| 摘要 |
The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein 11b/IIIa antagonists for imaging of thrombi. |
| 主权项 |
1. Compounds of Formula III: wherein
R3 is selected from the group consisting of H, F, CF3, COR9, COOR10, SOR10, SO2R10, CN and NO2;R7 is selected from the group consisting of Y, —O(CH2)n—Y, —(OCH2CH2)m—Y, Z,—OCH2—Z; —CH2—CH2—Z, —CH═CH—Z and —C≡C—Z;X is selected from CH or N;Y is selected from 18F or F;R9 is hydrogen or (C1-C6) alkyl;R10 is (C1-C6) alkyl;Z is a group wherein * indicates the atom of connection of Z;R5 is selected from the group consisting of H, CF3, COR9, COOR10, SOR10, SO2R10, CN and NO2;R8 is selected from the group consisting of Y, —O(CH2)n—Y and —(OCH2CH2)m—Y;n is 1-3;and m is 2-3; with the proviso that if R7 has the meaning of Y, R3 has the meaning of CF3, COR9, COOR10, SOR10, SO2R10, CN or NO2 and with the proviso that if R8 has the meaning of Y, R5 has the meaning of CF3, COR9, COOR10, SOR10, SO2R10, CN or NO2;including E and Z-isomers and diastereomers, mixtures thereof, and any pharmaceutically acceptable salt or complex thereof. |
