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1. 发明授权

US08399429B2 Uracyl cyclopropyl nucleotides 有权
标题翻译：尿嘧啶环丙基核苷酸
公开(公告)号：US08399429B2
公开(公告)日：2013-03-19
申请号：US13130602
申请日：2009-12-08
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Steven Maurice Paula Van Hoof , Leen Anna Maria Vandekerckhove , Koen Vandyck
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Steven Maurice Paula Van Hoof , Leen Anna Maria Vandekerckhove , Koen Vandyck
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： C07H19/10
摘要： Compounds of the formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen or halo; R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is a group of formula R7 is optionally substituted phenyl; naphthyl; indolyl or N—C1-C6alkyloxycarbonyl-indolyl; R8 is hydrogen, C1-C6alkyl, benzyl; R8′ is hydrogen, C1-C6alkyl, benzyl; or R8 and R8′ together with the carbon atom to which they are attached form C3-C7cycloalkyl; R9 is C1-C10alkyl, benzyl, or optionally substituted phenyl; or a pharmaceutically acceptable salt or solvate thereof. pharmaceutical formulations and the use of compounds I as HCV inhibitors.
摘要翻译：式I化合物：包括其任何可能的立体异构体，其中：R 1是氢或卤素; R4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 4是式R7的基团是任选取代的苯基; 萘基; 吲哚基或N-C 1 -C 6烷氧基羰基 - 吲哚基; R8是氢，C1-C6烷基，苄基; R 8'是氢，C 1 -C 6烷基，苄基; 或R 8和R 8'与它们所连接的碳原子一起形成C 3 -C 7环烷基; R 9为C 1 -C 10烷基，苄基或任选取代的苯基; 或其药学上可接受的盐或溶剂合物。药物制剂和化合物I用作HCV抑制剂。

2. 发明申请

US20110230436A1 Uracyl Cyclopropyl Nucleotides 有权
标题翻译：尿酰基环丙基核苷酸
公开(公告)号：US20110230436A1
公开(公告)日：2011-09-22
申请号：US13130602
申请日：2009-12-08
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Steven Maurice Paula Van Hoof , Leen Anna Maria Vandekerckhove , Koen Vandyck
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Steven Maurice Paula Van Hoof , Leen Anna Maria Vandekerckhove , Koen Vandyck
IPC分类号： A61K31/7072 , C07H19/10 , A61P31/14
CPC分类号： C07H19/10
摘要： Compounds of the formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen or halo; R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is a group of formula R7 is optionally substituted phenyl; naphthyl; indolyl or N—C1-C6alkyloxycarbonylindolyl; R8 is hydrogen, C1-C6alkyl, benzyl; R8′ is hydrogen, C1-C6alkyl, benzyl; or R8 and R8′ together with the carbon atom to which they are attached form C3-C7cycloalkyl; R9 is C1-C10alkyl, benzyl, or optionally substituted phenyl; or a pharmaceutically acceptable salt or solvate thereof. pharmaceutical formulations and the use of compounds I as HCV inhibitors.
摘要翻译：式I化合物：包括其任何可能的立体异构体，其中：R 1是氢或卤素; R4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 4是式R7的基团是任选取代的苯基; 萘基; 吲哚基或N-C 1 -C 6烷氧基羰基吲哚基; R8是氢，C1-C6烷基，苄基; R 8'是氢，C 1 -C 6烷基，苄基; 或R 8和R 8'与它们所连接的碳原子一起形成C 3 -C 7环烷基; R 9为C 1 -C 10烷基，苄基或任选取代的苯基; 或其药学上可接受的盐或溶剂合物。药物制剂和化合物I用作HCV抑制剂。

3. 发明授权

US09006209B2 Uracyl spirooxetane nucleoside phosphoramidates 有权
标题翻译：尿嘧啶螺吡啶核苷氨基磷酸酯
公开(公告)号：US09006209B2
公开(公告)日：2015-04-14
申请号：US13884835
申请日：2011-11-10
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
IPC分类号： A61K31/70 , C07H19/00 , A01N43/04 , C07H19/10 , C07H19/06
CPC分类号： C07H19/10 , C07H19/06
摘要： This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate which inhibits the hepatitis C virus (HCV).
摘要翻译：本发明涉及抑制丙型肝炎病毒（HCV）的立体化学纯的尿嘧啶螺吡啶核苷氨基磷酸酯。

