Conjugates of methyltrithio antitumor agents and...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 16/00 (2006.01) A61K 47/48 (2006.01) C07H 15/203 (2006.01) C07K 14/475 (2006.01)

Patent

CA 2150785

This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.

L'invention concerne des conjugués vecteurs de médicament préparés à l'aide d'analogues disulfurés de la famille des calicheamicines et de leurs dérivés, des antibiotiques ayant un effet antitumoral puissant, de même que d'analogues similaires d'antibiotiques antitumoraux apparentés comme les esperamicines. Le vecteur peut être un anticorps, un facteur de croissance ou un stéroïde, qui cible une population de cellules non désirées, par exemple celles d'une tumeur. Les vecteurs de protéines entières, de même que leurs fragments reconnaissant un antigène et leurs équivalents chimiquement ou génétiquement manipulés sont utiles pour ce qui est de la portion ciblée des conjugués. Cette invention porte aussi sur les composés nécessaires à la synthèse de ces conjugués, la composition pharmaceutique des conjugués vecteurs de médicament et la méthode d'utilisation.

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