Targeting tumor angiogenesis to treat cancer has been the focus of intense research in recent decades. The resulting increase in our knowledge of cancer biology has lead to the development of several new classes of investigational agents that inhibit the angiogenic process. While many clinical trials on antiangiogenic compounds have had disappointing results, the recent approval of the first effective drug targeting tumor vessels has revived interest in further drug development for angiogenesis inhibitors. Of the plethora of new patents for antiangiogenic compounds, only a few describe compounds that will become effective and non-toxic therapies for patients with cancer. This review examines representative patents related to cancer angiogenesis in the context of our current knowledge of the biological processes leading to tumor vascularization and explores the future of multi-targeted therapy and nanoformulation technology in the field of angiogenic therapy.