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1. 发明申请

US20070287672A1 Macromolecular Gsh-Activiated Glyoxylase I Inhibitors 审中-公开
标题翻译：大分子Gsh活化的乙氧基化酶I抑制剂
公开(公告)号：US20070287672A1
公开(公告)日：2007-12-13
申请号：US11587160
申请日：2005-04-20
申请人： Donald Creighton , Donald Creighton , Zhe-Bin Zheng
发明人： Donald Creighton , Donald Creighton , Zhe-Bin Zheng
IPC分类号： C07C333/00 , A61K31/10 , A61K38/06 , C07C50/22 , C08F2/06 , C12N5/00 , C07K5/08 , C07C49/543 , A61P35/00
CPC分类号： C07C381/14 , A61K31/10 , A61K47/00 , C07B2200/11
摘要： This invention relates to macromolecular prodrugs having antitumor activity when activated by GSH, and methods for synthesizing and administering these to patients. More particularly, this invention relates to, inter alia, the synthesis and use of polyacrylamide carriers to target anticancer prodrugs to tumors, and to release active antitumor agents selectively in tumor cells. These active antitumor agents target the active site of the methylglyoxal-detoxifying enzyme glyoxalase I to thereby cause tumor regression.
摘要翻译：本发明涉及通过GSH活化时具有抗肿瘤活性的大分子前药，以及用于合成和给予患者的方法。更具体地说，本发明尤其涉及将抗癌前药靶向肿瘤的聚丙烯酰胺载体的合成和用途，以及在肿瘤细胞中选择性释放活性抗肿瘤剂。这些活性抗肿瘤剂靶向甲基乙二醛解毒酶乙二醛酶I的活性位点，从而引起肿瘤消退。

2. 发明授权

US07700560B2 Inactivators and bivalent inhibitors of glyoxalase I and methods of inhibiting tumor growth 失效
标题翻译：乙二醛酶I的失活剂和二价抑制剂以及抑制肿瘤生长的方法
公开(公告)号：US07700560B2
公开(公告)日：2010-04-20
申请号：US10559410
申请日：2004-05-28
申请人： Donald J. Creighton , Zhe-Bin Zheng
发明人： Donald J. Creighton , Zhe-Bin Zheng
IPC分类号： A61K38/08 , C07K5/02 , C07K5/08 , C07K5/10
CPC分类号： C07K7/02 , A61K38/00 , A61K47/55 , A61K47/60 , A61K47/64 , C07K5/0202 , C07K5/0215
摘要： Compounds comprising two human GlxI inhibitors covalently linked via a chemical linker are provided, wherein each of said two human GlxI inhibitors, which may be the same or different, is an S-substituted glutathione or an S-substituted glutathione prodrug, wherein said GlxI inhibitors each have a γ-glutamyl amino group, wherein said chemical linker is covalently bound to each GlxI inhibitor via said γ-glutamyl amino group, and wherein said chemical linker has a length of at least 50 Angstroms. Monovalent irreversible inactivators of human GlxI are also provided. An antineoplastic composition is provided, which comprises a compound described above and a pharmaceutically acceptable carrier. In vitro and in vivo methods of preventing or inhibiting the growth and proliferation of neoplastic cells and/or tumors are also provided.
摘要翻译：提供了包含通过化学接头共价连接的两个人GlxI抑制剂的化合物，其中所述两种可以相同或不同的人类GlxI抑制剂中的每一种都是S-取代的谷胱甘肽或S-取代的谷胱甘肽前药，其中所述GlxI抑制剂每个具有γ-谷氨酰氨基，其中所述化学连接体经由所述γ-谷氨酰氨基共价结合到每个GlxI抑制剂，并且其中所述化学连接体具有至少50埃的长度。还提供了人GlxI的单价不可逆灭活剂。提供抗肿瘤组合物，其包含上述化合物和药学上可接受的载体。还提供了预防或抑制肿瘤细胞和/或肿瘤的生长和增殖的体外和体内方法。

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