MONOMETHYLVALINE COMPOUNDS CAPABLE OF FORMING CONJUGATES WITH LIGANDS Russian patent published in 2012 - IPC C07K16/46 C07K5/08 A61K39/395 A61K38/06 

Abstract RU 2448117 C2

FIELD: chemistry.

SUBSTANCE: invention relates to auristatin peptides, including MeVal-Val-Dil-Dap-norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), and these peptides were attached to ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting "ligand-drug" conjugates are active in vitro and in vivo.

EFFECT: high activity of the compounds.

118 cl, 19 dwg, 12 tbl, 33 ex

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RU 2 448 117 C2

Authors

Doronina Svetlana O.

Senter Piter D.

Toki Brajan Eh.

Ehbens Allen Dzh.

Klajn Toni Bet

Polakis Pol

Slivkovski Mark Ks.

Spenser Sjuzan D.

Dates

2012-04-20Published

2004-11-05Filed