Labelled Quinoxaline Derivatives as Multimodal Radiopharmaceuticals and Their Precursors

摘要

The present invention relates to the compound of formula (I), in which R1 represents Sn(R)3, B(OH)2, B(OR)2, a halogen atom, NO2, a radionuclide or a —N+(R)3 group, where R is a (C1-C6) alkyl group, R2 represents a hydrogen atom or a (C1-C6)alkyl group, R3 represents: a —(CH2CH2O)n2—(CH2)n3—X group, or a —(CH2CH2O)n4—(CH2)n5—Y group with Y representing a —C═C—H, a —N3 or a —Ar—(CH2)n6—(OCH2CH2)n7—X group, and X represents a halogen atom, a radionuclide or a —OSO2R′ group, where R′ is a CF3, CH3, t-Bu, Ph, p-NO2Ph, p-BrPh or p-CH3Ph group, and their addition salts with pharmaceutically acceptable acids, The present invention also relates to pharmaceutical compositions comprising them and to their use in diagnosis, in particular with SPECT or PET imaging and in therapy of melanoma, via targeted radionuclide therapy.;

主权项

1. Compound of formula (I): in which R1 represents Sn(R)3, B(OH)2, B(OR)2, a halogen atom, NO2, a radionuclide or a —N+(R)3 group, where R is a (C1-C6) alkyl group, n1 is an integer varying from 1 to 4, R2 represents a hydrogen atom or a (C1-C6)alkyl group, R3 represents:
a —(CH2CH2O)n2—(CH2)n3—X group, where n2 is an integer varying from 1 to 12 and n3 is an integer varying from 1 to 4, ora (CH2CH2O)n4—(CH2)n5—Y group with n4 representing an integer varying from 0 to 12, n5 representing an integer from 1 to 4, and Y representing a —C≡C—H, a —N3 or a —Ar—(CH2)6—(OCH2CH2)n7—X group with Ar beingn6 representing an integer varying from 1 to 4 and n7 an integer varying from 0 to 12, and
X represents a halogen atom, a radionuclide or a —OSO2R′ group, where R′ is a CF3, CH3, t-Bu, Ph, p-NO2Ph, p-BrPh or p-CH3Ph group, and their addition salts with pharmaceutically acceptable acids.