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81. 发明授权

US5344638A Compositions of iodobenzoic acid derivatives for visualization of the gastrointestinal tract 失效
标题翻译：碘苯甲酸衍生物用于胃肠道可视化的组合物
公开(公告)号：US5344638A
公开(公告)日：1994-09-06
申请号：US031384
申请日：1993-03-11
申请人： Carl R. Illig , Brent D. Douty
发明人： Carl R. Illig , Brent D. Douty
IPC分类号： A61K49/04 , C07C69/76 , C07C69/767 , C07C69/773 , C07C69/78 , C07C69/82 , C07C69/92
CPC分类号： A61K49/0433 , C07C69/76 , C07C69/92
摘要： Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinwhereinZ=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-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 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 alkylin an aqueous, pharmaceutically acceptable carrier.
摘要翻译：公开了含水组合物中含有的式“IMAGE”的造影剂及其用于胃肠道诊断放射学的方法，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以被卤素或卤代低级烷基取代; R = C1-C25烷基，环烷基或卤代低级烷基，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，（CR1R2 ）p - （CR 3 = CR 4）m Q或（CR 1 R 2） 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; 并且Q是在水性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。

82. 发明授权

US5330739A Iodinated benzoyl acetals and ketals for x-ray imaging 失效
标题翻译：碘化苯甲酰缩醛和缩酮用于X射线成像
公开(公告)号：US5330739A
公开(公告)日：1994-07-19
申请号：US985415
申请日：1992-12-04
申请人： Carl R. Illig
发明人： Carl R. Illig
IPC分类号： A61K49/04 , C07C43/303 , C07C43/305 , C07C43/307 , C07C43/313 , C07C233/54 , C07C69/76 , C07C205/00 , C07C229/00
CPC分类号： C07C233/54
摘要： Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid; R is alkyl, cycloalkyl, aryl, aralkyl, ##STR2## or alkenyl; R.sup.1 is H, alkyl, cycloalkyl, aryl, aralkyl, or --CH.sub.2 --.sub.m CO.sub.2 R.sup.3 ;R.sup.2 is H, alkyl, cycloalkyl, aryl, aralkyl, --CH.sub.2 --.sub.n CO.sub.2 R.sup.4, or a ##STR3## group, wherein Z, R and R.sup.1 are as defined above;or R.sup.1 and R.sup.2, taken together with the carbon atom to which they are attached represent cycloalkyl;R.sup.3 is H, alkyl, cycloalkyl, aryl or aralkyl;R.sup.4 is H, alkyl, cycloalkyl, aryl or aralkyl; andm, n and p are independently an integer of from 0 to 17;provided that R.sup.1 and R.sup.2 can not both be H;are useful in the preparation of x-ray contrast compositions for medical imaging.
摘要翻译：具有结构的化合物，其中（Z-COO是碘化芳族酸的残基; R是烷基，环烷基，芳基，芳烷基，烯基或者烯基; R1是H，烷基，环烷基，芳基，芳烷基或 -CH2-mCO2R3; R2是H，烷基，环烷基，芳基，芳烷基，-CH2-nCO2R4或者一个基团，其中Z，R和R1如上定义;或者R1和R2与碳一起它们所连接的原子代表环烷基; R3是H，烷基，环烷基，芳基或芳烷基; R4是H，烷基，环烷基，芳基或芳烷基; m，n和p独立地是0至17的整数; R1和R2不能都是H;可用于制备用于医学成像的x射线对比组合物。

83. 发明授权

US5318768A Polymeric x-ray contrast compositions containing an organic crystalline x-ray contrast agent 失效
标题翻译：含有有机结晶X射线造影剂的聚合X射线对比组合物
公开(公告)号：US5318768A
公开(公告)日：1994-06-07
申请号：US18606
申请日：1993-02-17
申请人： Carl R. Illig , Eugene R. Cooper
发明人： Carl R. Illig , Eugene R. Cooper
IPC分类号： A61K47/30 , A61K49/04 , A61K31/715
CPC分类号： 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 polymeric material in combination with a divalent cation capable of forming a coating on the gastrointestinal tract and a crystalline contrast agent in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
摘要翻译：公开了用于口腔或逆行检查胃肠道的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和药学上可接受的载体中的结晶造影剂的聚合物材料; 以及它们用于胃肠道诊断放射学的方法。

84. 发明授权

US5310760A 3,4-disubstituted anilines-immunomodulating agents 失效
标题翻译： 3,4-二取代的苯胺 - 免疫调节剂
公开(公告)号：US5310760A
公开(公告)日：1994-05-10
申请号：US89007
申请日：1993-07-09
申请人： William N. Washburn , Lee H. Latimer , Barbara B. Lussier , Carl R. Illig , Alexander L. Weis
发明人： William N. Washburn , Lee H. Latimer , Barbara B. Lussier , Carl R. Illig , Alexander L. Weis
IPC分类号： A61K31/165 , C07C237/44 , C07C233/65
CPC分类号： A61K31/165 , C07C237/44
摘要： Certain 3,4-disubstituted anilines and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --NH.sub.2 or --NHCH.sub.3 ;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.
摘要翻译：提供了通过诱导IL-2合成和随后的IL-2受体表达而模拟IL-1活性的某些3,4-二取代的苯胺及其药学上可接受的盐。具体地说，本发明提供了式I化合物及其酸加成盐：其中Y是NH 3或SO 2 NH，其中R 4是H; Z是-O-，-NH-，-NR-，-S-或能够与R4氢键合的其它杂原子，以产生优选的构象; R是烷基; R1是-NH2或-NHCH3; R2是H，烷基，环烷基，芳烷基，取代或未取代的芳基或取代或未取代的具有4至5个核碳原子的氮杂环基; 并且R 3是亲脂性部分。

85. 发明授权

US5310537A Compositions of iodoaniline derivatives for visualization of the gastrointestinal tract 失效
标题翻译：用于可视化胃肠道的碘苯胺衍生物的组合物
公开(公告)号：US5310537A
公开(公告)日：1994-05-10
申请号：US24555
申请日：1993-03-01
申请人： Carl R. Illig , Thomas J. Caulfield
发明人： Carl R. Illig , Thomas J. Caulfield
IPC分类号： A61K49/04 , C07C211/52 , C07C225/22 , C07C229/18 , C07C229/28 , C07C233/15 , C07C211/45 , G01N21/00
CPC分类号： A61K49/0461 , C07C211/52 , C07C233/15
摘要： Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions 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.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl or halo-lower-alkyl, wherein said C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl and halo-lower-alkyl are optionally substituted with fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy,n is 1-4;y is 1-4; andx is 1 or 2.
摘要翻译：公开了含水组合物中含有的式“IMAGE”的造影剂及其用于胃肠道诊断放射学的方法，其中Z = H，卤素，C 1 -C 20烷基，环烷基，低级烷氧基，氰基，其中烷基和环烷基基团可以被卤素或卤代低级烷基取代; R 1和R 2独立地为H，C 1 -C 25烷基，环烷基，乙酰基或卤代低级烷基，其中所述C 1 -C 25烷基，环烷基，乙酰基和卤代低级烷基任选被氟 - 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，n为1-4; y为1-4; x为1或2。

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