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公开(公告)号：US5010088A
公开(公告)日：1991-04-23
申请号：US398219
申请日：1989-08-24
IPC分类号： C07D215/22 , A61K31/47 , A61P9/00 , A61P9/10 , C07D215/38 , C07D401/04
CPC分类号： C07D401/04
摘要： The present invention is concerned with the compound of formula (I) ##STR1## and esters and acid addition salts thereof having positive inotrope effect.
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公开(公告)号：US4356165A
公开(公告)日：1982-10-26
申请号：US140158
申请日：1980-04-14
IPC分类号： A61K47/48 , A61K51/04 , C07C45/00 , C07C45/54 , C07C45/56 , C07D263/04 , C07D263/10 , G01N33/56 , B65D71/00 , G01N33/60
CPC分类号： C07D263/10 , A61K47/4833 , A61K51/0406 , C07C255/00 , C07C45/00 , C07C45/54 , C07C45/56 , C07D263/04
摘要： A radioimmunoassay proceedure has been discovered for bupropion [(.+-.)-2-t-butylamino-3-chloropropiophenone], an antidepressant compound, in biological fluids. Novel compounds of formula ##STR1## wherein either R.sub.2 is oxygen and R.sub.1 is (CH.sub.2).sub.n --O--(CO).sub.m --(CH.sub.2).sub.p --COOH where n is an integer from 0 to 5, m is 0 or 1, and p is an integer from 1 to 4; or R.sub.1 is hydrogen and R.sub.2 is N--O--(CH.sub.2).sub.q --COOH where Q is an integer from 1 to 3, and novel methods of making them and novel intermediates useful therein are disclosed. Novel immunogens for raising bupropion specific antisera, and novel methods of making them are disclosed comprising conjugates of the novel compounds and suitable carrier material. The drug is added to the antisera together with novel radiolabeled competitor of formula ##STR2## wherein R' is a suitable radioisotope as described above and R.sub.3 is hydrogen, R.sub.4 is Cl, and R.sub.5 is oxygen, orR' is hydrogen and either(a) R.sub.3 is H and R.sub.4 is Cl and R.sub.5 is NO(CH.sub.2).sub.q CO-X where q is as defined for formula I and X is a group having formula III ##STR3## wherein R.sub.6 is a suitable radioisotope as described above, R.sub.7 is hydroxyl, and s is an integer from 1 to 4;(b) R.sub.4 is Cl, R.sub.5 is oxygen, and R.sub.3 is (CH.sub.2).sub.n --O--(CO).sub.m --(CH.sub.2).sub.p --CO--X where n, m, and p are as defined for formula I and X is as defined above; or(c) R.sub.3 is hydroxy, R.sub.5 is oxygen and R.sub.4 is a suitable radioisotope as defined above. The measure of radioactivity of the antisera bound radiolabeled competitor provides a measure of the amount of drug in the assayed biological fluid sample. A standard curve can be constructed from which the amount of drug in the assay sample can be interpolated. A kit is disclosed for practicing the radioimmunoassay.
摘要翻译： 已经发现了用于生物液体中的安非他酮[（+/-） - 2-叔丁基氨基-3-氯苯丙酮]的放射免疫测定法，一种抗抑郁药。 式（IMA）的新型化合物，其中R2是氧，R1是（CH2）nO-（CO）m-（CH2）p-COOH，其中n是0-5的整数，m是0或1，p是 1到4的整数; 或R 1为氢，R 2为N-O-（CH 2）q -COOH，其中Q为1至3的整数，并且公开了制备它们的新方法和可用于其中的新型中间体。 公开了用于提高安非他酮特异性抗血清的新型免疫原及其制备方法，其包括新化合物和合适的载体材料的缀合物。 将药物与新的放射性标记的式（IMAGE）竞争剂一起加入到抗血清中，其中R'是如上所述的合适的放射性同位素，R 3是氢，R 4是Cl，R 5是氧，或者R'是氢， ）R3是H，R4是Cl，R5是NO（CH2）qCO-X，其中q如式I所定义，X是具有式III的基团，其中R6是如上所述的合适的放射性同位素，R7是 羟基，s为1至4的整数; （b）R4是Cl，R5是氧，R3是（CH2）nO-（CO）m-（CH2）p-CO-X，其中n，m和p如式I所定义，X如上定义 以上; 或（c）R3是羟基，R5是氧，R4是如上定义的合适的放射性同位素。 抗血清结合的放射性标记的竞争者的放射性测量值提供测定的生物流体样品中药物的量的量度。 可以构建标准曲线，由此可以插入测定样品中的药物量。 公开了用于实施放射免疫测定的试剂盒。
