The acyl urea functionality and related analogs are increasingly used in medicinal chemistry and drug design to prove well-defined pharmacological actions and optimal physicochemical properties. This review paper aimed to summarize information related to synthesis methods of acyl urea derivatives, marketed products, and patents to explore their applications in counteracting CNS-related diseases by multiple targeting. Comprehensive data related to acyl urea and related compounds of the last 15 years is collected from various resources to provide enormous information to the readers. The content of the study uniformly includes considerable evidence linked to the common and unique synthesis techniques of acyl urea from starting materials like benzamide, isocyanates, substituted iodoglycals, 2 chloro nicotinic acid, and methyl hydrazines, as well as patents related to the same. This work describes the reactions of several substrates that can be used to manufacture various acyl urea derivatives. An understanding of patents related to acyl urea analogs with specific targets for CNS action may also help researchers working on additional synthesis of acyl urea derivatives with potential CNS action.