The present invention relates to a kind of thiadiazoles derivatives with DPP-IV inhibitory activity shown in formula I and preparation method thereof, its pharmaceutical composition, and its treat the purposes of the disease for the what DPP-IV inhibition that is benefited, and especially treat the purposes of type-2 diabetes mellitus. Thiadiazoles derivative provided by the invention has extraordinary DPP-IV inhibitory activity. And there is extraordinary internal metaboilic level and most suitable Half-life in vivo, it is expected to become suitable DPP-IV inhibitor class drug.本發明涉及一種如式I所示的具有DPP-IV抑制活性的噻二唑衍生物及其製備方法、其藥物組合物,及其治療受益於DPP-IV抑制的疾病的用途,尤其是治療II型糖尿病的用途。本發明提供的噻二唑衍生物具有非常好的DPP-IV抑制活性。並具有非常好的體內代謝水平和非常合適的體內半衰期,有望成爲合適的DPP-IV抑制劑類藥物。