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1. 发明授权

US5385721A Compositions of alkylbenzenes and cellulose derivatives for visualization of the gastrointestinal tract 失效
标题翻译：用于胃肠道可视化的烷基苯和纤维素衍生物的组合物
公开(公告)号：US5385721A
公开(公告)日：1995-01-31
申请号：US217138
申请日：1994-03-22
申请人： Edward J. Baker , Kurt A. Josef , Edward R. Bacon , Kimberly G. Estep , Carl R. Illig , Brent D. Douty , John L. Toner , Robert W. Lee
发明人： Edward J. Baker , Kurt A. Josef , Edward R. Bacon , Kimberly G. Estep , Carl R. Illig , Brent D. Douty , John L. Toner , Robert W. Lee
IPC分类号： A61K49/00 , A61K49/04 , C07C17/00 , C07C17/12 , C07C17/26 , C07C25/02 , C07C25/13 , C07C25/24 , C07C33/46 , C07C43/225 , C07C69/65 , C07C69/76 , C07C69/92 , A61K31/715 , A61K31/02
CPC分类号： C07C17/354 , A61K49/04 , A61K49/0404 , A61K49/0409 , A61K49/0433 , C07C17/12 , C07C17/2635 , C07C25/02 , C07C25/24 , C07C69/65
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof ##STR1## wherein R is methyl, ethyl, n-propyl, C.sub.4 -C.sub.25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl; (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, lower-alkyl, optionally substituted with halo;n is 2-5;m is 2-5;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;in a pharmaceutically acceptable carrier comprising a cellulose derivative.
摘要翻译：公开了用于口服或逆行检查胃肠道的x射线造影剂组合物，其包含下式的x射线产生剂或其药学上可接受的盐，其中R是甲基，乙基，正丙基，C 4 -C 25烷基，环烷基，不饱和烯丙基或卤代低级烷基，其各自可以任选被卤素，氟代低级烷基，芳基，低级烷氧基，羟基，羧基或低级烷氧基羰基取代; （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，低级烷基，任选被卤素取代; n为2-5; m为2-5; p为1-10; 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可药用载体中。

2. 发明授权

US5525327A Polymeric x-ray contrast compositions containing iodinated polymeric beads and microcrystaline cellulose 失效
标题翻译：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
申请人： Edward J. Baker , Robert W. Lee , Carl R. Illig , John L. Toner
发明人： Edward J. Baker , Robert W. Lee , Carl R. Illig , John L. Toner
IPC分类号： A61K49/04
CPC分类号： A61K49/0409 , A61K49/04 , A61K49/0404 , A61K49/0433 , Y10S514/941 , Y10S514/942
摘要： 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.
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。

3. 发明授权

US5543132A X-ray contrast compositions containing a barium salt and a cellulose derivative 失效
标题翻译：含有钡盐和纤维素衍生物的X射线对比组合物
公开(公告)号：US5543132A
公开(公告)日：1996-08-06
申请号：US227422
申请日：1994-04-14
申请人： Edward J. Baker , Robert W. Lee , John L. Toner , Carl R. Illig
发明人： Edward J. Baker , Robert W. Lee , John L. Toner , Carl R. Illig
IPC分类号： A61K49/04
CPC分类号： A61K49/0409 , A61K49/04 , A61K49/0404 , 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 barium salt in a pharmaceutically acceptable carrier comprising a cellulose derivative; and methods for their use in diagnostic radiology of the gastrointestinal tract.
摘要翻译：公开了用于口服或逆行检查胃肠道的x射线造影剂组合物，其包含在包含纤维素衍生物的药学上可接受的载体中的钡盐; 以及它们用于胃肠道诊断放射学的方法。

4. 发明授权

US5466435A Compositions of iodophenoxy alkylene ethers and cellulose derivatives for visualization of the gastrointestinal tract 失效
标题翻译：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
申请人： Edward J. Baker , Edward R Bacon , Carl R. Illig , Thomas J. Caulfield , Brent D. Douty , Kurt A. Josef , John L. Toner , Robert W. Lee
发明人： 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分类号： A61K49/04 , C07C43/225 , C07C43/23 , C07C69/92 , C07C255/54
CPC分类号： A61K49/0404 , A61K49/04 , A61K49/0409 , A61K49/0461 , C07C43/225
摘要： 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.
摘要翻译：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。

5. 发明授权

US5443814A X-ray contrast compositions containing iodophenoxyalkanes and cellulose derivatives 失效
标题翻译：含有碘苯氧基烷烃和纤维素衍生物的X射线对比组合物
公开(公告)号：US5443814A
公开(公告)日：1995-08-22
申请号：US206552
申请日：1994-03-04
申请人： Carl R. Illig , John L. Toner , Robert W. Lee , Edward J. Baker
发明人： Carl R. Illig , John L. Toner , Robert W. Lee , Edward J. Baker
IPC分类号： A61K47/30 , A61K49/04
CPC分类号： A61K49/04 , A61K49/0404 , A61K49/0409 , A61K49/0442 , A61K49/0461 , 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 nonionic x-ray producing agent in combination with a cellulose derivative in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
摘要翻译：公开了用于口服或逆行检查胃肠道的x射线造影剂组合物，其包含与药学上可接受的载体中的纤维素衍生物组合的非离子X射线产生剂; 以及它们用于胃肠道诊断放射学的方法。

