Macrocyclic congugates and their use as diagnostic and therapeutic agents
AssigneeThe Dow Chemical Company
InventorsRoberta C. Cheng, William A. Fordyce, William F. Goeckleler, William J. Kruper, Jr., Richard K. Frank, Joseph R. Garlich, Garry E. Kiefer, Kenneth McMillan, Jaime Simon, David A. Wilson, Sharon Braughman
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Abstract
A group of functionalized macrocyclic polyaminocarboxylate chelants that form complexes with rare earth-type metal ions are disclosed. The complexes, covalently attached to an antibody or antibody fragment, can be used for therapeutic and/or diagnostic purposes for cancer.
Claims40
A conjugate comprising of a compound of the formula:
- ##STR16## wherein:
- each Q is CHR.sup.5 CO.sub.2 R;
- each R is hydrogen;
- m is 0;
- R.sup.3 is selected from the group consisting of methoxy and hydroxy;
- R.sup.4 is selected from the group consisting of amino, and isothiocyanato;
- each R.sup.5 is hydrogen;
- or
- a pharmaceutically acceptable salt thereof;
- complexed with an ion of a metal selected from the group consisting of La, Ce, Pr, Nd, Pm, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Y and Sc;
- and covalently attached to an antibody or antibody fragment.
A method for the diagnosis of cancer in a mammal which comprises administering to said mammal an amount effective for the diagnosis of cancer of a formulation comprising a conjugate of a compound of the formula ##STR17## wherein:
- each Q is CHR.sup.5 CO.sub.2 R;
- each R is hydrogen;
- m is 0;
- R.sup.3 is selected from the group consisting of methoxy and hydroxy;
- R.sup.4 is selected from the group consisting of amino, and isothiocyanato;
- each R.sup.5 is hydrogen;
- or
- a pharmaceutically acceptable salt thereof;
- complexed with an ion of a metal selected from the group consisting of La, Ce, Pr, Nd, Pm, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Y and Sc;
- and covalently attached to an antibody or antibody fragment;
- with a pharmaceutically acceptable carrier.
A conjugate comprising of a compound of the formula:
- ##STR18## wherein:
- each Q is CHR.sup.5 CO.sub.2 R;
- each R is hydrogen;
- m is 0;
- R.sup.3 is selected from the group consisting of methoxy and hydroxyl
- R.sup.4 is selected from the group consisting of amino, and isothiocyanato;
- each R.sup.5 is hydrogen;
- or
- a pharmaceutically acceptable salt thereof;
- complexed with an ion of a metal selected from the group consisting of La, Ce, Pr, Nd, Pm, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Y and Sc;
- and covalently attached to an antibody or antibody fragment.
A method for the diagnosis of cancer in a mammal which comprises administering to said mammal an amount effective for the diagnosis of cancer of a formulation comprising a conjugate of a compound of the formula ##STR19## wherein:
- each Q is CHR.sup.5 CO.sub.2 R;
- each R is hydrogen;
- m is 0;
- R.sup.3 is selected from the group consisting of methoxy and hydroxy;
- R.sup.4 is selected from the group consisting of amino, and isothiocyanato;
- each R.sup.5 is hydrogen;
- or
- a pharmaceutically acceptable salt thereof;
- complexed with an ion of a metal selected from the group consisting of La, Ce, Pr, Nd, Pm, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Y and Sc;
- and
- covalently attached to an antibody or antibody fragment;
- with a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.