Bentamapimod (AS602801) a newly developed, orally-active, ATP competitive inhibitor of JNK, which is in phase IIa clinical trials for the treatment of endometriosis. Bentamapimod showed selective cytotoxic activity against serum-cultured cancer cells and cancer stem cells in vitro. It blocks T-cell proliferation and induces apoptosis. Bentamapimod was discovered by Merck Serono. Then PregLem (a member of the Richter Group) acquired worldwide rights in 2010.

AEE-788 is an orally available anticancer agent that was being developed by Novartis. AEE-788 is a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. At the enzyme level, AEE-788 inhibited EGFR and VEGF receptor tyrosine kinases in the nm range (IC(50)s: EGFR 2 nm, ErbB2 6 nm, KDR 77 nm, and Flt-1 59 nm). In cells, growth factor-induced EGFR and ErbB2 phosphorylation was also efficiently inhibited (IC(50)s: 11 and 220 nm, respectively). AEE-788 demonstrated antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines (including EGFRvIII-dependent lines) and inhibited the proliferation of epidermal growth factor- and VEGF-stimulated human umbilical vein endothelial cells. These properties, combined with a favorable pharmacokinetic profile, were associated with a potent antitumor activity in a number of animal models of cancer, including tumors that overexpress EGFR and or ErbB2. Oral administration of AEE-788 to tumor-bearing mice resulted in high and persistent compound levels in tumor tissue. Moreover, AEE-788 efficiently inhibited growth factor-induced EGFR and ErbB2 phosphorylation in tumors for >72 h, a phenomenon correlating with the antitumor efficacy of intermittent treatment schedules. AEE-788 has potential as an anticancer agent targeting deregulated tumor cell proliferation as well as angiogenic parameters. AEE-788 had been in phase Ⅱ clinical trials by Novartis for the treatment of glioblastoma multiforme. However, this research has been discontinued.

Mecinarone is a benzofuranic chalcone. It exerts vasodilating activity. Mecinarone has also antibradykinin, antiserotonin and antiaggregation properties. Mecinarone induces an increase of melanin content of pigmented skin and mucosae.

Tiametonium (also known as Thiamethon) is a lanthionamine derivative with ganglionic blocking activity. In preclinical models, Thiamethon prevents nicotine-induced convulsions in mice.

Denbufylline is a selective xanthine derivative that inhibits PDE IV and has bronchodilatory properties. Shown to exhibit negative inotropic effects by acting on verapamil-sensitive sites of Ca2+ channels in guinea pig ventricle papillary muscle independently of its PDE inhibitory activity. Denbufylline, a selective type 4 phosphodiesterase (PDE-4) inhibitor, is a potent activator of the hypothalamo-pituitary-adrenal (HPA) axis when given orally or intraperitoneally (i.p.) to adult male rats. Denbufylline was being developed as an agent for the therapy of dementia.

Cresotamide of o-cresotinic acid with analgesic, antipyretic and anti-inflammatory action.

Crotoniazide is a derivative of isonicotinic hydrazide. Crotoniazide demonstrated antituberculous activity in vitro and in vivo.

Cloximate is a non-steroidal anti-inflammatory drug, developed in the Dutch company Philips-Duphar B.V. Research Laboratories in the 1970s. Cloximate acts by inhibition of PGE2 biosynthesis. In preclinical experiments, cloximate showed good inhibitory activities in local exudative tests, in the proliferative and functional aspects of experimental inflammation, as well as in the bradykinin-evoked bronchoconstriction test. Cloximate showed almost no harmful effects on the gastrointestinal mucosa and no influence upon the emptying rate of the stomach. Cloximate was evaluated in double-blind clinical trials, where different formulations were compared with naproxen. Gastrointestinal blood loss increased more in the naproxen group than in the group treated with non-enteric coated cloximate.

Cortisuzol is a glucocorticoid corticosteroid, discovered by the French company Roussel Uclaf, and claimed to have anti-inflammatory activity in a number of clinical case reports.

Clorotepine (aka octoclothepin or octoclothepine) is an antipsychotic from the tricyclic group derived from perathiepin. It was originally developed in 1965 and marketed in the Czech Republic by Spofa in or around 1971 for the treatment of schizophrenic psychosis. Clorotepine has a high affinity for the dopamine (D1, D2, D3, D4), receptors the serotonin 5-HT (2A, 2B, 2C, 6, 7) receptors, the alpha-adrenergic receptors (1A, 1B, 1D), and the histamine H1 receptors. In most instances, it acts as an antagonist (or inverse agonist). Clorotepine will also block the reuptake of norepinephrine by inhibiting the norepinephrine transporter.