Alletorphine (R & S 218-M) is a potent analgesic said to have a reduced respiratory depressant action. It was isolated by Bentley and Hardy (1967) while they were examining a series of derivatives of tetrahydrothebaine of which the potent analgesic etorphine (propylorvinolhydrochloride: M99 Reckitt) is a member. R&S 218-M bears the same relationship to etorphine as does nalorphine to morphine. It has been the subject of experiments in animals and human volunteers.

Ethoxazene (2,4-diamino-4-ethoxyazobenzene) is an analgesic compound. It may be used as an indicator of acidity in an examination of gastric function.

Imisopasem Manganese is a manganese-based non-peptidyl mimetic of the human mitochondrial manganese superoxide dismutase (MnSOD), with potential antioxidant and radioprotective activities. Metaphore Pharmaceuticals Inc. is developing Imisopasem Manganese for the potential treatment of pain, dermatological disease and inflammation. Upon administration, imisopasem manganese mimics the activity of MnSOD and scavenges reactive oxygen species (ROS), such as superoxide anion, which prevents oxygen free radical damage to macromolecules such as DNA. This reduces ROS-mediated lipid peroxidation, prevents apoptosis and protects against oxygen free radical-induced toxicity in normal tissues.

Girisopam (GYKI 51189), a 2,3-benzodiazepine, is a compound with anxiolytic and antipsychotic action. It has shown these effects in several animal models. Girisopam differs from the traditional 1,4-benzodiazepines because of its selective anxiolytic action without muscle relaxant and anticonvulsive activity, and because it does not have affinity for 1,4-benzodiazepine receptors. Antidepressant activity of girisopam was also reported. The binding site of girisopam in neuronal cells in the central nervous system is located exclusively to the basal ganglia. Because the danger of tolerance and dependence is lower for 2,3-benzodiazepine than 1,4-benzodiazepines, girisopam may potentially be used in treatment of addiction and affective disorders. No clinical trials were conducted in the US.

Melizame is a sugar substitute for sweetening caloric or noncaloric materials.

Evobrutinib is a highly selective, irreversible inhibitor of Bruton's tyrosine kinase (BTK). It potently inhibits BCR- and Fc receptor-mediated signaling and, thus, subsequent activation and function of B cells and innate immune cells such as monocytes and basophils. Evobrutinib demonstrated effectivity in autoimmune disease preclinical models. Evobrutinib is being developed by Merck Serono for the treatment of various autoimmune disorders.

Emitefur or BOF-A2 is a fluorinated pyrimidine antimetabolite exerting antineoplastic properties. It is a compound composed of 5-fluorouracil (5-FU) and 3-cyano-2,6-dihydroxypyridine (CNDP), an inhibitor of 5-FU degradation by dihydrouracil dehydrogenase in order to prolong the blood 5-FU level as well as increase selective toxicity to a tumor. Emitefur demonstrated clinical activity in preliminary studies in Japan. Emitefur development for the treatment of solid tumors has been discontinued.

(-)-3-(3-hydroxyphenyl)-N-n-propylpiperidine ((-)-3-PPP, also known as preclamol) has a dual action towards to dopamine D2 autoreceptor: it activates it and also acts concomitantly as an antagonist at postsynaptic DA receptors. It was shown, that (-)-3PPP/preclamol was a safe drug for study in the treatment of schizophrenia and may have antipsychotic efficacy. Besides, the motor effects of the drug were evaluated in nine patients with Parkinson's disease using a double-blind, placebo-controlled design. However, the small number of patients manifesting a clinically significant response and the frequently inconsistent effects could indicate that this class of agents may have relatively limited clinical utility.

As a narcotic antagonist similar in action to naloxone, DIPRENORPHINE is used to remobilize animals after analgesia by super-potent opioid analgesics such as etorphine and carfentanil. It is not used in humans. Diprenorphine binds approximately equally to the three subtypes of opioid receptors (mu, delta, and kappa) and antagonizes them. This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene. The therapeutic efficacy of many other compounds can be decreased when used in combination with Diprenorphine (54 compounds mentioned on www.drugbank.ca).

Terbogrel, an agent having two pharmacodynamic actions, namely inhibition of thromboxane A2 synthase and antagonism of the thromboxane A2 receptor. The antithrombotic effect of terbogrel was dose-dependent and was associated with enhanced prostacyclin production. The drug was studied for the treatment of peripheral vascular disorders, pulmonary hypertension, and thrombosis. Terbogrel participated in phase II clinical trial to investigate its safety and efficacy in patients with primary pulmonary hypertension, however, this study was discontinued due to terbogrel’s induction of leg pain.