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71. 发明授权

US06235778B1 Aminoguanidines and alkoxyguanidines as protease inhibitors 失效
标题翻译：氨基胍和烷氧基胍作为蛋白酶抑制剂
公开(公告)号：US06235778B1
公开(公告)日：2001-05-22
申请号：US08979234
申请日：1997-11-26
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 R114 R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and mare 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NR9，R114R4，R6-R9，R11，R12，Ra，Rb，Rc，Y，Z，n和母本也在说明书中列出描述了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连接于制造用于血液收集，血液循环和血液储存中的装置的材料的抗凝剂，例如导管，血液透析机，采血注射器和管，血线和支架。

72. 发明授权

US6133315A Amidino protease inhibitors 有权
公开(公告)号：US6133315A
公开(公告)日：2000-10-17
申请号：US270734
申请日：1999-03-16
申请人： Tianbao Lu , Bruce E. Tomczuk , Carl R. Illig , Richard M. Soll
发明人： Tianbao Lu , Bruce E. Tomczuk , Carl R. Illig , Richard M. Soll
IPC分类号： C07D295/14 , A61K31/00 , A61K31/18 , A61K31/24 , A61K31/445 , A61K31/495 , A61P1/00 , A61P1/18 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P29/00 , A61P43/00 , C07C309/73 , C07C311/21 , C07D211/22 , C07D211/26 , C07D211/28 , C07D295/195 , A61K31/155 , C07C257/14 , C07C311/46
CPC分类号： C07D295/195 , C07C309/73 , C07C311/21 , C07D211/22 , C07D211/26
摘要： Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

73. 发明授权

US5607660A Compositions of iodophenoxy alkanes and iodophenyl ethers in combination with cellulose derivatives for visualization of the gastrointestinal tract 失效
标题翻译：碘苯氧基烷烃和碘苯基醚与纤维素衍生物的组合，用于胃肠道的可视化
公开(公告)号：US5607660A
公开(公告)日：1997-03-04
申请号：US246888
申请日：1994-05-20
申请人： Robert W. Lee , Carl R. Illig , Thomas J. Caulfield
发明人： Robert W. Lee , Carl R. Illig , Thomas J. Caulfield
IPC分类号： A61K49/00 , A61K49/04 , C07C43/225 , C07C43/247 , C07C255/54
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 iodophenoxy alkane, iodophenyl alkenylalkyl ether or an iodophenyl alkynylalkyl ether 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，其包含碘苯氧基烷烃，碘苯基烯基烷基醚或碘苯基炔基烷基醚x-射线产生剂与药学上可接受的载体中的纤维素衍生物的组合; 以及它们用于胃肠道诊断放射学的方法。

74. 发明授权

US5472683A Nanoparticulate diagnostic mixed carbamic anhydrides as X-ray contrast agents for blood pool and lymphatic system imaging 失效
标题翻译：纳米颗粒诊断混合氨基酸酐作为血液池和淋巴系统成像的X射线造影剂
公开(公告)号：US5472683A
公开(公告)日：1995-12-05
申请号：US401570
申请日：1995-03-09
申请人： Carl R. Illig
发明人： Carl R. Illig
IPC分类号： A61K49/04 , C07C271/12 , C07C271/22 , C07C271/28 , C07J41/00 , C07C271/02
CPC分类号： B82Y5/00 , A61K49/049 , C07C271/12 , C07C271/22 , C07C271/28 , C07J41/0055
摘要： This invention relates to methods of x-ray diagnostic imaging the blood pool, liver, spleen, and/or lymph system of a mammal comprising administering a contrast effective amount of a mixed carbamic anhydride as a contrast agent having the structure ##STR1## X is H, NR.sup.1 R.sup.2 or CONR.sup.1 R.sup.3, R.sup.1 is H or alkylR.sup.2 is COR.sup.3R.sup.3 is H, alkyl or arylY is NR.sup.1 R.sup.2 or CONR.sup.1 R.sup.3 andN is NR.sup.1 R.sup.4 andR.sup.4 is H, alkyl, aryl or CH(R.sup.5)CO.sub.2 R.sup.1.This invention further relates to novel mixed carbamic anhydride contrast agents having the above structure to x-ray contrast compositions comprising such agents, and to methods of x-ray diagnostic imaging utilizing such agents.
摘要翻译：本发明涉及对哺乳动物的血液池，肝脏，脾脏和/或淋巴系统进行x射线诊断成像的方法，该方法包括施用对比有效量的混合氨基甲酸酐作为具有结构kyl R2的造影剂，即COR3 R3 是H，烷基或芳基Y是NR1R2或CONR1R3，N是NR1R4，R4是H，烷基，芳基或CH（R5）CO2R1。本发明还涉及具有上述结构的新型混合氨基甲酸酐造影剂，其包含这些试剂的X射线造影剂，以及利用这种试剂的X射线诊断成像方法。

75. 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。

76. 发明授权

US5449691A 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：US5449691A
公开(公告)日：1995-09-12
申请号：US80546
申请日：1993-06-24
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 , A61K31/16 , A61K31/215 , A61K31/24
CPC分类号： A61K31/165 , C07C237/44
摘要： A method for inducing the production of interleukin 2 in a warm blooded animal by administering an effective amount of a compound of the formula (I) ##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：通过施用有效量的式（I）NHSO 2或SO 2 NH的化合物，其中R 4是H，在温血动物中诱导白细胞介素2的产生的方法; 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; R 1是-NH 2或-NHCH 3; 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。

77. 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。

78. 发明授权

US5405600A X-ray contrast compositions containing film-forming materials 失效
标题翻译：含有成膜材料的X射线造影剂
公开(公告)号：US5405600A
公开(公告)日：1995-04-11
申请号：US104744
申请日：1993-08-11
申请人： Carl R. Illig , John L. Toner
发明人： Carl R. Illig , John L. Toner
IPC分类号： A61K47/30 , A61K49/04 , A61K31/715
CPC分类号： A61K49/0442 , A61K49/04 , A61K49/0404 , A61K49/0409 , 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 capable of forming a coating on the gastrointestinal tract and a nonionic x-ray producing 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，其包含能够在胃肠道上形成涂层的聚合物材料和药学上可接受的载体中的非离子X射线产生剂; 以及它们用于胃肠道诊断放射学的方法。

79. 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。

80. 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。

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