Cicloprolol is a beta-adrenoceptor antagonist patented by French pharmaceutical company Synthelabo S. A. for treatment of heart disorders. Cicloprolol has a weak beta-agonistic effect at normal levels of adrenergic discharge and acts as an antagonist at high levels of discharge. In clinical trials, Cicloprolol did not affect resting heart rate and blood pressure, but it reduced significantly peak exercise heart rate and peak rate-pressure product. The effect was especially significant in patients with sinus rhythm. The drug did not induce bradycardia or arrhyth- mias. Resting and exercise ejection rate were not affected. Cicloprolol improved the quality of life and the work capacity of 40% of patients with congestive failure due to ischemic etiology. Side effects were few and similar to placebo and cicloprolol.

Adaprolol is a beta-adrenergic antagonist that is being developed as a topical agent to treat glaucoma. Adaprolol demonstrated a safer cardiovascular profile, especially in the population over 70 years old. It was in Phase II clinical trials for the treatment of glaucoma. This research has been discontinued.

Picumeterol (GR114297A) is a potent and highly selective beta2-adrenoceptor agonist with a longer duration of action than salbutamol, but shorter than salmeterol. Picumeterol is the (R)-isomer of the racemic entity GR63411B, and picumeterol has been shown to be about 40 times more potent than the (S)-isomer (GR114744A) in various in vitro pharmacological models of beta2-agonist activity. Picumeterol is of potential value in the treatment of asthma and related diseases in man following inhalation administration. In the clinical studies, the bronchodilator potencies of picumeterol and GR 63411B were similar. However, both drugs were short-acting, which is at odds with their activity in vitro. These compounds display dissociation between bronchodilator activity and protection against methacholine-induced bronchoconstriction.

2,2-DIMETHYLBUTYRIC ACID (HQK-1001) is an orally administered SCFAD (Short Chain Fatty Acid Derivative), which has shown an excellent safety profile and biologic effects on fetal hemoglobin induction and red blood cell production in the laboratory, relevant animal models, and in clinical trials carried out in healthy human subjects as well as patients with sickle cell disease and beta thalassemia. The compound has received Orphan Drug Designation in the United States and Europe for both sickle cell disease and beta thalassemia. HemaQuest Pharmaceuticals was developing HQK-1001 for the oral treatment of sickle cell anaemia and beta thalassaemia. HQK-1001 has been evaluated in phase II trials for beta thalassaemia and sickle cell anaemia.

Cefetecol is a broad-spectrum cephemcarboxylate derivative with antibacterial activity patented by British pharmaceutical company Glaxo Group Ltd.

Cefcanel is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcanel is active against the species E. coli, K. aerogenes and Proteus mirabilis; H. influenzae and M. catarrhalis has reasonable susceptibility. Cefcanel inhibits 90% of S. aureus strains at 2 µg/ml, irrespective of the presence of a β-lactamase. Cefcanel binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.

Pirazmonam is a potent anti-gram-negative monobactam that is differentiated from aztreonam by its high intrinsic activity against Ps. aeruginosa and good activity against Pseudomonas species. Pirazmonam has generally poor activity against gram-positive aerobic bacteria and anaerobic bacteria. Pirazmonam is a Trojan Horse molecule containing a b-lactam antibiotic that has been developed based on bacterial iron uptake systems. It features high structural similarity to aztreonam attached to a 3-hydroxy-4-pyridinone iron chelating group. Pirazmonam exhibited strong affinity to penicillin-binding protein 3 (PBP3) of Escherichia coli and moderate to negligible affinity to the other E. coli PBPs.

Exaprolol is a non-selective antagonist at beta-adrenoceptors exerting antiarrhythmic and local anesthetic activity. It inhibits the inotropic and chronotropic responses. Exaprolol liberates histamine from isolated mast cells and decreases the uptake of extracellular histamine. It acts on mast cells due to the direct and indirect ion exchange mechanism resulted in disproportion between histamine and granule liberation.

Piridicillin is the semi-synthetic penicillin. It has exhibited broad-spectrum activity in vitro against gram-positive cocci, except penicillin G-resistant Staphylococcus aureus, and against gram-negative bacilli. Piridicillin is reported to be more active in-vitro than piperacillin, azlocillin or ticarcillin against Ps. aeruginosa. It is unstable at alkaline pH and displays marked inoculum independence.

Levopropylcillin – is a penicillin derivative, L-enantiomer of antibiotic Propicillin. Levopropylcillin properties are similar to benzylpenicillin particularly used in streptococcal infections, not resistant to penicillinase. Levopropylcillin is acid resistant and can be used orally as the potassium salt.