Since platelet aggregation is implicated in many pathological situations such as myocardial infarction, stroke, unstable angina and coronary artery disease, potent and safe antiplatelet agents would be useful for treating and preventing these diseases. Exposure of glycoprotein (GP)IIb/IIIa is the final common pathway leading to platelet activation and aggregate formation. Thus, the development of agents acting on this complex is an active area of research. Indeed, three GPIIb/IIIa antagonists are currently marketed but can only be intravenously administrated. Therefore, efforts are made to discover orally-active agents of this class, in order to use them for treatment of chronic disease or prevention of cardiovascular events. Although some clinical evaluation of orally-active compounds gave disappointing and discouraging results, research is still conducted to find compounds characterised by a better binding profile. This review describes 16 patents on new GPIIb/IIIa antagonists and more than 40 molecules characterised by strong activity against GPIIb/IIIa.