The invention provides non-hydrolyzable nucleoside polyphosphate derivatives, e.g., 2MeS-adenosine-&bgr;,γ-CH2-5′-O-(1-boranotriphosphate), 2MeS-adenosine-&bgr;,γ-CCl2-5′-O-(1-boranotriphosphate), 2-MeS-adenosine-5′-dichloro methylene-diphosphate, 2-MeS-adenosine-5′-difluoromethylene-diphosphate and 2MeS-adenosine-5′-O-(1-boranodiphosphate), as well as pharmaceutical compositions thereof. These compounds are useful for prevention or treatment of diseases or disorders modulated by P2Y-receptors such as type 2 diabetes, and for pain control.