Monomethylvaline compounds capable of conjugation to ligands

Details Monomethylvaline compounds capable of conjugation to ligands Monomethylvaline compounds capable of conjugation to ligands

C - Chemistry, Metallurgy

07

K

C07K 5/027 (2006.01) A61K 38/06 (2006.01) A61K 39/395 (2006.01) A61K 47/48 (2006.01) A61P 31/00 (2006.01) A61P 35/00 (2006.01) A61P 37/00 (2006.01) C07K 5/00 (2006.01) C07K 16/00 (2006.01) C07K 16/28 (2006.01) C07K 16/30 (2006.01) C12Q 1/04 (2006.01) G01N 33/574 (2006.01)

Patent

CA 2543888

Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal- Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.

La présente invention a trait à des peptides d'auristatine, comprenant de la MeVal-Val-Dil-Dap-phénylpropanolamine (MMAE) de la MeVal-Val-Dil-Dap-Phe (MMAF), préparés et fixés à des ligands par divers lieurs, comprenant le maléimidocaproyl-val-cit-PAB. Les conjugués médicament/ligand obtenus ont présenté une activité in vitro et in vivo.

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