Cyclopamine analogues and methods of use thereof

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 407/04 (2006.01) A61K 31/4355 (2006.01) A61K 31/438 (2006.01) C07D 307/94 (2006.01) C07D 405/04 (2006.01)

Patent

CA 2579078

The present invention provides compositions and methods for modulating smoothened~dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of~function mutations. The compounds of the present invention are particularly useful in treating cancers.

L'invention concerne des compositions et des procédés destinées à moduler l'activité du signal Smoothened. Cette invention concerne également des analogues de cyclopamine pouvant être utilisés afin de neutraliser les effets phénotypiques d'une activation non désirée d'une voie Hedgehog, notamment obtenue par des mutations de gain de fonction Hedgehog, de perte de fonction Patched ou de gain de fonction Smoothened. Les composés de cette invention sont particulièrement utiles dans le traitement de cancers.

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