Leteprinim is the synthetic purine. It has both anti-excitotoxic neuroprotective properties and enhances the regenerative response of surviving neurons within the central nervous system. Moreover, the experiments in vitro and in vivo reveal that leteprinim can be administered after an excitotoxic event and still produce neuroprotection. This is clearly crucial for any drug designed to treat stroke or any acute central nervous system injury. Therefore, leteprinim has the pharmacological properties required by a drug intended to treat acute stroke as well as a spinal injury. It may be useful in reducing brain injury; it possesses clinical relevance for the treatment of hypoxic-ischemic encephalopathy in the newborn. Leteprinim has the therapeutic potential for use in clinical trials in the treatment of neuronal deterioration in depression.

Liarozole is an imidazole-containing compound that inhibits the cytochrome P-450-dependent metabolism of all-trans-retinoic acid (RA). Liarozole, a retinoic acid (RA) metabolism-blocking agent (RAMBA) in clinical development, has been granted orphan drug designation for congenital ichthyosis by the European Commission and the U.S. Food and Drug Administration. Later, based on the mixed results from a phase II/III trial of liarozole for the treatment of ichthyosis, Barrier decided to discontinue the development of liarozole. Liarozole displays antitumor activity against androgen-dependent and independent rat prostate carcinomas.A large phase III international study was completed comparing liarozole 300 mg twice daily with cyproterone acetate (CPA) 100 mg twice daily in a total of 321 patients with metastatic prostate cancer in relapse after first-line endocrine therapy. The results indicate that liarozole might be a possible treatment option for prostate cancer (PCA) following failure of first-line endocrine therapy.

Leptacline is the respiratory analeptic.

Niceverine is a spasmolytic, antihypertensive agent.

Mivotilate is an orally active hepatoprotective agent for the treatment of liver cirrhosis and hepatitis-B infection. Mivotilate was shown to exert multiple effects on the hepatic cytochrome P450 system, particularly to inhibit CYP2E1 expression and to up-regulate the CYP1A1 expression. The low oral bioavailability of Mivotilate in rats could be primarily attributed to poor absorption and considerable hepatic and gastrointestinal first-pass effects. The thermal reversible microemulsion system of YH439 greatly enhances the bioavailability of YH439 after oral administration. Mivotilate prevents mutagenesis caused by agents such as benzopyrene and reduces skin tumours induced by these agents.

Sulfonamide derivative Disulfamide was developed as diuretic agent.

Disogluside (Trillin) is an active ingredient isolated from Dioscorea nipponica Makino. Trillin reduces liver chronic inflammation and fibrosis in carbon tetrachloride (CCl4) induced liver injury in mice. Trillin exhibited protective effect on LPS-induced ALI by the regulations of related inflammatory events via the activations of Nrf2, HO-1 and NF-κB pathway. Trillin has being shown to exert protective effects against hyperlipidemia and oxidative stress. Trillin induced multinucleation in HL-60, NB4 and K562 cells, indicating it could induce mitotic arrest in these leukemia cells.

PR-104 is a phosphate ester dinitrobenzamide mustard pre-prodrug that is rapidly hydrolyzed systemically to PR-104A, a bioreductive prodrug. PR-104A is in turn activated via reduction by NADPH:cytochrome P450 oxidoreductase and other one-electron reductases in hypoxic cells, and by aldo-keto reductase 1C3 (AKR1C3) independently of oxygen, to the corresponding hydroxylamine (PR-104H) and amine (PR-104M) metabolites. Subsequently, these reactive nitrogen mustards crosslink DNA and cause cytotoxicity in cells. PR-104 is known to have preclinical anti-tumor activity in human tumor xenograft models as mono-therapy and in combination with radiotherapy and chemotherapy. Thrombocytopenia, and to a lesser extent neutropenia, was the dose-limiting toxicity of weekly PR-104. Combination of PR-104 with docetaxel or gemcitabine caused dose-limiting and severe myelotoxicity in patients with advanced solid tumors. PR-104 had been in phase II clinical trial for the treatment of acute myeloid leukemia.

Ditiomustine is a nitrosourea compound with alkylating activity. Ditiomustine crosslinks DNA, resulting in the inhibition of DNA replication and eventually cellular proliferation. It was developed as antineoplastic agent.

Rifametane (SPA-S-565) is a semisynthetic derivative of rifamycin (a natural antibiotic produced by Amycolatopsis rifamycinica). It was being evaluated for treatment of bacterial infections. A phase I study showed that administration of rifametane is safe with minor, reversible adverse events such as mild headache, metallic taste and slightly elevated temperature for 3 to 4 hours. Rifametane has anti-tuberculosis activity and was suggested to be a good candidate for phase II clinical trials.