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    Prostaglandins
    4.
    发明公开
    Prostaglandins 失效
    前列腺素

    公开(公告)号：EP0043292A3

    公开(公告)日：1982-12-15

    申请号：EP81303000

    申请日：1981-07-01

    申请人： NATIONAL RESEARCH DEVELOPMENT CORPORATION

    发明人： Jones, Robert Leslie ,  Wilson, Norman Happer

    IPC分类号： C07C177/00 ,  C07D493/08 ,  C07C175/00 ,  C07C109/12 ,  C07C109/14 ,  C07C109/16 ,  C07C133/02 ,  C07C159/00 ,  C07C143/825 ,  C07C131/00 ,  A61K31/557

    CPC分类号： C07D493/08 ,  C07C45/305 ,  C07C45/44 ,  C07C47/225 ,  C07C47/47 ,  C07C57/26 ,  C07C251/72 ,  C07C403/20 ,  C07C405/0041 ,  C07C405/0066 ,  C07C405/0091 ,  C07C2601/16 ,  C07C47/198

    摘要： Novel compounds have a formula (I)
    wherein
    represents a bicyclo (2,2,1) hept-2Z-ene, bicyclo (2,2,1) heptane, 7-oxabicyclo (2,2,1) hept-2Z-ene, 7-oxabicyclo (2,2,1) heptane, bicyclo (2,2,2) oct-2Z-ene or bicyclo (2,2,2) octane substituted at the 5-position by the group R 1 and at the 6-position by the group C(R 2 )=NR, a 6,6-dimethyl-bicyclo (3,1,1) heptane substituted at the 5- position by the group R' and at the 6-position by the group C(R 2 )=NR or at the 5-position by the group C(R 2 )=NR and at the 6-position by the group R 1 , a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R 1 and at the 5-position by the group C(R 2 )=NR, or a 1-hydroxycyclopentane substituted at the 2-position by the group R 1 and at the 2-position by the group C(R 2 )=NR, R 1 is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein, R 2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R is a group -OR 3 , -OR 4 , -A-R 3 or -N=R 5 in which A is -NH-, -NH.CO-, -NH.CO.CH 2 N(R 6 )-, -NH.SO 2 -, -NH.CO.NH or -NH.CS.NH- and wherein R 3 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, R 4 is an aliphatic hydrocarbon group which is substituted through an oxygen atom by an aliphatic hydrocarbon group which is itself substituted by an aromatic group, R 5 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, and R 6 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly or through an oxygen or sulphur atom by an aromatic group, with the proviso that when R is a group -OR 3 , -NH.COR 3 or-NH.CO.NHR3 then excludes bicyclo (2,2,1) hept-2Z-enes and bicyclo (2,2,1) heptanes. The compounds are of value for use in phar. maceutical compositions particularly in the context of the inhibition of thromboxane activity.

    摘要翻译： 新化合物具有式（I）表示双环[2,2,1]庚-2Z-烯，双环[2,2,1]庚烷，7-氧杂双环[2,2,1]庚-2 - 烯基，7-氧杂二环[2,2,1]庚烷，双环[2,2,2]辛-2Z-烯或在5位被基团R 1取代的双环[2,2,2]辛烷 并且在C（R 2）= NR基团的6位上，在5位被基团R 1取代的6,6-二甲基 - 双环[3,1,1]庚烷和 在C（R 2）= NR基的6-位上或在C（R 2）= NR基的5位，在6位由基团R 1取代，a 环己-1-烯或环己基在4-位被基团R 1取代，在5-位被C（R 2）= NR取代，或在2-位取代的1-羟基环戊烷 通过基团R 1和基团C（R 2）= NR的2-位，R 1是如本文所定义的6-羧基己-2-烯基或其修饰， 2>是氢，脂族烃基或脂族烃基直接或通过氧或磺取代 R 1是-OR 3，-OR 4，-AR 3或-N = R 5，其中A是-NH-，-CH.CO- ，-NH.CO.CH 2 N（R 6） - ， - NHS 2 - ， - NH.CO.NH或-NH.CS.NH-，并且其中R 3是脂族烃基，芳族基团 或通过芳族基团直接或通过氧或硫原子取代的脂族烃基，R 4是脂族烃基，其被本身被芳基取代的脂族烃基经氧原子取代，R 5是脂肪族烃基，芳香族基团或脂肪族烃基，其被芳基直接或者被氧原子或硫原子取代，R 6是氢，脂肪族烃基，芳香族基团或脂肪族烃基 烃基直接或通过芳族基团通过氧或硫原子取代，条件是当R为基团-OR 3，-NHCOR 3或-NH.CO.NHR 3时， CHEM>不包括双环[2,2,1]庚-2Z-en es和双环[2,2,1]庚烷。 这些化合物在药物组合物中是有用的，特别是在抑制血栓素活性的情况下。

    Preparation of alkyl thiosemicarbazides
    7.
    发明公开
    Preparation of alkyl thiosemicarbazides 失效
    烷基硫代氨基甲酸酯的制备

    公开(公告)号：EP0308225A3

    公开(公告)日：1990-01-10

    申请号：EP88308542.5

    申请日：1988-09-15

    申请人： ICI AMERICAS INC.

