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1. 发明申请

WO2008099022A1 10-SULFONYL-DIBENZODIAZEPINONES USEFUL AS HEPATITIS C VIRUS INHIBITORS 审中-公开
标题翻译： 10-SULFONYL-DIBENZODIAZEPINONES有用的丙型肝炎病毒抑制剂
公开(公告)号：WO2008099022A1
公开(公告)日：2008-08-21
申请号：PCT/EP2008/051905
申请日：2008-02-15
申请人： TIBOTEC PHARMACEUTICALS LTD. , RABOISSON, Pierre Jean-Marie Bernard , VENDEVILLE, Sandrine Marie Helene , BONFANTI, Jean-François , MC GOWAN, David , VANDYCK, Koen , DOUBLET, Frédéric Marc Maurice , HU, Lili , NYANGUILE, Origène
发明人： RABOISSON, Pierre Jean-Marie Bernard , VENDEVILLE, Sandrine Marie Helene , BONFANTI, Jean-François , MC GOWAN, David , VANDYCK, Koen , DOUBLET, Frédéric Marc Maurice , HU, Lili , NYANGUILE, Origène
IPC分类号： C07D243/38 , C07D471/04 , C07D401/12 , C07D403/12 , C07D413/12 , C07D495/04 , C07D513/04 , A61K31/5513 , A61P31/12
CPC分类号： C07D243/38 , C07D401/12 , C07D403/12 , C07D413/12 , C07D471/04 , C07D495/04 , C07D513/04
摘要： Inhibitors of HCV replication of formula (I) and the stereoisomers, prodrugs, tautomers, racemics, salts, hydrates or solvates thereof, wherein X, Y, R 1 ; R 2 ; R 3 ; R 4a and R 4b 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 in HCV therapy.
摘要翻译：式（I）的HCV复制抑制剂及其立体异构体，前体药物，互变异构体，外消旋物，盐，水合物或溶剂合物，其中X，Y，R 1， [R ^{2 ; [R ^{3 ; R 4a和R 4b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在HCV治疗中的用途。}}

2. 发明申请

WO2008099019A1 6-HYDROXY-DIBENZODIAZEPINONES USEFUL AS HEPATITIS C VIRUS INHIBITORS 审中-公开
标题翻译： 6-羟基 - 二苯并恶嗪类作为丙型肝炎病毒抑制剂
公开(公告)号：WO2008099019A1
公开(公告)日：2008-08-21
申请号：PCT/EP2008/051902
申请日：2008-02-15
申请人： TIBOTEC PHARMACEUTICALS LTD. , RABOISSON, Pierre Jean-Marie Bernard , MC GOWAN, David Craig , VANDYCK, Koen , VENDEVILLE, Sandrine Marie Helene , BONFANTI, Jean-François , VAN DEN BROECK, Walter Marcel Mathilde , NYANGUILE, Origène , AMSSOMS, Katie Ingrid Eduard , HU, Lili , BOUTTON, Carlo Willy Maurice , TAHRI, Abdellah , LAST, Stefaan Julien , ROMBAUTS, Klara , REBSTOCK, Anne-Sophie Helene Marie , FORTIN, Jérôme Michel Claude , MULLER, Philippe
发明人： RABOISSON, Pierre Jean-Marie Bernard , MC GOWAN, David Craig , VANDYCK, Koen , VENDEVILLE, Sandrine Marie Helene , BONFANTI, Jean-François , VAN DEN BROECK, Walter Marcel Mathilde , NYANGUILE, Origène , AMSSOMS, Katie Ingrid Eduard , HU, Lili , BOUTTON, Carlo Willy Maurice , TAHRI, Abdellah , LAST, Stefaan Julien , ROMBAUTS, Klara , REBSTOCK, Anne-Sophie Helene Marie , FORTIN, Jérôme Michel Claude , MULLER, Philippe
IPC分类号： C07D243/38 , C07D401/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D407/04 , C07D407/06 , C07D407/14 , C07D409/04 , C07D413/06 , C07D417/06 , C07D513/04 , A61K31/5513 , A61P1/16
CPC分类号： C07D243/38 , C07D401/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D407/04 , C07D407/06 , C07D407/14 , C07D409/04 , C07D413/06 , C07D417/06
摘要： Inhibitors of HCV replication of formula (I) the stereoisomers, prodrugs, tautomers, racemics, salts, hydrates or solvates thereof wherein R 1 , R 2 ; R 3 ; R 4 a and R 4b 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 in HCV therapy.
摘要翻译：式（I）的HCV复制抑制剂其立体异构体，前药，互变异构体，外消旋物，盐，水合物或溶剂合物，其中R 1，R 2， [R ^{3 ; R＆lt; 4＆gt;＆lt; SUP＆gt; a}

