Pirnabine is the synthetic dibenzopyran drug. It was developed as anti-glaucoma drug.

Pentisomicin (Sch 21420) is semisynthetic aminoglycosides with marked antibacterial activity. Like many new aminoglycosides prepared by chemical modification or mutational biosynthesis, Pentisomicin was designed either to enhance potency of the parent compound and/or resist enzymatic inactivation. The activity of Pentisomicin was comparable to gentamicin, sisomicin, netilmicin, and tobramycin but greater than amikacin or kanamycin against S. aureus and most genera of Enterobacteriaceae.

Tarenflurbil (Flurizan or R-flurbiprofen) is the single enantiomer of the racemate NSAID flurbiprofen. Tarenflurbil is a first in class, selective amyloid-beta42 (A42) lowering agent (SALA), which acts by modulating the activity of gamma-secretase, an enzyme that converts amyloid precursor protein to amyloid-beta. The reduction of A42 may prevent the development of the amyloid plaques thought to be a key pathological process associated with Alzheimer’s disease. For several years, research and trials for the drug were conducted by Myriad Genetics, to investigate its potential as a treatment for Alzheimer's disease. In a brief statement issued June 30, Myriad Genetics reports that tarenflurbil (Flurizan) failed to have a significant effect in a phase 3 trial of patients with mild Alzheimer's disease (AD). The failure of Flurizan™ is generally attributed to its insufficient pharmacodynamics, i.e., inadequate ability to penetrate the brain and engage its target protein at doses sufficient to yield an effect. Two additional Phase 3 trials were terminated and further development of Flurizan™ was discontinued. Separate clinical development of Flurizan™ for prostate cancer has also been discontinued following negative Phase 2 results. Tarenflurbil activates c-Jun N terminal kinase, increases AP-1 binding to DNA, and downregulates cyclin D1 expression, resulting in the arrest of tumour cells in the G1 phase of the cell cycle and apoptosis. This agent also affects the expression of nuclear factor kappa B, a rapid response transcription factor that stimulates the immune response to tumour cells. Tarenflurbil does not inhibit the enzyme cyclooxygenase. The Fraunhofer Institute for Molecular Biology and Applied Ecology is currently developing tarenflurbil for the treatment of relapsing, remitting multiple sclerosis.

Clazosentan is an endothelin receptor antagonist, developed by the Swiss pharmaceutical company Actelion, and licensed to its spin-off, Idorsia. The drug was designed to inhibit endothelin-mediated cerebral vasospasm and associated delayed ischaemic neurological deficit. The drug has been investigated in a phase III clinical trials in patients with aneurysmal subarachnoid hemorrhage. Clazosentan at 5 mg/h had no significant effect on mortality and vasospasm-related morbidity or functional outcome. Clinical investigation of a higher dose of the drug is underway.

Tigestol is an Estrene derivative patented by Organon Laboratories Ltd. as an anabolic, androgenic, and progestative agent.

Pirtenidine is the antimicrobial agent. Pirtenidine was found to be highly efficacious against oral plaque-forming microorganisms. Adherence of Candida spp. to buccal epithelial cells in vitro was significantly reduced after both short- and long-term periods of yeast exposure to sub-inhibitory concentrations of pirtenidine. The drug was shown to cause extensive leakage of cytoplasmic contents from the Candida albicans cells which was correlated with morphological and ultrastructural changes in the yeast. Pirtenidine affects the lipids and sterol composition of C. albicans.

Pytamine is a nitrosamine derivative patented by Hercules Powder Co. as antioxidants, stabilizers, rubber additives, insecticides, fungicides, bactericides, and pharmaceutical intermediates. In preclinical trials Pytamine shows potent psychotropic effects associated modulation of GABAA receptors.

Efipladib is an inhibitor of cytosolic phospholipase A2 alpha both in vitro and in vivo. It is able to relieve inflammatory pain in animal model. Additionally, efipladib exerts antitumor potential. Efipladib was in clinical trials for the treatment of asthma and arthritis however its development has been discontinued.

Sufosfamide is an oxazaphosphorine derivative patented by Asta-Werke A.-G as immunosuppressives agent. Sufosfamide is a mixed-function oxazaphosphorine differing from ifosfamide in that the extracyclic 2-chloroethyl function has been replaced by a mesyl-oxyethyl group. It is characterized by an extraordinary intensifi¬cation of the immunosuppressive component of action compared to the carcinotoxic component. Sufosfamide activates of a specific immune tolerance in models of humoral end cell-bound antibodies.