Use of substituted acryloyl distamycin derivatives in the...

A - Human Necessities – 61 – K

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A61K 31/395 (2006.01) A61K 31/40 (2006.01) A61K 31/4025 (2006.01) A61K 31/415 (2006.01) A61K 31/4155 (2006.01) A61K 31/4164 (2006.01) A61K 31/4178 (2006.01) A61K 31/4196 (2006.01) A61K 31/506 (2006.01) A61K 45/06 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2409664

Compounds which are .alpha.-halogenoacryloyl distamycin derivatives of formula (I) wherein R1 is a bromine or chlorine atom; R2 is a distamycin or distamycin- like framework as set forth in the specification; or a pharmaceutically acceptable salt thereof; are cytotoxic agents particularly effective in the treatment of tumors over expressing GSH/GSTs system and which are poorly responsive or even resistant to conventional antitumor therapies.

L'invention concerne des composés lesquels sont des dérivés d'.alpha.-halogènoacryloyle distamycine de la formule (I) dans laquelle R¿1? représente un atome de brome ou de chlore, R?2¿ représente une structure de distamycine ou analogue à la distamycine telle que présentée dans la description, ou un sel pharmaceutiquement acceptable de ceux-ci, lesquels composés sont des agents cytotoxiques particulièrement efficaces dans le traitement de tumeurs surexprimant un système GSH/GSTs et lesquelles sont faiblement réactives ou même résistantes à des thérapies antitumorales classiques.

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