LASINAVIR, a hydroxyethylene derivative, is highly specific human immunodeficiency virus (HIV) protease inhibitor with an IC50 of 1 nM. Its clinical development was discontinued.

Mipitroban (previously known as UP 11677), a thromboxane A2 receptor antagonist that was investigated to treat thrombosis. However, further studies were apparently discontinued.

Hydroxypethidine, an opioid analgesic is an opioid receptor agonist. Hydroxypethidine is under the control of narcotic drugs according to US Single Convention 1961.

Lefradafiban, an orally active prodrug of fradafiban, is a novel glycoprotein (IIb/IIIa) inhibitor for the treatment of unstable angina. The pharmacokinetic and pharmacodynamic properties of lefradafiban were assessed in 130 healthy male volunteers who received a single dose of 10, 50, 75, 100, or 150 mg or multiple doses of 25, 50, 60, 75, 90, or 100 mg three times daily for one week. After both single and multiple doses, receptor occupancy and plasma lefradafiban levels correlated with platelet aggregation. Lefradafiban had been in phase II clinical trials by Boehringer Ingelheim for the treatment of thrombosis. However, it has been terminated.

Fosfosal (2-phosphonoxybenzoic acid) is a O-phosphorylated derivative of salicylic acid used in analgesic and anti-inflammatory therapy. Fosfosal showed analgesic effect in the acetic acid-induced writhing and in the hot plate tests in mice, and showed antiinflammatory effect in the xylene induced mice ears swelling and in acetic acid induced increased vascular permeability tests in mice. Both the effects had no significant differences between fosfosal and aspirin, but the former had less stomach irritation.

ISOFEZOLAC is a non-steroid anti-inflammatory drug, prostaglandin synthetase inhibitor. It is indicated for use in various forms of rheumatoid arthritis and osteoarthritis.

Acetiamine (syn. thianeurone or diacetamine) is a thiamine derivative which is rarely used in pharmaceuticals. It is lipid-soluble. It has been studied for the treatment of rheumatic diseases.

Duometacin is indomethacin derivative. It was developed as analgesic and anti-inflammatory agent.

Brofezil (ICI 54594) is an ibuprofen derivative with anti-inflammatory and analgesic activity.