Piperamide is substituted piperazine with a tertiary amine group. It was used as an anthelmintic agent. Initially, it was investigated because of its effectiveness against Trypanosoma. Piperamide distorts choroid plexus epithelial ultrastructure by engendering hydropic vacuoles.

Clocinizine is an antihistamine derivative of diphenylmethylpiperazine. Clocinizine is a competitive and reversible H1 receptor antagonist. The drug is marketed in Spain under tradename Senioral in combination with phenylpropanolamine for temporary relief of nasal congestion in colds, rhinitis, and sinusitis.

Retaspimycin (IPI-504) was previously under development by manufacturer Infinity Pharmaceuticals in conjunction with MedImmune, a part of AstraZeneca. Retaspimycin is a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis. Orphan drug designation was assigned to the compound by the FDA for the treatment of gastrointestinal stromal cancer (GIST). Infinity Pharmaceuticals has discontinued the development of retaspimycin (IPI-504) an inhibitor of the HSP-90) complex, for the treatment of cancer due to lack of efficacy in 1913.

Radezolid (RX-1741) is a novel oxazolidinone antibiotic agent and is the first biaryloxazolidinone in clinical development. It is being developed by Rib-X Pharmaceuticals, Inc. for the treatment of serious multi-drug–resistant infections. Radezolid has completed two phase-II clinical trialsfor the treatment of community-acquired pneumonia; uncomplicated skin and skin structure infections. The mechanism of action for this drug seems to be an inhibition of 50S ribosomal subunit.

Barusiban, a long-acting oxytocin antagonist, has been studied to stop preterm labor in pregnant women at late gestational age. The experiments failed to demonstrate the effectiveness and were discontinued. However, barusiban participates in phase II clinical trials for female infertility.

Ecopladib) is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α, type IVA phospholipase). Inhibitors of cPLA2alpha are predicted to be efficacious in treating asthma as well as the signs and symptoms of osteoarthritis, rheumatoid arthritis, and pain. It displayed oral efficacy in the rat carrageenan air pouch and rat carrageenan-induced paw edema models.

LY-518674 is a highly potent and selective proliferator-activated receptor (PPAR)-alpha agonist. LY-518674 produced a much greater increase in serum high-density lipoprotein-cholesterol (HDL-c) than the known fibrate drugs. The increase in HDL-c was associated with de novo synthesis of apolipoprotein A-1. It was being developed for the treatment of dyslipidemias with atherogenic potential.

Mapinastine (E 4716) is a selective antagonist of histamine H1 receptors. In animal models, mapinastine exerts antiallergic and anti-asthmatic properties. It demonstrated a lack of central effects. Mapinastine development has been discontinued.

Meglitinide (HB 699) is an antidiabetic compound. Meglitinide is a short-acting insulin secretagogue that targets one of the main defects that characterizes type 2 diabetes: the progressive loss of early phase prandial insulin secretion. It acts in a glucose-dependent manner to close adenosine triphosphate (ATP)-dependent potassium channels on the β-cell membrane, depolarize the β-cell, resulting in the opening of calcium channels, increased calcium influx and insulin secretion.

Lexofenac is an ibufenac derivative. It was developed as anti-inflammatory and analgesic agent.