American Cyanamid Company

Other

William A Hallett

Dennis W Powell

Martin J Weiss

Hwei-Ru Tsou

Philip R Hamann

Minu D Dutia

Dan Maarten Berger

Rolf Paul

Lois M Hinman

Irwin J Hollander

Ryan Holcomb

Mark E Salvati

Nancy H Eudy

The invention provides novel substituted dibenzothiophenes of Formulae (I), (II), (III) and (IV) which have antiangiogenic activity and further provides a method using substituted dibenzothiophenes of Formula (V) as antiangiogenic agents.

Substituted dibenzothiophenes having antiangiogenic activity

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

Compounds of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are herein described, A is a straight or branched (C.sub.2 -C.sub.12)alkyl or a phenyl moiety and B is a moiety of the formula: ##STR2## The compounds are effective in potentiating the activity of chemotherapeutic anti-cancer agents by increasing the sensitivity of multi-drug resistant cells to such chemotherapeutic agents.

MDR reversal agents

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William A Hallett