Activated cytotoxic compounds for attachment to targeting...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) C07D 207/46 (2006.01)

Patent

CA 2663375

Activated cytotoxic compounds are described for attachment to targeting molecules for the treatment of a mammalian disease condition which comprise, an activator, a spacer linker, a linker (e.g., self-immolative), and a cytotoxic drug selected from the group consisting of AMINO-SUBSTITUTED (E)-2,6-DIALKOXYSTYRYL 4-SUBSTITUTED BENZYLSULFONES, AMINO-AND- HYDROXY SUBSTITUTED STYRYLSULFONANILIDES, and SUBSTITUTED PHENOXY- AND PHENYLTHIO-STYRYLSULFONE DERIVATIVES. Activated cytotoxic compound attached to a targeting molecule are described wherein the targeting molecule is selected from the group consisting essentially of an antibody, a receptor, a ligand, a cytokine, a hormone, and a signal transduction molecule. The invention is further directed to a method of treatment of disease conditions.

La présente invention concerne des composés cytotoxiques activés destinés à se fixer à des molécules de ciblage, dans le traitement de maladies touchant des mammifères. Lesdits composés comprennent un activateur, un espaceur-lieur, un lieur (auto-immolant, par exemple), et un médicament cytotoxique choisi dans le groupe constitué des BENZYLSULFONES AMINO-SUBSTITUÉES (E)-2,6-DIALCOXYSTYRYLE 4-SUBSTITUÉES, des STYRYLSULFONANILIDES AMINO- ET HYDROXY-SUBSTITUÉS, et des DÉRIVÉS de PHÉNOXY- ET DE PHÉNYLTHIO-STYRYLSULFONE SUBSTITUÉES. Dans le cas des composés cytotoxiques activés fixés à la molécule de ciblage décrits ici, ladite molécule de ciblage est choisie dans le groupe constitué essentiellement d'un anticorps, d'un récepteur, d'un ligand, d'une cytokine, d'une hormone, et d'une molécule de transmission de signal. L'invention concerne en outre un procédé de traitement de maladies.

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