Cytotoxins, prodrugs, linkers and stabilizers useful therefor

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/407 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2448319

The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.

La présente invention concerne des analogues de duocarmycines qui constituent des cytotoxines puissantes. Elle concerne également des lieurs peptidyle et disulfure qui subissent un clivage in vivo. Ces lieurs sont utiles dans la formation de promédicaments et de conjugués des cytotoxines selon l'invention ainsi que d'autres fractions diagnostiques et thérapeutiques. L'invention concerne des promédicaments et des conjugués des analogues de duocarmycine comprenant les bras lieurs selon l'invention.

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