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1. 发明申请

WO2010078229A1 ANTI-VIRAL COMPOUNDS, TREATMENT, AND ASSAY 审中-公开
标题翻译：反虚构化合物，治疗和测定
公开(公告)号：WO2010078229A1
公开(公告)日：2010-07-08
申请号：PCT/US2009/069556
申请日：2009-12-28
申请人： SOUTHERN RESEARCH INSTITUTE , MADDRY, Joseph, A. , SEVERSON, William , JONSSON, Colleen, B. , NOAH, James, W. , NOAH, Diana, L. , CHEN, Xi
发明人： MADDRY, Joseph, A. , SEVERSON, William , JONSSON, Colleen, B. , NOAH, James, W. , NOAH, Diana, L. , CHEN, Xi
IPC分类号： A61K31/505
CPC分类号： C07D239/70 , C07D405/04 , C07D471/04 , C07D487/04 , C07D491/052 , C07D495/04
摘要： The compounds provided herein are suitable for inhibiting a virus in a patient and for treating a patient suffering from a viral infection such as an influenza virus. Also provided is a method for screening of compounds for use in treating and preventing viral infections. The assay screens compounds for activity against an influenza virus by measuring the cytopathogenic effect (CPE) of the compound on influenza infected-cells using precent cell viability as the end point.
摘要翻译：本文提供的化合物适合于抑制患者中的病毒和治疗患有病毒感染的患者，例如流感病毒。还提供了用于筛选用于治疗和预防病毒感染的化合物的方法。通过使用优先细胞活力作为终点，通过测量化合物对流感感染细胞的细胞致病作用（CPE），该测定屏蔽了针对流感病毒的活性的化合物。

2. 发明申请

WO2011047129A1 TREATMENT OF NEURODEGENERATIVE DISEASES, CAUSATION OF MEMORY ENHANCEMENT, AND ASSAY FOR SCREENING COMPOUNDS FOR SUCH 审中-公开
标题翻译：治疗神经细胞增生性疾病，记忆增强的原因及其筛选化合物的测定
公开(公告)号：WO2011047129A1
公开(公告)日：2011-04-21
申请号：PCT/US2010/052624
申请日：2010-10-14
申请人： SOUTHERN RESEARCH INSTITUTE , GRIMALDI, Maurizio , HOBRATH, Judith, Varady , ANANTHAN, Subramaniam , MADDRY, Joseph, A.
发明人： GRIMALDI, Maurizio , HOBRATH, Judith, Varady , ANANTHAN, Subramaniam , MADDRY, Joseph, A.
IPC分类号： A01N57/00 , A61K31/675
CPC分类号： A61K31/5377 , A61K31/136 , A61K31/36 , A61K31/426 , A61K31/427 , A61K31/444 , A61K31/675
摘要： Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, and Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.
摘要翻译：描述了通过施用某些杂环和芳族化合物增强记忆和/或学习和预防神经变性的方法。这些方法对于治疗患有神经变性疾病的患者特别有用，例如（但不限于）阿尔茨海默病，帕金森氏症和Lou Gehrig氏病（ALS）疾病或记忆障碍或学习障碍。还提供了使用荧光素酶报告基因评估NF-kB基因上调的基于神经元的基于人细胞的测定法，其筛选用于增强记忆或学习的方法中的化合物。

