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DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS
专利权人:
发明人:
Michel PEREZ,Ian RILATT,Marie LAMOTHE
申请号:
US15708685
公开号:
US20180222858A1
申请日:
2017.09.19
申请国别(地区):
US
年份:
2018
代理人:
摘要:
The present invention concerns a compound of following formula (I): where: —R1 is H or OH, —R2 is a (C1-C6)alkyl, COOH, COO—((C1-C6)alkyl) or thiazolyl group, —R3 is H or a (C1-C6)alkyl group, and —R4 is: ▪a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR5R6, ▪—(CH2CH2X1)(CH2CH2X2)a2(CH2CH2X3)a3(CH2CH2X4)a4(CH2CH2X5)a5R7, ▪an aryl-(C1-C8)alkyl group substituted by one or more groups chosen from among OH and NR9R10 groups, or ▪a heterocycle-(C1-C8)alkyl group optionally substituted by one or more groups chosen from among (C1-C6)alkyl, OH and NR12R13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.
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