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1. 发明申请

WO2011087712A3 TRICYCLIC DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS 审中-公开
标题翻译： TRICYCLIC衍生物及其药物用途和组合物
公开(公告)号：WO2011087712A3
公开(公告)日：2011-09-29
申请号：PCT/US2010060937
申请日：2010-12-17
申请人： CEPHALON INC , BACON EDWARD R , BAILEY THOMAS R , DUNN DEREK D , HOSTETLER GREG A , MCHUGH ROBERT J , MORTON GEORGE C , ROSSE GERARD C , SALVINO JOSEPH M , SUNDAR BABU G , TRIPATHY RABINDRANATH
发明人： BACON EDWARD R , BAILEY THOMAS R , DUNN DEREK D , HOSTETLER GREG A , MCHUGH ROBERT J , MORTON GEORGE C , ROSSE GERARD C , SALVINO JOSEPH M , SUNDAR BABU G , TRIPATHY RABINDRANATH
IPC分类号： C07D491/048 , A61K31/4355 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/36 , C07D491/153 , C07D491/20 , C07D513/04
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）化合物的组合物及其用途。

2. 发明申请

WO2009097567A1 SUBSTITUTED SPIROCYCLIC PIPERIDINE DERIVATIVES AS HISTAMINE-3 (H3) RECEPTOR LIGANDS 审中-公开
标题翻译：作为组胺-3（3H）受体配体的取代的螺环哌嗪衍生物
公开(公告)号：WO2009097567A1
公开(公告)日：2009-08-06
申请号：PCT/US2009/032709
申请日：2009-01-30
申请人： CEPHALON, INC. , PHARMACOPEIA, INC. , BACON, Edward, R. , DANDU, Reddeppareddy , GUISE-ZAWACKI, Lisa , HUANG, Chia-yu , HUDKINS, Robert, L. , TAO, Ming
发明人： BACON, Edward, R. , DANDU, Reddeppareddy , GUISE-ZAWACKI, Lisa , HUANG, Chia-yu , HUDKINS, Robert, L. , TAO, Ming
IPC分类号： C07D491/10 , A61K31/438 , A61P25/00
CPC分类号： C07D491/10
摘要： The present invention provides compounds of Formula (I): their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceuticals 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

WO2008063232B1 SUBSTITUTED PYRAZOLOPYRIMIDINES 审中-公开
标题翻译：取代的吡唑啉酮
公开(公告)号：WO2008063232B1
公开(公告)日：2008-09-18
申请号：PCT/US2007011619
申请日：2007-05-15
申请人： CEPHALON INC , BACON EDWARD R , BAILEY THOMAS R , BECKNELL NADINE C , GINGRICH DIANE E , HOSTETLER GREG , HUDKINS ROBERT L , LEARN KEITH S , WAGNER JASON C
发明人： BACON EDWARD R , BAILEY THOMAS R , BECKNELL NADINE C , GINGRICH DIANE E , HOSTETLER GREG , HUDKINS ROBERT L , LEARN KEITH S , WAGNER JASON C
IPC分类号： C07D401/14 , A61K31/517 , A61K31/52 , A61P3/10 , A61P25/16 , A61P25/18 , A61P25/28 , C07D403/04 , C07D473/00 , C07D487/04
CPC分类号： C07D401/14 , C07D403/04 , C07D487/04
摘要： The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , X, W, and ring A are as defined herein; pharmaceutical compositions of substituted heterobicyclic pyrimidines of Formula (I); and their use in the treatment of chronic neurodegenerative diseases, neurotraumatic diseases, depression and/or diabetes. More particularly, the present invention relates to substituted pyrazolopyrimidines of Formula (I).
摘要翻译：本发明涉及化学组成，其制备方法和组合物的用途。特别地，本发明涉及包含式（I）的取代的杂双环嘧啶的组合物：其中R 1，R 2，R 3， R 4，R 5，X，W和环A如本文所定义; 式（I）的取代杂双环嘧啶的药物组合物; 及其用于治疗慢性神经变性疾病，神经创伤性疾病，抑郁症和/或糖尿病的用途。更具体地，本发明涉及式（I）的取代的吡唑并嘧啶。

