Embusartan or BAY106734 (6-n-butyl-4-methoxycarbonyl-2-oxo-1[(2'-(1H-tetrazol-5-yl) -3-fluorobiphenyl-4-yl)methyl] 1,2-dihydropyridine) is an angiotensin II receptors antagonist. Embusartan has beneficial effects in different animal hypertension models. Embusartan appears as a potent and specific new inhibitor of angiotensin II-induced growth-related events in vascular smooth muscle cells. It was being developed for the treatment of hypertension.

Agouron (Pfizer) was developing AG-24322 (AG-024322), a small-molecule cyclin-dependent kinase (CDK) inhibitor, for the treatment of cancer. AG-024322 is a potent inhibitor of CDK1, CDK2, and CDK4 that produces cell-cycle arrest and antitumor activity in preclinical models. AG-24322 is a potent ATP-competitive inhibitor of CDK1, CDK2, and CDK4 with Ki values in the 2–3 nM range and selectivity over other non-CDKs. This compound has been shown to inhibit Rb phosphorylation in cells, elicit cell-cycle arrest, and have antiproliferative activity in multiple human tumor cell lines (IC50 values from 30 to 200 nM). AG-24322 was reported to be undergoing phase I trials for cancer in the US, however the development was discontinued.

KOS-1584 is a second-generation epothilone D analog designed to have less toxicity, more potency, and higher solubility compared with epothilone D. It has a broad spectrum of potent antiproliferative activity on tumor cells. Currently, KOS-1584 is under clinical evaluation.

Elsamitrucin is a heterocyclic antineoplastic antibiotic isolated from the bacterium Actinomycete strain J907-21. Elsamitrucin intercalates into DNA at guanine-cytosine (G-C)-rich sequences and inhibits topoisomerase I and II, resulting in single-strand breaks and inhibition of DNA replication. It demonstrated a broad spectrum of in vitro cytotoxicity against tumor cell lines. According to the results of Phase II trials elsamitrucin is not an active drug in patients with metastatic breast cancer, colorectal cancer, non-small cell lung cancer or ovarian cancer, however, it showed modest activity in patients with relapsed or refractory non-Hodgkin's lymphoma.

Dexivacaine is a local anesthetic drug that has minimal and non-significant side effects.

Ramifenazone is pyrazolone derivative with analgesic, antipyretic, and anti-inflammatory activity. In preclinical studies, Ramifenazone shows potent inhibition of prostaglandin production, carrageenan edema, and yeast fever.

Gemopatrilat is a vasopeptidase inhibitor, that was found to inhibit plasma and renal angiotensin converting enzyme (ACE), as well as renal neutral endopeptidase (NEP). Gemopatrilat is rapidly absorbed, and causes inhibition of circulating and renal ACE and renal NEP after a single oral dose for up to 48 hours in rats. Potentially, this is because the free sulfhydryl group of gemopatrilat forms reversible disulfide linkages with plasma and tissue proteins and is thus eliminated from the body at a very slow rate. Similar metabolism of the compound was found in rat, dog, and human. Gemopatrilat was evaluated for its potential in treatment of antihypertensive activity in hypertension (independent of age, renin and salt status or ethnic origin), as well as its potential as a new therapeutic modality for the treatment of congestive heart failure. The drug was never marketed. A phase II study for treatment of hypertension and heart failure has been discontinued.

Pibaxizine is diphenylmethyl piperazine derivatives. It is a histamine H1 receptor antagonist. Animal experiments have shown that it has spasmolytic properties for smooth muscle, particularly in the bronchi, as well as anticholinergic and anti-serotonin activities. It can be concluded that Pibaxizine has a strong protective effect against bronchospasm caused by inhalation of a histamine aerosol. Protection against methacholine-induced bronchospasm was less marked. Pibaxizine had been in phase II clinical trial for the treatment of chronic obstructive pulmonary disease. However, this development was discontinued.

Sopromidine is a neuroprotective drug. Sopromidine is a potent and stereoselective isomer of the achiral H2-agonist impromidine. The chiral impromidine isomer sopromidine is of special interest as the (R)-configurated compound behaves as gpH2R agonist, whereas the (S)-configurated counterpart is devoid of agonist activity. Both Sopromidine and its S enantiomer acted as antagonists of histamine at H3-autoreceptors with similar potencies (Ki = 5.6 X 10(-8) M and 4.5 X 10(-8) M), whereas Sopromidine acted as an H2-receptor agonist and the S-enantiomer as an H2-receptor antagonist.

Spirendolol (LI 32-468) is a β adrenergic receptor antagonist. It possesses high affinity for metabolic beta-adrenoreceptors which mediate glycogenolysis that is 100 times more potent than propranolol. In human volunteer studies, a single dose of 2 mg LI 32-468 elicited virtually no cardiac beta-adrenoreceptor blockade (predominantly beta-1), whereas a maximal metabolic beta-adrenoreceptor blocking effect (beta-2) was demonstrated. Spirendolol was a potent inhibitor of ocular beta-adrenoceptors, with a 9-12 fold selectivity over inhibition of beta-adrenoceptors in cardiac tissue. When applied topically, Spirendolol was more effective than timolol in decreasing intraocular pressure in normal albino rabbits.