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1. 发明申请

WO2004087714A1 INDOLE ACETAMIDES AS INHIBITORS OF THE HEPATITIS C VIRUS NS5B POLYMERASE 审中-公开
标题翻译：作为乙型肝炎病毒NSVB聚合酶抑制剂的吲哚乙酸
公开(公告)号：WO2004087714A1
公开(公告)日：2004-10-14
申请号：PCT/GB2004/001437
申请日：2004-04-02
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA , AVOLIO, Salvatore , DI FILIPPO, Marcello , HARPER, Steven , NARJES, Frank , PACINI, Barbara , POMPEI, Marco , ROWLEY, Michael , STANSFIELD, Ian
发明人： AVOLIO, Salvatore , DI FILIPPO, Marcello , HARPER, Steven , NARJES, Frank , PACINI, Barbara , POMPEI, Marco , ROWLEY, Michael , STANSFIELD, Ian
IPC分类号： C07D487/10
CPC分类号： C07D413/14 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/24 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/06 , C07D417/06 , C07D417/12 , C07D487/04 , C07D487/10
摘要： The present invention relates to indole and azaindole compounds of formula (I): wherein X 1 , X 2 , X 3 , X 4 , A 1 , Ar 1 , R 1 , R 2 and n are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
摘要翻译：本发明涉及式（I）的吲哚和氮杂吲哚化合物：其中X 1，X 2，X 3，X 4，A 1，Ar 1，R 1， R 2和n如本文所定义，及其药学上可接受的盐，可用于预防和治疗丙型肝炎感染。

2. 发明申请

WO2005034941A1 INDOLES AND AZAINDOLES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：吲哚和亚胺醇作为抗病毒剂
公开(公告)号：WO2005034941A1
公开(公告)日：2005-04-21
申请号：PCT/GB2004/004306
申请日：2004-10-08
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA , AVOLIO, Salvatore , HARPER, Steven , NARJES, Frank , PACINI, Barbara , ROWLEY, Michael
发明人： AVOLIO, Salvatore , HARPER, Steven , NARJES, Frank , PACINI, Barbara , ROWLEY, Michael
IPC分类号： A61K31/404
CPC分类号： C07D401/04 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/14 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
摘要： The present invention relates to indoles and azaindoles of formula (I): wherein X 1 , X 2 , X 3 , X 4 , A 1 , Ar 1 , Ar, n, p and q are as defined herein and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C virus infections.
摘要翻译：本发明涉及式（I）的吲哚和氮杂吲哚：其中X 1，X 2，X 3，X 4，A 1，Ar 1，Ar，n，p 和q如本文所定义及其药学上可接受的盐，其可用于预防和治疗丙型肝炎病毒感染。

3. 发明申请

WO2006046030A2 TETRACYCLIC INDOLE DERIVATIVES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：四环唑吲哚衍生物作为抗病毒药物
公开(公告)号：WO2006046030A2
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004127
申请日：2005-10-25
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA , CONTE, Immacolata , ERCOLANI, Caterina , NARJES, Frank , POMPEI, Marco , ROWLEY, Michael , STANSFIELD, Ian
发明人： CONTE, Immacolata , ERCOLANI, Caterina , NARJES, Frank , POMPEI, Marco , ROWLEY, Michael , STANSFIELD, Ian
IPC分类号： C07D243/10 , C07D413/04 , A61K31/407 , A61P31/00
CPC分类号： C07D245/04 , C07D267/22 , C07D487/04 , C07D491/14 , C07D495/14
摘要： The present invention relates to tetracyclic indole compounds of formula (I); wherein R 1 , R 2 , A, Ar, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
摘要翻译：式（I）的四环吲哚化合物本发明涉及式（I）的四环吲哚化合物; 其中R 1，R 2，A，Ar，W，X，Y和Z如本文所定义，及其药学上可接受的盐，包含它们的药物组合物及其用途用于治疗或预防丙型肝炎病毒感染。

4. 发明申请

WO2006046039A3 TETRACYCLIC INDOLE DERIVATIVES AS ANTIVIRAL AGENTS 审中-公开
公开(公告)号：WO2006046039A3
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004144
申请日：2005-10-25
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA , ERCOLANI, Caterina , HABERMANN, Joerg , NARJES, Frank , PONZI, Simona , ROWLEY, Michael , STANSFIELD, Ian
发明人： ERCOLANI, Caterina , HABERMANN, Joerg , NARJES, Frank , PONZI, Simona , ROWLEY, Michael , STANSFIELD, Ian
IPC分类号： C07D223/18 , A61K31/407 , A61P31/00
摘要： The present invention relates to tetracyclic indole compounds of formula (I); wherein R 1 , R 2 , R 14 , R 15 , A, Ar, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.

