Analogs of benzoquinone-containing ansamycins for the...

C - Chemistry – Metallurgy – 07 – D

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C07D 225/06 (2006.01) A61K 31/395 (2006.01) A61P 35/00 (2006.01) C07D 211/60 (2006.01) C07D 498/08 (2006.01) C07F 5/02 (2006.01)

Patent

CA 2547343

The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer ( formula (I) and (IV). The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting (17)-~ammonium hydroquinone ansamycin analog.

L'invention concerne des analogues d'ansamycines contenant de la benzoquinone et leurs utilisations dans le traitement et la modulation de troubles associés à une hyperprolifération, tel que le cancer. L'invention concerne également des analogues d'ansamycines contenant de la benzoquinone dans lesquels la benzoquinone est réduite à une hydroquinone et piégée par réaction avec un acide approprié, de préférence des acides qui augmentent la solubilité et la stabilité de l'air de l'analogue d'ansamycines contenant de l'hydroquinone et du 17-ammonium ainsi obtenu.

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