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1. 发明授权

US07608242B2 Peptide-chelate conjugates 失效
标题翻译：肽 - 螯合物
公开(公告)号：US07608242B2
公开(公告)日：2009-10-27
申请号：US10469801
申请日：2002-03-01
申请人： Alan Cuthbertson , Marivi Mendizabal , Mark Dixon , Anthony E. Storey , Edward R. Bacon , Vinay Chandrakant Desai , Sudhakar Kasina , Henry Raphael Wolfe
发明人： Alan Cuthbertson , Marivi Mendizabal , Mark Dixon , Anthony E. Storey , Edward R. Bacon , Vinay Chandrakant Desai , Sudhakar Kasina , Henry Raphael Wolfe
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07K7/06 , A61K51/088 , C07K14/245 , G01N33/57419
摘要： A peptide-chelate conjugate with affinity for the ST receptor is disclosed, wherein the chelate is tetradentate. The peptide-chelate conjugate of the invention may be labelled with a radiometal to provide a metal complex. A radiopharmaceutical composition comprising the metal complex is provided. which is suitable for the diagnostic imaging of colorectal cancer. Also provided for in the invention is a kit for the preparation of the radiopharmaceutical preparation.
摘要翻译：公开了对ST受体具有亲和性的肽 - 螯合物缀合物，其中螯合物是四齿酸盐。本发明的肽 - 螯合物缀合物可用放射性金属标记以提供金属络合物。提供了包含金属络合物的放射性药物组合物。这适用于结肠直肠癌的诊断成像。本发明还提供了用于制备放射性药物制剂的试剂盒。

2. 发明申请

US20140296212A1 SUBSTITUTED PHENOXYPROPYLCYCLOAMINE DERIVATIVES AS HISTAMINE-3 (H3) RECEPTOR LIGANDS 审中-公开
标题翻译：作为HISTAMINE-3（H3）受体配体的取代的羟基丙烯酰胺衍生物
公开(公告)号：US20140296212A1
公开(公告)日：2014-10-02
申请号：US14177046
申请日：2014-02-10
申请人： Edward R. Bacon , Thomas R. Bailey , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Allison L. Zulli , Brigitte Lesur , Babu G. Sundar , Christophe Yue
发明人： Edward R. Bacon , Thomas R. Bailey , Sankar Chatterjee , Derek Dunn , Greg A. Hostetler , Robert L. Hudkins , Allison L. Zulli , Brigitte Lesur , Babu G. Sundar , Christophe Yue
IPC分类号： C07D403/12 , C07C217/54 , C07D211/22 , C07D209/44 , C07D215/02 , C07D207/08 , C07D217/04
CPC分类号： C07D403/12 , C07C217/54 , C07D207/06 , C07D207/08 , C07D207/10 , C07D207/27 , C07D209/44 , C07D211/14 , C07D211/22 , C07D211/38 , C07D211/46 , C07D215/02 , C07D215/06 , C07D217/04 , C07D241/08 , C07D295/108 , C07D295/185 , C07D401/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
摘要翻译：本发明提供式I化合物：它们用作H3拮抗剂/反向激动剂，其制备方法及其药物组合物。

3. 发明申请

US20120295882A1 Tricyclic Derivatives and Their Pharmaceutical Use and Compositions 失效
标题翻译：三环衍生物及其药物用途和组合物
公开(公告)号：US20120295882A1
公开(公告)日：2012-11-22
申请号：US13529378
申请日：2012-06-21
申请人： Edward R. Bacon , Thomas R. Bailey , Derek D. Dunn , Greg A. Hostetler , Robert J. McHugh , George C. Morton , Gerard C. Rosse , Joseph M. Salvino , Babu G. Sundar , Rabindranath Tripathy
发明人： Edward R. Bacon , Thomas R. Bailey , Derek D. Dunn , Greg A. Hostetler , Robert J. McHugh , George C. Morton , Gerard C. Rosse , Joseph M. Salvino , Babu G. Sundar , Rabindranath Tripathy
IPC分类号： A61K31/4355 , C07D491/20 , A61K31/438 , A61K31/444 , A61K31/506 , C07D495/20 , A61K31/497 , A61K31/4709 , A61K31/5377 , C07D491/22 , C07D513/04 , A61K31/4725 , A61K31/496 , A61P25/22 , A61P25/08 , A61P25/24 , A61P25/18 , A61P25/28 , A61P25/16 , A61P25/20 , A61P25/30 , A61P3/04 , A61P25/00 , C07D491/048
CPC分类号： C07D491/153 , C07D491/048 , C07D491/20 , C07D513/04
摘要： This application relates to tricyclic compounds of Formula I: including all stereoisomers, mixtures of stereoisomers, and salts thereof. This application also relates to compositions comprising compounds of Formula I and uses therefore.
摘要翻译：本申请涉及式I的三环化合物：包括所有立体异构体，立体异构体的混合物及其盐。本申请还涉及包含式I化合物的组合物并因此使用。

