申请人:D-Pharm LTD.
公开号:US20010007865A1
公开(公告)日:2001-07-12
The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.
本发明涉及一种药学上可接受的原药,它是药理活性化合物和细胞内转运佐剂的共价结合物,其特征是存在对细胞内酶活性裂解敏感的共价键。该原药可用于治疗哺乳动物与超常细胞内酶活性有关的病症或疾病的技术中,在给患有这种病症或疾病的人用药时,键会因这种活性而断裂,药理活性化合物会在具有这种超常细胞内酶活性的细胞内被选择性激活。