Novartis AG has identified diaminocyclopentylpyridine derivatives acting as proprotein convertase subtilisin/kexin-type 9 (PCSK9) inhibitors and thus reported to be useful for the treatment of hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, sitosterolemia, vascular inflammation, atherosclerosis, peripheral vascular and coronary heart disease, among others.