6. 发明授权

US5385720A Compositions of iodobenzoic acid derivatives and cellulose derivatives for visualization of the gastrointestinal tract 失效
标题翻译：碘苯甲酸衍生物和纤维素衍生物用于胃肠道可视化的组合物
公开(公告)号：US5385720A
公开(公告)日：1995-01-31
申请号：US216988
申请日：1994-03-23
申请人： Edward J. Baker , Robert W. Lee , Carl R. Illig , Brent D. Douty , John L. Toner
发明人： Edward J. Baker , Robert W. Lee , Carl R. Illig , Brent D. Douty , John L. Toner
IPC分类号： A61K47/30 , A61K49/04 , C08K5/07 , A61K31/235 , A61K31/715
CPC分类号： A61K49/0404 , A61K49/04 , A61K49/0409 , A61K49/0433 , Y10S514/941 , Y10S514/942
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof ##STR1## wherein Z is 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 is C.sub.1 -C.sub.25 alkyl, cycloalkyl, 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 =CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p -- C.dbd.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--3y 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 alkyl in a pharmaceutically acceptable carrier comprising a cellulose derivative.
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，其包含下式的x射线产生剂或其药学上可接受的盐，其中Z为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; R是C 1 -C 25烷基，环烷基或卤代低级烷基，其各自可以任选被卤素，氟代低级烷基，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; （CR 1 R 2）p - （CR 3 = CR 4）m Q或（CR 1 R 2）p -C = C-Q; 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1-3 y为1-4; n为1-5; m为1-15; p为1-10; Q为包含纤维素衍生物的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。

7. 发明授权

US5368837A X-ray contrast compositions containing an organic crystalline X-ray contrast agent and a cellulose derivative 失效
标题翻译：含有有机晶体X射线造影剂和纤维素衍生物的X射线造影剂组合物
公开(公告)号：US5368837A
公开(公告)日：1994-11-29
申请号：US227423
申请日：1994-04-14
申请人： Edward J. Baker , Robert W. Lee , Eugene R. Cooper , John L. Toner , Carl R. Illig
发明人： Edward J. Baker , Robert W. Lee , Eugene R. Cooper , John L. Toner , Carl R. Illig
IPC分类号： A61K49/04
CPC分类号： A61K49/0433 , A61K49/0404 , A61K49/0409 , A61K49/0461 , Y10S514/941 , Y10S514/942
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a crystalline contrast agent in a pharmaceutically acceptable carrier comprising a cellulose derivative; and methods for their use in diagnostic radiology of the gastrointestinal tract.
摘要翻译：公开了用于口服或逆行检查胃肠道的X射线造影剂组合物，其包含在包含纤维素衍生物的药学上可接受的载体中的结晶造影剂; 以及它们用于胃肠道诊断放射学的方法。

8. 发明授权

US5385722A Compositions of iodophenyl esters and iodophenyl sulfonates and cellulose derivatives for visualization of the gastrointestinal tract 失效
标题翻译：碘苯基酯和碘苯基磺酸盐和纤维素衍生物的组合物用于胃肠道可视化
公开(公告)号：US5385722A
公开(公告)日：1995-01-31
申请号：US229048
申请日：1994-04-18
申请人： Edward J. Baker , Robert W. Lee , Edward R. Bacon , Sol J. Daum , Kimberly G. Estep , Kurt A. Josef , Brent D. Douty , Carl R. Illig , John L. Toner
发明人： Edward J. Baker , Robert W. Lee , Edward R. Bacon , Sol J. Daum , Kimberly G. Estep , Kurt A. Josef , Brent D. Douty , Carl R. Illig , John L. Toner
IPC分类号： A61K49/04 , C07C69/017 , C07C69/63 , C07C69/675 , C07C69/708 , C07C69/74 , C07C69/773 , C07C255/55 , C07C309/65 , C07C309/67 , C07C309/68 , C07C309/71 , C07C309/72 , A61K31/22 , A61K31/71
CPC分类号： B82Y5/00 , A61K49/04 , A61K49/0404 , A61K49/0409 , A61K49/0433 , C07C309/65 , C07C69/017 , C07C69/63 , C07C69/74
摘要： Disclosed are contrast agents of the formula ##STR1## wherein ##STR2## Z is H, halo, C.sub.5 -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 is C.sub.1 -C.sub.25 alkyl, cycloalkyl, aryl or halo-lower-alkyl, each of which may be optionally substituted with lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene or lower-alkoxy-carbonyloxy;n is 1-5;y is 0-4; andw is 1-4;in a pharmaceutically acceptable carrier comprising a cellulose derivative.
摘要翻译：公开了式IMAMA的造影剂，其中Z是H，卤素，C 5 -C 20烷基，环烷基，低级烷氧基，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是C 1 -C 25烷基，环烷基，芳基或卤代低级烷基，其各自可以任选地被低级烷氧基，羟基，羧基或低级烷氧基羰基，低级烯基，低级 - 炔基，低级亚烷基或低级烷氧基 - 羰基氧基; n为1-5; y为0-4; w为1-4; 在包含纤维素衍生物的可药用载体中。

9. 发明授权

US5326553A Compositions of iodophenoxy alkanes and iodophenyl ethers in film-forming materials for visualization of the gastrointestinal tract 失效
标题翻译：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。

10. 发明授权

US5476644A Cyclic triamine chelating agents 失效
标题翻译：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
申请人： Carl R. Illig , Thomas J. Caulfield , John L. Toner , Peng Guo , David L. Ladd
发明人： Carl R. Illig , Thomas J. Caulfield , John L. Toner , Peng Guo , David L. Ladd
IPC分类号： 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分类号： A61K49/06 , C07C229/16 , C07C2101/14
摘要： 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.
摘要翻译：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。

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