4. 发明申请

WO1996000210A1 2,4,6-TRIIODO-5-SUBSTITUTED-AMINO-ISOPHTHALATE ESTERS USEFUL AS X-RAY CONTRAST AGENTS FOR MEDICAL DIAGNOSTIC IMAGING 审中-公开
标题翻译： 2,4,6-TRIIODO-5-取代的氨基异癸酸酯作为用于医学诊断成像的X射线对比剂
公开(公告)号：WO1996000210A1
公开(公告)日：1996-01-04
申请号：PCT/US1995007400
申请日：1995-06-09
申请人： EASTMAN KODAK COMPANY , BACON, Edward, R. , DAUM, Sol, J. , ESTEP, Kimberly, G.
发明人： EASTMAN KODAK COMPANY
IPC分类号： C07C233/54
CPC分类号： C07C233/54 , A61K49/0433
摘要： Compounds having structure (I) wherein Q is (II); n is an integer from 0 to 20; R is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl; R , R , R and R are independently H, alkyl, fluoroalkyl, halogen, hydroxy, acylamino, acetamidoalkyl, cyano, sulfonyl, carboxamido or sulfonamido; R is alkyl, cycloalkyl, aryl or aralkyl; and R is H or -COR are useful as contrast agents in medical diagnostic x-ray imaging compositions and methods.
摘要翻译：具有结构（I）的化合物，其中Q是（II）; n为0〜20的整数， R 1是H，烷基，氟代烷基，环烷基，芳基，芳烷基，烷氧基烷基或乙酰氨基烷基; R 2，R 3，R 4和R 5独立地是H，烷基，氟烷基，卤素，羟基，酰氨基，乙酰氨基烷基，氰基，磺酰基，甲酰氨基或亚磺酰氨基; R 6是烷基，环烷基，芳基或芳烷基; 和R 7是H或-COR 6可用作医学诊断x射线成像组合物和方法中的造影剂。

5. 发明申请

WO2011087712A2 TRICYCLIC DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS 审中-公开
标题翻译：三环衍生物及其药物用途和组合物
公开(公告)号：WO2011087712A2
公开(公告)日：2011-07-21
申请号：PCT/US2010/060937
申请日：2010-12-17
申请人： CEPHALON, INC. , BACON, Edward R. , BAILEY, Thomas R. , DUNN, Derek D. , HOSTETLER, Greg A. , MCHUGH, Robert J. , MORTON, George C. , ROSSE, Gerard C. , SALVINO, Joseph M. , SUNDAR, Babu G. , TRIPATHY, Rabindranath
发明人： BACON, Edward R. , BAILEY, Thomas R. , DUNN, Derek D. , HOSTETLER, Greg A. , MCHUGH, Robert J. , MORTON, George C. , ROSSE, Gerard C. , SALVINO, Joseph M. , SUNDAR, Babu G. , TRIPATHY, Rabindranath
IPC分类号： C07D491/048 , C07D491/20 , C07D513/04 , C07D491/153 , A61K31/4355 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/36
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，立体异构体混合物及其盐。本申请还涉及包含式（I）化合物并因此使用的组合物。

6. 发明申请

WO2011002984A1 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：WO2011002984A1
公开(公告)日：2011-01-06
申请号：PCT/US2010/040757
申请日：2010-07-01
申请人： CEPHALON, INC. , CEPHALON FRANCE , BACON, Edward R. , BAILEY, Thomas , CHATTERJEE, Sankar , DUNN, Derek , HOSTETLER, Greg A. , HUDKINS, Robert L. , LESUR, Brigitte , SUNDAR, Babu G. , YUE, Christophe , ZULLI, Allison L.
发明人： BACON, Edward R. , BAILEY, Thomas , CHATTERJEE, Sankar , DUNN, Derek , HOSTETLER, Greg A. , HUDKINS, Robert L. , LESUR, Brigitte , SUNDAR, Babu G. , YUE, Christophe , ZULLI, Allison L.
IPC分类号： C07D207/06 , C07D207/10 , C07D209/44 , C07D211/14 , C07D211/38 , C07D211/46 , A61K31/496 , A61K31/5377 , A61P25/00 , C07D215/06 , C07D217/04 , C07D241/08 , C07D401/12 , C07D403/12 , C07D407/12
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 H 3 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。