3. 发明申请

WO2002088323A2 GENE DELIVERY COMPOUNDS 审中-公开
标题翻译：基因递送化合物
公开(公告)号：WO2002088323A2
公开(公告)日：2002-11-07
申请号：PCT/US2002/013895
申请日：2002-05-02
申请人： UAB RESEARCH FOUNDATION , SOUTHERN RESEARCH INSTITUTE , SORSCHER, Eric, J. , HONG, Jeong, S. , HARRIS, Jennifer, E. , CURLEE, Kimberly, V. , MADDRY, Joseph, A. , PARKER, William, B. , WAUD, William, R.
发明人： SORSCHER, Eric, J. , HONG, Jeong, S. , HARRIS, Jennifer, E. , CURLEE, Kimberly, V. , MADDRY, Joseph, A. , PARKER, William, B. , WAUD, William, R.
IPC分类号： C12N
CPC分类号： C07D213/53 , A61K31/15 , A61K31/7076 , A61K45/06 , A61K48/0008 , A61K2300/00
摘要： Compounds having the structure (I) wherein R 1 , R 2 and R 3 are each independently a C O-12 substituent selected from the group consisting of: hydrogen, a heteroatom, alkyl, alkenyl, alkynyl, heteroatom substituted alkyl, heteroatom substituted alkenyl, heteroatom substituted alkynyl, aryl, arylalkyl, arylalkenyl, arylalkynyl; where the heteroatom is selected from the group consisting of: N, O and S; and where (A) is a single or double bond between N and R 3 . Further the C O-12 substituent is linear, branched or cyclic and optionally includes a pendant moiety selected from the group consisting of: carbonyl, hydroxyl, carboxyl, amine, thiol, thioester, thioether, phosphate, alkoxy, aryl, arylalkyl, sulfonamide and alkyl halide. Further, compounds (6883, 6898, 6975, 7036, 7064 and 8496) are provided. A process is provided for activating gene transfer in a subject by administering a pharmaceutically effective amount of a gene transfer activating compound to a subject and delivering pharmaceutically effective amount of a vector containing a nucleic so that the nucleic acid is transcribed in a target cell of the subject. A process for activating gene transfer to a cell is provided. A kit for activating gene transfer is provided.
摘要翻译：具有结构（I）的化合物，其中R 1，R 2和R 3各自独立地是选自以下的CO-12取代基：氢，杂原子，烷基，烯基，炔基，杂原子取代的烷基，杂原子取代的烯基，杂原子取代的炔基，芳基，芳基烷基，芳基烯基，芳基炔基; 其中杂原子选自：N，O和S; 其中（A）是N和R3之间的单键或双键。此外，CO-12取代基是直链，支链或环状的，并且任选地包括选自羰基，羟基，羧基，胺，硫醇，硫酯，硫醚，磷酸酯，烷氧基，芳基，芳基烷基，磺酰胺和烷基卤化物。此外，提供了化合物（6883,6898,6975,7036,7064和8496）。提供了通过向受试者施用药学有效量的基因转移活化化合物并递送药学有效量的含有核酸的载体以使得核酸被转录到靶细胞的靶细胞中来激活受试者中的基因转移的方法学科。提供了一种激活基因转移至细胞的方法。提供用于激活基因转移的试剂盒。

4. 发明申请

WO2009114651A3 USE OF '-THIO-2'-DEOXYNUCLEOSIDES AS ANRI ORTHOPOXVIRUS AGENTS 审中-公开
标题翻译： '二硫代脱氧核糖核苷酸作为角叉菜病毒剂使用
公开(公告)号：WO2009114651A3
公开(公告)日：2010-03-18
申请号：PCT/US2009036869
申请日：2009-03-12
申请人： SOUTHERN RES INST , SECRIST JOHN A III , TIWARI KAMAL N , MADDRY JOSEPH A
发明人： SECRIST JOHN A III , TIWARI KAMAL N , MADDRY JOSEPH A
IPC分类号： A01N43/04
CPC分类号： A61K31/513 , A61K9/2054 , A61K9/4858 , A61K9/4866 , A61K2300/00
摘要： Compound represented by the formulae: wherein each R individually is H or aliphatic acyl or aromatic acyl group; X is selected from the group consisting of hydrogen, fiuoro, chloro, bromo, iodo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano, aryl and nitro; pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are used as inhibitors of orthopoxviruses and for treating patients suffering from an orthopoxvirus infection such as, but not limited to, smallpox, cowpox, monkeypox and camelpox.
摘要翻译：由下式表示的化合物：其中每个R各自为H或脂族酰基或芳族酰基; X选自氢，氟，氯，溴，碘，烷氧基，烷基，卤代烷基，烯基，卤代烯基，炔基，氨基，单烷基氨基，二烷基氨基，氰基，芳基和硝基。其药学上可接受的盐，其前药及其混合物用作正痘病毒的抑制剂并用于治疗患有正痘病毒感染的患者，例如但不限于天花，牛痘，猴痘和骆驼痘。