4. 发明授权

US06670358B2 Substituted thioacetamides 失效
公开(公告)号：US06670358B2
公开(公告)日：2003-12-30
申请号：US10014645
申请日：2001-10-26
申请人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , John P. Mallamo , Matthew S. Miller , Rabindranath Tripathy , Jeffry L. Vaught
发明人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , John P. Mallamo , Matthew S. Miller , Rabindranath Tripathy , Jeffry L. Vaught
IPC分类号： C07D21302
CPC分类号： C07D263/34 , C07C317/44 , C07C323/60 , C07C323/63 , C07C2603/18 , C07C2603/32 , C07D207/16 , C07D207/273 , C07D207/416 , C07D211/88 , C07D213/34 , C07D219/04 , C07D231/54 , C07D233/64 , C07D261/08 , C07D263/16 , C07D263/32 , C07D275/02 , C07D277/26 , C07D277/56 , C07D307/68 , C07D311/84 , C07D333/18 , C07D335/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/06 , C07D495/04
摘要： The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.

5. 发明授权

US06492396B2 Substituted thioacetamides 有权
公开(公告)号：US06492396B2
公开(公告)日：2002-12-10
申请号：US09855228
申请日：2001-05-15
申请人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , John P. Mallamo , Jeffry L. Vaught , Matthew S. Miller
发明人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , John P. Mallamo , Jeffry L. Vaught , Matthew S. Miller
IPC分类号： C07D40102
CPC分类号： C07D495/04 , C07C317/44 , C07C323/60 , C07C2603/18 , C07D207/16 , C07D207/416 , C07D211/88 , C07D213/34 , C07D219/04 , C07D231/54 , C07D233/64 , C07D261/08 , C07D263/16 , C07D263/32 , C07D263/34 , C07D275/02 , C07D277/26 , C07D277/56 , C07D307/68 , C07D311/84 , C07D333/18 , C07D335/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/06
摘要： The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.

6. 发明授权

US5620677A Compositions of iodophenoxy alkanes and iodophenyl ethers for visualization of the gastrointestinal tract 失效
标题翻译：碘苯氧基烷烃和碘苯醚的组合物，用于胃肠道的可视化
公开(公告)号：US5620677A
公开(公告)日：1997-04-15
申请号：US189949
申请日：1994-02-01
申请人： Carl R. Illig , Eugene R. Cooper , John L. Toner , Donald A. Upson , Brent D. Douty , Thomas J. Caulfield , Edward R. Bacon , 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 , Edward R. Bacon , Kimberly G. Estep , Kurt A. Josef , Shaughnessy Robinson , Paul P. Spara
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 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=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 1-4;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.
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 = 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1-4; n为1-5; m为1-15; p为1-10; 并且Q是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

US5466433A Polyiodinated aroyloxy esters 失效
标题翻译：多碘化芳酰基酯
公开(公告)号：US5466433A
公开(公告)日：1995-11-14
申请号：US261794
申请日：1994-06-20
申请人： Edward R. Bacon , Sol J. Daum , Paul P. Spara
发明人： Edward R. Bacon , Sol J. Daum , Paul P. Spara
IPC分类号： C07C69/76 , A61K49/04 , C07C233/54 , C07C233/88 , C07C233/91
CPC分类号： A61K49/0433 , C07C233/54 , C07C233/88 , C07C233/91
摘要： Compounds having the structure ##STR1## wherein Z--COO).sub.m is the residue of a polyiodinated aromatic acid; m is 1, 2, 3 or 4;n is an integer from 1 to 20;R.sup.1 and R.sup.2 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy or acylamino; andR.sup.5 is H, alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl;are useful as contrast agents in x-ray imaging compositions and methods.
摘要翻译：具有结构的化合物，其中Z-COO）m是多元芳族酸的残基; m为1,2,3或4; n为1〜20的整数， R 1和R 2独立地为H，烷基，氟烷基，环烷基，芳基，芳烷基，烷氧基或芳氧基; R 3和R 4独立地为H，烷基，氟代烷基，环烷基，芳基，芳烷基，烷氧基，芳氧基，卤素，羟基或酰基氨基; R5是H，烷基，环烷基，芳基，芳烷基，烷氧基烷基或乙酰氨基烷基; 作为x射线成像组合物和方法中的造影剂是有用的。

