BI-2536, an inhibitor of Polo-like kinase 1 (Plk-1) was being investigated by Boehringer Ingelheim as a possible treatment for cancer. BI-2536 inhibits Plk1 enzyme activity at low nanomolar concentrations. The compound potently causes a mitotic arrest and induces apoptosis in human cancer cell lines of diverse tissue origin and oncogenome signature. BI-2536 inhibits growth of human tumor xenografts in nude mice and induces regression of large tumors with well-tolerated intravenous dose regimens. In treated tumors, cells arrest in prometaphase, accumulate phosphohistone H3, and contain aberrant mitotic spindles. This mitotic arrest is followed by a surge in apoptosis, detectable by immunohistochemistry and noninvasive optical and magnetic resonance imaging. For addressing the therapeutic potential of Plk1 inhibition, BI-2536 has progressed into clinical studies in patients with locally advanced or metastatic cancers. It underwent phase II clinical studies for the treatment of breast cancer; non-small cell lung cancer; pancreatic cancer; prostate cancer; small cell lung cancer, but these studies were discontinued later.

Quadazocine is a substituted hexahydro-2,6-methano-3-benzazocine patented by Sterling Drug Inc. as analgesics and narcotic antagonist. Quadazocine is a potent antagonist of μ opioid receptor, less potent antagonist of κ and δ opioid receptors. In monkeys for whom responding was reinforced by food delivery, quadazocine blocks the rate-decreasing effects of the µ-agonists alfentanil and fentanyl with greater potency than it blocked the rate-decreasing effects of the κ-agonists U69,593

PF-232798 is a potent oral CCR5 antagonist with a primary and selectivity/safety pharmacology profile similar to maraviroc (MVC). PF-232798 shows increased binding affinity and improved oral absorption compared to maraviroc. In addition, it retains activity against a laboratory generated maraviroc-resistant HIV-1 strain, indicating an alternative drug resistance profile. PF-232798 binds to the same pocket as MVC within the transmembrane region of CCR5, but shows additional interactions at the ECL2 hinge region. PF-232798 is well tolerated in normal volunteers. PF-232798 had been in a phase-II clinical trial for the treatment of HIV infections. However, this development was discontinued.

HKI-357 is a potent, dual irreversible inhibitor of ErbB2 (HER2) and EGFR. HKI-357 suppresses ligand-induced EGFR autophosphorylation and cell proliferation in NCI-H1975 cells containing L858R and T790M mutations.

LAUROGUADINE is a bactericide, topical antiseptic.

Trimeperidine (promedol) is the earliest and mostly studied opioid analgesic. Trimeperidine stimulates opioid receptors in the central nervous system. Compared with morphine, it has a weaker and shorter analgesic effect, less affects the respiratory, vomiting and vagal centers, does not cause smooth muscle spasm (except for the myometrium), and has a moderate antispasmodic and hypnotic effect. It is used to treat severe pain syndrome, acute left ventricular failure, pulmonary edema, cardiogenic shock, preparation for surgery, childbirth, high fever, post-transfusion complications, poisoning with atropine, barbiturates, barium, gasoline, boric acid, strong acids, carbon monoxide, turpentine, formalin, formalin. It has several side effects. Administration of this substance is associated with the development of life-threatening conditions accompanied by the suppression of respiration center. Analgesic trimeperidine (promedol) was included into the health care kits by various Ministries of the Russian Federation at different times.

Ulimorelin (TZP101) is a small molecule, intravenously administered, ghrelin receptor agonist that is being developed by Lyric Pharmaceuticals. Ulimorelin stimulates intestinal motility, but also reduces blood pressure in rodents and humans and dilates blood vessels. It has been proposed as a treatment for intestinal motility disorders. Ulimorelin has progressed to phase III human clinical trials for the treatment of postoperative ileus.

INCB9471 is a non-competitive, potent and selective CCR5 small-molecule antagonist patented by pharmaceutical company Incyte Corporation for treatment of human immunodeficiency virus infection. INCB9471 potently inhibited macrophage inflammatory protein-1beta-induced monocyte migration and infection of peripheral blood mononuclear cells by a panel of R5-HIV-1 strains. INCB9471 was shown to be safe and highly efficacious in reducing HIV viral load in phase I and II human clinical trials

Aspaminol (1,1 diphenyl-3-piperidinobutanol hydrochloride) is a nonspecific smooth muscle relaxant. It inhibits calcium uptake. The relaxation of smooth muscle induced by aspaminol may be due to a combining of aspaminol with calcium ions at the binding sites on the surface of smooth muscle, thus decreasing the supply of calcium ions to the contractile element.