A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 47/48 (2006.01) A61K 39/395 (2006.01) C07H 15/252 (2006.01) C07K 16/30 (2006.01)
Patent
CA 2010164
The present invention relates to novel immuno-conjugates, methods for their production, pharmaceutical compositions and methods for delivering cytotoxic anthracyclines to a selected population of cells desired to be eliminated. More particularly, the invention relates to immunoconjugates comprised of an antibody reactive with a selected cell population, having a number of anthracycline molecules linked to its structure. Each anthracycline molecule, having a keto group at the C-13 position, is conjugated to the antibody via a linker arm and is bound to that linker arm via an acid-sensitive acylhydrazone bond at the 13-keto position of the anthracycline. A preferred embodiment of the invention relates to an adriamycin immunoconjugate wherein a 13-keto acylhydrazone bond is the site of the adriamycin attachment to the linker arm, the linker additionally containing a disulfide or thioether linkage as part of the antibody attachment to the immunoconjugate. In addition, novel anthracycline acylhydrazone derivatives are disclosed that are useful in the preparation of the immunoconjugates of this invention. The acid-sensitive hydrazone bond of the immunoconjugates of this invention allows the release of free anthracycline from the immunoconjugates in the acidic external or internal environment of the target cell. The immunoconjugates and methods of the invention are therefore useful in antibody-mediated drug delivery systems for the preferential killing of a selected cell population in the treatment of diseases such as cancers and other tumors, non-cytocidal viral or other pathogenic infections, and autoimmune disorders.
Braslawsky Gary R.
Greenfield Robert S.
Kaneko Takushi
Olech Lee J.
Bristol-Myers Squibb Company
Cassan Maclean
LandOfFree
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