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1. 发明授权

US4865767A Novel radioactive steroids 失效
标题翻译：新型放射性类固醇
公开(公告)号：US4865767A
公开(公告)日：1989-09-12
申请号：US797140
申请日：1985-12-19
申请人： Alain Jouquey , Daniel Philibert , Martine Moguilewsky , Jean-Noel Veltz
发明人： Alain Jouquey , Daniel Philibert , Martine Moguilewsky , Jean-Noel Veltz
IPC分类号： A61K51/00 , C07J1/00 , G01N33/534 , G01N33/74
CPC分类号： C07J1/0048 , C07J1/0011 , G01N33/534 , G01N33/743
摘要： Novel radioactive steroids labelled with tritium of the formula ##STR1## wherein .sup.3 H is tritium and R and R.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic carboxylic acid of 1 to 10 carbon atoms useful for revealing receptors of glucocorticoids and in determining the number of fixation sites of glucocorticoids and novel intermediates.
摘要翻译：新型放射性类固醇用式Ⅺ标记的氚，其中3H是氚，R和R 1分别选自氢，1至6个碳原子的烷基和1至10个碳原子的有机羧酸的酰基可用于揭示糖皮质激素受体的原子和确定糖皮质激素和新型中间体的固定位点的数量。

2. 发明授权

US4664850A Novel radioactive steroids 失效
标题翻译：新型放射性类固醇
公开(公告)号：US4664850A
公开(公告)日：1987-05-12
申请号：US620457
申请日：1984-06-14
申请人： Alain Jouquey , Daniel Philibert , Martine Moguilewsky , Jean-Noel Veltz
发明人： Alain Jouquey , Daniel Philibert , Martine Moguilewsky , Jean-Noel Veltz
IPC分类号： A61K51/00 , C07J1/00 , G01N33/534 , G01N33/74
CPC分类号： C07J1/0048 , C07J1/0011 , G01N33/534 , G01N33/743
摘要： Novel radioactive steriods labelled with tritium of the formula ##STR1## wherein .sup.3 H is tritium and R and R.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic carboxylic acid of 1 to 10 carbon atoms useful for revealing receptors of glucocorticoids and in determining the number of fixation sites on glucocorticoids and novel intermediates.
摘要翻译：新型放射性放射性标记物，其具有下式的氚：其中3H是氚，R和R 1分别选自氢，1至6个碳原子的烷基和1至10个碳的有机羧酸的酰基可用于揭示糖皮质激素受体的原子和确定糖皮质激素和新型中间体的固定位点数。

3. 发明授权

US4565876A Process 失效
标题翻译：处理
公开(公告)号：US4565876A
公开(公告)日：1986-01-21
申请号：US612606
申请日：1984-05-21
申请人： Alain Jouquey , Peter F. Hunt
发明人： Alain Jouquey , Peter F. Hunt
IPC分类号： C07J1/00 , C07C67/00 , C07C239/00 , C07C253/00 , C07C255/31 , C07C255/47 , C07C271/00 , C07J41/00 , C07J73/00 , C07J75/00 , C07D209/56
CPC分类号： C07J41/0016 , C07J73/005 , C07C2103/26
摘要： A novel process for the preparation of a 16-imino-17-aza-steroid of the formula ##STR1## wherein A is selected from the group consisting of hydrogen and tritium comprising reacting a compound of the formula ##STR2## wherein A has the above definition and R is an acyl of an organic carboxylic acid of 1 to 8 carbon atoms with an oximation agent to obtain a compound of the formula ##STR3## reacting the latter with an agent to form an acid chloride to obtain a compound of the formula ##STR4## reacting the latter with ammonia to obtain a compound of the formula ##STR5## reacting the latter with an alkali metal hypohalite in the presence of a base to obtain a compound of the formula ##STR6## wherein X is a halogen and reacting the latter with a base to obtain the desired compound and the novel compound of formula I wherein A is tritium and the novel intermediates of formulae III, IV, V and VI.
摘要翻译：一种用于制备式I的16亚氨基-17-氮杂类固醇的新方法，其中A选自氢和氚，包括使下式化合物II与式上述定义，R为具有1至8个碳原子的有机羧酸的酰基与肟化剂反应，得到下式化合物，其中后者与试剂反应形成酰氯，得到化合物 IV使后者与氨反应，得到下式的化合物，其中R 1在碱的存在下与碱金属次卤酸盐反应，得到式VI的化合物，其中X为卤素并使其与碱反应以获得所需化合物和式I的新型化合物，其中A是氚，以及式III，IV，V和VI的新型中间体。

