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Pharmaceutical agents for labeling inhibitors of prostate-specific membrane antigen (PSMA), their use as imaging agents, and treatment of PSMA-expressing cancers
Pharmaceutical agents for labeling inhibitors of prostate-specific membrane antigen (PSMA), their use as imaging agents, and treatment of PSMA-expressing cancers
In the present invention, the formulas (1) (I) [in the formula, Y 3 is O or S, s, t, u and w are 0 or 1, i is an integer of 1 to 3, and j. Is an integer from 3 to 5, and Z 1 , Z 2 and Z 3 are selected from the group consisting of CO 2 H, -SO 2 H, -SO 3 H, -OSO 3 H, and -OPO 3 H 2. , R 1 is -CH 3 or H, X is selected from the group consisting of alkylaryls, aryls, alkyl heteroaryls and heteroaryls, and Y 1 and Y 2 are aryls, alkylaryls, cycloalkyls, heterocyclos. Selected from the group consisting of alkyl, heteroaryl and alkyl heteroaryl, A is (Ia), (Ib) and (Ic) (in the formula, R 2 , R 3 , R 4 and R 5 are H, -CH. Selected from the group consisting of 2 -COOH and -CH 2 -C (= O) -NH 2, or R 2 and R 4 form a-(CH 2 ) n -bridge, where n is 1-3. It is an integer, n is preferably 2, r, v and q are 0 or 1, but when u and w are 0, q and v are 0). (A) u and w are 1 or (B) u is 0, w is 1 and A is from (Ia) or (Ib). Selected or (C) A is not]. The compounds are disclosed for use in the treatment of PSMA-expressing cancers. [Selection diagram] None
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