4. 发明授权

US09012428B2 Uracyl spirooxetane nucleoside phosphoramidates 有权
标题翻译：尿嘧啶螺吡啶核苷氨基磷酸酯
公开(公告)号：US09012428B2
公开(公告)日：2015-04-21
申请号：US13884852
申请日：2011-11-10
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
IPC分类号： A01N43/04 , A61K31/70 , A61K9/28 , C07H19/06 , C07H19/10 , A61K9/20
CPC分类号： C07H19/10 , A61K9/2068 , A61K9/284 , A61K9/2866 , C07H19/06
摘要： This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate useful in the treatment of patients infected with the hepatitis C virus (HCV).
摘要翻译：本发明涉及可用于治疗感染丙型肝炎病毒（HCV）的患者的立体化学纯的尿嘧啶螺吡啶核苷氨基磷酸酯。

5. 发明申请

US20130244968A1 Uracyl Spirooxetane Nucleoside Phosphoramidates 有权
标题翻译：尿嘧啶螺吡啶核苷磷酰胺
公开(公告)号：US20130244968A1
公开(公告)日：2013-09-19
申请号：US13884852
申请日：2011-11-10
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
IPC分类号： C07H19/10
CPC分类号： C07H19/10 , A61K9/2068 , A61K9/284 , A61K9/2866 , C07H19/06
摘要： This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate useful in the treatment of patients infected with the hepatitis C virus (HCV).
摘要翻译：本发明涉及用于治疗感染丙型肝炎病毒（HCV）的患者的立体化学纯的尿嘧啶螺吡啶核苷氨基磷酸酯。

6. 发明申请

US20130225520A1 Uracyl Spirooxetane Nucleoside Phosphoramidates 有权
标题翻译：尿嘧啶螺吡啶核苷磷酰胺
公开(公告)号：US20130225520A1
公开(公告)日：2013-08-29
申请号：US13884835
申请日：2011-11-10
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck , Steven Maurice Paula Van Hoof , Lili Hu , Abdellah Tahri
IPC分类号： C07H19/10
CPC分类号： C07H19/10 , C07H19/06
摘要： This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate which inhibits the hepatitis C virus (HCV).
摘要翻译：本发明涉及抑制丙型肝炎病毒（HCV）的立体化学纯的尿嘧啶螺吡啶核苷氨基磷酸酯。

7. 发明授权

US08846672B2 Imidazopyridines as respiratory syncytial virus antiviral agents 有权
标题翻译：咪唑并吡啶类作为呼吸道合胞病毒抗病毒剂
公开(公告)号：US08846672B2
公开(公告)日：2014-09-30
申请号：US13993692
申请日：2011-12-16
申请人： Ludwig Paul Cooymans , Lili Hu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Steven Maurice Paula Van Hoof , Sandrine Marie Helene Vendeville
发明人： Ludwig Paul Cooymans , Lili Hu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Steven Maurice Paula Van Hoof , Sandrine Marie Helene Vendeville
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/495 , A61K31/4427 , C07D413/14 , C07D417/04 , C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04
摘要： A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.
摘要翻译：满足式I的化合物，前药，N-氧化物，加成盐，季胺，金属络合物或其立体化学异构形式; 组合物含有这些化合物作为活性成分和制备这些化合物和组合物的方法。

8. 发明申请

US20130324527A1 IMIDAZOPYRIDINES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS 有权
标题翻译：咪达唑啶作为呼吸道同源病毒抗病毒剂
公开(公告)号：US20130324527A1
公开(公告)日：2013-12-05
申请号：US13993692
申请日：2011-12-16
申请人： Ludwig Paul Cooymans , Lili Hu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdella Tahri , Steven Maurice Paula Van Hoof , Sandrine Marie Helene Vendeville
发明人： Ludwig Paul Cooymans , Lili Hu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdella Tahri , Steven Maurice Paula Van Hoof , Sandrine Marie Helene Vendeville
IPC分类号： C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04
摘要： A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof: compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.
摘要翻译：满足式I的化合物，前药，N-氧化物，加成盐，季胺，金属络合物或其立体化学异构形式：含有这些化合物作为活性成分的组合物和制备这些化合物和组合物的方法。

