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Benzo 1,2,5 oxadiazole and benzo 1,2,5 thiadiazole useful as histopathological stains, contrast agents and biomarkers

机译:苯并[1,2,5]恶二唑和苯并[1,2,5]噻二唑可用作组织病理学染色剂,造影剂和生物标志物

摘要

The present invention relates to novel benzo[1,2,5]oxadiazoles and benzo[1,2,5]thiadiazoles of formula (I) wherein X is O or S, R1 is 5-(2-fluoro-ethylamino)-thiazol-2-yl, 5-(2-18F-ethylamino)-thiazol-2-yl or a group of formula (a) wherein Y is CH or N, R2 is NHCH3, NH11CH3, N(CH3)11CH3, N(CH3)2, N(11CH3)2, NH(CH2)nF, NH(CH2)n18F, N(CH3)(CH2)nF, N(CH3)-(CH2)n18F, O-(CH2)nF, O-(CH2)n18F, CONH(CH2)nF or CONH(CH2)n18F (n being in each case 2 to 4) and R3 is hydroxy, (C1-4)alkoxy, hydrogen or nitro, in free base or acid addition salt form; their preparation, their use as markers in diagnosis and compositions containing them.
机译:本发明涉及式(I)的新型苯并[1,2,5]恶二唑和苯并[1,2,5]噻二唑,其中X是O或S,R1是5-(2-氟-乙基氨基)-噻唑-2-基,5-(2-18F-乙基氨基)-噻唑-2-基或其中Y为CH或N,R2为NHCH3,NH11CH3,N(CH3)11CH3,N(CH3 )2,N(11CH3)2,NH(CH2)nF,NH(CH2)n18F,N(CH3)(CH2)nF,N(CH3)-(CH2)n18F,O-(CH2)nF,O-( CH 2)n 18 F,CONH(CH 2)n F或CONH(CH 2)n 18 F(n分别为2-4),并且R 3为羟基,(C1-4)烷氧基,氢或硝基,呈游离碱或酸加成盐形式;它们的制备,它们在诊断中的标记以及包含它们的组合物的用途。

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