The use of natural compounds from biodiversity, as well as ethnobotanical knowledge, for the development of new drugs is the gate leading to support the conservation of natural resources in developing countries. Recent technological advances and the development of new methods are revolutionizing the screening of natural products and offer a unique opportunity to replace natural products as major source of drug leads. Over the past decades, the Brazilian government established a legislation aiming to grant patent protection in all technological fields. The Convention on Biological Diversity, an international agreement that recognizes the sovereign rights of States over their natural resources, and the Brazilian legislation (Decreto n degree 2186-12/01) set for legislative, administrative or policy measures regarding the share of research and product development benefits could be the key for progress in issues related to rational employment of the Brazilian biodiversity and economy, but are far from being effective. Based on literature review, this article provides a brief description of the Brazilian legislation policy regarding intellectual property and biodiversity access, places natural drug discovery in context, analyzes patent cases and highlights critical key issues responsible for the drawback of the whole process that has a direct impact on industrial and research development, nature protection and benefit share with our society.