Dolastatin 15 derivatives

Details Dolastatin 15 derivatives Dolastatin 15 derivatives

C - Chemistry, Metallurgy

07

K

C07K 7/06 (2006.01) A61K 38/08 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2296036

Compounds of the present invention include cell growth inhibitors which are peptides of Formula (I):, A - B - D - E - F - (G)r - (K)s - L and acid salts thereof wherein A, B, D, E, F, G and K are .alpha.- amino acid residues, and s and r are each, independently, 0 or 1. L is a monovalent radical, such as, for example, an amino group, an N- substituted amino group, a .beta.-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, or an oximato group. The present invention also includes a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula (I) in a pharmaceutically acceptable composition.

La présente invention concerne des composés renfermant des inhibiteurs de croissance cellulaire, lesquels sont des peptides de formule (I): A - B - D - E - F - (G)r - (K)s - L ainsi que des sels acides de ceux-ci, A, B, D, E, F, G et K étant des restes alpha-aminoacides, et s et r représentant indépendamment 0 ou 1. L est un radical monovalent, par exemple un groupe amino, un groupe amino N-substitué, un groupe bêta-hydroxylamino, un groupe hydrazido, un groupe alcoxy, un groupe thioalcoxy, un groupe aminoxy, ou un groupe oximato. La présente invention concerne également un procédé de traitement du cancer chez un mammifère tel qu'un humain, ce procédé consistant à administrer à ce mammifère une quantité efficace d'un composé de formule I dans une composition pharmaceutiquement acceptable.

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