Improvements in or relating to modified haptens useful as imaging and therapeutic agents
申请人:HYBRITECH INCORPORATED
公开号:EP0327365A2
公开(公告)日:1989-08-09
The present invention discloses a method for modifying the pharmacokinetics of a hapten which is useful as an in vivo radioimaging or radiotherapeutic agent. Compositions comprising a derivatized hapten of the invention are provided for in vivo imaging and therapy. A compound of Formula (I): p-R1-C6H4-CH2-EDTA-M (I) wherein R1 is
R2 is hydrogen, an amino group, -OC(̵Y), -p-phenyl-CH2-Y, an unsubstituted C1 to C30 branched or straight chain alkyl group; a substituted C1 to C30 branched or straight chain alkyl, cycloalkyl, aryl or arylalkyl group, in which the substituents are one or more of any of: hydroxy, carboxy, =O, =S,
-S-, -SR4, fluoro, chloro, bromo, iodo, amino, nitro, -S03H, -NHR3, -NHR4, -N(R3)2, -CONHR3, -COOR3, -SO4, -PO4, phenyl, benzyl, imidazolo, or a group of the formulae:
wherein R3 is hydrogen, a C1 to C30 straight or branched chain alkyl group, -p-phenyl-CH2-Y,
or a non-reactive functional group; Y is EDTA, DTPA, DOTA, HETA, TRITA or TETA; R4 is H or
and, M is a metal ion, or a pharmaceutically-acceptable salt thereof.
本发明公开了一种改变合生元药代动力学的方法,该合生元可用作体内放射成像剂或放射治疗剂。提供了包含本发明衍生化合素的用于体内成像和治疗的组合物。式 (I) 的化合物: p-R1-
C6H4-
CH2-
EDTA-M (I) 其中 R1 是
R2 是氢、
氨基、-OC(̵Y)、-p-苯基- -Y、未取代的 C1 至 C30 支链或直链烷基;取代的 C1 至 C30 支链或直链烷基、环烷基、芳基或芳烷基,其中取代基是羟基、羧基、=O、=S 中的一个或多个、
-S-、-SR4、
氟、
氯、
溴、
碘、
氨基、硝基、-S03H、-NHR3、-NHR4、-N(R3)2、-CONHR3、-COOR3、-SO4、-PO4、苯基、苄基、
咪唑基或式中的一个基团:
其中 R3 为氢、C1-C30 直链或支链烷基、-p-苯基- -Y、
或非反应性官能团;Y 是
EDTA、
DTPA、DOTA、HETA、TRITA 或 TETA;R4 是 H 或 M。
M 是
金属离子或其药学上可接受的盐。