AST-1306, also known as Allitinib, is an orally active potent, selective, irreversible inhibitor of the HER family of receptor tyrosine kinases. AST-1306 inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems. AST1306 potently suppressed tumor growth in ErbB2-overexpressing adenocarcinoma xenograft and FVB-2/N(neu) transgenic breast cancer mouse models. Allitinib is in Phase I clinical trial for the treatment of advanced solid tumors. Serious adverse effects detected were: diarrhea, dehydration and hyperbilirubinemia.

Flupranone was invented as an antihypertensive agent that has never been marketed. Information about the current use of this drug is not available.

Alvocidib (also known as Flavopiridol or HMR-1275) is a flavonoid alkaloid CDK9 kinase inhibitor under clinical development for the treatment of acute myeloid leukemia, by Tolero Pharmaceuticals, Inc. As a broad spectrum CDK inhibitor, Alvocidib can inhibit cell cycle progression in either G1 or G2 and induces G1 arrest in either MCF-7 or MDA-MB-468 cells by inhibition of the CDK4 or CDK2 kinase activity. Alvocidib exhibits potent cytotoxicity against a wide variety of tumor cell lines (LNCAP, HCT116, A2780, K562, PC3, and Mia PaCa-2) with IC50 values ranging from 16 nM for LNCAP to 130 nM for K562. Administration of Alvocidib at 7.5 mg/kg for 7 days displays slight antitumor activity against P388 murine leukemia, and active against the human A2780 ovarian carcinoma implanted sc in nude mice). Alvocidib treatment at 1-2.5 mg/kg for 10 days significantly suppresses collagen-induced arthritis in mice in a dose-dependent manner, by inhibiting synovial hyperplasia and joint destruction, whereas serum concentrations of anti-collagen type II (CII) Abs and proliferative responses to CII are maintained. Tolero Pharmaceuticals Inc. announced that the FDA has granted orphan drug designation for Alvocidib, its cyclin-dependent kinase small molecule inhibitor, for the treatment of patients with acute myeloid leukemia.

Tinazoline is an imidazole derivative patented by Ciba-Geigy A.-G. as vasoconstrictors, particularly as nasal decongestants in the treatment of common cold. Tinazoline showing potent and long-acting vasoconstrictor activity on several vascular beds in dogs, guinea-pigs, cats, and rabbits. The vasoconstrictor effect has been shown in animals to be due to a stimulation of the 1-adrenoceptors and the compound does not exhibit any B-adrenoceptor agonist activity.

Nonaperone, a butyrophenone, is a neuroleptic agent. It is antipsychotic in schizophrenics at doses which do not elicit extrapyridal side effects.

Praxadine is the anti-inflammatory and analgesic agent. Praxadine inhibited the activity of purified inducible NOS (iNOS), endothelial NOS (eNOS), and neuronal NOS (nNOS) isoforms to a similar extent.

Omaciclovir (previously known as H2G), a cyclic guanosine analog that is structurally similar to acyclovir and was in clinical development for the treatment of herpesvirus infections. This drug acted against varicella-zoster virus (VZV), by the formation of high concentrations of relatively stable H2G-triphosphate, which is a potent inhibitor of the viral DNA polymerases. However, further development of this drug was discontinued.

Minalrestat was developed by Wyeth-Ayerst as an aldose reductase inhibitor. It is known, the aldose reductase inhibition might ameliorate diabetic complications through the correction of the altered microvascular reactivity by a mechanism that involves NO and membrane hyperpolarization. That is why minalrestat was studied for patients with diabetic retinopathy. However, Wyeth discontinued development of minalrestat.

Tinabinol is a thiopyranobenzopyran derivative patented by Sharps Associates as tranquilizing agent. In preclinical modes Tinabinol shows good analgesic properties and causes ataxia in dogs at low doses.

Lombazole is an antimicrobial agent of the imidazole class. It induced profound ultrastructural changes in Staphylococcus epidermidis and Candida albicans. Like other members of the imidazole series, such as clotrimazole, miconazole, and bifonazole, the compound has a broad spectrum of activity. It is active against several budding and filamentous fungi as well as gram-positive bacteria. Lombazole most probably interferes with fungal lipid synthesis by inhibiting sterol C-14 demethylation. Lipid biosynthesis is the primary site of action of lombazole in the bacterium Staphylococcus epidermidis. Lombazole was recommended against akne.