Semapimod (CNI-1493) is a cytokine inhibitor and synthetic guanylhydrazone mitogen-activated protein kinase blocker, is being developed by Cytokine PharmaSciences as a potential treatment for Crohn's disease and other inflammatory conditions. As of December 2001, a phase I study demonstrating the safety of the compound had been completed and phase II trials for psoriasis and Crohn's disease were ongoing. In April 2003, preclinical and early clinical studies were underway for a variety of indications, including congestive heart failure and pancreatitis. Semapimod inhibits activation of p38 MAPK and NF-κB and induction of cyclooxygenase-2 by TLR ligands, but not by IL-1β or stresses. Semapimod inhibits TLR4 signaling (IC50 ≈0.3 umol) and acts by desensitizing cells to LPS; it fails to block responses to LPS concentrations of ≥5 ug/ml. Semapimod had been in phase II clinical trials by Ferring Pharmaceuticals for the treatment of Crohn's disease. However, this research has been discontinued. Semapimod is in phase I clinical trials for the treatment of autoimmune disorders and inflammation.

Lupitidine (SKF 93479) is a histamine H2 receptor antagonist. Lupitidine is a potent inhibitor of gastric acid secretion with a long duration of action. It lacks an antiandrogenic effect. It enhances pituitary thyroid stimulating hormone drive by increasing thyroid hormone clearance. It exerts an antinociceptive effect in rodents.

Semotiadil (also known as sesamodil or SD 3211) is a (+)-(R)-stereoisomer, the corresponding (−)-(S)-stereoisomer is called levosemotiadil. Semotiadil, a benzothiazine derivative was developed as a novel Ca2+ channel blocker with antiplatelet activity. Experiments on rodents have revealed that the drug had an advantage in the treatment of angina with regard to long-lasting action and selectivity for coronary artery and myocardium. In addition, semotiadil improved survival of rats with monocrotaline-induced pulmonary hypertension: comparison with diltiazem. Semotiadil was studied in phase II clinical trials for the treatment of angina pectoris and hypertension in Europe, and in Japan for the treatment of arrhythmias. However, the further development of semotiadil has now been discontinued.

Enpiprazole is a heterocyclic three-ringed pyrazolylalkyl piperazine derivative. Enpiprazole has a cataleptic action very similar to that of neuroleptics, and its effect on muscle relaxation is comparable with that of diazepam. Enpiprazole exerts anxiolytic properties in animals.

Thiazesim (also known as ) is a benzothiazepine derivative patented by Olin Mathieson Chemical Corp. as an oral anti-depressant and tranquilizer useful in the treatment of Parkinsonism. Thiazesim is chemically related to the tranquilizing drugs chlordiazepoxide and diazepam but possesses a unique action on the limbic system, namely a selective depression of the lateral amygdaloid nucleus in experimental animals. Thiazesim shows potent anti-depressant activity in clinical trials.

Suxethonium is a depolarising muscle relaxant, with low incidence of postoperative muscle pain.

Pimetine has been reported to be an antiatherogenic agent of particular interest since its activities are unrelated to blood cholesterol levels. Pimetine hydrochloride (IN 379) alters the production and utilization of acid mucopolysaeeharides and may block the formation of atherosclerotic plaque. The initial clinical evaluation of pimetine in neuropsychiatric disorders was performed in hospitalized patients with the diagnosis of "chronic brain syndrome". Behavioral effects of pimetine were increased alertness, interest and sociability with improvement in organization of thought processes. In patients suffering from chronic organic diseases, pimetine was reported to produce a feeling of "more energy", a general feeling of "well being" and mild insomnia was reported as a non-limiting side effect. Pimetine was found to be a less active stimulant than amphetamine.

Chromocarb is benzo-γ-pyrone derivative with vasoprotection activity used to eliminate lipoperoxidation post-vitrectomy. Peroral treatment of rats with chromocarb significantly reduced the degradation of the vascular wall by intravenous collagenase, as demonstrated by a lesser permeability increase of the blood-brain barrier, a shorter recovery time, lower hydroxyproline levels in the cerebrospinal fluid and a lesser decrease of the collagen content of the brain capillary basal lamina.

Tubulozole is a stereospecific microtubule inhibitor. Structurally it is related to the benzimidazole carbamates by its carbamate moiety, which is essential for the activity of both types of compounds. The compound exists as a cis-isomer called tubulozole-C (R 46 846) and as a trans-isomer called tubulozole-T. The cis-isomer appears to be a potent and specific microtubule inhibitor, the trans-isomer being inactive at 100 times higher concentrations. At low concentrations, both isomers of tubulozole (C, T) inhibit Plasmodium falciparum but only tubulozole C inhibits mammalian cells. Since tubulozole C prevents polymerization of mammalian tubulin whereas tubulozole T does not, the antimalarial action of tubulozoles may not involve microtubules. Tubulozole-C, a new synthetic anticancer drug, interfered with the structure and function of microtubules in both interphase and mitotic cells. The activity of Tubulozole-C in experimental tumor systems can be explained partly by a direct antimitotic effect and partly by the disintegration of the normal subcellular organization of the nondividing cells. At concentrations which affect the microtubule system, tubulozole-C arrested directional migration of transformed cells and malignant invasion in a three-dimensional organ culture system. Investigations in vivo show that malignant L1210 leukemia cells are more susceptible to the antimicrotubular effect of tubulozole-C than are the normal leukocytes of the host. The trans-isomer of tubulozole (tubulozole-T, R 48 265), which has no antitumor activity in vivo, did not affect the microtubule system of cells in vitro or their capacity for directional migration or for malignant invasion.

Orconazole, an imidazole derivative, was developed by Janssen Pharmaceutical as an antifungal agent, however, this drug has never been marketed