3. 发明申请

WO2007014919A1 MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译： HEPATITIS C病毒的大肠抑制剂
公开(公告)号：WO2007014919A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064813
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , RABOISSON, Pierre, Jean-Marie, Bernard , DE KOCK, Herman, Augustinus , VENDEVILLE, Sandrine, Marie, Helene , HU, Lili , VAN DE VREKEN, Wim , MC GOWAN, David, Craig , TAHRI, Abdellah , SURLERAUX, Dominique, Louis, Nestor, Ghislain , SIMMEN, Kenneth, Alan
发明人： RABOISSON, Pierre, Jean-Marie, Bernard , DE KOCK, Herman, Augustinus , VENDEVILLE, Sandrine, Marie, Helene , HU, Lili , VAN DE VREKEN, Wim , MC GOWAN, David, Craig , TAHRI, Abdellah , SURLERAUX, Dominique, Louis, Nestor, Ghislain , SIMMEN, Kenneth, Alan
IPC分类号： C07D487/04 , C07K5/078 , A61K38/05 , A61P31/14 , C07K5/06
CPC分类号： C07D487/04 , C07K5/06165
摘要： Inhibitors of HCV of formula (I), and the N -oxides, salts, and stereochemically isomeric forms thereof, wherein R 1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 8 to 12 membered bicyclic heterocyclic ring system containing one nitrogen, and optionally one to three oxygen, sulfur or nitrogen, wherein said ring system may be optionally substituted; L is a direct bond, -O-. -O-C 1-4 alkanediyl-, -O-CO-, -O-C(=O)-NR 5a - or -O-C(=O)-NR 5a -C 1-4 alkanediyl-; R 2 is hydrogen, -OR 6 , -C(O)OR 6 , -C(=O)R 7 , -C(=O)NR 5a R 5b , -C(=O)NHR 5c , -NR 5a R 5b , -NHR 5c , -NHSO p NR 5a R 5b , -NR 5a SO p R 8 , or -B(OR 6 ) 2 ; R 3 and R 4 are hydrogen or C 1-6 alkyl; or R 3 and R 4 taken together may form a C 3-7 cycloalkyl ring; n is 3, 4, 5, or 6; p is 1 or 2; aryl is phenyl, naphthyl, indanyl, or 1,2,3,4-tetrahydronaphthyl, each of which may be optionally substituted Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, being optionally condensed with a benzene ring, and wherein the group Het as a whole may be optionally substituted ; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
摘要翻译：式（I）的HCV抑制剂及其N-氧化物，盐和立体化学异构形式，其中R 1是芳基或饱和的部分不饱和或完全不饱和的5或6元单环或含有一个氮和任选地一至三个氧，硫或氮的8至12元双环杂环体系，其中所述环系可以任选被取代; L是直接键，-O-。 -OC 1-4烷基 - ， - O-CO-，-OC（= O）-NR 5a - 或-OC（= O）-NR 图5a -C _{1-4 烷二; R 2是氢，-OR 6，-C（O）OR 6，-C（= O）R 7， -C（= O）NR 5a R 5b，-C（= O）NHR 5c，-NR 5a，5b 5b，-NHR 5c，-NHSO 5，R 5，R 5，R 5，或者-B（OR 6），-NR 5a，或者B（OR 6） > 2 ; R 3和R 4是氢或C 1-6烷基; 或R 3和R 4一起可以形成C 3〜7的环烷基环; n为3,4,5或6; p为1或2; 芳基是苯基，萘基，茚满基或1,2,3,4-四氢萘基，其各自可以被任选地取代。Het是含有1至4个杂原子的5或6元饱和，部分不饱和或完全不饱和的杂环，各自独立地选择来自氮，氧和硫，任选地与苯环稠合，并且其中基团Het作为整体可以任选被取代; 含有化合物（I）的药物组合物和制备化合物（I）的方法。还提供了式（I）的HCV抑制剂与利托那韦的生物可利用组合。}