5. 发明申请

WO2007054741A1 TETRACYCLIC INDOLE DERIVATIVES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：四环素衍生物作为抗病毒剂
公开(公告)号：WO2007054741A1
公开(公告)日：2007-05-18
申请号：PCT/GB2006/050378
申请日：2006-11-09
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI SPA , DI FILIPPO, Marcello , HARPER, Steven , NARJES, Frank , PACINI, Barbara , PETROCCHI, Alessia , ROWLEY, Michael , STANSFIELD, Ian
发明人： DI FILIPPO, Marcello , HARPER, Steven , NARJES, Frank , PACINI, Barbara , PETROCCHI, Alessia , ROWLEY, Michael , STANSFIELD, Ian
IPC分类号： C07D487/04 , C07D498/04 , A61K31/5517 , A61K31/553 , A61P31/00
CPC分类号： C07D487/04
摘要： The present invention relates to tetracyclic indole derivatives of formula (I); wherein Ar, D 1 , D 2 , D 3 , D 4 , W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
摘要翻译：本发明涉及式（I）的四环吲哚衍生物; 其中Ar，D 1，D 2，D 3，D 4，W，X，Y和Z 在本文中定义，及其药学上可接受的盐，包含它们的药物组合物及其用于治疗或预防丙型肝炎病毒感染的用途。

6. 发明申请

WO2005023819A1 THIENOPYRROLES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：噻吗啉作为抗病毒剂
公开(公告)号：WO2005023819A1
公开(公告)日：2005-03-17
申请号：PCT/GB2004/003838
申请日：2004-09-07
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA , ATTENNI, Barbara , HERNANDO, Jose Ignacio Martin , MALANCONA, Savina , NARJES, Frank , ONTORIA ONTORIA, Jesus Maria , ROWLEY, Michael
发明人： ATTENNI, Barbara , HERNANDO, Jose Ignacio Martin , MALANCONA, Savina , NARJES, Frank , ONTORIA ONTORIA, Jesus Maria , ROWLEY, Michael
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X 1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
摘要翻译：本发明涉及式（I）的噻吩并吡咯化合物; 其中A，B，Y，Ar，n，Z和X 1如本文所定义，及其药学上可接受的盐，其可用于预防和治疗丙型肝炎感染。

7. 发明申请

WO2004110442A1 PYRIDINE N-OXIDES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：吡啶N-氧化物作为抗病毒剂
公开(公告)号：WO2004110442A1
公开(公告)日：2004-12-23
申请号：PCT/EP2004/005971
申请日：2004-06-01
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA , COLARUSSO, Stefania , NARJES, Frank
发明人： COLARUSSO, Stefania , NARJES, Frank
IPC分类号： A61K31/4412
CPC分类号： C07D213/89 , C07D409/12
摘要： The present invention relates to pyridinone derivatives of formula (I) wherein Z represents C 2-6 alkynyl, aryl or heteroaryl, any of which groups may be optionally substituted, and R 1 represents hydrogen, C 1-6 alkyl, C 3-7 heterocycloalkyl(C 1-6 )alkyl, di(C 1-6 )alkylamino(C 1-6 )alkyl, C 2-6 alkylcarbonyloxy(C 1-6 )alkyl or C 3-7 cycloalkoxycarbonyloxy(C 1-6 )alkyl, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C virus infections.
摘要翻译：本发明涉及式（I）的吡啶酮衍生物，其中Z表示C 2-6炔基，芳基或杂芳基，其中任何一个基团可任选被取代，R 1表示氢，C 1-6烷基，C 3-7杂环烷基（C 1-6）烷基，二（C 1-6）烷基氨基（C 1-6）烷基，C 2-6烷基羰基氧基（C 1-6）烷基或C 3-7环烷氧羰基氧基（C 1-6）烷基，及其药学上可接受的盐，在预防和治疗丙型肝炎病毒感染。

8. 发明申请

WO2006119975A1 THIENOPYRROLES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：噻吗啉作为抗病毒剂
公开(公告)号：WO2006119975A1
公开(公告)日：2006-11-16
申请号：PCT/EP2006/004347
申请日：2006-05-03
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPA , COLARUSSO, Stefania , HABERMANN, Joerg , NARJES, Frank , PONZI, Simona , RICO FERREIRA, Maria del Rosario
发明人： COLARUSSO, Stefania , HABERMANN, Joerg , NARJES, Frank , PONZI, Simona , RICO FERREIRA, Maria del Rosario
IPC分类号： C07D498/14 , C07D495/14 , C07D495/22 , A61K31/55 , A61P31/00
CPC分类号： C07D495/14
摘要： The present invention relates to tetracyclic thienopyrrole compounds of formula (I), wherein Ar, A, D1, D2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
摘要翻译：本发明涉及式（I）的四环噻吩并吡咯化合物，其中Ar，A，D1，D2，W，X，Y和Z如本文所定义，及其药学上可接受的盐，包含它们的药物组合物及其用于治疗或预防丙型肝炎病毒感染。

