The invention relates to novel prodrugs or conjugates of the general formula (Ia), in which La, n, R and D have the definitions given in the description and which have a structural motif reduced to an asparagine derivative as cleavage site for tumour-associated proteases such as legumain, in which cytotoxic drugs, for example kinesin spindle protein inhibitors, are released by legumain cleavage, and to the use of these prodrugs or conjugates for treatment and/or prevention of diseases, and to the use of these prodrugs or conjugates for production of medicaments for treatment and/or prevention of diseases, especially of hyperproliferative and/or angiogenic disorders, for example cancers. Reduction of the legumain-cleavable substrate peptide sequence to an asparagine derivative as structural motif, as a result of slowed legumain cleavage, achieves an increase in stability in the lysosomes of healthy organs while simultaneously maintaining the high anti-tumour effect.本發明係關於通式(Ia)之新穎前藥或偶聯物，,其中La、n、R及D具有說明書中所給出之定義，且該等新穎前藥或偶聯物具有還原成天門冬醯胺衍生物以作為用於腫瘤相關蛋白酶、例如天門冬醯胺內肽酶(legumain)之裂解位點之結構基序，其中藉由天門冬醯胺內肽酶裂解來釋放細胞毒性藥劑、例如紡錘體驅動蛋白抑制劑；且係關於該等前藥或偶聯物用於治療及/或預防疾病之用途；及該等前藥或偶聯物用以產生用於治療及/或預防疾病(尤其是過度增殖性及/或血管生成病症，例如癌症)之藥劑之用途。因緩慢的天門冬醯胺內肽酶裂解而將天門冬醯胺內肽酶可裂解受質肽序列還原成作為結構基序之天門冬醯胺衍生物達成在健康器官之溶酶體中穩定性的增加且同時維持高抗腫瘤效應。