9. 发明授权

US08431588B2 Cyclopropyl polymerase inhibitors 有权
标题翻译：环丙基聚合酶抑制剂
公开(公告)号：US08431588B2
公开(公告)日：2013-04-30
申请号：US12999263
申请日：2009-07-01
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07H19/073
摘要： Compounds of formula I: wherein: R2 is hydrogen or C1-C4alkyl; R3 and R4 are hydrogen, —C(═O)R5, or —C(═O)CHR6—NH2; or R3 is hydrogen and R4 is a monophosphate-, diphosphate-, or triphosphate ester; or R3 is hydrogen, —C(═O)CHR5, or —C(═O)CHR6—NH2 and R4 is each R5 is hydrogen, C1-C6alkyl, or C3-C7cycloalkyl; R6 is hydrogen or C1-C6alkyl; R7 is optionally substituted phenyl; naphthyl; or indolyl; R8 and R8′ are hydrogen, C1-C6alkyl, benzyl; or R8 and R8′ combined form C3-C7cycloalkyl; R9 is C1-C6alkyl, benzyl, or optionally substituted phenyl; provided that R2, R3 and R4 are not all hydrogen; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations with the compounds I; the use of compounds I, including the compounds of formula I wherein R2, R3 and R4 are all hydrogen, as HCV inhibitors.
摘要翻译：式I化合物：其中：R 2是氢或C 1 -C 4烷基; R3和R4是氢，-C（= O）R5或-C（= O）CHR6-NH2; 或R3是氢，R4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 3是氢，-C（= O）CHR 5或-C（= O）CHR 6 -NH 2，R 4各自是氢，C 1 -C 6烷基或C 3 -C 7环烷基; R6是氢或C1-C6烷基; R7是任选取代的苯基; 萘基; 或吲哚基; R8和R8'是氢，C1-C6烷基，苄基; 或R 8和R 8'组合形式的C 3 -C 7环烷基; R 9为C 1 -C 6烷基，苄基或任选取代的苯基; 条件是R2，R3和R4不都是氢; 或其药学上可接受的盐或溶剂化物; 具有化合物I的药物制剂; 使用化合物I，包括其中R2，R3和R4均为氢的式Ⅰ化合物作为HCV抑制剂。

10. 发明申请

US20110092460A1 CYCLOPROPYL POLYMERASE INHIBITORS 有权
标题翻译：环丙基聚合酶抑制剂
公开(公告)号：US20110092460A1
公开(公告)日：2011-04-21
申请号：US12999263
申请日：2009-07-01
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Koen Vandyck
IPC分类号： A61K31/513 , C07D405/04 , A61K31/675 , A61P31/12 , A61P31/14
CPC分类号： C07H19/073
摘要： Compounds of formula I: wherein: R2 is hydrogen or C1-C4alkyl; R3 and R4 are hydrogen, —C(═O)R5, or —C(═O)CHR6—NH2; or R3 is hydrogen and R4 is a monophosphate-, diphosphate-, or triphosphate ester; or R3 is hydrogen, —C(═O)CHR5, or —C(═O)CHR6—NH2 and R4 is each R5 is hydrogen, C1-C6alkyl, or C3-C7cycloalkyl; R6 is hydrogen or C1-C6alkyl; R7 is optionally substituted phenyl; naphthyl; or indolyl; R8 and R8′ are hydrogen, C1-C6alkyl, benzyl; or R8 and R8′ combined form C3-C7cycloalkyl; R9 is C1-C6alkyl, benzyl, or optionally substituted phenyl; provided that R2, R3 and R4 are not all hydrogen; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations with the compounds I; the use of compounds I, including the compounds of formula I wherein R2, R3 and R4 are all hydrogen, as HCV inhibitors.
摘要翻译：式I化合物：其中：R 2是氢或C 1 -C 4烷基; R3和R4是氢，-C（= O）R5或-C（= O）CHR6-NH2; 或R3是氢，R4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 3为氢，-C（= O）CHR 5或-C（= O）CHR 6 -NH 2，且R 4各自为R 5为氢，C 1 -C 6烷基或C 3 -C 7环烷基; R6是氢或C1-C6烷基; R7是任选取代的苯基; 萘基; 或吲哚基; R8和R8'是氢，C1-C6烷基，苄基; 或R 8和R 8'组合形式的C 3 -C 7环烷基; R 9为C 1 -C 6烷基，苄基或任选取代的苯基; 条件是R2，R3和R4不都是氢; 或其药学上可接受的盐或溶剂化物; 具有化合物I的药物制剂; 使用化合物I，包括其中R2，R3和R4均为氢的式Ⅰ化合物作为HCV抑制剂。

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