Glycogen synthase kinase 3 (GSK-3) is a constitutively active, ubiquitous expressed ser/thr kinase that is involved in a large number of signaling pathways. GSK-3 is a key target of a remarkably large number of cellular processes and diseases such as diabetes type II, cancer, immune disorder, neurodegenerative pathologies among others diseases and surely in regenerative medicine. During the last decades the scientific community has been working to understand the role of GSK-3 with the aim in mind of design efficient and selectivity GSK-3 inhibitors (GSK3i). However so far clinical and preclinical GSK3i have been both sub-optimal regarding potency, poor GSK-3 selectivity over other CNS targets and closely related kinases, low CNS exposure, and chronic toxicity. Research into GSK inhibitors relay primarily on identification of the new use of the know GSK3i and the development of them in order to improve selectivity and toxicity.This review covers patent literature on GSK3i and their application published between 2016 and 2019.Thanks to the past, present, and future research, in the next few years we will see progress in the treatment of some diseases with GSK3i, for instance in regenerative medicine immunotherapy applications among others.