American Cyanamid Company

Ryan Holcomb

Martin J Weiss

Hwei-Ru Tsou

Philip R Hamann

William A Hallett

Lois M Hinman

Irwin J Hollander

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.

Process for preparing conjugates of methyltrithio antitumor agents

Conjugates of methyltrithio antitumor agents and intermediates for their

Linkers useful for the synthesis of conjugates of methyltrithio

Enediyne derivatives useful for the synthesis of conjugates of

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Glen Rock, NJ, United States of America

Ryan Holcomb