7. 发明申请

WO2009097567A4 SUBSTITUTED SPIROCYCLIC PIPERIDINE DERIVATIVES AS HISTAMINE-3 (H3) RECEPTOR LIGANDS 审中-公开
标题翻译：取代的螺环哌啶衍生物作为组胺-3（H3）受体配体
公开(公告)号：WO2009097567A4
公开(公告)日：2009-10-29
申请号：PCT/US2009032709
申请日：2009-01-30
申请人： CEPHALON INC , PHARMACOPEIA INC , BACON EDWARD R , DANDU REDDEPPAREDDY , GUISE-ZAWACKI LISA , HUANG CHIA-YU , HUDKINS ROBERT L , TAO MING
发明人： BACON EDWARD R , DANDU REDDEPPAREDDY , GUISE-ZAWACKI LISA , HUANG CHIA-YU , HUDKINS ROBERT L , TAO MING
IPC分类号： C07D491/10 , A61K31/438 , A61P25/00
CPC分类号： C07D491/10
摘要： The present invention provides compounds of Formula (I): their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceuticals compositions thereof.
摘要翻译：本发明提供了式（I）的化合物：它们作为H3拮抗剂/反向激动剂的用途，它们的制备方法，以及它们的药物组合物。

8. 发明申请

WO0025819A9 ENHANCED RADIATION THERAPY 审中-公开
标题翻译：增强辐射治疗
公开(公告)号：WO0025819A9
公开(公告)日：2000-09-21
申请号：PCT/US9925558
申请日：1999-10-29
申请人： GEN HOSPITAL CORP , NYCOMED IMAGING AS , WOLF GERALD L , MCINTIRE GREGORY L , BACON EDWARD R
发明人： WOLF GERALD L , MCINTIRE GREGORY L , BACON EDWARD R
IPC分类号： A61K9/127 , A61K31/167 , A61K31/235 , A61K33/06 , A61K33/18 , A61K33/22 , A61K33/24 , A61K33/26 , A61K33/32 , A61K33/38 , A61K41/00 , A61K45/00 , A61K49/04 , A61K51/00 , A61N5/10 , A61P35/00 , C08G73/02 , C08K3/08 , C08K5/00 , C08L79/02
CPC分类号： A61K41/0038 , A61N2005/1091 , A61N2005/1098
摘要： The invention features new methods of enhanced radiation therapy based on the discovery that by using controlled combinations of (i) specific radiodense compositions, (ii) specific modes of administration of these radiodense compositions, and (iii) specific energy bands and sources of radiation, that the effect of radiation on tumors and other diseased tissues can be effectively and safely enhanced to provide significantly improved radiation therapy.
摘要翻译：本发明的特征在于基于以下发现的新的增强放射治疗方法：通过使用（i）特定的放射线组合物的受控组合，（ii）这些放射性组合物的特定给药模式，和（iii）特定能带和辐射源，辐射对肿瘤和其他病变组织的影响可以有效和安全地增强，以提供显着改善的放射治疗。

