Quinuclium Bromide Anhydrous is quinuclidinium derivative with potential analgesic activity. In preclinical studies, Quinuclium possessed significant chronic antihypertensive activity in mecamylamine- and renal-hypertensive dogs. Quinuclium was approximately 4 times more potent than guanethidine in the former model and 3 times as potent in the latter. Quinuclium reduced orthostatic blood pressure responses in unanesthetized rabbits but was approximately 10 times less potent than guanethidine. Quinuclium did not affect cardiac output, heart rate or stroke volume in anesthetized open-chest dogs and moderately increased mean blood pressure and total peripheral resistance. It produced diuresis and saluresis in anesthetized dogs but did not influence water or electrolyte urinary excretion in conscious rats. Quinuclium was more effective than guanethidine in blocking adrenergic neurons and depleting heart norepinephrine levels in experimental animals.

CEP-32496 (RXDX 105) is an orally administered, small molecule, VEGFRsparing, RET, BRAF, EGFR tyrosine kinase inhibitor, for the treatment of solid tumours, including malignant melanoma and colorectal cancer. CEP-32496 was originally discovered by Ambit Biosciences (now Daiichi Sankyo) and Cephalon (now owned by Teva) as part of a research programme to develop orally administered kinase inhibitors. The worldwide rights to the compound were licensed to Teva by Ambit, following the acquisition of Cephalon by Teva. Teva, in March 2015, entered into an asset purchase agreement with Ignyta, pursuant to which, Ignyta has acquired worldwide rights and assets of four oncology development programmes, including CEP-32496. Following the acquisition of the compound by Ignyta, CEP 32496 has been renamed to RXDX 105. Phase I/Ib development of RXDX 105 for the treatment of advanced solid tumours is underway in the US.

Amedalin (UK-3540) is a selective norepinephrine reuptake inhibitor developed in the 1970s. Amedalin was a potential antidepressant compound. It has no significant effect on reuptake of serotonin and dopamine and no antihistamine or anticholinergic properties. This drug was never marketed.

Benzethidine an opioid analgesic that was forbidden for use.

Betaprodine is an opioid analgesic under international control according to the UN Single Convention 1961. It has been used in obstetrics, as pre-operative medication, for minor surgical procedures.

Boehringer Ingelheim is developing BI-671800, an orally administered treatment for seasonal allergic rhinitis and asthma. BI-671800 is an antagonist of the PGD2 receptor, CRTH2. PGD2 stimulates bronchoconstriction and allergic airway inflammation in animal models. Inhibition of CRTH2 may reduce airway inflammatory cells, IL -4, -5, -13 production, serum IgE and airway hyper reactivity. Treatment with BI-671800 in poorly controlled asthmatic patients receiving FP was associated with a significant improvement in FEV1. BI-671800 was well tolerated at a total daily dose of 800 mg for 6 weeks.

ISAMFAZONE is a non-steroidal antiinflammatory, analgesic agent.

Panamesine (also known as EMD 57445) was studied as a sigma receptor ligand alleged to have antipsychotic effects. Panamesine reached phase II clinical trials for schizophrenia before the discontinuation of its development.

FEPRADINOL is an analgesic, antipyretic and anti-inflammatory agent. Its anti-inflammatory activity does not seem to be related to an inhibitory effect on prostaglandin biosynthesis.