Rocepafant (also known as BN 50730 or LAU 8080) is a hetrazepinic derivative and a platelet-activating factor (PAF) receptor antagonist. PAF is a mediator of cerebral ischemic injury and administration of rocepafant in neonatal rats was found to have a neuroprotective role, attenuating hypoxic-ischemic brain injury in neonatal rats. Combined with two other types of compounds, rocepafant was shown to modulate the stress-induced up-regulation of cycloooxygenase-2 and prostaglandin E2 in humans, which may be of potential therapeutic value in the design of treatment for complex neuroinflammatory disorders. This compound has been evaluated for treatment of asthma, arrhytmias and rheumatic disorders, but development of rocepafant has been discontinued in 2003.

Nosantine (NPT 15392) is a novel heterocyclic immunomodulatory compound related to inosine in structure and isoprinosine in action. Nosantine enhances a variety of lymphoid functional activities including proliferative responses to various antigenic and mitogenic stimuli. Such activities imply potential therapeutic use in immunodeficiency related to defects of the thymus and thymus-derived lymphocytes. In head and neck cancer patients the drug induced transitory, immune stimulation during or after treatment without any side effects. NPT 15392 seemed to selectively exert an action on T lymphocytes. Nosantine was found to be a potent and relatively selective inhibitor of mouse lymphocyte cyclic GMP phosphodiesterase, with IC50 values 15-180 times greater for cyclic AMP than cyclic GMP phosphodiesterases. Immunopharmacologic activities of NPT 15392 may include specific cyclic GMP phosphodiesterase inhibition as one of several possible mechanisms.

Dimetholizine has antihypertensive activity. It is an antihistaminic agent too. Histamine H1 receptor was predicted as a primary target for dimetholizine. Moreover, it was found to bind the Dopamine D2 and 5-HT1A receptors. Dimetholizine was predicted to be alpha1D-Adrenergic blocker.

Norletimol is a Schiff base with promising anti-inflammatory properties. The time taken for elimination of 50% of the Norletimol dose in the urine was approximately five hours. As an antirheumatic agent it was tested in clinical trials in Iraq. It was used in progressive myopia in children.

Nortetrazepam is a benzodiazepine derivative, it is one of the major metabolites of tetrazepam. Nortetrazepam is a psychosedative agent.

Dabuzalgron is an orally active and selective alpha1A/1L-adrenoreceptor partial agonist, developed by Roche. In anesthetized micropigs and rabbits, dabuzalgron produced non-selective, dose-dependent increases in intraurethral and arterial blood pressures. In conscious micropigs, both agents produced dose-dependent increases in urethral tension. Dabuzalgron was investigated in a clinical study in women with stress urinary incontinence (SUI). It was demonstrated that 1.5 mg of the drug administered twice daily lead to a significantly lower mean weekly number of SUI episodes with little or no cardiovascular effect. Despite positive results, no development of the drug was reported by Roche.

Denufosol is a novel second-generation, metabolically stable, selective P2Y(2) receptor agonist. As ion channel regulator denufosol corrects the ion transport defect and increases the overall mucociliary clearance in cystic fibrosis (CF) lung disease by increasing chloride secretion, inhibiting sodium absorption, and increasing ciliary beat frequency in the airway epithelium independently of cystic fibrosis transmembrane conductance regulator genotype. Denufosol improved lung function relative to placebo in cystic fibrosis patients with normal to mildly impaired lung function. The drug half-life is 25 hours in ex vivo CF sputum and 3 hours when added in vitro to human respiratory epithelial cultures. Denufosol has been generally well-tolerated in healthy volunteers and patients with cystic fibrosis. The most common adverse events were in the respiratory system, with cough having the highest frequency.

Diniprofylline is a vasodilator, broncholytic agent and respiratory stimulant used in severe respiratory insufficiencies.

Dipiproverine is the spasmolytic agent. It was used as anticholinergic drug.

Acolbifene, the active metabolite of EM-800, was identified as a pure antagonist that acts on both activation domains of the ERs. It is in Phase III clinical trials for the prevention of breast cancer and vasomotor symptoms (Hot flush) in postmenopausal women. Most commonly reported adverse events included irregular menses, leg/muscle cramps, diarrhea, and hot flashes. No serious adverse events were reported.