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US 12,612,343 B2Granted
PSMA binder and use thereof
AssigneeShiya Pharmaceutical, Inc
InventorsShaoli Song, Xiaoping Xu, Chang Liu
Life of this patent
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Abstract
The present invention discloses a prostate specific membrane antigen (PSMA) binding compound, a radioactive isotope complex thereof, and the use thereof in nuclear medicine as a tracer and an imaging agent for different disease states of prostate cancer.
Claims13
A compound of formula (I-1) or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the formula (I-1) is:
- wherein:
- m is 1;
- n is 1;
- f and g each is 0 or 1;
- R and R′ each is independently selected from H and alkyl;
- Q is —COOH;
- X is naphthyl, which is optionally substituted by at least one R group;
- Y is phenyl, which is optionally substituted by at least one R group;
- AA1 is
- wherein i=1-3.
7 more elements
A preparation method of the 99mTc complex according to claim 4, comprising:
- formulating 0.5-2 ml of a mixture containing 1-100 ug of the compound according to claim 1, 0-500 μg of stannous chloride, 1-50 mg of a ligand L, 20-50 mg of disodium succinate, 5-30 mg of succinic acid, and 0-100 mg of mannitol in a 10-mL vial;
- adding 0.5-2 mL of Na99mTcO4 solution 10-100 mCi;
- heating the vial in a 100° C. water bath to carry out reaction for 10-20 minutes;
- and
- cooling at room temperature for 10 minutes after the reaction is completed;
- thus
- obtaining the 99mTc complex according to claim 6;
- wherein the ligand L is selected from N-tris(hydroxymethyl)methylglycine, ethylenediaminediacetic acid, triphenylphosphine-3,3′,3″-trisulfonate, disodium 3,3′-(phenylphosphinediyl)bis(benzene-1-sulphonate), sodium diphenylphosphinobenzene-3-sulfonate, nicotinic acid, glucoheptonate, glucosamine, mannitol, or diphenylphosphinobenzoic acid.
5 more elements
Dependencies are inferred from the claim text.