利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

70 条记录 (耗时 0.038 秒)

    Macrocyclic chelating agents and chelates thereof
    48.
    发明授权
    Macrocyclic chelating agents and chelates thereof 失效
    大环螯合剂及其螯合物

    公开(公告)号：US5132409A

    公开(公告)日：1992-07-21

    申请号：US449883

    申请日：1989-11-27

    申请人： Ernst Felder ,  Carlo Musu ,  Luciano Fumagalli ,  Fulvio Uggeri

    发明人： Ernst Felder ,  Carlo Musu ,  Luciano Fumagalli ,  Fulvio Uggeri

    IPC分类号： A61K49/06 ,  C07D257/02

    CPC分类号： A61K49/06 ,  C07D257/02

    摘要： Macrocyclic derivatives of 1,4,7,10-tetraazacyclododecane of general formula (I) hereinbelow, wherein A is a group of formula (II) hereinbelow, in which R is H or alkyl or optionally substituted benzyl or a H(OCH.sub.2 CH.sub.2).sub.1-4-, Me(OCH.sub.2 CH.sub.2).sub.1-4-, or Et(OCH.sub.2 CH.sub.2).sub.1-4- group, X or O--R.sub.1, in which R.sub.1 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group or X is --NR.sub.2 R.sub.3, in which R.sub.2 and R.sub.3 are H or alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl, and B.sub.1, B.sub.2 and B.sub.3 have the same meanings as A or are H or a group of formula (III) hereinbelow, in which R.sub.4 is H or alkyl, Y is a O--R.sub.5 group, wherein R.sub.5 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group, or Y is a --NR.sub.6 R.sub.7 group, wherein R.sub.6 and R.sub.7 are H or alkyl, hydroxyalkyl, alkoxyalkyl, or alkoxyhydroxyalkyl, said derivatives optionally being salified, and the complex salts thereof, are used as pharmaceuticals and/or diagnostic agents. ##STR1##

    摘要翻译： 其中A为下式（Ⅱ）基团，其中R为H或烷基或任意取代的苄基或H（OCH 2 CH 2）1的式（I）的基团，其通式（I）的1,4,7,10-四氮杂环十二烷的大环衍生物 -4-，Me（OCH 2 CH 2）1-4 - 或Et（OCH 2 CH 2）1-4 - 基，X或O-R 1，其中R 1是H或烷基，羟基烷基，烷氧基烷基，烷氧基羟基烷基或多氧杂烷基或X是 -NR2R3，其中R2和R3为H或烷基，羟烷基，烷氧基烷基或烷氧基羟烷基，B1，B2和B3与A相同，或为H或下式（III）的基团，其中R4为H或 烷基，Y是O-R5基团，其中R5是H或烷基，羟基烷基，烷氧基烷基，烷氧基羟基烷基或聚氧杂烷基，或Y是-NR6R7基团，其中R6和R7是H或烷基，羟基烷基，烷氧基烷基或烷氧基羟烷基 所述衍生物任选地被盐化，并且其络合盐用作药物和/或诊断剂。 （一）图像（二）<图像>（三）

    Paramagnetic chelates
    49.
    发明授权
    Paramagnetic chelates 失效
    顺磁螯合物

    公开(公告)号：US4980502A

    公开(公告)日：1990-12-25

    申请号：US411906

    申请日：1989-09-25

    申请人： Ernst Felder ,  Fulvio Uggeri ,  Luciano Fumagalli ,  Giorio Vittadini

    发明人： Ernst Felder ,  Fulvio Uggeri ,  Luciano Fumagalli ,  Giorio Vittadini

    IPC分类号： A61K49/00 ,  A61K31/28 ,  C07C229/22 ,  C07C229/40 ,  C07C229/46 ,  C07C233/10 ,  C07D401/12 ,  C07F5/00 ,  C07F13/00 ,  C07F15/02