5. 发明申请

WO2010022126A1 AZO-SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS 审中-公开
标题翻译： AZO取代的吡啶和吡嗪衍生物及其在治疗病毒感染中的应用
公开(公告)号：WO2010022126A1
公开(公告)日：2010-02-25
申请号：PCT/US2009/054269
申请日：2009-08-19
申请人： SCHERING CORPORATION , SOUTHERN RESEARCH INSTITUTE , NJOROGE, F. George , PIWINSKI, John J. , SHIH, Neng-Yang , KWONG, Cecil D. , ANANTHAN, Subramaniam , CLARK, Jeremy , GENG, Feng , KEZAR, III, Hollis S. , MADDRY, Joseph A. , REYNOLDS, Robert C. , ROYCHOWDHURY, Abhijit , SECRIST, III, John A.
发明人： NJOROGE, F. George , PIWINSKI, John J. , SHIH, Neng-Yang , KWONG, Cecil D. , ANANTHAN, Subramaniam , CLARK, Jeremy , GENG, Feng , KEZAR, III, Hollis S. , MADDRY, Joseph A. , REYNOLDS, Robert C. , ROYCHOWDHURY, Abhijit , SECRIST, III, John A.
IPC分类号： C07D239/50 , A61K31/505
CPC分类号： C07D239/50
摘要： The present invention provides compounds of Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R 1 , X, Y, Z, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 18 , R 19 , and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing dieases or disorders such as viral infections and virus-related disorders.
摘要翻译：本发明提供了式（I）化合物：（化学式应该插在这里，它以纸的形式出现）（I）和所述化合物的互变异构体，异构体和酯以及药学上可接受的盐，溶剂合物和前药的所述化合物，其中R，R 1，X，Y，Z，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 18，R 19和n各自独立地如本文所定义。还提供了包含这些化合物的组合物。本发明的化合物作为HCV的抑制剂是有效的，并且可单独使用和与其它治疗剂一起用于治疗或预防死亡或病症如病毒感染和病毒相关疾病。

6. 发明申请

WO2010022125A1 ETHYNYL-SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS 审中-公开
标题翻译：乙酰取代的吡啶和吡嗪衍生物及其在治疗病毒感染中的应用
公开(公告)号：WO2010022125A1
公开(公告)日：2010-02-25
申请号：PCT/US2009/054268
申请日：2009-08-19
申请人： SCHERING CORPORATION , SOUTHERN RESEARCH INSTITUTE , NJOROGE, F., George , ARASAPPAN, Ashok , BENNETT, Frank , PIWINSKI, John, J. , SHIH, Neng-Yang , KWONG, Cecil, D. , ANANTHAN, Subramaniam , CLARK, Jeremy , FOWLER, Anita, T. , GENG, Feng , KEZAR, III, Hollis, S. , MADDRY, Joseph, A. , REYNOLDS, Robert, C. , ROYCHOWDHURY, Abhijit , SECRIST, III, John, A.
发明人： NJOROGE, F., George , ARASAPPAN, Ashok , BENNETT, Frank , PIWINSKI, John, J. , SHIH, Neng-Yang , KWONG, Cecil, D. , ANANTHAN, Subramaniam , CLARK, Jeremy , FOWLER, Anita, T. , GENG, Feng , KEZAR, III, Hollis, S. , MADDRY, Joseph, A. , REYNOLDS, Robert, C. , ROYCHOWDHURY, Abhijit , SECRIST, III, John, A.
IPC分类号： C07D239/46 , C07D401/06 , C07D403/06 , C07D405/06 , C07D401/14 , C07D409/06 , C07D413/06 , C07D417/06 , A61K31/505 , A61K31/506
CPC分类号： C07D239/46 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The present invention provides compounds of Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R 1 , X, Y, Z, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 18 , R 19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing dieases or disorders such as viral infections and virus-related disorders.
摘要翻译：本发明提供了式（I）化合物：（化学式应该插在这里，它以纸的形式出现）（I）和所述化合物的互变异构体，异构体和酯以及药学上可接受的盐，溶剂合物和前药的所述化合物，其中R，R 1，X，Y，Z，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 18，R 19和n各自独立地如本文所定义。还提供了包含这些化合物的组合物。本发明的化合物作为HCV的抑制剂是有效的，并且可单独使用和与其它治疗剂一起用于治疗或预防死亡或病症如病毒感染和病毒相关疾病。

