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Tetracyclic indole derivatives as imaging agents in vivo and having affinity for peripheral benzodiazepine receptors (PBR)
专利权人:
HAMMERSMITH IMANET; LTD
发明人:
ARSTAD, ERIK,WILSON, IAN,LUTHRA, SAJINDER KAUR,BRADY, FRANK,LANGSTROEM, BENGT,KARIMI, FARHAD,ROBINS, EDWARD GEORGE,SHAN, BO
申请号:
ES06808621
公开号:
ES2451642T3
申请日:
2006.11.20
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of formula I: ** Formula ** or one of its salts or solvates, wherein said compound is marked with an image forming residue, and in which: X1 and X2 are independently selected from hydrogen, halogen, alkoxy C1-6, C1-6 alkyl; R1 and R2 are independently selected from C1-6 alkyl, C1-6 aminoalkyl, (C1-6 alkoxy) alkyl, C1-6 alkoxy, C1-6 hydroxyalkyl, a polyethylene glycol (PEG) group, C3-10 cycloalkyl, C3- cycloethers 10, and C3-10 cycloamines; R3 is the group -A-R5, in which: A is the optional group - (CH2) z-R6-, in which z>; = 0-6, R6 is a 5- or 6-membered heterocycle that has 1- 3 hetero atoms selected from N, S and O, and in which R 5 is a substituent selected from hydrogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkenyl, C 1-6 alkynyl, C 1-6 alkanoyl, C 1-6 haloalkyl , haloalkenyl C1-6, haloalkynyl C1-6, haloalkoxy C1-6, haloalkylthiol C1-6, haloalkylsulfinyl C1-6, haloalkylsulfonyl C1-6, haloalkyl ketone C1-6, (haloalkyl C1-6) sulfinyl, (haloalkyl C1-6 ) sulfonyl, a polyethylene glycol (PEG), hydroxy C1-6 alkyl group, a C2-10 alkyl containing nitrogen and hydroxy; R4 is hydrogen, C1-6 alkyl, C1-6 alkanoyl, C1-6 cycloalkyl, C1-6 fluoroalkyl, hydroxy, or halogen; Y1 is S, SO, SO2, or CH2; n is from 0 to 10; and wherein said remaining imaging is selected from: (i) a radioactive metal ion; (ii) a paramagnetic metal ion; (iii) a radioactive halogen emitting gamma rays; (iv) a non-metal radioactive positron emitter; (v) an active core in hyperpolarized NMR; (vi) an indicator suitable for the formation of optical images in vivo; and (vii) a β-emitter suitable for intravascular detectionUn compuesto de fórmula I:**Fórmula** o una de sus sales o solvatos, en el que dicho compuesto está marcado con un resto de formación de imágenes, yen el que: X1 y X2 se seleccionan independientemente de hidrógeno, halógeno, alcoxi C1-6, alquilo C1-6; R1 y R2 se seleccionan independientemente de alquilo C1-6, aminoalquilo C1-6, (alcoxi C1-6)alquilo, alcoxi C1-6,hidroxialquilo C1-6,
来源网站:
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