The present invention is directed to novel compounds having thrombolytic, free radical scavenging and thrombus-targeting activities; and the processes for preparation and uses thereof. In the present invention, a thrombolytic peptide, a free radical scavenger and a thrombus-targeting/antithrombotic peptide are joined together via a linking arm to give a three-component conjugate, thereby providing a compound of the present invention which has simultaneously the functions of overcoming the blood-brain barrier, dissolving thrombus, scavenging free radicals, and targeting thrombus/inhibiting the formation of thrombus. The present invention is further directed to pharmaceutical compositions comprising the compounds of the invention, wherein the compounds are in the form of nanoparticles. The compounds of the present invention show a better free radical scavenging activity, and superior thrombolytic and thrombus-targeting/antithrombotic activities. The compounds of the present invention also show an excellent anti-stroke activity, such that they can be used in making drugs for treating cerebral thrombosis.本發明涉及一種同時具有溶血栓、清除自由基和血栓靶向/抗血栓三種功能的新穎化合物及其製備方法和用途。本發明以連接臂將溶血栓肽、自由基清除劑和血栓靶向/抗血栓肽組合在一起形成三元綴合物,得到集跨血腦屏障、溶血栓、清除自由基、血栓靶向/抗血栓等作用於一體的所述化合物。本發明還涉及含有所述化合物的藥物組合物,其中所述化合物形成奈米球結構。本發明化合物具有較高的清除NO自由基活性、優異的溶血栓活性和血栓靶向/抗血栓活性。本發明化合物還具有優異的抗缺血性中風活性,可製備成治療腦梗塞的臨床藥物。