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1.发明申请
公开(公告)号：WO0195945A3
公开(公告)日：2002-08-15
申请号：PCT/US0118903
申请日：2001-06-11
Applicant: CORIXA CORP
Inventor： NIEDER MATTHEW H , DUBOIS VINCENT , GANGWAR SANJEEV , LOBL THOMAS J , PICKFORD LESLEY B , TROUET ANDRE , YARRANTON GEOFFREY T
CPC classification number: A61K47/65
Abstract: The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the enzyme Thimet oligopeptidase, or TOP. Also disclosed are methods of designing prodrugs by utilizing TOP-cleavage sequences within the conjugate and methods of treating patients with prodrugs of the invention.
Abstract translation: 本发明的前药是治疗剂的修饰形式，并且包含治疗剂，寡肽，稳定基团和任选的连接基团。 前药可通过Thimet寡肽酶或TOP切割。 还公开了通过利用缀合物内的TOP-切割序列设计前药的方法和用本发明的前药治疗患者的方法。
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公开(公告)号：WO0200263A3
公开(公告)日：2002-08-15
申请号：PCT/US0140925
申请日：2001-06-11
Applicant: CORIXA CORP , BEBBINGTON CHRISTOPHER R , DUBOIS VINCENT , GANGWAR SANJEEV , LOBL THOMAS J , NIEDER MATTHEW H , PICKFORD LESLEY B , TROUET ANDRE , YARRANTON GEOFFREY T
Inventor： BEBBINGTON CHRISTOPHER R , DUBOIS VINCENT , GANGWAR SANJEEV , LOBL THOMAS J , NIEDER MATTHEW H , PICKFORD LESLEY B , TROUET ANDRE , YARRANTON GEOFFREY T
IPC: A61K31/704 , A61K38/00 , A61K47/48 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07K5/02 , C07K5/08 , C07K5/083 , C07K5/087 , A61K49/00
CPC classification number: B82Y5/00 , A61K38/00 , A61K47/65 , A61K47/67 , C07K5/0202 , C07K5/0808 , C07K5/081 , C07K5/0812
Abstract: The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide of three amino acids, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by a trouase enzyme such as Thimet oligopeptidase. Also disclosed are methods of making and using the prodrug compounds.
Abstract translation: 本发明的前药是治疗剂的修饰形式，并且包含治疗剂，三种氨基酸的寡肽，稳定基团和任选的接头基团。 该前体药物可通过诸如Thimet寡肽酶之类的休眠酶切割。 还公开了制备和使用前药化合物的方法。
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