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1. 发明授权

US09422250B2 Pyrimidine derivatives for the treatment of viral infections 有权
标题翻译：嘧啶衍生物用于治疗病毒感染
公开(公告)号：US09422250B2
公开(公告)日：2016-08-23
申请号：US14110054
申请日：2012-04-10
申请人： David Mc Gowan , Pierre Jean-Marie Bernard Raboisson , Werner Embrechts , Tim Hugo Maria Jonckers , Stefaan Julien Last , Serge Maria Aloysius Pieters , Jaromir Vlach
发明人： David Mc Gowan , Pierre Jean-Marie Bernard Raboisson , Werner Embrechts , Tim Hugo Maria Jonckers , Stefaan Julien Last , Serge Maria Aloysius Pieters , Jaromir Vlach
IPC分类号： A61K31/535 , A61K31/50 , A61K31/495 , A61K31/505 , C07D239/04 , C07D401/12 , C07D413/12 , C07D471/04 , C07D403/12 , C07D405/12 , C07D239/48 , C07D487/04 , C07D495/04
CPC分类号： A61K31/505 , A61K31/506 , A61K31/5377 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.
摘要翻译：本发明涉及嘧啶衍生物，其制备方法，药物组合物及其在治疗病毒感染如HCV或HBV中的用途。

2. 发明授权

US09045463B2 Phenyl ethynyl derivatives as hepatitis C virus inhibitors 有权
标题翻译：苯乙炔衍生物作为丙型肝炎病毒抑制剂
公开(公告)号：US09045463B2
公开(公告)日：2015-06-02
申请号：US13389269
申请日：2010-08-06
申请人： David McGowan , Samuel Dominique Demin , Stefaan Julien Last , Koen Vandyck , Pierre Jean-Marie Bernard Raboisson
发明人： David McGowan , Samuel Dominique Demin , Stefaan Julien Last , Koen Vandyck , Pierre Jean-Marie Bernard Raboisson
IPC分类号： A61K31/4178 , C07D403/14 , C07D403/04 , C07D405/14 , C07D413/14
CPC分类号： C07D403/14 , C07D403/04 , C07D405/14 , C07D413/14
摘要： Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R* have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in the treatment or prophylaxis of HCV.
摘要翻译：式I的HCV复制抑制剂包括立体化学异构体形式，以及其盐，水合物，溶剂化物，其中R和R *具有权利要求中限定的含义。本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其用途，单独或与其它HCV抑制剂组合用于治疗或预防HCV。

3. 发明授权

US08754116B2 Macrocyclic inhibitors of hepatitis C virus 有权
标题翻译：丙型肝炎病毒的大环抑制剂
公开(公告)号：US08754116B2
公开(公告)日：2014-06-17
申请号：US13451660
申请日：2012-04-20
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Dominique Louis Nestor Ghislain Surleraux , Wim Van De Vreken
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Dominique Louis Nestor Ghislain Surleraux , Wim Van De Vreken
IPC分类号： A61K31/407 , C07D487/04
CPC分类号： C07D487/04 , C07D403/04
摘要： Inhibitors of HCV replication of formula (I) wherein W is a heterocycle of formula and the remaining variables are as defined in the specification.
摘要翻译：式（I）的HCV复制抑制剂，其中W是式的杂环，其余变量如说明书中所定义。

4. 发明授权

US08637663B2 Macrocyclic inhibitors of hepatitis C virus 有权
标题翻译：丙型肝炎病毒的大环抑制剂
公开(公告)号：US08637663B2
公开(公告)日：2014-01-28
申请号：US12441812
申请日：2007-11-16
申请人： Pierre Jean-Marie Bernard Raboisson , Herman Augustinus De Kock , David Craig McGowan , Wim Van De Vreken , Lili Hu , Abdellah Tahri , Sandrine Marie Helene Vendeville
发明人： Pierre Jean-Marie Bernard Raboisson , Herman Augustinus De Kock , David Craig McGowan , Wim Van De Vreken , Lili Hu , Abdellah Tahri , Sandrine Marie Helene Vendeville
IPC分类号： C07D225/04
CPC分类号： C07D491/056 , A61K31/427 , A61K31/4741 , C07D401/12 , C07D491/04 , C07D491/048 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/393 , A61K2300/00
摘要： Inhibitors of HCV replication of formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-membered saturated heterocyclic ring; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).
摘要翻译：式（I）的HCV复制抑制剂及其盐和立体异构体，其中每个虚线（由表示任选的双键表示; X为N，CH，并且X为双键，其为C; R 1为-OR 7， -NH-SO 2 R 8; R 2是氢，并且其中X是C或CH，R 2也可以是C 1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 3-7环烷基; n是3,4,5 或6; R 4是C 1-6烷基或C 3-7环烷基; R 5是氢，卤素，C 1-6烷基，羟基，C 1-6烷氧基，多卤代C 1-6烷基; R 6是氢，C 1-6烷氧基，单或二C 1-6烷基氨基;或 R 5和R 6可以形成5-或6-元不饱和或部分不饱和的环，任选地包含一个或两个选自O，N和S; R 7是氢;任选地被C 1-6烷基取代的C 3-7环烷基; 被C 3-7环烷基取代; R8是任选被C 1-6烷基取代的C 3-7环烷基;任选被C 3-7环烷基取代的C 1-6烷基;或-NR 8 R 8 b; R 8a和R 8b是C 1-6烷基，或两者可以形成5-或 6元饱和杂环; 含有化合物（I）的药物组合物和制备化合物（I）的方法。

