Pargeverine (also known as a propinox) is an antispasmodic drug that was studied for the treatment of disorders of the gastrointestinal tract, the uterus, and the gallbladder. Pargeverine showed a dual mechanism of action, it binds to muscarinic and calcium receptors that can be related to its antispasmodic activity. The clinical trial has shown that pargeverine was an effective drug in the treatment of moderate to severe colic pain of biliary origin. In addition, its efficacy and tolerability were determined in patients with moderate-to-severe acute intestinal colic pain. As a result, no differences in blood pressure or heart rate were found among treatments. The incidence of mouth dryness was significantly more frequent with the 20 mg and 30 mg doses of propinox than with the placebo or the 10 mg dose. Information about the current development of this drug is not available.

Lipoprotein lipase (LPL) is a rate-limiting enzyme that hydrolyzes circulating triglyceride-rich lipoproteins such as very low-density lipoproteins and chylomicrons. Otsuka Pharmaceutical Factory, Inc. synthesized the LPL activator NO-1886 (ibrolipim, [4-(4-bromo-2-cyano-phenylcarbamoyl)-benzyl]-phosphonic acid diethyl ester, CAS 133208-93-2). NO-1886 increased LPL mRNA and LPL activity in adipose tissue, myocardium and skeletal muscle, resulting in an elevation of postheparin plasma LPL activity and LPL mass. It was discovered, that this agent has a potentially beneficial for the treatment of hypertriglyceridemia, hypo-HDL cholesterolemia, and protection from atherosclerosis. In addition, this agent may be used in the treatment of obesity and obesity-linked health problems in postmenopausal women.

Pargolol (also Kö 1400) is a beta-adrenergic receptor blocking agent that was developed as an antiarrhythmic agent. However, information about the further development of this drug is not available.

Lirimilast is representative of a new structural class of PDE4 inhibitors, the benzofurans. It it is highly selective type 4 cyclic nucleotide phosphodiesterase inhibitor. Lirimilast inhibited human inflammatory cell functions that previously were reported to be sensitive to PDE4 inhibitors. It showed some selectivity for neutrophil and eosinophil functions over those of monocytes and T lymphocytes when compared to cilomilast and other reference PDE4 inhibitors. Lirimilast exhibited a broad profile of anti-inflammatory activity in animal models of COPD and asthma. Lirimilast produced emesis in primates. 1 week of treatment with the selective PDE4 inhibitor lirimilast does not affect FEV1 and sputum cell numbers in patients with asthma or chronic obstructive pulmonary disease (COPD). However, such treatment does seem to reduce levels of albumin and eosinophil cationic protein in sputum samples obtained from patients with COPD.

Iotriside is triiodoisophthalic acid derivative patented by Schering A.-G. as nonionic contrast media.

Iotetric Acid is triiodobenzoic acid derivative with potential application as neutrophil imaging in diagnosis of cystic fibrosis.

Daniquidone, also known as Batracylin, is a water-insoluble heterocyclic amide with potential antineoplastic activity. Daniquidone inhibits topoisomerases I and II, thereby inhibiting DNA replication and repair, and RNA and protein synthesis. Batracylin advanced as an anticancer agent to Phase I clinical trials where dose limiting hemorrhagic cystitis (bladder inflammation and bleeding) was observed.

N-(4-Chloro-3-((3-Methyl-2-Butenyl)Oxy)Phenyl)-2-Methyl-3-Furancarbothioamide (also known as UC-781) is a thiocarboxanilide non-nucleoside reverse transcriptase inhibitor patented by Uniroyal Chemical Company, Inc. for prevention of HIV transmission. UC-781 is a potent inhibitor of reverse transcriptase-dependent pyrophosphorolysis, and purportedly restores the chain-terminating activity of zidovudine (AZT) against AZT-resistant virus. In clinical trials single and 7-day topical rectal exposure of UC-781 was safe with no significant adverse events, no detected UC-781 plasma drug levels, no significant mucosal changes, and high participant acceptability. Ex vivo biopsy infections demonstrated marked suppression of HIV infectibility, identifying a potential early biomarker of efficacy.

Azaprocin is an opioid analgesic that has never been marketed.

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.