Methods and compositions for degradation and/or inhibition...

Details Methods and compositions for degradation and/or inhibition... Methods and compositions for degradation and/or inhibition...

C - Chemistry, Metallurgy

07

D

C07D 403/02 (2006.01) A61K 31/395 (2006.01) A61P 35/00 (2006.01) C07D 225/06 (2006.01)

Patent

CA 2370007

Bifunctional molecules comprising two hsp-binding moieties which bind to hsp90 in the pocket to which ansamycin antibiotics bind connected via a linker are effective for inducing the degradation and/or inhibition of HER-family tyrosine kinases. For example, a compound of two geldanamycin moities joined by a four-carbon linker provides selective degradation of HER-family tyrosine kinases, without substantially affecting other kinases. These compounds can be used for treatment of HER-positive cancers with reduced toxicity, since these compounds potently kill cancer cells but affect fewer proteins than geldanamycin.

L'invention concerne des molécules bifonctionnelles comprenant deux fractions de liaison aux protéines hsp90, lesquelles se lient aux hps dans la poche dans laquelle se produit la liaison aux antibiotiques ansamycine, par l'intermédiaire d'une séquence de liaison. Ces molécules permettent d'induire une dégradation et/ou une inhibition des tyrosine kinases appartenant à la famille HER. Par exemple, un composé comprenant deux fractions geldanamycine reliées par une séquence de liaison à quatre atomes de carbone provoque la dégradation sélective des tyrosines kinases de la famille HER sans affecter de manière sensible les autres kinases. Ces composés peuvent être utilisé pour traiter les cancers HER-positifs avec une toxicité diminuée, étant donné que ces composés détruisent potentiellement les cellules cancéreuses mais affectent un moins grand nombre de protéines que la geldanamycine.

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