5. 发明申请

US20130267556A1 AZAINDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS 有权
标题翻译：作为呼吸道同种病毒抗病毒药物
公开(公告)号：US20130267556A1
公开(公告)日：2013-10-10
申请号：US13993543
申请日：2011-12-16
申请人： Ludwig Paul Cooymans , Samuël Dominique Demin , Lili Hu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Sandrine Marie Helene Vendeville
发明人： Ludwig Paul Cooymans , Samuël Dominique Demin , Lili Hu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Sandrine Marie Helene Vendeville
IPC分类号： C07D471/04
CPC分类号： C07D519/00 , A61K31/437 , C07D471/04
摘要： Azaindoles having inhibitory activity on RSV replication and having the formula I compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
摘要翻译：对RSV复制具有抑制活性的Azaindoles和具有含有这些化合物作为活性成分的式I组合物和制备这些化合物和组合物的方法。

6. 发明申请

US20130267508A1 BENZIMIDAZOLE RESPIRATORY SYNCYTIAL VIRUS INHIBITORS 有权
标题翻译：苯唑咪唑呼吸道同种病毒抑制剂
公开(公告)号：US20130267508A1
公开(公告)日：2013-10-10
申请号：US13993107
申请日：2011-12-16
申请人： Ludwig Paul Cooymans , Lili Wu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Sandrine Marie Helene Vendeville
发明人： Ludwig Paul Cooymans , Samuël Dominique Demin , Lili Wu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Sandrine Marie Helene Vendeville
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D235/26
摘要： Benzimidazoles having inhibitory activity on RSV replication and having the formula the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof, compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
摘要翻译：对RSV复制具有抑制活性的苯并咪唑，其具有前药，N-氧化物，加成盐，季胺，金属络合物及其立体化学异构形式的组合物，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。

7. 发明申请

US20130261151A1 AZABENZIMIDAZOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS 有权
公开(公告)号：US20130261151A1
公开(公告)日：2013-10-03
申请号：US13993141
申请日：2011-12-16
申请人： Ludwig Paul Cooymans , Samuël Dominique Demin , Lili Hu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Sandrine Marie Helene Vendeville
发明人： Ludwig Paul Cooymans , Samuël Dominique Demin , Lili Hu , Tim Hugo Maria Jonckers , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Sandrine Marie Helene Vendeville
IPC分类号： C07D471/04
CPC分类号： C07D519/00 , C07D471/04 , C07F5/025
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

8. 发明授权

US08436066B2 Compositions polymerizable/crosslinkable by cationic/radical irradiation 有权
标题翻译：通过阳离子/自由基照射可聚合/交联的组合物
公开(公告)号：US08436066B2
公开(公告)日：2013-05-07
申请号：US12309603
申请日：2007-07-23
申请人： Jean-Marc Frances , Philippe Barbeau , Jean-Marie Bernard , Damien Bourgeois
发明人： Jean-Marc Frances , Philippe Barbeau , Jean-Marie Bernard , Damien Bourgeois
IPC分类号： H05B6/68 , C08G18/67 , C08G65/18 , C08G2/10 , C08F20/22 , C07D303/40 , C03C25/10 , B29D22/00 , B29D23/00 , B32B1/08 , B32B27/08 , B32B9/00 , B32B33/00
CPC分类号： C08G18/792 , C08G18/003 , C08G59/22 , C08G65/18 , C08J7/18 , C09D175/04 , G03F7/038 , G03F7/0755 , G03F7/0757 , Y10T428/1352 , Y10T428/1457 , Y10T428/31515
摘要： Compositions that can be polymerized and/or crosslinked into coatings by cationic and/or radical irradiation contain at least one photoinitiator and at least one compound having at least one isocyanate function.
摘要翻译：可以通过阳离子和/或自由基照射聚合和/或交联成涂层的组合物含有至少一种光引发剂和至少一种具有至少一个异氰酸酯官能团的化合物。

9. 发明申请

US20130109694A1 COMPOUNDS WITH ANTIBACTERIAL ACTIVITY AGAINST CLOSTRIDIUM 失效
标题翻译：具有抗菌活性的化合物
公开(公告)号：US20130109694A1
公开(公告)日：2013-05-02
申请号：US13809238
申请日：2011-08-04
申请人： Jerome Emile Georges Guillemont , Pierre Jean-Marie Bernard Raboisson , Nacer Lounis
发明人： Jerome Emile Georges Guillemont , Pierre Jean-Marie Bernard Raboisson , Nacer Lounis
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention is related to novel compounds of formula (I) having antibacterial activity against Clostridium bacteria, in particular Clostridium perfringens, pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
摘要翻译：本发明涉及对具有针对梭菌属细菌，特别是产气荚膜梭菌，包含这些化合物的药物组合物和用于制备这些化合物的化学方法的抗细菌活性的式（I）化合物。

10. 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。

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