9. 发明申请

WO2010082050A1 MACROCYCLIC AND 7-AMINOALKYL-SUBSTITUTED BENZOXAZOCINES FOR TREATMENT OF HEPATITIS C INFECTIONS 审中-公开
标题翻译：用于治疗丙型肝炎感染的大环和7-氨基取代苯并噻唑
公开(公告)号：WO2010082050A1
公开(公告)日：2010-07-22
申请号：PCT/GB2010/050045
申请日：2010-01-14
申请人： ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A. , NARJES, Frank , STANSFIELD, Ian , PONZI, Simona , PACINI, Barbara , MACKAY, Angela , MEPPEN, Malte
发明人： NARJES, Frank , STANSFIELD, Ian , PONZI, Simona , PACINI, Barbara , MACKAY, Angela , MEPPEN, Malte
IPC分类号： C07D498/20 , C07D513/16 , A61K31/5517 , A61P31/00 , C07D513/20
CPC分类号： C07D498/20 , C07D513/16 , C07D513/20
摘要： The present invention provides a compound of formula (I), wherein R 1 is selected from hydrogen, hydroxyl, fluoro or a C 1-4 alkoxy group or R 1 is linked to R 3 to form a 4, 5 or 6-membered aliphatic ring optionally containing one N or O atom; R 2 is selected from cyclopentyl or cyclohexyl optionally substituted by a fluoro; R 3 is hydrogen or is linked to R 1 as hereinbeforedefined; R 4 is hydrogen, a C 1-4 alkyl group optionally substituted by a group NR 8 R 9 in which R 8 and R 9 are each hydrogen or a C 1-4 alkyl group or R 4 is linked to R 6 to form a (CH 2 ) m NR 10 SO 2 N group wherein m is an integer selected from 2 or 3 and R 10 is a C 1-4 alkyl group; R 5 is hydrogen or a C 1-4 alkyl group; R 6 is hydroxyl or is linked to R 4 as hereinbefore defined; R 7 is hydrogen or an aliphatic ring of 4-7 ring atoms containing one or two heteroatoms selected from O, N or S or a group S(O), S(O) 2 ,NH or NC 1-4 alkyl and optionally substituted by fluoro or R 7 is a 5- 10-membered heteroaromatic ring system containing 1 to 4 heteroatoms independently selected from N, O and S, which ring is optionally substituted by one or two halo atoms or C 1-4 alkyl or C 1-4 alkoxy groups; Y is a single bond or a CH 2 group; when R 4 is linked to R 6 and m is 3 then Y is a single bond; when R 4 is linked to R 6 and m is 2 then Y is a CH 2 group; n is an integer from zero to four, with the proviso that when R 1 is hydrogen, n is not zero; or a pharmaceutically acceptable salt thereof, pharmaceutical formulations containing it and its use in medicine, particularly for the treatment of HCV infections. Hepatitis C (HCV) is a cause of viral infections. Methods of preparing compounds of the formula (I) arc also disclosed.
摘要翻译：本发明提供式（I）化合物，其中R 1选自氢，羟基，氟或C 1-4烷氧基或R 1与R 3连接，形成任选含有一个N的4，5或6元脂肪环或O原子; R 2选自被氟取代的环戊基或环己基; R3是氢或连接到如上文所定义的R 1; R 4是氢，任选被NR 8 R 9基团取代的C 1-4烷基，其中R 8和R 9各自是氢或C 1-4烷基或R 4与R 6连接形成（CH 2）m NR 10 SO 2 N基团，其中m是选自 2或3，R 10为C 1-4烷基; R5是氢或C1-4烷基; R6是羟基，或者如前所定义与R4连接; R 7是氢或含有一个或两个选自O，N或S或S（O），S（O）2，NH或NC1-4烷基的杂原子的4-7个环原子的脂族环，并且任选地被氟或 R7是含有1至4个独立地选自N，O和S的杂原子的5至10元杂芳族环系，该环任选被一个或两个卤原子或C 1-4烷基或C 1-4烷氧基取代; Y是单键或CH2基; 当R4连接到R6并且m是3时，Y是单键; 当R4连接到R6并且m是2时，Y是CH2基团; n为0至4的整数，条件是当R1为氢时，n不为零; 或其药学上可接受的盐，含有它的药物制剂及其在医药中的用途，特别是用于治疗HCV感染。丙型肝炎（HCV）是病毒感染的原因。还公开了制备式（I）化合物的方法。

10. 发明申请

WO2007095269A3 NUCLEOSIDE ARYL PHOSPHORAMIDATES FOR THE TREATMENT OF RNA-DEPENDENT RNA VIRAL INFECTION 审中-公开
公开(公告)号：WO2007095269A3
公开(公告)日：2007-08-23
申请号：PCT/US2007/003862
申请日：2007-02-12
申请人： MERCK & CO., INC. , ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A. , MACCOSS, Malcolm , OLSEN, David, B. , DONGHI, Monica , GARDELLI, Cristina , HARPER, Steven , MEPPEN, Malte , NARJES, Frank , PACINI, Barbara
发明人： MACCOSS, Malcolm , OLSEN, David, B. , DONGHI, Monica , GARDELLI, Cristina , HARPER, Steven , MEPPEN, Malte , NARJES, Frank , PACINI, Barbara
IPC分类号： C07H19/06
摘要： The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention.

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