4. 发明申请

WO2002081478A3 BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2002081478A3
公开(公告)日：2002-10-17
申请号：PCT/EP2002/004012
申请日：2002-04-09
申请人： TIBOTEC PHARMACEUTICALS LTD. , SURLERAUX, Dominique, Louis, Nestor, Ghislain , VENDEVILLE, Sandrine, Marie, Helene , VERSCHUEREN, Wim, Gaston , DE BETHUNE, Marie-Pierre, T.M.M.G , DE KOCK, Herman, Augustinus , TAHRI, Abdellah , ERRA SOLÀ, Montserrat
发明人： SURLERAUX, Dominique, Louis, Nestor, Ghislain , VENDEVILLE, Sandrine, Marie, Helene , VERSCHUEREN, Wim, Gaston , DE BETHUNE, Marie-Pierre, T.M.M.G , DE KOCK, Herman, Augustinus , TAHRI, Abdellah , ERRA SOLÀ, Montserrat
IPC分类号： C07D493/04
摘要： The present invention concerns the compounds having the formula (I) N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-C1-6alkanediyl-C(=O)-, -NR8-C1-6alkanediyl-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2 ; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C1-4alkyl)aminoC(=O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, -C(=O)-, -C(=S)-, -S(=O)2-, C1-6alkanediyl-C(=O)-, C1-6alkanediyl-C(=S)- or C1-6alkanediyl-S(=O)2-; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxycarbonylamino or amino; and in case -A- is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; -A-R6 is hydroxyC1-6alkyl; R5 and -A-R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

5. 发明申请

WO2012080447A1 INDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS 审中-公开
标题翻译：作为呼吸道同源病毒抗病毒剂
公开(公告)号：WO2012080447A1
公开(公告)日：2012-06-21
申请号：PCT/EP2011/073011
申请日：2011-12-16
申请人： JANSSEN R&D IRELAND , COOYMANS, Ludwig Paul , DEMIN, Samuël Dominique , HU, Lili , JONCKERS, Tim Hugo Maria , RABOISSON, Pierre Jean-Marie Bernard , TAHRI, Abdellah , VENDEVILLE, Sandrine Marie Helene
发明人： COOYMANS, Ludwig Paul , DEMIN, Samuël Dominique , HU, Lili , JONCKERS, Tim Hugo Maria , RABOISSON, Pierre Jean-Marie Bernard , TAHRI, Abdellah , VENDEVILLE, Sandrine Marie Helene
IPC分类号： C07D403/06 , C07D471/04 , A61K31/437 , A61P31/12
CPC分类号： C07D471/04 , C07D209/10 , C07D209/12 , C07D235/26 , C07D403/06
摘要： Indoles having inhibitory activity on RSV replication and having the formula I 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：吲哚对RSV复制具有抑制活性，并具有式I的前药，N-氧化物，加成盐，季胺，金属络合物及其立体化学异构形式，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。

