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1. 发明申请

WO2011097607A1 ANTI-VIRAL TREATMENT AND ASSAY TO SCREEN FOR ANTI-VIRAL AGENT 审中-公开
标题翻译：反病毒治疗和测试可用于防病毒代理
公开(公告)号：WO2011097607A1
公开(公告)日：2011-08-11
申请号：PCT/US2011/023986
申请日：2011-02-08
申请人： SOUTHERN RESEARCH INSTITUTE , SEVERSON, Bill , CHUNG, Dong, Hong , JONSSON, Colleen, B. , WHITE, Ellie, Lucile , RASMUSSEN, Lynn , MADDOX, Clinton, Boykin , ANANTHAN, Subramaniam , PATHAK, Ashish, K. , MADDRY, Joseph, A.
发明人： SEVERSON, Bill , CHUNG, Dong, Hong , JONSSON, Colleen, B. , WHITE, Ellie, Lucile , RASMUSSEN, Lynn , MADDOX, Clinton, Boykin , ANANTHAN, Subramaniam , PATHAK, Ashish, K. , MADDRY, Joseph, A.
IPC分类号： A61K31/41 , A61K31/405 , A61K31/425 , A61K31/497
CPC分类号： C07H19/12 , A61K31/405 , A61K31/41 , A61K31/425 , A61K31/497 , C07D471/04 , C07D471/14 , C12Q1/025
摘要： The present disclosure relates to novel compounds of formulas (1) thorugh (19) and to a method for treating humans infected with a virus including various respiratory viruses such as members of the Paramyxoviridae family (respiratory syncytial virus (RSV), human metapneumovirus (HMPV), human parainfluenza virus (HPIV), measles virus, and mumps virus) with a compound of formulas (1) through (19). The present disclosure also relates to a cytopathic effect (CPE)-based assay that will assess virus-induced CPE for screening of compounds for treating viral diseases or inhibiting a virus.
摘要翻译：本公开涉及式（1）咳嗽（19）的新化合物和用于治疗感染病毒的人的方法，所述病毒包括各种呼吸道病毒如副粘病毒科（呼吸道合胞病毒（RSV），人间叶病毒（HMPV）），人副流感病毒（HPIV），麻疹病毒和腮腺炎病毒）与式（1）至（19）的化合物。本公开还涉及基于细胞病变效应（CPE）的测定法，其将评估用于筛选用于治疗病毒性疾病或抑制病毒的化合物的病毒诱导的CPE。

2. 发明申请

WO2008067002A3 AZOLE NUCLEOSIDES AND USE AS INHIBITORS OF RNA AND DNA VARIAL POLYMERASES 审中-公开
标题翻译：单核苷酸和用作RNA和DNA多肽的抑制剂
公开(公告)号：WO2008067002A3
公开(公告)日：2008-11-06
申请号：PCT/US2007078139
申请日：2007-09-11
申请人： SOUTHERN RES INST , UNIV NEW MEXICO , ARTERBURN JEFFREY B , JONSSON COLLEEN B , PARKER WILLIAM B
发明人： ARTERBURN JEFFREY B , JONSSON COLLEEN B , PARKER WILLIAM B
IPC分类号： A01N43/04 , A61K31/70 , C07H5/04 , C07H5/06 , C07H19/044 , C07H19/056
CPC分类号： C07H5/04 , C07H5/06 , C07H19/044 , C07H19/056
摘要： Azole nucleosides represented by the formulae (I) and (II); wherein A = C or N B = C or N X = H; C 1 -C 6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, C1, Br and I; OH, NH 2 , NH-(C 1 -C 6 alkyl, cycloalkyl, aryl, or heterocyclo); Z = H; C 1 -C 6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br, I; OH, NH 2 , NH-(C 1 -C 6 alkyl, cycloalkyl, aryl, or heterocyclo; E= (CH 2 )HONHR 1 ; n is an integer from 0-6 and more typically 0-3; R 1 = aryl or heterocyclo; each of W, Y, R is individually selected from the group consisting of H; C 1 -C 6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo; halogen such as F, Cl, Br, and I; O, OH, Oalkyl, Oaryl, NH 2 , NH-(C 1 -C 6 alkyl, cycloalkyl, aryl, or heterocyclo); provided that at least one of W, Y, and R is other than H and wherein both W and Y together can be =O; and each D individually is OH, Oalkyl, Oaryl, Fl and H;pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are provided. Compounds of this disclosure are useful as inhibitors of viral RNA and DNA polymerases such as, but not limited to, Influenza, Hantaan Virus, Crimean Congo hemorrhagic fever virus, hepatitis B, hepatitis C, Polio, Coxsackie A and B, Rhino, Echo, orthopoxvirus (small pox), HIV, Ebola, and West Nile virus polymerases; and especially orthopoxvirus, HIV, and hepatitis B.
摘要翻译：由式（I）和（II）表示的唑类核苷; 其中A = C或N B = C或N X = H; C 1 -C 6烷基，环烷基，烯基，环烯基，炔基，芳基，杂环基，卤素如F，Cl，Br和I; OH，NH 2，NH-（C 1 -C 6烷基，环烷基，芳基或杂环）; Z = H; C 1 -C 6烷基，环烷基，烯基，环烯基，炔基，芳基，杂环基，卤素如F，Cl，Br，I; OH，NH 2，NH-（C 1 -C 6烷基，环烷基，芳基或杂环; E =（CH 3） 2 HONHR 1; n是0-6，更典型地0-3的整数; R 1 =芳基或杂环; W，Y R 1独立地选自H; C 1 -C 6烷基，环烷基，烯基，环烯基，炔基，芳基，杂环;卤素如F， Cl，Br和I; O，OH，O烷基，芳基，NH 2，NH-（C 1 -C 6烷基，环烷基，芳基或杂环基）;条件是W，Y和R中的至少一个不是H，并且其中W和Y一起可以是= O;并且每个D分别是OH，O烷基，芳基，F 1和H; 本公开的化合物可用作病毒RNA和DNA聚合酶的抑制剂，例如但不限于流感，汉坦病毒，克里米亚刚果出血热病毒，乙型肝炎，肝炎 C，脊髓灰质炎，柯萨奇A和B，犀牛，回声，正痘病毒（小痘），HIV，埃博拉和西尼罗病毒聚合酶; 尤其是正痘病毒，艾滋病毒和乙型肝炎。

