The present invention relates to compounds showing pharmacological activity towards the subunit α2δ#of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels. More particularly, the invention relates to alkylaminoproline derivatives having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain and/or as neuroprotective agents.