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11 条记录 (耗时 0.02 秒)

    Steroids and their preparation
    4.
    发明授权
    Steroids and their preparation 失效
    类固醇及其制备

    公开(公告)号：US4165326A

    公开(公告)日：1979-08-21

    申请号：US891722

    申请日：1978-03-30

    申请人： Roland Bardoneschi ,  Alain Jouquey ,  Daniel Philibert

    发明人： Roland Bardoneschi ,  Alain Jouquey ,  Daniel Philibert

    IPC分类号： C07J9/00

    CPC分类号： C07J9/00

    摘要： Steroids 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, R.sub.1 is selected from the group consisting of hydrogen, acryl of an alkanoic acid of 1 to 5 carbon atoms and tetrahyropyranyl and the wavy line indicates that the OR.sub.1 group may be in either position about the carbon atom and a process and intermediates for their preparation which compounds are useful as intermediates to form novel tritium compounds of the formula ##STR2## wherein R and R.sub.1 have the above definition which are useful as intermediates for the production of (6,7-H.sup.3) 17.alpha.,21-dimethyl-19-nor-.DELTA..sup.4,9 -pregnadiene-3,20-dione.

    摘要翻译： 式I的类固醇，其中R选自氢，1至4个碳原子的烷基，四氢吡喃基，三苯甲基和三甲基甲硅烷基，R 1选自氢，链烷酸的丙烯酸1 至5个碳原子和四对吡喃基，波浪线表示OR1基团可以位于碳原子的任一位置，并且其制备方法和中间体，这些化合物可用作中间体以形成式ⅩⅥ的新型氚化合物 其中R和R 1具有上述定义，其可用作制备（6,7-H3）17α，21-二甲基-19-去甲-TATA 4,9-孕二烯-3,20-二酮的中间体。

    Novel radioactive estradienes labelled with iodine
    5.
    发明授权
    Novel radioactive estradienes labelled with iodine 失效
    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。

    Novel radioactive estratrienes
    6.
    发明授权
    Novel radioactive estratrienes 失效
    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。

    Process
    8.
    发明授权
    Process 失效
    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。

    Novel steroids
    9.
    发明授权
    Novel steroids 失效
    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。

    Preparation of tri-cyclo nitriles
    10.
    发明授权
    Preparation of tri-cyclo nitriles 失效
    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。