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Cell binding agent conjugates of analogues and derivatives of CC-1065

  • US 5,475,092 A
  • Filed: 03/21/1994
  • Issued: 12/12/1995
  • Est. Priority Date: 03/25/1992
  • Status: Expired due to Term
First Claim
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1. A cytotoxic agent comprising a cell binding agent linked via a disulfide bond to one or more analogues or derivatives of a cyclopropylbenzindole-containing cytotoxic drug,wherein said cell binding agent is a monoclonal antibody or an antigen-binding fragment of a monoclonal antibody having at least one binding site thereof, andwherein prior to linking said analogues or derivatives to said cell binding agent said analogues or derivatives are selected from the group consisting of analogues or derivatives formed from an A subunit of the formulae (A-3) or (A-4) and a B-C subunit of the formulae (F-3), (F-4), (F-5) or (F-6), said B-C subunit having a B moiety shown on the left-hand side of the formulae and a C moiety shown on the right-hand side of the formulae and wherein said A subunit is covalently linked to said B-C subunit via an amide bond from the secondary amino group of the pyrrole moiety of the A subunit to the C-2 carboxyl group of the B moiety of the B-C subunit,wherein the formulae (A-3) and (A-4) are as follows:

  • ##STR6## wherein the formulae (F-3) to (F-6) are as follows;

    ##STR7## wherein in a given formula, one of either R or R4 represents a group that enables linkage of the analogue or derivative of the cyclopropylbenzindole-containing cytotoxic drug via a disulfide bond to said cell binding agent;

    when R represents a moiety that enables linkage, then R1 to R6, which may be the same or different, represent hydrogen, C1 -C3 linear alkyl, methoxy, hydroxyl, primary amino, secondary amino, tertiary amino, or amido; and

    when R4 represents a moiety that enables linkage, R, R1, R2, R3, R5 and R6, which may be the same or different, represent hydrogen, C1 -C3 linear alkyl, methoxy, hydroxyl, primary amino, secondary amino, tertiary amino, or amido.

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