| 发明名称 |
FLUORO LINKERS AND THEIR USE AS LINKERS FOR ENZYME-ACTIVATED DRUG CONJUGATES |
| 摘要 |
<p>The present invention provides compounds or formula (1) R<SUB>1</SUB>-HN-CH<SUB>2</SUB>-CF<SUB>2</SUB>-(CH<SUB>2</SUB>)<SUB>l</SUB>-CR<SUB>3</SUB>R<SUB>4</SUB>-CO-R<SUB>2</SUB>, wherein: l is 0, 1 or 2, R<SUB>1 </SUB>is a labile amino protecting group, R<SUB>2 </SUB>is hydroxy group or the residue or an activated ester or halogen atom; R<SUB>3 </SUB>and R<SUB>4 </SUB>are independently hydrogen atom or C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl chain. There are also provided their preparation and the water-soluble conjugates based on these linkers, endowed with selective anticancer activity.</p> |
| 申请公布号 |
EP1414792(A1) |
申请公布日期 |
2004.05.06 |
| 申请号 |
EP20020751168 |
申请日期 |
2002.07.29 |
| 申请人 |
PHARMACIA ITALIA S.P.A. |
发明人 |
ANGELUCCI, FRANCESCO;SUARATO, ANTONINO;CARUSO, MICHELE;SCOLARO, ALESSANDRA;PESENTI, ENRICO;FAIARDI, DANIELA |
| 分类号 |
C07D491/22;A61K38/00;A61K47/48;A61P35/00;A61P35/02;C07C271/22;C07D207/46;C07D209/48;C07K5/10;C07K7/06;(IPC1-7):C07C271/22;C07K5/103 |
主分类号 |
C07D491/22 |
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