公开(公告)号：US20130085133A1

公开(公告)日：2013-04-04

申请号：US13577592

申请日：2011-02-08

申请人： Bill Severson ,  Dong Hong Chung ,  Colleen B. Jonsson ,  Ellie Lucile White ,  Lynn Rasmussen ,  Clinton Boykin Maddox ,  Subramaniam Ananthan ,  Ashish K. Pathak ,  Joseph A. Maddry

发明人： Bill Severson ,  Dong Hong Chung ,  Colleen B. Jonsson ,  Ellie Lucile White ,  Lynn Rasmussen ,  Clinton Boykin Maddox ,  Subramaniam Ananthan ,  Ashish K. Pathak ,  Joseph A. Maddry

IPC分类号： C07H19/12 ,  C07D471/14 ,  C12Q1/02 ,  C07D471/04

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) through (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）至（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。

公开(公告)号：US20120040966A1

公开(公告)日：2012-02-16

申请号：US13142678

申请日：2009-12-28

申请人： Joseph A. Maddry ,  Bill Severson ,  Colleen B. Jonsson ,  James W. Noah ,  Diana L. Noah ,  Xi Chen

发明人： Joseph A. Maddry ,  Bill Severson ,  Colleen B. Jonsson ,  James W. Noah ,  Diana L. Noah ,  Xi Chen

IPC分类号： A61K31/55 ,  C07D405/10 ,  C07D401/04 ,  C07D491/052 ,  C07D495/04 ,  A61P31/16 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  C12Q1/70 ,  A61P31/12 ,  A61P31/14 ,  C07D239/70 ,  C07D471/04

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 percent 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。 通过使用百分比细胞活力作为终点，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。

公开(公告)号：US20100129317A1

公开(公告)日：2010-05-27

申请号：US12440697

申请日：2007-09-11

申请人： Jeffrey B. Arterburn ,  Colleen B. Jonsson ,  William B. Parker

发明人： Jeffrey B. Arterburn ,  Colleen B. Jonsson ,  William B. Parker

IPC分类号： A61K38/20 ,  A61K38/21 ,  A61K31/7034 ,  A61K31/7056 ,  A61K31/7076 ,  C07H19/167 ,  C07H19/056 ,  C07H19/052 ,  A61P31/12

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; C1-C6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br and I; OH, NH2, NH—(C1-C6 alkyl, cycloalkyl, aryl or heterocyclo); Z═H; C1-C6 alkyl, cycloalkyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br, I; OH NH2, NH—(C1-C6 alkyl, cycloalkyl, aryl or heterocyclo; E=(CH2)HONHR; n is an interger from 0-6 and more typically 0-3; R1= aryl or heterocyclo; each of W, Y, R is individually selected from the group consisting of H; C1-C6 alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclo, halogen such as F, Cl, Br, and I; O, OH, Oalkyl, Oaryl, NH2, NH(C1-C6 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，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，芳基或杂环基; E =（CH 2）HONHR; n是0-6且更通常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，杂环基，卤素如F，Cl，Br和I; O，OH，O烷基，芳基， ，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各自是OH， 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，丙型肝炎，脊髓灰质炎，柯萨奇A和B，犀牛，回声，正痘病毒（小痘），艾滋病病毒，埃博拉病毒和西尼罗河病毒聚合酶;特别是或 痘病毒，艾滋病毒和乙型肝炎。