Conjugates useful in the treatment of prostate cancer

Details Conjugates useful in the treatment of prostate cancer Conjugates useful in the treatment of prostate cancer

C - Chemistry, Metallurgy

07

K

C07K 14/47 (2006.01) A61K 38/17 (2006.01) A61K 47/48 (2006.01) C07K 7/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2311615

Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. The conjugates of the invention are characterized by attachment of the cleavable oligopeptide to the oxygen atom at the 4-position on a vinca drug that has be desacetylated. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).

L'invention concerne des conjugués qui comportent des oligopeptides possédant des séquences d'acides aminés qui sont coupées protéolytiquement de manière sélective par des antigènes libres spécifiques de la prostate (PSA) et par des agents cytotoxiques connus. Les conjugués de l'invention sont caractérisés par la fixation de l'oligopeptide clivable à l'atome d'oxygène situé en position 4 sur un médicament à base de pervenche qui a été désacétylé. Ces conjugués sont utiles dans le traitement du cancer de la prostate et de l'hypertrophie prostatique bénigne (BPH).

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