T-817 is a thiophenylalkyl derivative patented by Toyama Chemical Co., Ltd. as a neuroprotectant for the treatment of Alzheimer's disease. T-817MA protects neurons against amyloid-b peptide- and hydrogen peroxide-induced neurotoxicity and promoted neurite outgrowth in hippocampal slice cultures and neuronal reaggregation culture. T-817MA protected against nitric oxide-induced neurotoxicity in cultured primary neurons. In a preclinical model of Alzheimer's disease, T-817 increases decreased dopamine levels and tyrosine hydroxylase immunostaining in mice's substantia nigra (SNc) and striatum. Systemic administration of T-817 rescues tau-induced synaptic abnormalities.

Qilu Pharmaceutical has developed selatinib, an orally available dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor 2 receptor (HER-2) for the treatment of cancer. Selatinib participates in phase I of the ongoing clinical trial to evaluate its safety and tolerability, and explore the maximum tolerated dose (MTD) and dose-limiting toxicity in patients with advanced breast cancer.

NSI-189 is a novel oral drug which was developed by Neuralstem for the treatment of cognitive disorders. Now the drug is being tested in phase II of clinical trials in patients suffering from major depressive disorder. The mechanism of NSI-189 action is explained by its ability to stimulate the generation of new neurons in the hippocampus, however the exact target molecule is still unknown.

Cilengitide is a cyclized Arg-Gly-Glu (RGD)-containing pentapeptide that selectively blocks activation of the αvβ3 and αvβ5 integrins. Its precursor was first synthesized in 1995 as c(RGDfV), and later modified by the incorporation of N-methyl Val c(RGDfMetV), generating the current form of the drug. Cilengitide displays subnanomolar antagonistic activity for αvβ3 and αvβ5, and is the first integrin antagonist evaluated in clinical phase I and II trials for treatment of glioblastoma and several other tumor types. Cilengitide-induced glioma cell death and inhibition of blood vessel formation may use different molecular mechanisms, including regulation of tumor hypoxia and activation of apoptotic pathways. Cilengitide inhibits cell signaling through FAK-Src-Akt and Erk mediated pathways in endothelial and tumor cells and attenuates the effect of VEGF stimulation on growth factor signaling. Cilengitide has shown encouraging activity in patients with glioblastoma as single agent, and in association with standard RT and temozolomide.

TAK-448 is an investigational oligopeptide analog of kisspeptin and a potent agonist of the GPR54 receptor. In animals, acute TAK-448 administration stimulates luteinizing hormone (LH)/follicle-stimulating hormone release, whereas continuous subcutaneous exposure rapidly down-regulates the pituitary-gonadal axis, with rapid reduction of testosterone levels in a dose-dependent manner. TAK-448 has exhibited potent antitumor activity in rat androgen-dependent prostate cancer models. In accordance with the T reductions, TAK-448 treatment showed also more rapid reduction in plasma prostate-specific antigen(PSA) levels. TAK-448 had been in phase II clinical trials for the treatment of prostate cancer. However, this research has been discontinued.

L-MTX is a second-generation tau protein aggregation inhibitor. It acts by reducing levels of aggregated or misfolded tau proteins, which are associated with the progressive neurodegeneration. It is currently under development for the treatment of Alzheimer’s disease.

Becliconazole (or 1-CBCMI) is an antimycotic agent. Information about the nowadays application of this drug is not available

Azabyperone was developed as tranquilizer and neuroleptic and has never been marketed.

ISOMETHADONE HYDROBROMIDE, DL- is a hydrobromide salt of isomethadone, a synthetic opioid analgesic. This is a controlled substance in the US.