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US 5,175,257 AGranted
Radiolabeled proteins for diagnostic or therapeutic use
AssigneeNeoRx Corporation
InventorsSudhakar Kasina, Ananthachari Srinivasan, John M. Reno, Linda M. Gustavson, Jeffrey N. Fitzner, David S. Jones
Life of this patent
Estimating the term…
Abstract
Chelating compounds of specified N.sub.2 S.sub.2 N.sub.3 S derived structure are useful for radiolabeling targeting molecules such as antibodies. Cleavable ester orthioester linkers connect the radionuclide metal chelates to the antibodies. The radiolabeled antibodies have improved biodistribution properties, including reduced localization within the intestines and kidneys.
Claims36
A compound of the formula:
- ##STR29## wherein:
- m is 0 or 1;
- R.sub.1 represents H or CH.sub.3 ;
- X represents O or S;
- each R.sub.3 is independently selected from H, CH.sub.2 OH, CH.sub.3, --(CH.sub.2).sub.n --CONH.sub.2, and --(CH.sub.2).sub.n --COOH, wherein n is 0 to about 2, with at least one R.sub.3 substituent being --(CH.sub.2).sub.n --COOH;
- T' and T each represent hydrogen or a sulfur protecting group;
- R.sub.2 represents a spacer;
- and
- P' represents a targeting molecule or a conjugation group.
6 more elements
A compound of the formula:
- ##STR32## wherein p is 0 or 1;
- one of the R' symbols represents ##STR33## and the others are selected from H, CH.sub.3, CH.sub.2 OH, --(CH.sub.2).sub.n --CONH.sub.2 and (CH.sub.2).sub.n --COOH wherein n is 0 to about 2;
- m is 0 or 1;
- R.sub.1 represents H or CH.sub.3 ;
- X represents O or S;
- T represents hydrogen or a sulfur protecting group;
- R.sub.2 represents a spacer;
- and
- P' represents a targeting molecule or a conjugation group.
6 more elements
A compound of the formula:
- ##STR36## wherein p is 0 or 1;
- each R.sub.4 is independently selected from H, CH.sub.3, CH.sub.2 OH, --(CH.sub.2).sub.n --CONH.sub.2 and --(CH.sub.2).sub.n --COOH wherein n is 0 to about 2;
- m is 0 or 1;
- R.sub.1 represents H or CH.sub.3 ;
- X represents O or S;
- T represents hydrogen or a sulfur protecting group;
- R.sub.2 represents a spacer;
- and
- P' represents a targeting molecule or a conjugation group.
6 more elements
A compound of the formula:
- ##STR39## wherein p is 0 or 1;
- each R.sup.4 is independently selected from H, CH.sub.3, CH.sub.2 OH, --(CH.sub.2).sub.n --CONH.sub.2 and (CH.sub.2).sub.n --COOH wherein n is 0 to about 2;
- q is 1, 2, or 3;
- R.sub.1 represent H or CH.sub.3 ;
- X represents O or S;
- T represents hydrogen or a sulfur protecting group;
- R.sub.2 represents a spacer;
- and
- P' represents a targeting molecule or a conjugation group.
6 more elements
A compound of the formula:
- ##STR42## wherein T represents hydrogen or a sulfur protecting group and P' represents a targeting molecule or a conjugation group.
A compound of the formula:
- ##STR43## and stereochemical isomers thereof, wherein:
- M represents a radionuclide metal or oxide thereof;
- m is 0 or 1;
- R.sub.1 represents H or CH.sub.3 ;
- X represents O or S;
- each R.sub.3 is independently selected from H, CH.sub.3, CH.sub.2 OH, --(CH.sub.2).sub.n --CONH.sub.2, and --(CH.sub.2).sub.n --COOH, wherein n is 0 to about 2, with at least one R.sub.3 substituent being --(CH.sub.2).sub.n --COOH;
- R.sub.2 represents a spacer;
- and
- P' represents a targeting molecule or a conjugation group.
6 more elements
A compound of the formula:
- ##STR46## and stereochemical isomers thereof, wherein M represents a radionuclide metal or oxide thereof;
- p is 0 or 1;
- one of the R' symbols represents ##STR47## and the others are selected from H, CH.sub.3, CH.sub.2 OH, (CH.sub.2).sub.n --CONH.sub.2 and (CH.sub.2).sub.n --COOH wherein n is 0 to about 2;
- m is 0 or 1;
- R.sub.1 represents H or CH.sub.3 ;
- X represents O or S;
- T represents hydrogen or a sulfur protecting group;
- R.sub.2 represents a spacer;
- and
- P' represents a targeting molecule or a conjugation group.
7 more elements
A compound of the formula:
- ##STR50## and stereochemical isomers thereof, wherein M represents a radionuclide metal or oxide thereof;
- p is 0 or 1;
- each R.sub.4 is independently selected from H, CH.sub.3, CH.sub.2 OH, (CH.sub.2).sub.n --CONH.sub.2 and --(CH.sub.2).sub.n --COOH wherein n is 0 to about 2;
- m is 0 or 1;
- R.sub.1 represents H or CH.sub.3 ;
- X represents O or S;
- R.sub.2 represents a spacer;
- and
- P' represents a targeting molecule or a conjugation group.
6 more elements
A compound of the formula:
- ##STR53## and stereochemical isomers thereof, wherein M represents a radionuclide metal or oxide thereof;
- p is 0 or 1;
- each R.sub.4 is independently selected from H, CH.sub.3, CH.sub.2 OH, --(CH.sub.2).sub.n --CONH.sub.2 and (CH.sub.2).sub.n --COOH wherein n is 0 to about 2;
- q is 1, 2, or 3;
- R.sub.1 represents H or CH.sub.3 ;
- X represents O or S;
- T represents hydrogen or a sulfur protecting group;
- R.sub.2 represents a spacer;
- and
- P' represents a targeting molecule or a conjugation group.
7 more elements
A compound of the formula:
- ##STR56## and stereochemical isomers thereof, wherein M represents a radionuclide metal selected from .sup.99m Tc, .sup.188 Re, and .sup.186 Re, and P' represents a targeting molecule or a conjugation group.
Dependencies are inferred from the claim text.