[EN] CANCER CELL SPECIFIC IMAGING PROBES AND METHODS OF USE<br/>[FR] SONDES D'IMAGERIE SPÉCIFIQUES DE CELLULE CANCÉREUSE ET PROCÉDÉS D'UTILISATION
申请人:RES FOUNDATION FOR THE STATE UNIVERISTY OF NEW YORK
公开号:WO2015021305A1
公开(公告)日:2015-02-12
The present invention provides a compound having the structure: wherein X is an imaging agent containing at least one amine nitrogen; Y is a chemical linker, wherein Y is present or absent, and when present Y is a chemical linker containing at least one amine nitrogen or Y is a para-aminobenzyl alcohol linker; Z is CH3 or CF3 ; R1 is -H, -NR2R3, -NH-C(=0) -R4, -NH-C ( =0) -OR4, -CH2-C ( =0) -NR5R6, - OR7, -CO2R7, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, aryl, or heteroaryl, wherein R2, R3, R4, R5, R6 and R7are each, independently, - H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, heteroalkyl, cycloalkyl, heterocyclyl, aryl, aikylaryl, heteroaryl, alkylheteroaryl, an amino acid or an oligopeptide; wherein an amine of the amino acid or oligopeptide is substituted or unsubstituted; and n is an integer from 0 to 6; or a diastereomer, enantiomer or pharmaceutically acceptable salt of the compound.
本发明提供了一种化合物,其结构为:其中X是含有至少一个胺氮的成像剂;Y是化学连接剂,其中Y存在或不存在,当Y存在时,Y是含有至少一个胺氮的化学连接剂或Y是对氨基苯甲醇连接剂;Z是CH3或CF3;R1是-H、-NR2R3、-NH-C(=0)-R4、-NH-C(=0)-OR4、-CH2-C(=0)-NR5R6、-OR7、-CO2R7、C1-6烷基、C2-6烯基、C2-6炔基、芳基或杂环芳基,其中R2、R3、R4、R5、R6和R7分别是独立的-H、C1-6烷基、C2-6烯基、C2-6炔基、杂原子烷基、环烷基、杂环烷基、芳基、烷基芳基、杂环芳基、烷基杂环芳基、氨基酸或寡肽;其中氨基酸或寡肽的胺基被取代或未取代;n是从0到6的整数;或化合物的对映异构体、对映体或药学上可接受的盐。