    发明人： Bright, Danielle Angrand

    IPC分类号： C07C159/00

    CPC分类号： C07C337/06 ,  C07C331/16

    摘要： The present invention relates to a process for the preparation of alkyl semicarbazides by reaction of a dithiocarbamate and hydrazine in a weakly basic reaction media using a metal rearrangement catalyst.

    摘要翻译： 本发明涉及通过使用金属重排催化剂在弱碱性反应介质中使二硫代氨基甲酸铵和肼反应制备烷基氨基脲的方法。

    Preparation of radiolabeled conjugates
    8.
    发明公开
    Preparation of radiolabeled conjugates 失效
    on。。。。。。。。。。。。。

    公开(公告)号：EP0306168A1

    公开(公告)日：1989-03-08

    申请号：EP88307510.3

    申请日：1988-08-12

    申请人： IMMUNOMEDICS, INC.

    发明人： Wu, Robert Sundoro

    IPC分类号： C07B59/00 ,  A61K43/00 ,  A61K49/02 ,  C07C159/00

    CPC分类号： C07D207/404 ,  A61K51/04 ,  A61K51/1093 ,  A61K2121/00

    摘要： A method is provided for preparing a radiolabeled conjugate, which comprises the steps of:

    (a) contacting an active ester derivative or a thiol-reactive derivative of the bis-thiosemicarbazone of a 1,2-, 1,3- or 1,4-­dicarbonyl compound with a radioisotope solution of reduced pertechnetate or perrhenate or of copper, mercury or lead/bismuth ions, to form a radiolabeled bis-thiosemicarbazone chelate without substantially affecting the active ester or the thiol-reactive function; and
    (b) reacting the radiolabeled bis-thiosemicarbazone chelate with (i) an amine in the case of an active ester derivative, or (ii) a thiol in the case of a thiol-reactive derivative, to form a radiolabeled conjugate.

    Also provided are chelators for radioisotopes, radiolabeling agents for labeling an amine or a thiol, kits and injectable preparations for use therewith, and improved imaging methods for in vivo human use employing the foregoing compositions and methods.

    摘要翻译： 提供了一种制备放射性标记缀合物的方法，其包括以下步骤：（a）使双缩水甘油缩酮的活性酯衍生物或硫醇反应性衍生物与1,2-，1,3-或1,4 二羰基化合物与高锝酸盐或高铼酸盐或铜，汞或铅/铋离子的放射性同位素溶液形成放射性标记的双缩氨基硫脲螯合物，而基本上不影响活性酯或硫醇反应性功能; 和（b）在活性酯衍生物的情况下使放射性标记的双 - 缩氨基硫脲螯合物与（i）胺反应，或（ii）在硫醇反应性衍生物的情况下的硫醇，以形成放射性标记的缀合物。 还提供了用于放射性同位素的螯合剂，用于标记胺或硫醇的放射性标记试剂，用于其的试剂盒和可注射制剂，以及使用前述组合物和方法的体内人类使用的改进的成像方法。

    Dopamine-beta-hydroxylase inhibitors
    9.
    发明公开
    Dopamine-beta-hydroxylase inhibitors 失效
    β-羟化酶 - 阴离子多巴胺。

    公开(公告)号：EP0225718A2

    公开(公告)日：1987-06-16

    申请号：EP86308481.0

    申请日：1986-10-30

    申请人： SMITHKLINE BECKMAN CORPORATION

    发明人： Finkelstein, Joseph Alan ,  Kaiser, Carl ,  Kruse, Lawrence Ivan

    IPC分类号： C07D249/12 ,  A61K31/41 ,  C07C159/00

    CPC分类号： C07D249/12

    摘要： Compounds of formula
    in which:

    n is 0-5;
    R is hydrogen or C 1-4 alkyl; and
    X is hydrogen, halo, C 1-4 alkyl, CN, N0 2 S0 2 NH 2 , COOH, CHO, OH, CH 2 0H, C 1-4 alkoxy, CF 3 , S0 2 CH 3 , S0 2 CF 3 , or CO 2 C a H 2a+1 where a is 1-5, or any accessible combination thereof of up to 5 substituents; processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them and their use in therapy as dopamine-β-hydroxylase inhibitors.

    摘要翻译： 式中的化合物 ...其中：... n为0-5; ... R为氢或C1-4烷基; 和... X是氢，卤素，C 1-4烷基，CN，NO 2 SO 2 NH 2，COOH，CHO，OH，CH 2 OH，C 1-4烷氧基，CF 3，SO 2 CH 3，SO 2 CF 3或CO 2 C a H 2a + 1，其中a是1-5， 最多5个取代基的可及组合; 其制备方法，可用于其制备的中间体，含有它们的药物组合物及其在治疗中作为多巴胺-β-羟化酶抑制剂的用途。