4. 发明授权

US4191697A Novel steroids 失效
标题翻译：新型类固醇
公开(公告)号：US4191697A
公开(公告)日：1980-03-04
申请号：US915601
申请日：1978-06-15
申请人： Alain Jouquey , Jean-Pierre Raynaud , Jean Salmon
发明人： Alain Jouquey , Jean-Pierre Raynaud , Jean Salmon
IPC分类号： A61K51/00 , C07J1/00 , C07J17/00 , C07J51/00 , G01N33/534 , G01N33/60
CPC分类号： C07J1/007
摘要： Novel .DELTA..sup.1,3,5(10),6 -estratetraenes of the formula ##STR1## R is selected from the group consisting of hydrogen, acyl of an alkanoic acid of 1 to 5 carbon atoms, optionally substituted benzoyl, tetrahydropyranyl, trityl and trimethylsilyl and R.sub.1 is selected from the group consisting of acyl of an alkanoic acid of 1 to 5 carbon atoms, optionally substituted benzoyl, tetrahydropyranyl, trityl and trimethylsilyl, novel intermediates therefore, process for the preparation of estradiols marked with a tritium atom and the novel tritiated estradiols which are useful to the study and dosage of specific receptors of estrogen.
摘要翻译：新型的DELTA 1,3,5（10），式VI的6-季四烯选自氢，1至5个碳原子的链烷酸的酰基，任选取代的苯甲酰基，四氢吡喃基，三苯甲基和三三甲基甲硅烷基，R 1选自由1-5个碳原子的链烷酸酰基，任选取代的苯甲酰基，四氢吡喃基，三苯甲基和三甲基甲硅烷基组成的组，因此，新的中间体是制备标有氚原子的雌二醇的方法，氚化雌二醇可用于雌激素特异性受体的研究和剂量。

5. 发明授权

US4639336A Novel radioactive estradienes labelled with iodine 失效
标题翻译：用碘标记的新型放射性碘化物
公开(公告)号：US4639336A
公开(公告)日：1987-01-27
申请号：US620455
申请日：1984-06-14
申请人： Alain Jouquey , Jean Salmon , Michel Mouren , Gaetan Touyer
发明人： Alain Jouquey , Jean Salmon , Michel Mouren , Gaetan Touyer
IPC分类号： C07J41/00 , G01N33/534 , G01N33/74 , C07J1/00
CPC分类号： C07J41/0016 , C07J41/0083 , G01N33/534 , G01N33/743 , A61K2123/00
摘要： Novel radioactive estradienes labelled with iodine of the formula ##STR1## in the form of their syn or anti isomers or mixtures thereof wherein the wavy line indicates anti or syn position, R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic carboxylic acid of 1 to 12 carbon atoms and R.sub.1 is the residue of an amino acid R.sub.1 NH.sub.2 possessing an iodine acceptor group or a derivative thereof labelled with iodine .sup.125 or .sup.131 and their preparation and novel intermediates, antigens prepared from the compounds of formula I and bovine seric albumin or human seric albumin and their preparation and their use for the preparation of antibodies.
摘要翻译：以其顺式或反式异构体或其混合物的形式用碘标记的新型放射性碘化物，其中波浪线表示抗或顺式位置，R选自氢，1至6的烷基碳原子和碳原子数为1〜12的有机羧酸的酰基，R 1为具有用碘125或131标记的碘受体基团或其衍生物的氨基酸R 1 NH 2的残基及其制备和新型中间体，由式I化合物和牛血清白蛋白或人血清白蛋白及其制备及其用于制备抗体的用途。