7. 发明申请

WO2009114651A8 USE OF '-THIO-2'-DEOXYNUCLEOSIDES AS ANRI ORTHOPOXVIRUS AGENTS 审中-公开
标题翻译： '二硫代脱氧核糖核苷酸作为角叉菜病毒剂使用
公开(公告)号：WO2009114651A8
公开(公告)日：2009-12-03
申请号：PCT/US2009036869
申请日：2009-03-12
申请人： SOUTHERN RES INST , SECRIST JOHN A III , TIWARI KAMAL N , MADDRY JOSEPH A
发明人： SECRIST JOHN A III , TIWARI KAMAL N , MADDRY JOSEPH A
IPC分类号： A61K31/513
CPC分类号： A61K31/513 , A61K9/2054 , A61K9/4858 , A61K9/4866 , A61K2300/00
摘要： Compound represented by the formulae: wherein each R individually is H or aliphatic acyl or aromatic acyl group; X is selected from the group consisting of hydrogen, fiuoro, chloro, bromo, iodo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano, aryl and nitro; pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are used as inhibitors of orthopoxviruses and for treating patients suffering from an orthopoxvirus infection such as, but not limited to, smallpox, cowpox, monkeypox and camelpox.
摘要翻译：由下式表示的化合物：其中每个R各自为H或脂族酰基或芳族酰基; X选自氢，氟，氯，溴，碘，烷氧基，烷基，卤代烷基，烯基，卤代烯基，炔基，氨基，单烷基氨基，二烷基氨基，氰基，芳基和硝基。其药学上可接受的盐，其前药及其混合物用作正痘病毒的抑制剂并用于治疗患有正痘病毒感染的患者，例如但不限于天花，牛痘，猴痘和骆驼痘。

8. 发明申请

WO2011062964A1 COMPOUNDS AND METHODS FOR ALTERING LIFESPAN OF EUKARYOTIC ORGANISMS 审中-公开
标题翻译：用于改变真菌生物活性成分的化合物和方法
公开(公告)号：WO2011062964A1
公开(公告)日：2011-05-26
申请号：PCT/US2010/056990
申请日：2010-11-17
申请人： UNIVERSITY OF ROCHESTER , SOUTHERN RESEARCH INSTITUTE , GOLDFARB, David, S. , MADDRY, Joseph, A. , RASMUSSEN, Lynn , WHITE, Ellie, Lucile , WENNERBERG, Krister
发明人： GOLDFARB, David, S. , MADDRY, Joseph, A. , RASMUSSEN, Lynn , WHITE, Ellie, Lucile , WENNERBERG, Krister
IPC分类号： A01N35/00 , A61K31/13
CPC分类号： C07C49/657 , C07C49/403 , C07C49/417 , C07C49/543 , C07C49/553 , C07C49/567 , C07C49/573 , C07C49/577 , C07C49/613 , C07C49/753 , C07C49/792 , C07C69/743 , C07C69/757 , C07C225/22 , C07C235/82 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D209/12 , C07D307/46 , C07D307/54 , C07D317/54 , C07D319/18 , C07D333/22
摘要： Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5 -butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation.
摘要翻译：提供通常具有三酮结构的化合物。化合物的实例包括1,3-环己二酮的衍生物，例如：1,3-环己二酮，2-丙酰基-5-环己基 - 2-丙酰基-5- [4-氟苯基] - ; 1,3-环己二酮，2-乙酰基-5-〔噻吩-2-基] - 1,3-环己二酮，2-乙酰基-5-丁基 - 和1,3-环己二酮，2-丙酰基-5- [双环[2.2.1]庚-2-烯-5-基] - 。这些化合物可用于改变真核生物的寿命并治疗炎症。

