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    Compositions of iodophenoxy alkanes and iodophenyl ethers in film-forming materials for visualization of the gastrointestinal tract
    2.
    发明授权
    Compositions of iodophenoxy alkanes and iodophenyl ethers in film-forming materials for visualization of the gastrointestinal tract 失效
    用于可视化胃肠道的成膜材料中碘苯氧基烷烃和碘苯基醚的组成

    公开(公告)号：US5326553A

    公开(公告)日：1994-07-05

    申请号：US12171

    申请日：1993-02-02

    Applicant: Carl R. Illig ,  Eugene R. Cooper ,  John L. Toner ,  Donald A. Upson ,  Brent D. Douty ,  Thomas J. Caulfield ,  Bacon, Edward R. ,  Kimberly G. Estep ,  Kurt A. Josef ,  Shaughnessy Robinson ,  Paul P. Spara

    Inventor： Carl R. Illig ,  Eugene R. Cooper ,  John L. Toner ,  Donald A. Upson ,  Brent D. Douty ,  Thomas J. Caulfield ,  Bacon, Edward R. ,  Kimberly G. Estep ,  Kurt A. Josef ,  Shaughnessy Robinson ,  Paul P. Spara

    IPC: A61K49/04 ,  A61K31/075

    CPC classification number: A61K49/0433 ,  Y10S514/941 ,  Y10S514/942

    Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract whereinZ=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxycarbonyloxy, (CR.sub.1 R.sub.2).sub.p-- (CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-5;m is 1-15;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkylin a pharmaceutically acceptable carrier.

    Abstract translation: 公开了用于口腔或逆行检查胃肠道的x射线造影剂组合物，其包含能够在胃肠道上形成涂层的聚合物材料和具有式“IMAGE”的X射线产生剂及其用于诊断放射学的方法 的胃肠道，其中Z = H，卤素，C 1 -C 20烷基，环烷基，低级烷氧基，氰基，其中烷基和环烷基可被卤素或卤代低级烷基取代; 任选被卤素，氟 - 低级 - 烷基，芳基，低级 - 烷氧基，羟基，羧基，低级 - 烷氧基羰基或低级 - 烷氧基羰基氧基取代的C 1 -C 25烷基，环烷基或卤代低级烷基，（CR 1 R 2）p - （CR3 = CR4）mQ，或（CR1R2）pC 3BOND CQ; R 1，R 2，R 3和R 4独立地为低级烷基，任选被卤素取代; x为1-4; n为1-5; m为1-15; p为1-10; Q为药学上可接受的载体中的H，低级烷基，低级烯基，低级炔基，低级亚烷基，芳基或芳基 - 低级烷基。

    Polymeric x-ray contrast compositions containing iodinated polymeric beads and microcrystaline cellulose
    3.
    发明授权
    Polymeric x-ray contrast compositions containing iodinated polymeric beads and microcrystaline cellulose 失效
    含有碘化聚合物珠粒和微晶纤维素的聚合X射线对比组合物

    公开(公告)号：US5525327A

    公开(公告)日：1996-06-11

    申请号：US227415

    申请日：1994-04-14

    Applicant: Edward J. Baker ,  Robert W. Lee ,  Carl R. Illig ,  John L. Toner

    Inventor： Edward J. Baker ,  Robert W. Lee ,  Carl R. Illig ,  John L. Toner

    IPC: A61K49/04

    CPC classification number: A61K49/0409 ,  A61K49/04 ,  A61K49/0404 ,  A61K49/0433 ,  Y10S514/941 ,  Y10S514/942

    Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodinated polymeric, water-insoluble beads having a particle size of from about 0.01 to about 1000.mu. wherein said iodinated polymeric beads comprise a polymer containing repeating units of the formula (I) ##STR1## wherein A is a repeating organic unit in the backbone chain of the polymer; and X is an organic moiety containing or iodinated eromatic group and a hydrophilic group, said moiety having an iodine content within the range of from about 40 to about 80 weight percent based or the molecular weight of X, in a pharmaceutically acceptable carrier comprising a cellulose derivative.

    Abstract translation: 公开了用于口腔或逆行检查胃肠道的X射线造影剂组合物，其包含粒径为约0.01至约1000μm的碘化聚合物，水不溶性珠粒，其中所述碘化聚合物珠粒包含含有式 （I）其中A是聚合物的主链中的重复有机单元; 并且X是含有或碘化的丙烯酸基团和亲水基团的有机部分，所述部分在药学上可接受的载体中具有在约40至约80重量％的范围内或基于X的分子量的碘含量，其包含纤维素 衍生物。

    Cyclic triamine chelating agents
    4.
    发明授权
    Cyclic triamine chelating agents 失效
    环状三胺螯合剂

    公开(公告)号：US5476644A

    公开(公告)日：1995-12-19

    申请号：US227161

    申请日：1994-04-13

    Applicant: Carl R. Illig ,  Thomas J. Caulfield ,  John L. Toner ,  Peng Guo ,  David L. Ladd

    Inventor： Carl R. Illig ,  Thomas J. Caulfield ,  John L. Toner ,  Peng Guo ,  David L. Ladd

