6 h (elimination). Neither significant accumulation nor enzyme induction was observed after prolonged treatment.

Tetrazolast (also known as MDL 26,024GO) is a tetrazoloquinoline derivative patented by Merrell Dow Pharmaceuticals, Inc. as an antiallergic and antiasthmatic agent. Tetrazolast was shown to be an orally absorbed mediator release inhibitor in the rat passive cutaneous anaphylaxis and passive peritoneal anaphylaxis tests. In addition, the compound was shown to both elicit and inhibit elicitation of the Bezold-Jarisch reflex in the dog. Tetrazolast also significantly reduced Ascaris-induced changes in pulmonary mechanics in cynomolgus monkeys. The compound inhibited both early and late phase antigen induced-changes in Ascaris-sensitive sheep, as well as the increased airway hyperreactivity which normally follows antigen challenge.

Midesteine (previously known as MR 889), a thiolactic acid derivative was developed as an inhibitor of the chymotrypsin and elastolytic activity of leukocyte elastase. Midesteine participated in clinical trials for patients with chronic obstructive pulmonary disease. The drug is also studied to treat asthma, cystic fibrosis, and emphysema. However, all these studies were discontinued.

Resocortol is a synthetic corticosteroid. Information about current use of this compound is not available.

Terlakiren (also known as CP80794) is a cysteinamide derivative patented by Pfizer Inc. as potent renin inhibitor. Terlakirens inhibitory potency against plasma renin of guinea pigs, dogs, and monkeys ranges from 0.3 to 0.7 nM. In preclinical models, Terlakiren caused significantly greater increases in renal blood flow and suppressed renin activity to a greater degree than captopril.

Spiroxasone is a synthetic, steroidal antimineralocorticoid of the spirolactone group patented by Merck & Co., Inc. as a diuretic and antihypertensive agent. Spiroxasone acts as potent aldosterone antagonists in animals and humans.