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1. 发明申请

WO1981001145A1 HYDROLYTIC ENZYME-ACTIVATIBLE PRO-DRUGS 审中-公开
标题翻译：水解酶促活性成分
公开(公告)号：WO1981001145A1
公开(公告)日：1981-04-30
申请号：PCT/US1980001290
申请日：1980-10-01
申请人： UNIVERSITY OF ILLINOIS FOUNDATION
发明人： UNIVERSITY OF ILLINOIS FOUNDATION , CARL P , KATZENELLENBOGEN J , WEBER M
IPC分类号： C07C103/52
CPC分类号： B82Y5/00 , A61K38/00 , A61K47/65 , A61K47/6899 , C07C271/28 , C07D261/04 , C07K5/0804 , C07K5/101 , C07K14/575
摘要： Antineoplastic agents are rendered tumor-specific by derivatization with a peptide specifier so as to convert the antineoplastic agent into a pharmacologically inactive pro-drug which is selectively activatible at the tumor site. The peptide specifier has an amino acid residue sequence such that it will be selectively enzymatically cleaved from the antineoplastic agent by tumor-associated fibrinolytic and/or blood-coagulating proteases, such as plasmin and plasminogen activator, so as to effect release of the antineoplastic agent in pharmacologically active form in the vicinity of the tumor. These and other similar hydrolytic enzyme-activatible pro-drugs may be formed with their specifier moiety and their drug moiety covalently linked together through an intermediate self-immolative connector moiety having a molecular structure such that enzymatic cleavage of the bond covalently linking it to the specifier moiety will initiate spontaneous cleavage of the bond covalently linking it to the drug moiety to thereby effect release of the drug in pharmacologically active form.
摘要翻译：抗肿瘤剂通过用肽说明物衍生化而变成肿瘤特异性，以将抗肿瘤剂转化成在肿瘤部位选择性活化的药理学无活性的前药。肽说明符具有氨基酸残基序列，使得其将通过肿瘤相关的纤维蛋白溶解和/或血液凝固蛋白酶（例如纤溶酶原和纤溶酶原激活物）从抗肿瘤剂中被有选择地酶切，从而释放抗肿瘤剂在肿瘤附近具有药理学活性。这些和其他类似的水解酶活化的前药可以与其说明部分形成，并且它们的药物部分通过具有分子结构的中间体自 - 残留连接体部分共价连接在一起，使得共价键连接到说明符的键的酶切割部分将引发共价连接其与药物部分的键的自发切割，从而以药理活性形式释放药物。

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