Vintoperol (also known as RGH 2981), a peripheral circulation-enhancing compound that was developed as a moderate serotonin and calcium channel antagonist. Vintoperol was studied for the treatment of arterial occlusive disease and peripheral vascular disorders. It was shown that this compound interfered with platelet aggregation both in vitro and in vivo and possessed potent antithrombotic effects in thrombosis models in which platelet activation was mainly involved. Vintoperol participated in phase II clinical trials in Japan for the treatment patients with arterial occlusive disorders, peripheral vascular disorders, and thrombosis. However, because of its toxic side effects, vintoperol was discontinued from the clinical practice.

Tiliquinol in combination with tilbroquinol and tiliquinol lauryl sulfate are the active components of Intetrix, a medicine prescribed to adults who suffer from amoebiasis. Amoebiasis refers to an infection caused by the parasite Entamoeba histolytica. Intetrix is marketed as a capsule and is administered orally.

Tigloidine is a tropane alkaloid and a naturally occurring analog of atropine, found in small quantities in Duboisia myoporoides. Tigloidine has been found to be beneficial in the treatment of Parkinsonism, Huntington’s Chorea and spastic paraplegia. Tigloidine may provide relief in parkinsonian patients by increasing the gamma-efferent activity and reducing alpha motoneurone activity. In preclinical models, Tigloidine failed to reverse sedation and ptosis in rats induced by reserpine and tetrabenazine. In mice, amphetamine response was not significantly affected by Tigloidine or atropine. However, in the cat and dog, it was markedly facilitated by Tigloidine but not by atropine.

Timofibrate is a thiazolidine derivative patented by Italchemi S.p.A.-Istituto Chimico Farmaceutico as antiatherosclerosis, anticholesteremic, and liver protecting agent.

MK-0873 is a novel selective phosphodiesterase-4 inhibitor, which has been in development for the treatment of chronic obstructive pulmonary disease (COPD). In preclinical studies, intravenous administration of MK-0873 produced potent, dose-dependent inhibition of antigen-induced bronchoconstriction in sensitized guinea pigs. MK-0873 protected against both the early- and late-phase bronchoconstrictor response to antigen challenge in Ascaris-sensitive sheep. In healthy volunteers, MK-0873 has been shown to be safe and generally well tolerated in single oral doses up to 6 mg and in multiple oral doses up to 4 mg for 28 days. The most commonly reported adverse events were similar to those reported in other studies with drugs in its class: i.e. headaches and gastrointestinal complaints.

Tinofedrine is a dithienylamine derivative patented by Deutsche Gold- und Silber-Scheideanstalt vorm. Roessler for improvement of cerebral and peripheral blood flow. In anesthetized dogs, Tinofedrine causes a remarkable increase of cardiac output by positive inotropic and chronotropic stimulation of the heart and simultaneous reduction of peripheral vascular resistance. In comparison with typical beta-agonists Tinofedrine at isotropically equieffective doses, has a much weaker effect on the heart rate. In coronary circulation, Tinofedrine causes vasodilation so that in a therapeutic dose range increased workload is equalized by sufficient myocardial supply.

Mabuprofen (aminoprofen, AU 7801) is an amide prodrug of ibuprofen, a non-steroidal anti-inflammatory drug with analgesic, antipyretic and anti-inflammatory properties. It is used for topical treatment of various painful processes that occur with inflammation (tendonitis, synovitis, torticollis, lumbago, contusions, sprains, etc).

Flindokalner (BMS 204352; MaxiPost™) is a neuroprotective agent with potential in the treatment of stroke developed by Bristol-Myers Squibb. Flindokalner is a potent and effective opener of two important subtypes of neuronal potassium channels, the calcium-activated, big-conductance potassium channels (K(Ca) channels) and voltage-dependent, non-inactivating potassium channels known as KCNQ channels. Flindokalner significantly reduced cortical infarct volume in a animal models of stroke. Flindokalner failed to show superior efficacy in acute stroke patients compared to placebo in a Phase III study.

Tiapirinol is a thiazine derivative patented by Tanabe Seiyaku Co., Ltd. as a low toxic compound useful to prevent hypohepatia. In acute toxicity tests on mice, the toxicity of Tiapirinol is lower than that of pyridoxal phosphate and other vitamin B6 derivative. Tiapirinol showed vitamin B6 activity approximately equivalent to that of pyridoxal phosphate or pyridoxine for the growth of vitamin B6 deficient rats and also for the convulsions caused by antivitamin B6 agents.