Water-soluble 4-thio-maleimido derivatives and methods for...

C - Chemistry – Metallurgy – 07 – D

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C07D 403/12 (2006.01) A61K 31/4025 (2006.01) A61K 47/42 (2006.01) A61K 47/48 (2006.01) A61P 9/12 (2006.01) A61P 31/04 (2006.01) A61P 35/00 (2006.01) C07K 16/00 (2006.01) C07D 225/06 (2006.01)

Patent

CA 2338000

The present invention provides water-soluble drugs of the formula, (see above formula) in particular, a water-soluble analogues of geldanamycin, and compositions comprising the same. This invention also provides a method of rendering water-insoluble drugs soluble in water through derivatization with a bifunctional linking molecule and subsequent conjugation to a polar moiety through a thio ether. The present invention further provides use of the compounds to treat cancer that expresses heat shock protein 90 (Hsp90) in a mammal.

L'invention concerne des médicaments solubles à l'eau, en particulier des analogues solubles à l'eau de geldanamycine et des compositions contenant ces derniers. L'invention concerne également un procédé permettant de rendre solubles dans l'eau des médicaments normalement insolubles à l'eau au moyen d'une dérivatisation avec une molécule de liaison bi-fonctionnelle suivie d'une conjugaison à une fraction polaire par l'intermédiaire d'un thio-éther. L'invention concerne en outre une méthode de traitement du cancer chez le mammifère.

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