公开(公告)号：EP0327365B1

公开(公告)日：1994-06-15

申请号：EP89301012.4

申请日：1989-02-02

申请人： HYBRITECH INCORPORATED

发明人： Anderson, Leslie DeRiemer ,  Frincke, James Martin ,  Meyer, Damon Lawrence ,  Sullivan, Brian William ,  Battersby, Thomas Robert ,  Kusnierz, Edward

IPC分类号： C07C335/04 ,  A61K31/17 ,  A61K49/02 ,  A61K43/00

CPC分类号： C07C335/22 ,  A61K51/048 ,  A61K51/1093 ,  A61K2121/00 ,  A61K2123/00 ,  C07C237/06 ,  C07C323/60 ,  C07C335/20

公开(公告)号：EP0327365A3

公开(公告)日：1990-09-26

申请号：EP89301012.4

申请日：1989-02-02

申请人： HYBRITECH INCORPORATED

发明人： Anderson, Leslie DeRiemer ,  Frincke, James Martin ,  Meyer, Damon Lawrence ,  Sullivan, Brian William ,  Battersby, Thomas Robert ,  Kusnierz, Edward

IPC分类号： C07C335/04 ,  A61K31/17 ,  A61K49/02 ,  A61K43/00

CPC分类号： C07C335/22 ,  A61K51/048 ,  A61K51/1093 ,  A61K2121/00 ,  A61K2123/00 ,  C07C237/06 ,  C07C323/60 ,  C07C335/20

摘要： 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-R 1 -C 6 H 4 -CH 2 -EDTA-M (I) wherein R 1 is
R 2 is hydrogen, an amino group, -OC(̵Y), -p-phenyl-CH 2 -Y, an unsubstituted C 1 to C 30 branched or straight chain alkyl group; a substituted C 1 to C 30 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-, -SR 4 , fluoro, chloro, bromo, iodo, amino, nitro, -S0 3 H, -NHR 3 , -NHR 4 , -N(R 3 ) 2 , -CONHR 3 , -COOR 3 , -SO 4 , -PO 4 , phenyl, benzyl, imidazolo, or a group of the formulae:
wherein R 3 is hydrogen, a C 1 to C 30 straight or branched chain alkyl group, -p-phenyl-CH 2 -Y,
or a non-reactive functional group; Y is EDTA, DTPA, DOTA, HETA, TRITA or TETA; R 4 is H or
and, M is a metal ion, or a pharmaceutically-acceptable salt thereof.

公开(公告)号：EP0327365A2

公开(公告)日：1989-08-09

申请号：EP89301012.4

申请日：1989-02-02

申请人： HYBRITECH INCORPORATED

发明人： Anderson, Leslie DeRiemer ,  Frincke, James Martin ,  Meyer, Damon Lawrence ,  Sullivan, Brian William ,  Battersby, Thomas Robert ,  Kusnierz, Edward

IPC分类号： C07C335/04 ,  A61K31/17 ,  A61K49/02 ,  A61K43/00

CPC分类号： C07C335/22 ,  A61K51/048 ,  A61K51/1093 ,  A61K2121/00 ,  A61K2123/00 ,  C07C237/06 ,  C07C323/60 ,  C07C335/20

摘要： 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-R 1 -C 6 H 4 -CH 2 -EDTA-M (I) wherein R 1 is


R 2 is hydrogen, an amino group, -OC(̵Y), -p-phenyl-CH 2 -Y, an unsubstituted C 1 to C 30 branched or straight chain alkyl group; a substituted C 1 to C 30 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-, -SR 4 , fluoro, chloro, bromo, iodo, amino, nitro, -S0 3 H, -NHR 3 , -NHR 4 , -N(R 3 ) 2 , -CONHR 3 , -COOR 3 , -SO 4 , -PO 4 , phenyl, benzyl, imidazolo, or a group of the formulae:
wherein R 3 is hydrogen, a C 1 to C 30 straight or branched chain alkyl group, -p-phenyl-CH 2 -Y,
or a non-reactive functional group; Y is EDTA, DTPA, DOTA, HETA, TRITA or TETA; R 4 is H or
and, M is a metal ion, or a pharmaceutically-acceptable salt thereof.

摘要翻译： 本发明公开了一种可用作体内放射成像或放射治疗剂的半抗原的药代动力学的方法。 提供包含本发明的衍生化半抗原的组合物用于体内成像和治疗。 式（I）的化合物：其中R 1是-NH-，-NH-R 2，-NHR 2，-NH-，-CH 2 -R 2， - NH-，-CH 2 -NH-R 2，-NH-R 2，-NH-， - NH-R 2或-NH- @ -CH 2 -S-R 2; R2是氢，氨基，-OC-Y），对苯基-CH2-Y，未取代的C1至C30支链或直链烷基; 取代基为C 1〜C 30支链或直链烷基，环烷基，芳基或芳烷基，其中取代基为羟基，羧基，= O，= S， S，-SR 4，氟，氯，溴，碘，氨基，硝基，-SO 3 H，-NHR 3，-NHR 4，-N（R 3）2，-CONHR 3，-COOR 3，-SO 4，-PO 4，苯基， 咪唑基或下式的基团：-NH-，= NH-R3，-NH-，-NH-R3或NH-; -NH-R3; 其中R 3为氢，C 1至C 30直链或支链烷基，对苯基-CH 2 -Y 1 - ，-CH 3或非反应性官能团; Y是EDTA，DTPA，DOTA，HETA，TRITA或TETA; R 4是H或-CH 2 - ; -NHR 3; M是金属离子或其药学上可接受的盐。