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公开(公告)号：US4355179A
公开(公告)日：1982-10-19
申请号：US140165
申请日：1980-04-14
IPC分类号： A61K47/48 , A61K51/04 , C07C45/00 , C07C45/54 , C07C45/56 , C07D263/04 , C07D263/10 , C07C103/30 , C07G7/00 , G01N33/54
CPC分类号： C07D263/10 , A61K47/4833 , A61K51/0406 , C07C255/00 , C07C45/00 , C07C45/54 , C07C45/56 , C07D263/04
摘要： A radioimmunoassay procedure has been discovered for bupropion [(.+-.)-2-t-butylamino-3-chloropropiophenone], an antidepressant compound, in biological fluids. Novel compounds of formula ##STR1## wherein either R.sub.2 is oxygen and R.sub.1 is (CH.sub.2).sub.n --O--(CO).sub.m --(CH.sub.2).sub.p --COOH where n is an integer from 0 to 5, m is 0 or 1, and p is an integer from 1 to 4; or R.sub.1 is hydrogen and R.sub.2 is N--O--(CH.sub.2).sub.q --COOH where q is an integer from 1 to 3, and novel methods of making them and novel intermediates useful therein are disclosed. Novel immunogens for raising bupropion specific antisera, and novel methods of making them are disclosed comprising conjugates of the novel compounds and suitable carrier material. The drug is added to the antisera together with novel radiolabeled competitor of formula ##STR2## wherein R' is a suitable radioisotope as described above and R.sub.3 is hydrogen, R.sub.4 is Cl, and R.sub.5 is oxygen, orR' is hydrogen and either(a) R.sub.3 is H and R.sub.4 is Cl and R.sub.5 is NO(CH.sub.2).sub.q CO--X where q is as defined for formula I and X is a group having formula III ##STR3## wherein R.sub.6 is a suitable radioisotope as described above, R.sub.7 is hydroxyl, and s is an integer from 1 to 4;(b) R.sub.4 is Cl, R.sub.5 is oxygen, and R.sub.3 is (CH.sub.2).sub.n --0--(CO).sub.m --(CH.sub.2).sub.p --CO--X where n, m, and p are as defined for formula I and X is as defined above; or(c) R.sub.3 is hydroxy, R.sub.5 is oxygen and R.sub.4 is a suitable radioisotope as defined above.The measure of radioactivity of the antisera bound radiolabeled competitor provides a measure of the amount of drug in the assayed biological fluid sample. A standard curve can be constructed from which the amount of drug in the assay sample can be interpolated. A kit is disclosed for practicing the radioimmunoassay.
摘要翻译： 已经发现了用于生物液体中的安非他酮[（+/-） - 2-叔丁基氨基-3-氯苯丙酮]（一种抗抑郁药）的放射免疫测定方法。 式（IMA）的新型化合物，其中R2是氧，R1是（CH2）nO-（CO）m-（CH2）p-COOH，其中n是0-5的整数，m是0或1，p是 1到4的整数; 或R 1为氢，R 2为N-O-（CH 2）q-COOH，其中q为1至3的整数，并且公开了制备它们的新方法和可用于其中的新型中间体。 公开了用于提高安非他酮特异性抗血清的新型免疫原及其制备方法，其包括新化合物和合适的载体材料的缀合物。 将药物与新的放射性标记的式（IMAGE）竞争剂一起加入到抗血清中，其中R'是如上所述的合适的放射性同位素，R 3是氢，R 4是Cl，R 5是氧，或者R'是氢， ）R3是H，R4是Cl，R5是NO（CH2）qCO-X，其中q如式I所定义，X是具有式III的基团，其中R6是如上所述的合适的放射性同位素，R7是 羟基，s为1至4的整数; （b）R4是Cl，R5是氧，R3是（CH2）n-O-（CO）m-（CH2）p-CO-X，其中n，m和p如式I所定义，X是 如上所述; 或（c）R3是羟基，R5是氧，R4是如上定义的合适的放射性同位素。 抗血清结合的放射性标记的竞争者的放射性测量值提供测定的生物流体样品中药物的量的量度。 可以构建标准曲线，由此可以插入测定样品中的药物量。 公开了用于实施放射免疫测定的试剂盒。