9. 发明申请

WO1996000089A1 DIATRIZOXY ESTER AS X-RAY CONTRAST AGENTS FOR IMAGING THE BLOOD POOL AND LYMPHATIC SYSTEM 审中-公开
标题翻译： DIATRIZOXY ESTER作为X射线对比剂用于成像血液池和淋巴系统
公开(公告)号：WO1996000089A1
公开(公告)日：1996-01-04
申请号：PCT/US1995007336
申请日：1995-06-08
申请人： EASTMAN KODAK COMPANY , BACON, Edward, R. , ILLIG, Carl, R. , OSIFO, Irennegbe, K. , CAULFIELD, Thomas, S.
发明人： EASTMAN KODAK COMPANY
IPC分类号： A61K49/04
CPC分类号： B82Y5/00 , A61K49/0485
摘要： This invention relates to methods of x-ray diagnostic imaging the blood pool and/or lymph system of a mammal comprising administering a contrast effective amount of a particulate iodinated aroyloxy ester contrast agent having structure (I) wherein n is an integer from 3 to 20; R is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl; R , R and R are independently H, alkyl, fluoroalkyl, alkoxy, aryloxy, halogen, hydroxy, acylamino, acetamidoalkyl, -COO-alkyl, -COO-aryl, -COO-aralkyl, cyano, sulfonyl, carboxamido or sulfonamido; R is H, alkyl, fluoroalkyl, halogen, hydroxy, acylamino, acetamidoalkyl, cyano, sulfonyl, carboxamido or sulfonamido; R and R are independently alkyl, cycloalkyl, aryl or aralkyl; and R and R are independently H or -COR . This invention further relates to novel iodinated aroyloxy ester contrast agents having the above structure wherein n is an integer from 5 to 20, 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和/或淋巴系统进行X射线诊断成像的方法，包括给予对比有效量的具有结构（I）的结构（I）的颗粒状碘化芳氧基酯造影剂，其中n为3-20的整数 ; R 1是H，烷基，氟代烷基，环烷基，芳基，芳烷基，烷氧基烷基或乙酰氨基烷基; R 2，R 3和R 4独立地是H，烷基，氟代烷基，烷氧基，芳氧基，卤素，羟基，酰氨基，乙酰氨基烷基，-COO-烷基，-COO-芳基，-COO-芳烷基，氰基，磺酰基，甲酰氨基或亚磺酰氨基; 羟基，酰氨基，乙酰氨基烷基，氰基，磺酰基，甲酰氨基或亚磺酰氨基; R 5是H，烷基，氟代烷基，卤素，羟基， R 6和R 7独立地是烷基，环烷基，芳基或芳烷基; R 8和R 9独立地为H或-COR 6。本发明还涉及具有上述结构的具有上述结构的新型碘化芳氧基酯造影剂，其中n为5-20的整数，以及包含这些试剂的x射线对比剂组合物，以及利用这些试剂的X射线诊断成像方法。

10. 发明申请

WO2005100309A1 TRICYCLIC AROMATIC AND BIS-PHENYL SULFINYL DERIVATIVES 审中-公开
标题翻译：三元芳香和二苯基硫代衍生物
公开(公告)号：WO2005100309A1
公开(公告)日：2005-10-27
申请号：PCT/US2005/012930
申请日：2005-04-13
申请人： CEPHALON, INC. , BACON, Edward, R. , CHATTERJEE, Sankar , DUNN, Derek , GRUNER, John, A. , TRIPATHY, Rabindranath
发明人： BACON, Edward, R. , CHATTERJEE, Sankar , DUNN, Derek , GRUNER, John, A. , TRIPATHY, Rabindranath
IPC分类号： C07C317/44
CPC分类号： C07C317/44 , C07C317/10 , C07C317/12 , C07C317/18 , C07C317/28 , C07C321/22 , C07C323/12 , C07C323/22 , C07C323/25 , C07C323/49 , C07C323/52 , C07C323/60 , C07C323/61 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D249/12 , C07D307/38 , C07D333/18 , C07D333/22
摘要： The present invention provides compounds of the structure (I) wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases such as for example excessive sleepiness, promotion and/or improvement of wakefulness.
摘要翻译：本发明提供了其中组成成分在本文中定义的结构（I）的化合物，包括其药物组合物和治疗诸如过度嗜睡，促进和/或改善觉醒的疾病的方法。

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