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2. 发明申请

WO03014377A2 DIRECT BINDING ASSAY FOR IDENTIFYING INHIBITORS OF HCV POLYMERASE 审中-公开
标题翻译：用于鉴定HCV聚合酶抑制剂的直接结合测定
公开(公告)号：WO03014377A2
公开(公告)日：2003-02-20
申请号：PCT/CA0201214
申请日：2002-08-05
申请人： BOEHRINGER INGELHEIM CA LTD , KUKOLJ GEORGE , BEAULIEU PIERRE L , MCKERCHER GINETTE
发明人： KUKOLJ GEORGE , BEAULIEU PIERRE L , MCKERCHER GINETTE
IPC分类号： G01N33/50 , C12N15/09 , C12Q1/48 , G01N21/76 , G01N21/78 , G01N33/15 , G01N33/542 , C12Q1/00
CPC分类号： G01N33/542 , C12Q1/48 , G01N2333/18 , G01N2333/91245 , G01N2500/02 , G01N2500/04
摘要： A method for identifying compounds binding to HCV polymerase comprising the steps of:contacting said HCV polymerase or an analog thereof with a probe formula I:wherein A is O, S, N, NR1, or CR1, wherein R1 is defined herein;----- represents either a single or a double bond;R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein;B is NR3 or CR3, wherein R3 is defined herein;with the proviso that, when A is not N, then one of A or B is either CR1 or CR3, K is N or CR4, wherein R4 is defined herein;L is N or CR5, wherein R5 has the same definition as R4 defined above;M is N or CR7, wherein R7 has the same definition as R4 defined above;R5 is C(Y1)Z wherein Y1 is O or S; and Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het;or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S;R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, all of which optionally substituted with R90; or R9 is covalently bonded to either of R7 or R8 to form a 5- or 6-membered heterocycle;or a salt thereof; where the probe comprises a detectable label attached to any suitable position, whereby said probe binds to an HCV polymerase or an analog thereof and is capable of being displaced by an inhibitor thereof.
摘要翻译：用于鉴定结合HCV聚合酶的化合物的方法，包括以下步骤：使所述HCV聚合酶或其类似物与式I的探针接触：其中A是O，S，N，NR1或CR1，其中R 1在本文中定义; ---表示单键或双键; R2选自：H，卤素，R21，OR21，SR21，COOR21，SO2N（R22）2，N（R22）2，CON（R22）2，NR22C ）R 22或NR 22 C（O）NR 22，其中R 21和每个R 22如本文所定义; B是NR 3或CR 3，其中R 3在本文中定义;条件是当A不为N时，A或B中的一个为CR1或 CR 3，K是N或CR 4，其中R 4在本文中定义; L是N或CR 5，其中R5具有与上述定义的R4相同的定义; M是N或CR7，其中R7具有与上述定义的R4相同的定义; R5是 C（Y1）Z，其中Y1是O或S; 并且Z是N（R6a）R6或OR6，其中R6a是H或烷基或NR61R62，其中R61和R62在本文中定义; 并且R 6是H，烷基，环烷基，烯基，Het，烷基 - 芳基，烷基-Het;或R 6是其中R 7和R 8和Q如本文所定义; Y2是O或S; R9是H，（C1-6烷基），（C3-7）环烷基或（C1-6）烷基 - （C3-7）环烷基，芳基，Het，（C1-6）烷基 - 芳基或（C 1-6）烷基-Het，它们全部被R 90取代; 或R 9与R 7或R 8中的任一个共价键合以形成5-或6-元杂环;或其盐; 其中所述探针包含连接到任何合适位置的可检测标记，由此所述探针结合HCV聚合酶或其类似物，并且能够被其抑制剂置换。

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