申请人:CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
公开号:US20200353090A1
公开(公告)日:2020-11-12
The invention relates to new prodrugs of active molecules. These prodrugs allow, in particular, the subcutaneous or intramuscular administration of active molecules of which the subcutaneous or intramuscular administration is problematic or impossible, in particular because of the toxicity at the injection site. The prodrugs according to the invention comprise an active ingredient, covalently linked with a polymer chain, preferably a hydrophilic and/or thermosensitive polymer chain. The invention relates, in particular, to polymeric prodrugs comprising a polymer chain formed at least in part by acrylamide monomer or one of its derivatives, the polymer comprising a proximal part and a terminal part; a first pharmaceutically active molecule covalently coupled to the proximal part of the polymer; possibly a second pharmaceutically active molecule covalently coupled to the terminal part of the polymer.
该发明涉及新型活性分子的前药。这些前药允许特别是将活性分子皮下或肌肉内注射,而这些活性分子的皮下或肌肉内注射由于在注射部位的毒性而具有问题或不可能,特别是由于在注射部位的毒性。根据本发明的前药包括一种活性成分,与一根聚合物链共价连接,优选为一种亲水性和/或热敏感性聚合物链。该发明特别涉及包括由丙烯酰胺单体或其衍生物之一至少部分形成的聚合物链的聚合物前药,该聚合物包括一个近端部分和一个末端部分;第一种药用活性分子共价结合到聚合物的近端部分;可能第二种药用活性分子共价结合到聚合物的末端部分。