Cyheptropine is a tropine ester of dibenzo[a,d]cycloheptadiene-5-carboxylic acid, developed as an antiarrhythmic agent.

Xanoxic acid was developed as a bronchodilator that has never been marketed. Information about the current use of this agent is not available.

Darexaban (YM150) is a direct inhibitor of coagulation factor Xa (FXa), discovered by Astellas Pharmaceuticals. FXa is a crucial serine protease in the coagulation cascade, responsible for the cleavage of prothrombin to its active form thrombin, which then converts soluble fibrinogen to insoluble fibrin, activates platelets and causes a formation of a blood clot. Darexaban inhibits factor Xa with a Ki value of 31 nM and shows anticoagulant activity in human plasma. In venous and A-V shunt thrombosis models in rats, darexaban strongly suppressed thrombus formation without affecting bleeding time. Darexaban was investigated in a number of clinical trials for prevention of venous thromboembolism in patients undergoing surgery, prevention of ischaemic events in acute coronary syndrome, prophylaxis of stroke in atrial fibrillation. In 2011 Astellas announced the discontinuation of darexaban because of high competition on anti-FXa drugs market.

Afacifenacin is being developed by Sumitomo Dainippon Pharma (formerly Dainippon Sumitomo Pharma) and Sunovion Pharmaceuticals as an orally administered therapy for overactive bladder and nocturia. Afacifenacin is a new antimuscarinic that possesses the dual pharmacological actions of non-selective muscarinic receptor antagonist and inhibition of the bladder afferent pathway through sodium-channel blockade. Afacifenacin is in Phase II clinical tirals for the treatment of Nocturia by Nippon Shinyaku.

Lomevactone is a psychostimulant and antidepressant drug

Lilopristone (ZK 98.734) has a high affinity for progesterone receptors. The progesterone antagonistic effects of ZK 98.734 could be a result of the decrease in progesterone synthesis by the corpus luteum and/or placenta in addition to the interference with the progesterone binding to its cellular receptors in the target organ. ZK 98.734 has potential for fertility regulation. It is a very potent abortifacient in the common marmosets. Lilopristone could significantly suppress the proliferation of ectopic stromal cells in a time- and dose-dependent manner in vitro. The action mechanisms may be associated with the suppression of expression of NF-kappaB P65 mRNA and NF-kappaB P65.

Litomeglovir is an antiviral agent.

Becanthone is an antischistosomal agent possesses the ability to inhibit tumors.

Mespirenone (ZK 94679, 15β,16β-methylene-spironolactone) is a steroid aldosterone antagonist. In addition, it is a quite specific inhibitor of adrenocortical mineralocorticoid synthesis. In rodents mespirenone effectively prevents aldosterone-induced hypertension. It exerts natriuretic efficacy. Although it reached phase II clinical trials, it was discontinued in 1989.

Vindeburnol, a derivative of the plant alkaloid vincamine that that bears neuroprotective properties. Animal model for Alzheimer's disease has shown that vindeburnol reduced neuroinflammation and amyloid burden. In addition, the treatment with this drug can be of benefit in multiple sclerosis patients.