Oxaprotiline (also known as hydroxymaprotiline) is a norepinephrine reuptake inhibitor and blocked the histamine H1 receptor. Oxaprotiline was studied in the treatment of hospitalized depressive patients. However, this drug has never been marketed.

Proxorphan is a N-substituted 6-oxamorphinane patented by American pharmaceutical company Bristol-Myers Co. as opioid analgesic and antitussive drug. Proxorphan acts as a κ-opioid receptor partial agonist and to a lesser extent as a μ-opioid receptor partial agonist.

Ilmofosine (1-hexadecylthio; 2-methoxyethyl-racglycero-3-phosphocholine) is a synthetic 1-S-thioether alkyl lysophospholipid derivative with potential antineoplastic activity. In extensive preclinical evaluation against tumor cell lines and in the human tumor colony-forming assay, Ilmofosine was cytotoxic against both leukemias and solid tumors. Ilmofosine was effective against many tumor types, including ovary, non-small cell lung, kidney, and melanoma. Ilmofosine exhibited competitive inhibition of protein kinase C activity with respect to phosphatidyl-serine and inhibited the enzyme activated by diolein.

Fluthiacet-methyl, an isourazole herbicide is applied to actively growing weeds in soybeans to control annual broadleaf weeds. Fluthiacet-methyl induced the accumulation of protoporphyrin IX in cotyledons of cotton and inhibited chlorophyll biosynthesis in cotyledons of velvetleaf and cotton.

Furodazole, a benzimidazole derivative was studied as an anthelmintic drug. Information about the current use of this compound is not available.

Timobesone is a topical corticosteroid and thiol ester derivative with anti-inflammatory activity.

Josamycin propionate, a tasteless josamycin derivative suitable for the preparation of pediatric oral suspension. After oral administration Josamycin propionate underwent metabolic transformation to Josamycin, semi-synthetic 16-membered ring macrolide, that acts via protein synthesis inhibition.

Enisoprost is a prostaglandin E1 analog. Enisoprost exerts immunosuppressive activity and gastric antisecretory effect. Enisoprost was being studied for the treatment of peptic ulcer and transplant rejection. Enisoprost development has been discontinued.

Cebranopadol is a novel analgesic nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonist. Cebranopadol, by its combination of agonism at NOP and opioid receptors, affords highly potent and efficacious analgesia in various pain models with a favorable side effect profile. Cebranopadol displays analgesic, antiallodynic and antihyperalgesic properties in several rat models of acute nociceptive, inflammatory, cancer and neuropathic pain. Unlike morphine, cebranopadol did not disrupt motor coordination and respiration at doses within and exceeding the analgesic dose range possessing a broader therapeutic window than classical opioids. It is currently in clinical development for the treatment of severe chronic nociceptive and neuropathic pain.