Timelotem is a benzodiazepine derivative patented by Kali-Chemie Pharma G.m.b.H. as an anesthetic agent. In preclinical models, Timelotem shows atypical antipsychotic activity. Timelotem antagonizes DL-2-amino-5-phosphonovaleric acid (AP-5)-induced sniffing and the body turns in rats. Further, Timelotem antagonized amphetamine-induced stereotyped behavior in rats but was found less active than haloperidol in this test.

Tifluadom is an opioid benzodiazepine with potent analgesic activity. Studies using antagonists for κ-, δ-, and μ-opiate receptors in guinea pig myenteric plexus-longitudinal muscle preparation and mouse and rabbit vasa deferentia showed that Tifluadom is an opioid analgesic with a preference for opiate κ-receptors. In rat brain homogenates, tifluadom displaced kappa-antagonist naloxone from its binding sites with an IC50 of 12nM but had no effect on flunitrazepam binding. Tifluadom produced a dose-related diuresis in normally hydrated rats and the diuretic effect was antagonized by naloxone and blocked by morphine administration.

Rocastine (AHR-11325) is a potent, nonsedating antihistamine with a rapid onset of action. This H1-antagonist effectively protected guinea pigs challenged with a lethal dose of histamine. It has also been mentioned in patents as a candidate to treat eye conditions and cough/cold mixtures (in which the lack of sedative effects from a non-sedating antihistamine would be especially useful in children, because daytime sedation is especially undesirable in this group). However, information on current use is not available and other second-generation, non-sedative antihistamines are available.

Myrophine is an opiate analog and long-acting prodrug for morphine with a slow onset of effects. It is weaker than morphine as an analgesic but longer-lasting in effects and was thought to have a more local anesthetic effect than morphine, though with a somewhat greater tendency to cause histamine reactions like itching and rash. In addiction studies conducted in human subjects in the 1950s, myrophine did not substitute for morphine in withdrawal, did not produce notable morphine-like effects, and did not produce addiction or dependence regardless of dose or how it was administered.

Oxindanac, a non-steroidal anti-inflammatory drug, and is a weak cyclooxygenase inhibitor possessed antipyretic activity. This drug is used as a veterinary inflammatory drug. In addition, oxindanac was studied in phase III clinical trials for the treatment of rheumatic disorders. However, this study was discontinued.

Oxindanac, a non-steroidal anti-inflammatory drug, and is a weak cyclooxygenase inhibitor possessed antipyretic activity. This drug is used as a veterinary inflammatory drug. In addition, oxindanac was studied in phase III clinical trials for the treatment of rheumatic disorders. However, this study was discontinued.

Tomivosertib (eFT-508) is a dual inhibitor of MAP kinase-interacting kinases (MNK1 and MNK2) thereby controlling translation. It has potent in vivo antitumor activity in models of diffuse large cell B-cell lymphoma and solid tumors. Tomivosertib acts on multiple points in the cancer immunity cycle simultaneously, underscoring its therapeutic potential as both a monotherapy and in combination with existing checkpoint inhibitor treatments. Preclinical studies suggest combining tomivosertib with a checkpoint inhibitor can overcome mechanisms of resistance to checkpoint inhibitors, resulting in enhanced sensitivity to checkpoint inhibitors and a higher response rate. In addition, preclinical data demonstrate that tomivosertib as a single agent promotes antitumor immunity that persists after stopping drug treatment. Tomivosertib is currently being evaluated in Phase 2 clinical trials in solid tumors and lymphoma. Additionally, tomivosertib may be a new therapeutic for neuropathic pain.

AZD9164 was invented by AstraZeneca as a muscarinic M(3) receptor antagonist for evaluation of the potential as a treatment for chronic obstructive pulmonary disease. However, in 2010 studies were discontinued.

Olmidine (also known as dl-mandelamidine) is an antihypertensive drug that has never been marketed. Information about the current use of this drug is not available.