3. 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。

4. 发明申请

WO2008067002A8 AZOLE NUCLEOSIDES AND USE AS INHIBITORS OF RNA AND DNA VARIAL POLYMERASES 审中-公开
标题翻译： AZOLE核苷及其作为RNA和DNA变异聚合物的抑制剂的应用
公开(公告)号：WO2008067002A8
公开(公告)日：2008-09-12
申请号：PCT/US2007078139
申请日：2007-09-11
申请人： SOUTHERN RES INST , UNIV NEW MEXICO , ARTERBURN JEFFREY B , JONSSON COLLEEN B , PARKER WILLIAM B
发明人： ARTERBURN JEFFREY B , JONSSON COLLEEN B , PARKER WILLIAM B
IPC分类号： A01N43/04 , A61K31/70 , C07H5/04 , C07H5/06 , C07H19/044 , C07H19/056
CPC分类号： C07H5/04 , C07H5/06 , C07H19/044 , C07H19/056
摘要： Azole nucleosides represented by the formulae (I) and (II); wherein A = C or N B = C or N X = H; C 1 -C 6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, C1, Br and I; OH, NH 2 , NH-(C 1 -C 6 alkyl, cycloalkyl, aryl, or heterocyclo); Z = H; C 1 -C 6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br, I; OH, NH 2 , NH-(C 1 -C 6 alkyl, cycloalkyl, aryl, or heterocyclo; E= (CH 2 )HONHR 1 ; n is an integer from 0-6 and more typically 0-3; R 1 = aryl or heterocyclo; each of W, Y, R is individually selected from the group consisting of H; C 1 -C 6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo; halogen such as F, Cl, Br, and I; O, OH, Oalkyl, Oaryl, NH 2 , NH-(C 1 -C 6 alkyl, cycloalkyl, aryl, or heterocyclo); provided that at least one of W, Y, and R is other than H and wherein both W and Y together can be =O; and each D individually is OH, Oalkyl, Oaryl, Fl and H;pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are provided. Compounds of this disclosure are useful as inhibitors of viral RNA and DNA polymerases such as, but not limited to, Influenza, Hantaan Virus, Crimean Congo hemorrhagic fever virus, hepatitis B, hepatitis C, Polio, Coxsackie A and B, Rhino, Echo, orthopoxvirus (small pox), HIV, Ebola, and West Nile virus polymerases; and especially orthopoxvirus, HIV, and hepatitis B.
摘要翻译：由式（I）和（II）表示的唑核苷; 其中A = C或N B = C或N X = H; C 1-6烷基，环烷基，链烯基，环烯基，炔基，芳基，杂环基，卤素如F，Cl，Br和I; OH，NH 2，NH-（C 1 -C 6烷基，环烷基，芳基或杂环）。 Z = H; C 1-6烷基，环烷基，烯基，环烯基，炔基，芳基，杂环基，卤素如F，Cl，Br，I; OH，NH 2，NH-（C 1 -C 6）烷基，环烷基，芳基或杂环; E =（CH 2） 2）HONHR 1 1; n是0-6的整数，更典型的是0-3; R 1 =芳基或杂环; W，Y R独立地选自H，C 1 -C 6烷基，环烷基，烯基，环烯基，炔基，芳基，杂环基;卤素如F， Cl，Br和I; O，OH，O烷基，O芳基，NH 2，NH-（C 1 -C 6烷基，环烷基，芳基或杂环）;条件是W，Y和R中的至少一个不是H，并且其中W和Y一起可以是= O;并且每个D独立地是OH，O烷基，O芳基，F1和H; 本公开的化合物可用作病毒RNA和DNA聚合酶的抑制剂，例如但不限于流感病毒，汉坦病毒，克里米亚刚果出血热病毒，乙型肝炎，肝炎 C，小儿麻痹症，柯萨奇A和B，犀牛，回声，正痘病毒（小痘），HIV，埃博拉病毒和西尼罗河病毒聚合酶; 特别是正痘病毒，艾滋病毒和乙型肝炎。

