The present invention pertains to the field of medical technology, and particularly relates to a heterocyclic substituted pyrimidine compound represented by General Formula (I) and its pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description, the present invention also relates to a preparation method of the compound, a pharmaceutical composition containing the compound, and a use of the compound and the pharmaceutical composition in preparation of a medicine for enhancing a cGMP signal transduction function or a medicine for treating or preventing sexual dysfunction and diseases with lower urinary tract symptoms.本発明は医療技術の分野に属し、特に一般式(I)によって表される複素環置換ピリミジン化合物及びその薬学的に許容可能な塩に関する:【化1】(式中、R1、R2、R3、R4及びR5は本明細書に規定されるとおりである)。本発明はまた、上記化合物の調製方法、該化合物を含有する医薬組成物、並びにcGMPシグナル伝達機能を増進する薬剤又は性機能不全及び下部尿路症状を伴う疾患を治療若しくは予防する薬剤の調製における該化合物及び該医薬組成物の使用に関する。