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    Compositions of iodophenoxy alkylene ethers for visualization of the gastrointestinal tract
    11.
    发明授权
    Compositions of iodophenoxy alkylene ethers for visualization of the gastrointestinal tract 失效
    用于可视化胃肠道的碘苯氧基亚烷基醚的组合物

    公开(公告)号：US5348727A

    公开(公告)日：1994-09-20

    申请号：US29485

    申请日：1993-03-11

    申请人： Edward R. Bacon ,  Carl R. Illig ,  Thomas J. Caulfield ,  Brent D. Douty ,  Kurt A. Josef

    发明人： Edward R. Bacon ,  Carl R. Illig ,  Thomas J. Caulfield ,  Brent D. Douty ,  Kurt A. Josef

    IPC分类号： A61K49/04 ,  C07C43/225 ,  C07C43/23 ,  C07C69/92 ,  C07C255/54 ,  A61B5/055 ,  A61K31/075 ,  C07C41/00

    CPC分类号： A61K49/0404 ,  A61K49/04 ,  A61K49/0409 ,  A61K49/0461 ,  C07C43/225

    摘要： A compound of the formula: ##STR1## wherein Z.dbd.H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, wherein thealkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.dbd.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 [1-5]1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, these compounds are useful as X-ray contrast agents or aryl-lower alkyl.

    摘要翻译： 其中Z = 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 = C 1 -C 25烷基，环烷基，或低级烷基; 羟基，羧基，低级烷氧基羰基或低级烷氧基 - 羰基氧基（CR 1 R 2）p - （CR 3 = CR 4）m Q或任选被卤素，氟 - 低级 - 烷基，芳基， （CR1R2）pC 3BOND CQ; R 1，R 2，R 3和R 4独立地为H或被卤素取代的低级烷基; x为1-4; n是[1-5] 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，这些化合物可用作X射线造影剂或芳基 - 低级烷基。

    Polymeric X-ray compositions containing iodinated polymeric beads
    12.
    发明授权
    Polymeric X-ray compositions containing iodinated polymeric beads 失效
    含有碘化聚合物珠粒的聚合X射线组合物

    公开(公告)号：US5342605A

    公开(公告)日：1994-08-30

    申请号：US54119

    申请日：1993-04-26

    申请人： Carl R. Illig

    发明人： Carl R. Illig

    IPC分类号： A61K47/30 ,  A61K9/16 ,  A61K49/04 ,  A61K31/075 ,  A61K31/715

    CPC分类号： A61K49/0461 ,  A61K49/0442 ,  B82Y5/00 ,  Y10S514/941 ,  Y10S514/942

    摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material in combination with a divalent cation capable of forming a coating on the gastrointestinal tract and 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; andX 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.

    摘要翻译： 公开了用于胃肠道口服或逆行检查的X射线造影剂组合物，其包含与能够在胃肠道上形成涂层的二价阳离子结合的聚合物材料和具有约 0.01至约1000μm，其中所述碘化聚合物珠粒包含含有式（I）重复单元的聚合物，其中A是聚合物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的碘含量在约40至约80重量％的范围内或X的分子量。

    Compositions of iodophenoxy alkanes and iodophenyl ethers in film-forming materials for visualization of the gastrointestinal tract
    13.
    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

    申请人： 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

    发明人： 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分类号： A61K49/04 ,  A61K31/075

    CPC分类号： A61K49/0433 ,  Y10S514/941 ,  Y10S514/942

    摘要： 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.

    摘要翻译： 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。

    Aminoguanidines and alkoxyguanidines as protease inhibitors
    18.
    发明授权
    Aminoguanidines and alkoxyguanidines as protease inhibitors 有权
    氨基胍和烷氧基胍作为蛋白酶抑制剂

    公开(公告)号：US06638931B1

    公开(公告)日：2003-10-28

    申请号：US09722363

    申请日：2000-11-28

    申请人： Bruce E. Tomczuk ,  Richard M. Soll ,  Tianbao Lu ,  Cynthia L. Fedde ,  Carl R. Illig ,  Thomas P. Markotan ,  Thomas P. Stagnaro

    发明人： Bruce E. Tomczuk ,  Richard M. Soll ,  Tianbao Lu ,  Cynthia L. Fedde ,  Carl R. Illig ,  Thomas P. Markotan ,  Thomas P. Stagnaro

    IPC分类号： A61K31255

    CPC分类号： C07C309/73 ,  C07C309/75 ,  C07C309/76 ,  C07C309/77 ,  C07C311/16 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/21 ,  C07C317/14 ,  C07C323/66 ,  C07C2601/02 ,  C07C2601/14 ,  C07D211/96 ,  C07D213/42 ,  C07D213/74 ,  C07D215/36 ,  C07D217/02 ,  C07D217/22 ,  C07D239/42 ,  C07D295/13 ,  C07D295/26 ,  C07D307/66

    摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.

    摘要翻译： 氨基胍和烷氧基胍化合物，包括下式的化合物：其中X是O或NR 9和R 1 -R 4，R 6 -R 9，R 11，R 12， 说明书中列出的R a，R b，R c，Y，Z，n和m以及抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐是 描述。 还描述了制备式I化合物的方法。本发明的新化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，例如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。 某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。 本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。 本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂， 血线和支架。

    Aminoguanidines and alkoxyguanidines as protease inhibitors
    19.
    发明授权
    Aminoguanidines and alkoxyguanidines as protease inhibitors 有权
    氨基胍和烷氧基胍作为蛋白酶抑制剂

    公开(公告)号：US06518310B2

    公开(公告)日：2003-02-11

    申请号：US09809293

    申请日：2001-03-16

    申请人： Bruce E. Tomczuk ,  Richard M. Soll ,  Tianbao Lu ,  Cynthia L Fedde ,  Carl R Illig ,  Thomas P. Markotan ,  Thomas P Stagnaro

    发明人： Bruce E. Tomczuk ,  Richard M. Soll ,  Tianbao Lu ,  Cynthia L Fedde ,  Carl R Illig ,  Thomas P. Markotan ,  Thomas P Stagnaro

    IPC分类号： A61K31255

    CPC分类号： C07C309/73 ,  C07C309/75 ,  C07C309/76 ,  C07C309/77 ,  C07C311/16 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/21 ,  C07C317/14 ,  C07C323/66 ,  C07C2601/02 ,  C07C2601/14 ,  C07D211/96 ,  C07D213/42 ,  C07D213/74 ,  C07D215/36 ,  C07D217/02 ,  C07D217/22 ,  C07D239/42 ,  C07D295/13 ,  C07D295/26 ,  C07D307/66

    摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.

    摘要翻译： 氨基胍和烷氧基胍化合物，包括下式的化合物：其中X为O或NR 9，R 1 -R 4，R 6 -R 9，R 11，R 12，R a，R b，R c，Y，Z，n和m在说明书中阐述， 以及抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐。 还描述了制备式I化合物的方法。本发明的新化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，例如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。 某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。 本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。 本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂， 血线和支架。