6. 发明授权

US4632820A Novel radioactive estratrienes 失效
标题翻译：新型放射性三异构体
公开(公告)号：US4632820A
公开(公告)日：1986-12-30
申请号：US560184
申请日：1983-12-12
申请人： Alain Jouquey , Gaetan Touyer , Jean Salmon , Michel Mouren
发明人： Alain Jouquey , Gaetan Touyer , Jean Salmon , Michel Mouren
IPC分类号： C07J1/00 , C07J41/00 , G01N33/534 , A61K49/00 , A61K43/00
CPC分类号： C07J41/0016 , G01N33/534
摘要： Novel radioactive .DELTA..sup.4,9,11 -estratrienes marked with iodine 125 or 131 having the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic carboxylic acid of 2 to 12 carbon atoms, R.sub.1 is the reminder of an amino acid of the formula R.sub.1 NH.sub.2 or a derivative thereof being marked with iodine 125 or 131 and the wavy lines indicate the --OR is in the .alpha.- or .beta.-position and the oximido group is in the syn or anti position, a process and intermediates for their preparation, antigens prepared therefrom and use thereof to prepare antibodies.
摘要翻译：用碘125或131标记的新型放射性DELTA 4,9,11-雌三醇，其具有式I图1其中R选自氢，1至6个碳原子的烷基和2位有机羧酸的酰基至12个碳原子，R1是式R1NH2的氨基酸或其衍生物用碘125或131标记的波形，波浪线表示-OR为α或β-位，肟基为在syn或反位置，其制备方法和中间体，由其制备的抗原及其制备抗体的用途。

7. 发明授权

US4152325A Novel steroids and their use 失效
标题翻译：新颖的甾体及其使用
公开(公告)号：US4152325A
公开(公告)日：1979-05-01
申请号：US855177
申请日：1977-11-28
申请人： Alain Jouquey , Andre Pierdet
发明人： Alain Jouquey , Andre Pierdet
IPC分类号： A61K51/00 , C07J1/00 , C07J7/00 , C07J9/00 , C07J17/00 , G01N33/53 , G01N33/534 , C07J71/00
CPC分类号： C07J1/0081 , C07J1/0096 , C07J17/00 , C07J7/0045 , C07J9/00
摘要： Novel pregnatetraenes of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, tetrahydropyranyl, trityl and trimethylsilyl and intermediates therefore and a process for their preparation and a process for the preparation of tritium labelled steroids.

8. 发明授权

US4661295A Novel radioactive estradienes 失效
标题翻译：新型放射性染料
公开(公告)号：US4661295A
公开(公告)日：1987-04-28
申请号：US620454
申请日：1984-06-14
申请人： Alain Jouquey , Jean-Noel Veltz , Jean Salmon , Michel Mouren
发明人： Alain Jouquey , Jean-Noel Veltz , Jean Salmon , Michel Mouren
IPC分类号： G01N33/53 , A61K51/00 , A61K51/04 , C07J1/00 , C07J9/00 , C07J21/00 , C07J41/00 , C07J43/00 , G01N33/534 , G01N33/74
CPC分类号： A61K51/0493 , C07J41/0016 , C07J41/0083 , G01N33/534 , G01N33/743 , A61K2123/00
摘要： Novel radioactive estradienes labelled with tritium of the formula ##STR1## wherein .sup.3 H is tritium and R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic carboxylic acid of 1 to 10 carbon atoms and the study and radioimmunological determination of non-radioactive 11.beta.-(4-dimethylaminophenyl)-17.alpha.-(prop-1-ynyl)-.DELTA..sup.4,9 -estradiene-17.beta.-ol-3-one and its metabolites in biological fluids and novel intermediates.
摘要翻译：用式Ⅺ标示的氚的新型放射性碘化物，其中3H是氚，R选自氢，1至6个碳原子的烷基和1至10个碳原子的有机羧酸的酰基，研究和放射免疫测定非放射性11β-（4-二甲基氨基苯基）-17α-（丙-1-炔基）-TATA 4,9-雌二烯-17β-醇-3-酮及其在生物液体中的代谢物和新颖的中间体。