5. 发明申请

WO2008067002A2 AZOLE NUCLEOSIDES AND USE AS INHIBITORS OF RNA AND DNA VARIAL POLYMERASES 审中-公开
标题翻译： AZOLE核苷及其作为RNA和DNA变异聚合物的抑制剂的应用
公开(公告)号：WO2008067002A2
公开(公告)日：2008-06-05
申请号：PCT/US2007/078139
申请日：2007-09-11
申请人： SOUTHERN RESEARCH INSTITUTE , NEW MEXICO STATE UNIVERSITY , ARTERBURN, Jeffrey, B. , JONSSON, Colleen, B. , PARKER, William, B.
发明人： ARTERBURN, Jeffrey, B. , JONSSON, Colleen, B. , PARKER, William, B.
IPC分类号： A61K31/7056
CPC分类号： C07H5/04 , C07H5/06 , C07H19/044 , C07H19/056
摘要： Azole nucleosides represented by the formulae (I) and (II); wherein A = C or N B = C or N X = H; C 1 -C 6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, C1, Br and I; OH, NH 2 , NH-(C 1 -C 6 alkyl, cycloalkyl, aryl, or heterocyclo); Z = H; C 1 -C 6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br, I; OH, NH 2 , NH-(C 1 -C 6 alkyl, cycloalkyl, aryl, or heterocyclo; E= (CH 2 )HONHR 1 ; n is an integer from 0-6 and more typically 0-3; R 1 = aryl or heterocyclo; each of W, Y, R is individually selected from the group consisting of H; C 1 -C 6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo; halogen such as F, Cl, Br, and I; O, OH, Oalkyl, Oaryl, NH 2 , NH-(C 1 -C 6 alkyl, cycloalkyl, aryl, or heterocyclo); provided that at least one of W, Y, and R is other than H and wherein both W and Y together can be =O; and each D individually is OH, Oalkyl, Oaryl, Fl and H;pharmaceutically acceptable salts thereof, prodrugs thereof and mixtures thereof are provided. Compounds of this disclosure are useful as inhibitors of viral RNA and DNA polymerases such as, but not limited to, Influenza, Hantaan Virus, Crimean Congo hemorrhagic fever virus, hepatitis B, hepatitis C, Polio, Coxsackie A and B, Rhino, Echo, orthopoxvirus (small pox), HIV, Ebola, and West Nile virus polymerases; and especially orthopoxvirus, HIV, and hepatitis B.
摘要翻译：由式（I）和（II）表示的唑类核苷; 其中A = C或N B = C或N X = H; C 1 -C 6烷基，环烷基，烯基，环烯基，炔基，芳基，杂环基，卤素如F，Cl，Br和I; OH，NH 2，NH-（C 1 -C 6烷基，环烷基，芳基或杂环）。 Z = H; C 1 -C 6烷基，环烷基，烯基，环烯基，炔基，芳基，杂环基，卤素如F，Cl，Br，I; OH，NH 2，NH-（C 1 -C 6烷基，环烷基，芳基或杂环; E =（CH 2） 2）HONHR 1; n是0-6的整数，更典型的是0-3; R 1 =芳基或杂环; W，Y R独立地选自H，C 1 -C 6烷基，环烷基，烯基，环烯基，炔基，芳基，杂环基;卤素如F， Cl，Br和I; O，OH，O烷基，O芳基，NH 2，NH-（C 1 -C 6烷基，环烷基，芳基或杂环）;条件是W，Y和R中的至少一个不是H，并且其中W和Y一起可以是= O;并且每个D独立地是OH，O烷基，O芳基，F1和H; 本公开的化合物可用作病毒RNA和DNA聚合酶的抑制剂，例如但不限于流感病毒，汉坦病毒，克里米亚刚果出血热病毒，乙型肝炎，肝炎 C，小儿麻痹症，柯萨奇A和B，犀牛，回声，正痘病毒（小痘），HIV，埃博拉病毒和西尼罗河病毒聚合酶; 特别是正痘病毒，艾滋病毒和乙型肝炎。

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