Aditoprim is a long-acting, selective, reversible inhibitor of dihydrofolate reductase with application as a broad-spectrum antibacterial agent in animals. Aditoprim is low toxic and not mutagenic.Many gram-positive and gram-negative bacteria are highly susceptible or susceptible to Aditoprim, especially Salmonella and Streptococcus, while H. parasuis and Klebsiella were moderately susceptible to Aditoprim. Phase II clinical study of Aditoprim on therapeutic effect on swine streptococcosis has demonstrated that Aditoprim is as active as compound sulfadiazine, which provides reasonable theoretical foundation for the clinical application of Aditoprim.

Racemetirosine is an orally active inhibitor of the enzyme tyrosine 3-monooxygenase, and consequently of the synthesis of catecholamine. At dosages of 600 to 3500mg daily, it is effective in controlling the hypertensive episodes and symptoms of catecholamine excess in phaeochromocytoma during preparation for surgery. Oral Racemetirosine is well absorbed and absorption appears constant in each individual over a wide dosage range. The drug is largely excreted via the kidneys, but extrarenal elimination has not been studied. Case reports on the clinical use of Racemetirosine in phaeochromocytoma indicate that the drug controls hypertension and symptoms of catecholamine excess in most patients during preparation for surgical removal of a tumor. In some cases, the addition of Racemetirosine to phenoxybenzamine plus propranolol has resulted in adequate control of symptoms previously unresponsive to the adrenergic blocking regimen. Drowsiness and sedation have been the most frequently reported side effects of Racemetirosine treatment.

Falnidamol is an epidermal growth factor receptor inhibitor, developed by Boehringer Ingelheim. Falnidamol demonstrated anticancer activity in vitro. The phase I trial was discontinued due to a dose-limiting increase of liver enzymes, low bioavailability of the drug and the detection of a pharmacologically inactive metabolite.

Iniparib (BSI-201 or 4-iodo-3-nitrosobenzamide) inactivated poly(ADP-ribose) polymerase by zinc ejection from the first zinc finger of this nuclear protein. Iniparib, either alone or in combination with chemotherapy, had significant antitumor activity in preclinical studies in vitro and in vivo. In June 2013, Sanofi dropped the drug after it failed in a phase III trial of patients with squamous non–small-cell lung cancer and a phase II trial in platinum-resistant ovarian cancer.

Daxalipram is a selective inhibitor of phosphodiesterase (PDE) 4B.This compound is an R-isomer of mesopram and is known as (R)-mesopram. Mesopram is known to trigger ovulation and exhibits efficacy against experimental autoimmune encephalomyelitis and murine colitis in vivo. Moreover, is used in compositions for the treatment or prevention of respiratory inflammation.

Etamicastat (BIA 5453) is a peripherally selective chromanyl imidazolethione-based inhibitor of dopamine beta-hydroxylase, the enzyme that catalyzes the conversion of dopamine to noradrenaline in the sympathetic nerves. Prolonged downregulation of sympathetic drive with etamicastat results in a sustained decrease in the systolic blood pressure and the diastolic blood pressure. Etamicastat was being studied by BIAL for the oral treatment of hypertension and congestive heart failure. Etamicastat development has been discontinued.

Bardoxolone methyl, the C-28 methyl ester of 2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid (CDDO) known as CDDO-Me or RTA 402, is one of the derivatives of synthetic triterpenoids. Bardoxolone methyl directly blocks IKKbeta activity and thereby the NF-kappaB pathway by interacting with Cys-179 in the IKKbeta activation loop. Binding of bardoxolone methyl to Kelch-like erythroid cell-derived protein with CNC homology-associated protein 1 (Keap1) disrupts its critical cysteine residues, leading to the release of the nuclear factor erythroid 2-related factor 2 (Nrf2), which hinders its ubiquitination and finally leads to its stabilization and nuclear translocation. In the nucleus, Nrf2 activates the transcription of phase 2 response genes, leading to a coordinated antioxidant and anti-inflammatory response. In addition, it acts as an antagonist of the peroxisome proliferator-activated receptor gamma. Through Keap1/Nrf2 and nuclear factor-κB pathways, this agent can modulate the activities of a number of important proteins that regulate inflammation, redox balance, cell proliferation and programmed cell death. This agent is generally well tolerated, but it may increase adverse cardiovascular events. Presently, it is being further tested for the treatment of patients with chronic kidney disease, cancer, and pulmonary arterial hypertension.

Boehringer Ingelheim developed samixogrel as thromboxane A2 receptor antagonists. This drug participated in clinical trials for the treatment patients with diabetic complications, thrombosis, and unstable angina pectoris. However, all these studies were discontinued.

Brivanib is a pyrrolotriazine-based compound and an inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2) with potential antineoplastic activity. It specifically targets and strongly binds to human VEGFR-2, a tyrosine kinase receptor and pro-angiogenic growth factor expressed almost exclusively on vascular endothelial cells. Blockade of VEGFR-2 by this agent may lead to an inhibition of VEGF-stimulated endothelial cell migration and proliferation, thereby inhibiting tumor angiogenesis. Brivanib has a moderate potency compared to VEGFR-2 against VEGFR-1 and FGFR-1 as well. Brivanib is suggested to be efficient in treatment of hepatocellular carcinoma (HCC). As first-line and as second-line therapy brivanib demonstrated promising antitumor activity and a manageable safety profile in patients with advanced, unresectable HCC in phase II clinical trials. On 3 march 2011, orphan designation was granted by the European Commission to Bristol-Myers Squibb for brivanib alaninate for the treatment of hepatocellular carcinoma.[

Midaxifylline, a potent and selective xanthine adenosine A1 receptor antagonist, was investigated for the treatment of Alzheimer's disease, cardiovascular disorders, kidney disorders, and major depressive disorder. However, all studies were discontinued.