    CPC分类号： A61K31/28

    摘要： Compounds suitable for NMR imaging having the formula: ##STR1## wherein a is 2 or 3;b is an integer from 0 to 4;Me.sup.(a+) is Fe.sup.(2+), Fe.sup.(3+), Gd.sup.(3+), or Mn.sup.(2+) ;E.sup.(b+) is an ion of an alkali metal, alkaline earth metal, alkyl ammonium, alkanol ammonium, polyhydroxyalkyl ammonium, or basic protonated amino acid, said ions representing a total charge of b;m is an integer from 1 to 5;R is H, alkyl with from 1 to 8 carbon atoms, alkyl with from 1 to 8 carbon atoms wherein from 1 to 5 carbons are substituted with OH; aralkyl with 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, hydroxyl, carboxyl, carboxamide, ester, SO.sub.3 H, sulfonamide, lower alkyl, lower hydroxy alkyl, amino, acylamino; (poly)oxa-alkyl with 1 to 50 oxygen atoms and from 3 to 150 carbon atoms, wherein 1 to 5 hydrogen atoms may be substituted by OH; R.sub.1 is the same as R.sub.2 or is --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ, CH.sub.2 CH.sub.2 --N(CH.sub.2 COOZ).sub.2, a hydroxy arylalkyl, hydroxy pyridylalkyl, hydroxy aryl(carboxy)alkyl or hydroxy pyridyl-(carboxyl)-alkyl radical, where the aryl or pyridyl radical may be substituted by hydroxyl, hydroxy alkyl, alkyl, halogen, carboxyl or SO.sub.3 H; is --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ, ##STR2## wherein R.sub.3 is --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ or a monovalent radical having the structure ##STR3## X is a direct chemical bond, --O--, --S--, 13 NH--, n is the integer 2 or 3, with the proviso that when X represents a direct bond, n is 1, 2 or 3;Z is hydrogen or a unit of negative charge, and --(CH.sub.2).sub.m -- may also be --CH.sub.2 --C(CH.sub.3).sub.2 --.

    Process for the preparation of optically active alpha-acrylalkanoic acids and novel intermediates thereof
    50.
    发明授权
    Process for the preparation of optically active alpha-acrylalkanoic acids and novel intermediates thereof 失效
    制备光学活性α-丙烯酰基链烷酸的方法及其新型中间体

    公开(公告)号：US4810819A

    公开(公告)日：1989-03-07

    申请号：US81688

    申请日：1987-08-05

    申请人： Claudio Giordano ,  Graziano Castaldi ,  Fulvio Uggeri ,  Silvia Cavicchioli

    发明人： Claudio Giordano ,  Graziano Castaldi ,  Fulvio Uggeri ,  Silvia Cavicchioli

    IPC分类号： C07C45/46 ,  C07C49/807 ,  C07C51/00 ,  C07D317/32 ,  C07C69/76

    CPC分类号： C07D317/32 ,  C07C45/46 ,  C07C49/807 ,  C07C51/00

    摘要： A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represents a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration. This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.The esters of formula (C) have pharmacological activity analogous to that of the corresponding alpha-arylalkanoic acids.

    摘要翻译： 描述了通过以下方法制备光学活性α-芳基链烷酸的新的对映选择性方法：（a）在缩酮的α-脂肪族碳原子上卤化式（ⅠA）的缩酮，其中Ar表示任选取代的芳基; R代表C1-C4烷基; R1和R2表示羟基，O-M +，OR3或NR4R5基团; 由星号表示的碳原子同时为（R）或（S）构型。 该反应是非对映选择性的，因此获得了α-二酮的混合物，其中两个差向异构体中的一个占优势，并且通常强大地占优势。 （b）通过式（IMA）的（C）（C）的酯，将单体或两个连续阶段中的X为Cl，Br或I的式（A）所示的配子重新排列成α-芳基链烷酸 ）化合物（A）和（C）都是新的化合物。 重新布置步骤（b）可以在新的创造条件下进行。 式（C）的酯具有类似于相应的α-芳基链烷酸的药理活性。