发明名称 |
TUMOR PROTEASE ACTIVATED PRODRUGS OF PHOSPHORAMIDE MUSTARD ANALOGS |
摘要 |
<p>The composition, synthesis, and applications of tumor associated protease activated prodrugs of phosphoramide mustard, isophosphoramide mustard and analogs with detoxification functionalities are described. These drugs release a cytotoxic phosphoramide mustard analog following activation by tumor associated proteases and esterases. The general structure for these drugs is: <IMAGE> Wherein R1 is a beta-X-ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; wherein X is a good leaving group such as a halogen; R2 is a beta-X-ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; or an amino group (NH2) which may optionally be substituted. Wherein A is a benzyloxy derivative with one or more acyloxy or acylamino groups in para or ortho portions relative to the phosphoester; and wherein the acyloxy or acylamino groups are not (substituted or unsubstituted) p-guanidino-benzoyloxy groups or p-guanidino-benzoylamino groups.</p> |
申请公布号 |
GR3036796(T3) |
申请公布日期 |
2002.01.31 |
申请号 |
GR20010401658T |
申请日期 |
2001.10.04 |
申请人 |
DRUG INNOVATION & DESIGN, INC. |
发明人 |
GLAZIER, ARNOLD |
分类号 |
A61K38/00;A61K31/66;A61K38/46;A61K38/48;A61P35/00;C07F9/24;(IPC1-7):C07F9/24 |
主分类号 |
A61K38/00 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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