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US 12,559,521 B2Granted
PSMA imaging agents
AssigneeSiemens Medical Solutions USA, Inc.
InventorsEric Wang, Hartmuth C. Kolb, Anna Katrin Szardenings, Changhui Liu, Joseph C. Walsh, Gang Chen, Anjana Sinha, Dhanalakshmi Kasi, Chul Yu, Umesh B. Gangadharmath, Wei Zhang, Tieming Zhao, Vani P. Mocharla
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Abstract
Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.
Claims6
A method comprising administering to a patient, a compound of Formula VI:
- and pharmaceutically acceptable salts and stereoisomers thereof,
- wherein:
- X1 is CH;
- X19 is selected from the group consisting of:
- NO2 and (CH2)1-10—R16 wherein at least one CH2 of (CH2)1-10 is optionally replaced by CONH, aryl, a triazole or heteroaryl;
- X20 is selected from the group consisting of:
- H, NO2, and (CH2)1-10-R16 wherein at least one CH2 of (CH2)1-10 is optionally replaced by CONH, aryl, a triazole or heteroaryl;
- wherein in Formula VI, at least one CH2 of (CH2)1-10-R16 of either X19 or X20 is replaced by triazole;
- X21 is (CH2)1-3 wherein at least one CH2 of (CH2)1-3 is optionally replaced by a heteroaryl, and
- R16 is selected from the group consisting of N3, alkyne, protecting group, halo and a radioisotope;
- wherein at least one R16 from X19 or X20 is a radioisotope;
- or
- administering to a patient, a radio labelled-compound of Formula VIII:
- and pharmaceutically acceptable salts and stereoisomers thereof,
- wherein:
- X1 is CH;
- X24 is (CH2)1-6 wherein at least one CH2 of (CH2)1-6 is optionally replaced by at least one selected from the group consisting of NH, O, or S,
- X25 is N or CH;
- X26 is NH or CH2;
- X27 is selected from the group consisting of:
- H, NO2, and (CH2)1-10-R16 wherein at least one CH2 of (CH2)1-10 is optionally replaced by O, CONH, aryl, or heteroaryl;
- and
- R16 is a radioisotope;
- scanning the patient using positron emission tomography or single photon emission computed tomography;
- and
- imaging a tissue in the patient.
23 more elements
Dependencies are inferred from the claim text.