Back to results
US 12,583,887 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
Life of this patent
Estimating the term…
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.
Claims26
A method comprising:
- administering to a patient, a radio-labelled compound of Formula IV:
- or a pharmaceutically acceptable salts or stereoisomers thereof,
- wherein:
- X1 is CH2 or NH;
- X14 is selected from the group consisting of C(O) and heteroaryl, wherein at least one H of the heteroaryl is substituted with NO2;
- X15 is selected from the group consisting of NH, aryl, heteroaryl, cycloalkyl and heterocycloalkyl;
- X16 is at least one selected from the group consisting of
- a heteroaryl, (CH2)1-25, wherein at least one CH2 of (CH2)1-12 is optionally replaced with heteroaryl, CONH, and —O—;
- or
- R13 is selected from the group consisting of H, NO2, N3, alkyne, a protecting group, a halo and a radioisotope;
- or
- administering to a patient, a radio-labelled compound of Formula V:
- or a pharmaceutically acceptable salts or stereoisomers thereof,
- wherein:
- X1 is CH2 or NH;
- X17 s selected from the group consisting of:
- N and CH;
- X18 is selected from the group consisting of:
- (CH2)1-10 wherein at least one CH2 of (CH2)1-10 is optionally replaced by NH, aryl, heteroaryl and wherein at least one His optionally substituted with NO2;
- and
- R14 is selected from the group consisting of O and S;
- and
- R15 is selected from the group consisting of N3, alkyne, protecting group, halo and radioisotope;
- scanning the patient using positron emission tomography or single photon emission computed tomography;
- and
- imaging a tissue in the patient.
23 more elements
A compound of Formula IV:
- or a pharmaceutically acceptable salt or stereoisomer thereof,
- wherein:
- X1 is CH2 or NH;
- X14 is selected from the group consisting of:
- C(O) and heteroaryl, wherein at least one H of the heteroaryl is substituted with NO2;
- X15 is selected from the group consisting of NH, aryl, heteroaryl, cycloalkyl and heterocycloalkyl;
- X16 is at least one selected from the group consisting of:
- a heteroaryl, (CH2)1-25, wherein at least one CH2 of (CH2)1-12 is optionally replaced with heteroaryl, CONH, or —O—;
- and
- R13 is selected from the group consisting of H, NO2, N3, alkyne, a protecting group, a halo and a radioisotope.
7 more elements
The compound:
- or a pharmaceutically acceptable salt or a stereoisomer thereof, wherein R10 is selected from the group consisting of radionuclide and halo.
A compound of Formula V:
- or a pharmaceutically acceptable salts or a stereoisomers thereof,
- wherein:
- X1 is CH2 or NH;
- X17 is selected from the group consisting of N and CH;
- X18 is selected from the group consisting of (CH2)1-10 wherein at least one CH2 of (CH2)1-10 is optionally replaced by NH, aryl, heteroaryl, and wherein at least one His optionally substituted with NO2;
- and
- R14 is selected from the group consisting of O and S;
- and
- R15 is selected from the group consisting of N3, alkyne, protecting group, halo and radioisotope.
6 more elements
Dependencies are inferred from the claim text.