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公开(公告)号：US4347178A
公开(公告)日：1982-08-31
申请号：US140160
申请日：1980-04-14
IPC分类号： A61K47/48 , A61K51/04 , C07C45/00 , C07C45/54 , C07C45/56 , C07D263/04 , C07D263/10 , C07C123/00 , C07C131/00 , G01N33/54
CPC分类号： C07D263/10 , A61K47/4833 , A61K51/0406 , C07C255/00 , C07C45/00 , C07C45/54 , C07C45/56 , C07D263/04 , Y10S436/804 , Y10S436/822 , Y10S530/806
摘要： A radioimmunoassay procedure has been discovered for bupropion [(.+-.)-2-t-butylamino-3-chloropropiophenone], an antidepressant compound, in biological fluids. Novel compounds of formula ##STR1## wherein either R.sub.2 is oxygen and R.sub.1 is (CH.sub.2).sub.n -O-(CO).sub.m -(CH.sub.2).sub.p -COOH where n is an integer from 0 to 5, m is 0 or 1, and p is an integer from 1 to 4; or R.sub.1 is hydrogen and R.sub.2 is N-O-(CH.sub.2).sub.q -COOH where q is an integer from 1 to 3, and novel methods of making them and novel intermediates useful therein are disclosed. Novel immunogens for raising bupropion specific antisera, and novel methods of making them are disclosed comprising conjugates of the novel compounds and suitable carrier material. The drug is added to the antisera together with novel radiolabeled competitor of formula ##STR2## wherein R' is a suitable radioisotope as described above and R.sub.3 is hydrogen, R.sub.4 is Cl, and R.sub.5 is oxygen, or R' is hydrogen and either(a) R.sub.3 is H and R.sub.4 is Cl and R.sub.5 is NO(CH.sub.2).sub.q CO-X where q is as defined for formula I and X is a group having formula III ##STR3## wherein R.sub.6 is a suitable radioisotope as described above, R.sub.7 is hydroxyl, and s is an integer from 1 to 4;(b) R.sub.4 is Cl, R.sub.5 is oxygen, and R.sub.3 is (CH.sub.2).sub.n -O-(CO).sub.m -(CH.sub.2).sub.p -CO-X where n, m, and p are as defined for formula I and X is as defined above; or(c) R.sub.3 is hydroxy, R.sub.5 is oxygen and R.sub.4 is a suitable radioisotope as defined above.The measure of radioactivity of the antisera bound radiolabeled competitor provides a measure of the amount of drug in the assayed biological fluid sample. A standard curve can be constructed from which the amount of drug in the assay sample can be interpolated. A kit is disclosed for practicing the radioimmunoassay.
摘要翻译： 已经发现了用于生物液体中的安非他酮[（+/-） - 2-叔丁基氨基-3-氯苯丙酮]（一种抗抑郁药）的放射免疫测定方法。 式（IMA）的新型化合物，其中R2是氧，R1是（CH2）nO-（CO）m-（CH2）p-COOH，其中n是0-5的整数，m是0或1，p是 1到4的整数; 或R 1为氢，R 2为N-O-（CH 2）q-COOH，其中q为1至3的整数，并且公开了制备它们的新方法和可用于其中的新型中间体。 公开了用于提高安非他酮特异性抗血清的新型免疫原及其制备方法，其包括新化合物和合适的载体材料的缀合物。 将药物与新的放射性标记的式（IMAGE）竞争剂一起加入到抗血清中，其中R'是如上所述的合适的放射性同位素，R 3是氢，R 4是Cl，R 5是氧，或者R'是氢， ）R3是H，R4是Cl，R5是NO（CH2）qCO-X，其中q如式I所定义，X是具有式III的基团，其中R6是如上所述的合适的放射性同位素，R7是 羟基，s为1至4的整数; （b）R4是Cl，R5是氧，R3是（CH2）nO-（CO）m-（CH2）p-CO-X，其中n，m和p如式I所定义，X如上定义 以上; 或（c）R3是羟基，R5是氧，R4是如上定义的合适的放射性同位素。 抗血清结合的放射性标记的竞争者的放射性测量值提供测定的生物流体样品中药物的量的量度。 可以构建标准曲线，由此可以插入测定样品中的药物量。 公开了用于实施放射免疫测定的试剂盒。
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