Sulofenur is an orally active diarylsulfonylurea derivative patented by American pharmaceutical company Eli Lilly and Co. as an antitumor agent. In preclinical studies, Sulofenur exhibits significant activity against advanced colon adenocarcinoma xenografts intrinsically resistant to virtually all standard chemotherapeutic agents and also had very significant activity against several pediatric tumors grown as xenografts. Clinically, Sulofenur was disappointing, and although some responses were reported in phase I trials this was not confirmed for ovarian cancer in the phase II setting. Toxicity in man was due mainly to methemoglobinemia and anemia, which limited the concentrations of drug that could be achieved to levels well below those shown to elicit a therapeutic response in the xenograft models.

Tiacrilast (also known as Ro 22-3747) is a quinazolinyl-propenoic acid derivative patented by Hoffmann-La Roche, Inc. as an antihypertensive useful for anaphylaxis management. Tiacrilast acts as a potent mast cell degranulation inhibitor in vitro and inhibits of antigen-induced histamine release from passively sensitized rat peritoneal cells in vitro. In preclinical models, Tiacrilast shows marked activity in rat passive cutaneous anaphylaxis assay, rat anaphylactic bronchospasm assay. In vitro studies have confirmed that the mechanism of action of Tiacrilast in the in vivo models is through allergic mediator release inhibition. Clinical evaluations of Tiacrilast in patients with ragweed sensitive allergic asthma, Tiacrilast demonstrates significant inhibitory activity relative to placebo in reducing acute airway responses to inhaled pollen extracts

Thyropropic Acid (also known as Triopron) is a hydrocinnamic acid derivative and naturally occurring thyroid analog with antigoitrogenic and anticholesteremic activity. Thyropropic Acid acts as potent antagonist of thyroid hormone receptors and may be useful in the therapy of resistance to thyroid hormone and corticosteroid-induced skin atrophy. In preclinical models, Thyropropic Acid reduced serum cholesterol 27% and liver incorporation of acetate into cholesterol 37% but did not affect liver cholesterol levels.

Thiamiprine is a cytotoxic purine derivative patented by Wellcome Foundation Ltd. as an immunosuppressive and antineoplastic agent. In preclinical models, Thiamiprine is active against a variety of transplantable rodent tumors and in the rat adjuvant arthritis model.

Capuride is a a central nervous systemactive urea derivative of valnoctic acid patented by pharmaceutical company Abbott Laboratories as sedative therapeutic compound with a duration of hypnotic effect similar to that of the short‐acting barbiturates.

Rose Bengal lactone is a polyhalogenated derivative of Fluorescein. Rose Bengal lactone is a dye compound described to produce cell membrane damage. Rose Bengal lactone and other Fluorescein derivatives are also described to modulate the function of ATP-sensitive K+ channels. Rose bengal lactone reacts readily with bases so treatment with triethylamine immediately yields the Rose Bengal salt.

Khelloside is a component of Ammi visnaga L. fruits extract, a medicine which is used in Egypt as remedy for the treatment of kidney stones. Khelloside itself exhibits a wide variety of biological activities including anti-anginal, antiatherosclerotic, lipid altering, antipyretic and spasmolytic. It was clinically tested for asthma, angina pectoris and skin disease, however its develoment seems to be discontinued.

Quazodine (also known as MJ-1988) is a quinazoline derivative patented by Fujisawa Pharmaceutical Co. as a muscle relaxant. In cats anesthetized with sodium pentobarbitone. Quazodine decreased diastolic blood pressure, peripheral vascular resistance, systolic ejection time and left ventricular end-diastolic pressure in cats. Heart rate, cardiac effort, output, and external work and left ventricular dP/dt were markedly increased. In the intact dog, as well as in the heart-lung preparation., the stimulant action on the force of myocardial contraction was accompanied by increases in coronary blood flow, pulmonary vasodilation, and bronchodilation. Administration of larger doses caused depression of cardiac function and initiated cardiac arrhythmias.