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DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS
专利权人:
PIERRE FABRE MEDICAMENT
发明人:
PEREZ, Michel,RILATT, Ian,LAMOTHE, Marie
申请号:
TN2015000439
公开号:
TN2015000439A1
申请日:
2015.09.28
申请国别(地区):
TN
年份:
2017
代理人:
摘要:
The present invention concerns a compound of following formula (1): 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 l 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-C5)allcyl, OH and NR12R13 groups, or a phammceutically 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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