发明公开
EP0038071A3 New unlabelled and radioactive labelled derivatives of butylamino propiophenone, their preparation, immunogens obtained from the unlabelled derivatives and a process for immunogen preparation, antisera raised using the immunogens and a method for raising antisera, a radioimmunoassay method and a test kit for use in the assay method
失效
新的非特异性和放射性标记的丁基丙烯酸衍生物，其制备，免疫衍生物获得的免疫原和免疫原制备方法，使用免疫调节剂的抗生素和用于提高抗生素的方法，放射免疫测定方法和用于测定的试剂盒 方法
- 专利标题： New unlabelled and radioactive labelled derivatives of butylamino propiophenone, their preparation, immunogens obtained from the unlabelled derivatives and a process for immunogen preparation, antisera raised using the immunogens and a method for raising antisera, a radioimmunoassay method and a test kit for use in the assay method
- 专利标题（中）： 新的非特异性和放射性标记的丁基丙烯酸衍生物，其制备，免疫衍生物获得的免疫原和免疫原制备方法，使用免疫调节剂的抗生素和用于提高抗生素的方法，放射免疫测定方法和用于测定的试剂盒 方法
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申请号： EP81102833申请日： 1981-04-13
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公开(公告)号： EP0038071A3公开(公告)日： 1981-12-23
- 发明人: Welch, Richard Martin , Butz, Robert Frederick , Scharver, Jeffrey Douglas , Phillips, Arthur Page , Mehta, Nariman Bomanshaw , Findlay, John William Addison
- 申请人： THE WELLCOME FOUNDATION LIMITED
- 专利权人： THE WELLCOME FOUNDATION LIMITED
- 当前专利权人： THE WELLCOME FOUNDATION LIMITED
- 优先权： US140157 19800414; US140159 19800414; US140606 19800415; US140158 19800414; US140160 19800414; US140165 19800414
- 主分类号： C07C97/10
- IPC分类号： C07C97/10 ; C07C131/00 ; C07C103/52 ; C07C102/04 ; G01N33/56 ; C07B23/00 ; A61K47/00
摘要：
New compounds are prepared having the formula:
wherein (1) X, is Cl, R 2 is oxygen and
R 1 is -(CH 2 ) n -OH or -(CH 2 ) n -O-(CO) m (CH 2 ) P COZ or -O-(CH 2 ) P COZ or -O-(CH 2 ) p COOR 11 or is a radioisotope or (2) X 1 is Cl, R' is Hand R' is = N . O(CH 2 ) q COZ or (3) X, is a radioisotope, R 2 is oxygen and R, is OH in the 4-position and wherein n is an integer of 1-5, m is 0 or 1, p is an integer of 1-4, q is an integer of 1-3, R 11 is a C 1 -C 3 alkyl group and Z is OH or a group of formula:
where s in an integer of 1-4, R 6 is a radioactive nuclide and R, is OH. Various methods for their preparation are described. The unlabelled compounds in which R, and R, contains a free carboxy group can be coupled with an immunogenic carrier to give an immunogen which can be used to raise antisera in host animals e.g. rabbits. This antisera contains antibodies specific to the antidepressant bupropion. This antisera can be used, together with the radioactive labelled compounds I in a radioimmunoassay method for determining bupropion in biological fluids as bupropion and the labelled analogue thereof compete for binding sites in the antisera. A test kit for use in the radioimmunoassay contains antisera, radioactive labelled compound I and optionally bupropion.
wherein (1) X, is Cl, R 2 is oxygen and
R 1 is -(CH 2 ) n -OH or -(CH 2 ) n -O-(CO) m (CH 2 ) P COZ or -O-(CH 2 ) P COZ or -O-(CH 2 ) p COOR 11 or is a radioisotope or (2) X 1 is Cl, R' is Hand R' is = N . O(CH 2 ) q COZ or (3) X, is a radioisotope, R 2 is oxygen and R, is OH in the 4-position and wherein n is an integer of 1-5, m is 0 or 1, p is an integer of 1-4, q is an integer of 1-3, R 11 is a C 1 -C 3 alkyl group and Z is OH or a group of formula:
where s in an integer of 1-4, R 6 is a radioactive nuclide and R, is OH. Various methods for their preparation are described. The unlabelled compounds in which R, and R, contains a free carboxy group can be coupled with an immunogenic carrier to give an immunogen which can be used to raise antisera in host animals e.g. rabbits. This antisera contains antibodies specific to the antidepressant bupropion. This antisera can be used, together with the radioactive labelled compounds I in a radioimmunoassay method for determining bupropion in biological fluids as bupropion and the labelled analogue thereof compete for binding sites in the antisera. A test kit for use in the radioimmunoassay contains antisera, radioactive labelled compound I and optionally bupropion.
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