Novel peptide derivatives

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 5/027 (2006.01) A61K 38/07 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2218606

Peptide derivatives represented by general formula (I) or their salts, having an antitumor effect ten times as potent as that of dolastatin 10 and being useful as an anticancer and antitumor agent. In said formula (I), (a) Q1 represents 1-dimethylamino-2-methylpropyl; and Q2 represents (R)-or (S)-2- hydroxy-2-phenyl-ethylamino, 2-phenylcyclopropylamino or 1,2,3,4- tetrahydroisoquinolin-2-yl; or (b) Q1 represents 1-methyl-2-pyrrolidinyl; and Q2 represents .alpha..

L'invention porte sur des dérivés peptidiques représentés par la formule générale (I) ci-dessous, ou leurs sels, qui produisent un effet antitumoral dix fois plus puissant que celui dont fait montre de la dolastatine 10 et s'avérant très utiles comme agent anticancéreux et antitumoral. Dans cette formule, a), Q¿1? représente 1-diméthylamino-2-méthylpropyle et Q¿2? représente (R)- ou (S)-2-hydroxy-2-phényl-éthylamino, 2-phénylcycloprylamino ou 1, 2, 3, 4-tétrahydroisoquinoline-2-yle ou bien, b), Q¿1? représente 1-méthyl-2-pyrrolidinyle et Q¿2? représente .alpha..

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