8. 发明授权

US5384107A Iodinated aromatic compounds 失效
标题翻译：碘化芳族化合物
公开(公告)号：US5384107A
公开(公告)日：1995-01-24
申请号：US285595
申请日：1994-08-03
申请人： Baldev Singh , Edward R. Bacon , Carl R. Illig
发明人： Baldev Singh , Edward R. Bacon , Carl R. Illig
IPC分类号： C07C57/52 , A61K49/04 , C07C233/54 , C07C233/88 , C07C255/55
CPC分类号： A61K49/0433 , C07C233/54 , C07C233/88 , C07C255/55
摘要： Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid; n is an integer from 0 to 6;R.sup.1 and R.sup.2 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy or acylamino;Q represents the atoms necessary to complete a carbocyclic or heterocyclic unsaturated mono- or bicyclic aromatic ring; andR.sup.5 is H, alkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy, amino, acylamino, alkoxyalkyl, fluoroalkyl, acetamidoalkyl, COO-alkyl, cyano, carboxamido, sulfonate, sulfonamido, ureido, or carbamyl are useful as contrast agents in x-ray imaging compositions and methods.
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; n是0至6的整数; R 1和R 2独立地是H，烷基，氟代烷基，环烷基，芳基，芳烷基，烷氧基或芳氧基 R 3和R 4独立地为H，烷基，氟代烷基，环烷基，芳基，芳烷基，烷氧基，芳氧基，卤素，羟基或酰基氨基; Q表示完成碳环或杂环不饱和单环或双环芳环所必需的原子; H，烷基，环烷基，芳基，芳烷基，烷氧基，芳氧基，卤素，羟基，氨基，酰氨基，烷氧基烷基，氟代烷基，乙酰氨基烷基，COO-烷基，氰基，甲酰氨基，磺酸酯，亚磺酰氨基，脲基或氨基甲酰基可用作对比剂 x射线成像组合物和方法。

9. 发明授权

US5346688A Iodinated wetting agents 失效
标题翻译：碘化润湿剂
公开(公告)号：US5346688A
公开(公告)日：1994-09-13
申请号：US991640
申请日：1992-12-16
申请人： Edward R. Bacon , Gregory L. McIntire
发明人： Edward R. Bacon , Gregory L. McIntire
IPC分类号： A61K49/04 , C07C53/126 , C07C63/06 , C07C233/54
CPC分类号： C07C233/54
摘要： Compounds having the structure ##STR1## wherein (Z)--COO is the residue of an iodinated aromatic acid; M is H, a cation, --CH.sub.2 CH.sub.2 O--.sub.m H, and --CH.sub.2 CH(OH)O--.sub.p H;m is an integer from 1 to 150;p is an integer from 1 to 50; andL is one or more divalent linking groups selected from alkylene, cycloalkylene, arylene, arylenealkylene, and alkylenearylene are particularly useful as wetting agents in x-ray imaging compositions.
摘要翻译：具有结构（Z）COOLCO2M的化合物，其中（Z）-COO是碘化芳族酸的残基; M是H，阳离子，-CH2CH2O-mH和-CH2CH（OH）O-pH; m为1〜150的整数; p是1至50的整数; L是选自亚烷基，亚环烷基，亚芳基，亚芳基亚烷基和亚烷基亚芳基中的一个或多个二价连接基团，其特别用作x射线成像组合物中的润湿剂。

10. 发明授权

US4963561A Imidazopyridines, their preparation and use 失效
标题翻译：咪唑并吡啶，其制备和用途
公开(公告)号：US4963561A
公开(公告)日：1990-10-16
申请号：US486637
申请日：1990-02-28
申请人： George Y. Lesher , Edward R. Bacon , Baldev Singh , Gee-Hong Kuo
发明人： George Y. Lesher , Edward R. Bacon , Baldev Singh , Gee-Hong Kuo
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Novel 1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones having an aryl or heteroaryl group in the 6-position, useful as phosphodiesterase inhibitors, are prepared by reacting a 2-amino-5-(aryl or heteroaryl)pyridine-3-carboxylic acid with diphenylphosphoryl azide. The compounds are of the formula ##STR1## where R.sub.1 and R.sub.3 are hydrogen or lower-alkyl, R.sub.5 is lower-alkyl or fluorinated lower-alkyl, and Ar is 4- or 3-pyridinyl, or phenyl or substituted phenyl.
摘要翻译：具有6位芳基或杂芳基的新颖的1,3-二氢-2H-咪唑并[4,5-b]吡啶-2-酮可用作磷酸二酯酶抑制剂，通过2-氨基-5- （芳基或杂芳基）吡啶-3-羧酸与二苯基磷酰基叠氮化物。这些化合物具有式“IMAGE”，其中R 1和R 3是氢或低级烷基，R 5是低级烷基或氟代低级烷基，Ar是4-或3-吡啶基，或苯基或取代的苯基。

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