Monomethylvaline compounds having phenylalanine side-chain...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 7/02 (2006.01) A61K 38/04 (2006.01) A61K 38/05 (2006.01) A61K 38/08 (2006.01) A61K 47/48 (2006.01) A61P 35/00 (2006.01) C07K 5/027 (2006.01) C07K 19/00 (2006.01) G01N 33/574 (2006.01) C07K 16/00 (2006.01)

Patent

CA 2614436

Auristatin peptide analogs of MeVal-Val-Dil-Dap-Phe (MMAF) are provided having C-terminal phenylalanine residue side chain replacements or modifications which are provided alone or attached to ligands through various linkers. The rlated conjugates can target specific cell types to provide therapeutic benefit.

La présente invention se rapporte à des analogues peptidiques de l'auristatine MeVal-Val-Dil-Dap-Phe (MMAF), qui présentent des substitutions ou des modifications de la chaîne latérale du résidu phénylalanine C-terminal, et qui sont soit seuls soit liés à des ligands par l'intermédiaire de divers lieurs. Les conjugués associés peuvent cibler des types de cellules spécifiques pour apporter un bénéfice thérapeutique.

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