Sipoglitazar (TAK 654) was a novel, azolealkanoic acid derivative that possesses selective activity for the peroxisome proliferator-activated receptors (PPAR) PPARγ, PPARα, and PPARδ. Sipoglitazar was developed to improve peripheral insulin sensitivity, normalize circulating lipid profiles, and reduce body weight in patients with metabolic syndrome and type 2 diabetes mellitus (T2DM). Sipoglitazar was being developed by Takeda for the treatment of diabetes mellitus, however in September 2006, development was discontinued.

Tideglusib (NP031112, NP-12, Nypta, Noscira SA, Madrid, Spain), a drug, which belongs to the thiadiazolidinone family, is a GSK-3β inhibitor. Tideglusib was in phase II clinical trials for the treatment of Alzheimer disease (AD) and progressive supranuclear palsy. Participants showed no benefit on either of the primary outcome measures or exploratory endpoints and further development in the drug was halted for these two disease. However, Tideglusib is on phase II clinical trial to determine whether drug is safe and efficacious in the treatment of adolescents and adults with congenital and juvenile-onset Myotonic Dystrophy.

AGE-RELATED MACULAR DEGENERATION (AMD), PROLIFERATIVE DIABETIC RETINOPATHY (PDR) AND DIABETIC MACULAR EDEMA (DME) are collectively characterized by VEGF mediated retinal leakage, angiogenesis, and an underlying inflammatory process. TargeGen's TG100801 is designed to inhibit a select group of kinases involved in those three processes. Currently approved drug based therapy for macular degeneration requires repeated injection into the eye. TG100801 is the first topically applied, VEGFR)/Src kinase inhibitor to advance into the clinic for the treatment of Age-related macular degeneration, diabetic retinopathy. The formation of new blood vessels (angiogenesis), blood vessel leakage, and inflammation contribute to the progression of the eye disease, which is the leading cause of irreversible, severe loss of vision in people 55 years of age and older in the developed world. In cell based assays, following topical instillation, TG100572, the active drug produced by conversion of TG100801 as it penetrates the eye, was shown to induce apoptosis in proliferating endothelial cells responsible for neovasculariztion and to inhibit inflammatory-mediated processes as measured by endotoxin-induced nitric oxide release in vitro.

Benzindopyrine belongs to anticholinergic agents. It was studied as an antipsychotic drug.

FENYRIPOL is a skeletal muscle relaxant.

MSDC 0602, a first-in-class oral, once-daily, insulin sensitiser that acts by stimulating mitochondrial proteins, is being developed by Metabolic Solutions and Cirius Therapeutics for treatment Type 2 diabetes mellitus and Non-alcoholic steatohepatitis. MSDC-0602 prevented and reversed liver fibrosis and suppressed expression of markers of stellate cell activation in livers of mice fed a diet rich in trans-fatty acids, fructose, and cholesterol. Moreover, mice with liver-specific deletion of MPC2 were protected from development of NASH on this diet. MSDC-0602 directly reduced hepatic stellate cell activation in vitro, and MSDC-0602 treatment or hepatocyte MPC2 deletion also limited stellate cell activation indirectly by affecting secretion of exosomes from hepatocytes. Cirius Therapeutics plans the phase III trial for Type 2 diabetes mellitus and Non-alcoholic steatohepatitis in September 2019

Mebenoside is an anti-inflammatory agent.

Halonamine was studied as an antiparkinsonian agent.

Tropapride is dopamine D2 receptor antagonist, which potential high antipsychotic activity has been clearly shown in biochemical and pharmacological tests.

Masilukast (ZD 3523) is an antagonist of leukotriene D4 (LTD4). It opposes LTD4-induced bronchoconstriction. It was being developed for the treatment of asthma.