9. 发明申请

WO2010022128A1 ETHENYL-SUBSTITUTED PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE IN TREATING VIRAL INFECTIONS 审中-公开
标题翻译：乙基取代的吡啶和吡嗪衍生物及其在治疗病毒感染中的应用
公开(公告)号：WO2010022128A1
公开(公告)日：2010-02-25
申请号：PCT/US2009/054271
申请日：2009-08-19
申请人： SCHERING CORPORATION , SOUTHERN RESEARCH INSTITUTE , NJOROGE, F. George , PIWINSKI, John J. , SHIH, Neng-Yang , KWONG, Cecil D. , ANANTHAN, Subramaniam , CLARK, Jeremy , GENG, Feng , KEZAR, III, Hollis S. , MADDRY, Joseph A. , REYNOLDS, Robert C. , ROYCHOWDHURY, Abhijit , SECRIST, III, John A.
发明人： NJOROGE, F. George , PIWINSKI, John J. , SHIH, Neng-Yang , KWONG, Cecil D. , ANANTHAN, Subramaniam , CLARK, Jeremy , GENG, Feng , KEZAR, III, Hollis S. , MADDRY, Joseph A. , REYNOLDS, Robert C. , ROYCHOWDHURY, Abhijit , SECRIST, III, John A.
IPC分类号： C07D239/48 , A61K31/505 , A61P31/14
CPC分类号： C07D239/48
摘要： The present invention provides compounds of Formula (A): (Chemical formula should be inserted here as it appears on abstract in paper form) (A) and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, wherein wherein each of R, R 1 , X, Y, Z, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 18 , R 19 , R 22 , R 23 , and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing dieases or disorders such as viral infections and virus-related disorders.
摘要翻译：本发明提供了式（A）化合物：（化学式应该插在这里，它以纸质形式的摘要出现）（A）和所述化合物的互变异构体，异构体和酯以及药学上可接受的盐，溶剂合物和前药的所述化合物，其中R，R1，X，Y，Z，R2，R3，R4，R5，R6，R7，R8，R9，R18，R19，R22，R23和n各自独立地和定义于此。还提供了包含这些化合物的组合物。本发明的化合物作为HCV的抑制剂是有效的，并且可单独使用和与其它治疗剂一起用于治疗或预防死亡或病症如病毒感染和病毒相关疾病。

10. 发明申请

WO2010006251A1 5-QUINOLINONE AND IMIDAZOPYRIDINE COMPOUNDS AND USE THEREOF 审中-公开
标题翻译： 5-喹啉酮和咪唑并吡啶化合物及其用途
公开(公告)号：WO2010006251A1
公开(公告)日：2010-01-14
申请号：PCT/US2009/050239
申请日：2009-07-10
申请人： SOUTHERN RESEARCH INSTITUTE , MADDRY, Joseph, A. , KEETON, Adam , WHITT, Jason , PIAZZA, Gary
发明人： MADDRY, Joseph, A. , KEETON, Adam , WHITT, Jason , PIAZZA, Gary
IPC分类号： A01N43/42
CPC分类号： C07D215/54 , C07D401/04 , C07D407/04 , C07D487/04
摘要： 5-Quinolinone and Imidazopyrimidine compounds are provided that are useful for inhibiting the efflux of any therapeutic agent that is a MRP1 substrate. Also provided is a method for screening to identify additional MRP1 inhibitors.
摘要翻译：提供5-喹啉酮和咪唑并嘧啶化合物，其可用于抑制作为MRP1底物的任何治疗剂的流出。还提供了筛选以鉴定另外的MRP1抑制剂的方法。

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