    IPC: A61K49/00 ,  A61K49/06 ,  C07C227/02 ,  C07C229/16 ,  C07C229/76 ,  C07C237/06 ,  C07C237/08 ,  C07C265/12 ,  C07C327/38 ,  C07C331/28 ,  C07F5/00 ,  C07F9/00 ,  C07F11/00 ,  C07F13/00 ,  C07F15/02 ,  C07F15/04 ,  C07F15/06 ,  C09K3/00 ,  A61K51/00 ,  A61K31/28

    CPC classification number: A61K49/06 ,  C07C229/16 ,  C07C2101/14

    Abstract: The present invention provides compounds of the formula ##STR1## chelated with a paramagnetic metal ion wherein Z1 and Z2 each represent the atoms necessary to complete a monocyclic or polycyclic carbocyclic or heterocyclic ring system, said Z1 and Z2 independently optionally substituted with R.sup.6 and R.sup.7, respectively;R.sup.l, R.sup.2, R.sup.3 and R.sup.4 are independently carboxyalkyl (C.sub.1 -C.sub.2), --(CH.sub.2).sub.n --C(.dbd.O)--NH--R.sup.8, or --(CH.sub.2).sub.n --C(.dbd.O)--O--R.sup.8R.sup.5 is carboxyalkyl (C.sub.1 -C.sub.2);R.sup.6 and R.sup.7 are independently hydrogen, benzyl, or benzyloxy, said benzyl or benzyloxy optionally substituted with one, two or three substituents selected from the group consisting of amino, isocyanato (--N.dbd.C.dbd.O), isothiocyanato (--N.dbd.C.dbd.S), --NH--C(.dbd.O)--X or --NH--C(.dbd.S)--X;R.sup.8 is alkyl (C.sub.1 -C.sub.20), --(CH.sub.2).sub.m --Ar, or polyhydroxyalkyl (C.sub.1 -C.sub.20);n is 1 or 2;m is 1 to 15;X is a targeting moiety; andAr is phenyl optionally substituted with one, two or three substituents selected from the group consisting of amino, acylamino, hydroxy, alkyl (C1-C5) and halogen.

    Abstract translation: 本发明提供了与顺磁金属离子螯合的式“IMAGE”化合物，其中Z 1和Z 2各自表示完成单环或多环碳环或杂环系统所必需的原子，所述Z 1和Z 2独立地任选地被R6和R7取代， 分别; R1，R2，R3和R4独立地是羧基烷基（C1-C2）， - （CH2）nC（= O）-NH-R8或 - （CH2）nC（= O）-O-R8 R5是羧基烷基 C2）; R6和R7独立地是氢，苄基或苄氧基，所述苄基或苄氧基任选地被一个，两个或三个选自氨基，异氰酸酯基（-N = C = O），异硫氰酸酯（-N = C = S），-NH-C（= O）-X或-NH-C（= S）-X; R8是烷基（C1-C20）， - （CH2）m-Ar或多羟基烷基（C1-C20）; n为1或2; m为1〜15; X是靶向部分; 并且Ar是任选地被一个，两个或三个选自氨基，酰基氨基，羟基，烷基（C 1 -C 5）和卤素的取代基取代的苯基。

    Compositions of iodophenoxy alkylene ethers and cellulose derivatives for visualization of the gastrointestinal tract
    8.
    发明授权
    Compositions of iodophenoxy alkylene ethers and cellulose derivatives for visualization of the gastrointestinal tract 失效
    碘苯氧基亚烷基醚和纤维素衍生物用于胃肠道可视化的组合物

    公开(公告)号：US5466435A

    公开(公告)日：1995-11-14

    申请号：US222787

    申请日：1994-04-04

    Applicant: Edward J. Baker ,  Edward R Bacon ,  Carl R. Illig ,  Thomas J. Caulfield ,  Brent D. Douty ,  Kurt A. Josef ,  John L. Toner ,  Robert W. Lee

    Inventor： Edward J. Baker ,  Edward R Bacon ,  Carl R. Illig ,  Thomas J. Caulfield ,  Brent D. Douty ,  Kurt A. Josef ,  John L. Toner ,  Robert W. Lee

    IPC: A61K49/04 ,  C07C43/225 ,  C07C43/23 ,  C07C69/92 ,  C07C255/54

    CPC classification number: A61K49/0404 ,  A61K49/04 ,  A61K49/0409 ,  A61K49/0461 ,  C07C43/225

    Abstract: Disclosed are contrast agents of the formula ##STR1## wherein Z is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R is C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;(CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H or lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;in an aqueous, pharmaceutically acceptable carrier comprising a cellulose derivative.

    Abstract translation: 公开了式IMA的造影剂，其中Z是H，卤素，C 1 -C 20烷基，环烷基，低级烷氧基，烷氧基羰基，氰基，其中烷基和环烷基可以被卤素或卤代低级烷基取代; R为C1-C25烷基，环烷基，低级或低级烷基; 其中每一个可以任选被卤素，氟 - 低级 - 烷基，芳基，低级 - 烷氧基，羟基，羧基，低级 - 烷氧基羰基或低级 - 烷氧基 - 羰氧基取代; （CR 1 R 2）p - （CR 3 = CR 4）m Q或（CR 1 R 2）p -C 3OND C-Q; R 1，R 2，R 3和R 4独立地为H或低级烷基，任选被卤素取代; x为1-4; n为1-4; m为1-15; p是1-20; Q为H，低级烷基，低级烯基，低级炔基，低级亚烷基，芳基或芳基 - 低级烷基; 在包含纤维素衍生物的水性药学上可接受的载体中。

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