9. 发明授权

US4591461A Preparation of tri-cyclo nitriles 失效
标题翻译：三环腈的制备
公开(公告)号：US4591461A
公开(公告)日：1986-05-27
申请号：US791773
申请日：1985-10-28
申请人： Alain Jouquey , Peter F. Hunt
发明人： Alain Jouquey , Peter F. Hunt
IPC分类号： C07J1/00 , C07C67/00 , C07C239/00 , C07C253/00 , C07C255/31 , C07C255/47 , C07C271/00 , C07J41/00 , C07J73/00 , C07J75/00 , C07C121/46 , C07C121/47
CPC分类号： C07J41/0016 , C07J73/005 , C07C2103/26
摘要： A novel process for the preparation of a 16-imino-17-aza-steroid of the formula ##STR1## wherein A is selected from the group consisting of hydrogen and tritium comprising reacting a compound of the formula ##STR2## wherein A has the above definition and R is an acyl of an organic carboxylic acid of 1 to 8 carbon atoms with an oximation agent to obtain a compound of the formula ##STR3## reacting the latter with an agent to form an acid chloride to obtain a compound of the formula ##STR4## reacting the latter with ammonia to obtain a compound of the formula ##STR5## reacting the latter with an alkali metal hypohalite in the presence of a base to obtain a compound of the formula ##STR6## wherein X is a halogen and reacting the latter with a base to obtain the desired compound and the novel compound of formula I wherein A is tritium and the novel intermediates of formulae III, IV, V and VI.
摘要翻译：一种用于制备式I的16亚氨基-17-氮杂类固醇的新方法，其中A选自氢和氚，包括使下式化合物II与式上述定义，R为具有1至8个碳原子的有机羧酸的酰基与肟化剂反应，得到下式化合物，其中后者与试剂反应形成酰氯，得到化合物 IV使后者与氨反应，得到下式的化合物，其中R 1在碱的存在下与碱金属次卤酸盐反应，得到式VI的化合物，其中X为卤素并使其与碱反应以获得所需化合物和式I的新型化合物，其中A是氚，以及式III，IV，V和VI的新型中间体。

10. 发明授权

US4529713A Radioactive stilbene derivatives in radioimmunoassay 失效
标题翻译：放射免疫测定中的放射性二苯乙烯衍生物
公开(公告)号：US4529713A
公开(公告)日：1985-07-16
申请号：US390938
申请日：1982-06-22
申请人： Alain Jouquey , Gaetan Touyer
发明人： Alain Jouquey , Gaetan Touyer
IPC分类号： C07C59/68 , C07D233/54 , C07D233/64 , C07D233/68 , G01N33/531 , G01N33/60 , G01N33/56
CPC分类号： C07D233/64 , C07C59/68 , G01N33/531 , G01N33/60 , Y10S436/804
摘要： Novel radioactive stilbene derivatives marked with iodine 125 or 131 of the formula ##STR1## wherein each A and B are both hydrogen or together form a double bond and R is the remainder of amino acid of the formula R--NH.sub.2 or a derivative thereof possessing an iodine acceptor group and marked with iodine 125 or 131 and their preparation and antigens obtained therefrom and a process for preparing said antigens.
摘要翻译：新颖的放射性二苯乙烯衍生物用碘化合物125或131表示，其中每个A和B都是氢或一起形成双键，R是式R-NH 2的氨基酸的剩余部分或其衍生物具有碘受体组，并用碘125或131标记，其制备和抗原获得，以及制备所述抗原的方法。

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