6. 发明申请

WO2005111044A1 4-SUBSTITUTED-1,5-DIHYDRO-PYRIDO[3,2-B]INDOL-2-ONES 审中-公开
标题翻译： 4-取代的-1,5-二氢 - 吡啶并[3,2-b]吲哚-2-酮
公开(公告)号：WO2005111044A1
公开(公告)日：2005-11-24
申请号：PCT/EP2005/052265
申请日：2005-05-17
申请人： TIBOTEC PHARMACEUTICALS Ltd. , KESTELEYN, Bart, Rudolf, Romanie , VAN DE VREKEN, Wim , SURLERAUX, Dominique, Louis, Nestor, Ghislain , VENDEVILLE, Sandrine, Marie, Helene , RABOISSON, Pierre, Jean-Marie, Bernard , WIGERINCK, Piet, Tom, Bert, Paul , PEETERS, Annick, Ann
发明人： KESTELEYN, Bart, Rudolf, Romanie , VAN DE VREKEN, Wim , SURLERAUX, Dominique, Louis, Nestor, Ghislain , VENDEVILLE, Sandrine, Marie, Helene , RABOISSON, Pierre, Jean-Marie, Bernard , WIGERINCK, Piet, Tom, Bert, Paul , PEETERS, Annick, Ann
IPC分类号： C07D491/04
CPC分类号： C07D471/04 , C07D491/04 , C07D491/14
摘要： 4-substituted 1,5-dihydro-pyrido[3,2-b]indol-2-ones of formula (I): the N -oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein n is 1, 2 or 3; R 1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N -hydroxymethanimidamidyl, mono- or di(C 1-4 alkyl)methanimidamidyl, Het 1 or Het 2 ; X is NR 2 , O, S, SO, SO 2 ; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 3-7 cycloalkyl, which are optionally substituted; R 2 is aryl substituted with -COOR 4 ; or R 2 is: (b-1); (b-2); -C p H 2p -CH(OR 14 )-C q H 2q -R 15 (b-3); -CH 2 -CH 2 -(O-CH 2 -CH 2 ) m -OR 14 (b-4); -CH 2 -CH 2 -(O-CH 2 -CH 2 ) m -NR 5a R 5b (b-5); -a 1 =a 2 -a 3 =a 4 - is -CH=CH-CH=CH-; -N=CH-CH=CH-; -CH=N-CH=CH-; -CH=CH-N=CH-; -CH=CH-CH=N-; wherein hydrogen atoms in (c-1) - (c-5) may be replaced by certain radicals; R 3 is obtionally substituted phenyl or a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted; R 21 is halo, hydroxy, amino, carboxyl, C 1-6 alkyl, C 3-7 cycloalkyl, arylC 1-6 alkyl, formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonylo xy, -C(=O)-NR 13 R 14 ; C 1-6 alkyloxy, arylC 1-6 alkyloxy, polyhaloC 1-6 alkyloxy, amino, mono or di(C 1-6 alkyl)amino, formylamino, C 1-6 alkylcarbonylamino, C 1-6 alkylsulfo nylamino, mercapto, C 1-6 alkylthio, arylthio, aryloxy, arylC 1-6 alkylthio, C 1-6 alkylsulfynyl, C 1-6 alkylsulfo nyl, aryl, arylamino, Het 1 , Het 2 .
摘要翻译：式（I）的4-取代的1,5-二氢吡啶并[3,2-b]吲哚-2-酮：N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物，其中n 是1，2或3; R 1是氢，氰基，卤素，取代的羰基，甲亚氨基酰胺基，N-羟基甲酰亚胺基，单或二（C 1-4烷基）甲酰亚胺基，Het1或Het2; X是NR 2，O，S，SO，SO 2; R 2是氢，C 1-10烷基，C 2-10烯基，C 3-7环烷基，其任选被取代; R 2是被-COOR 4取代的芳基; 或R 2为：（b-1）; （B-2）; -CpH2p-CH（OR 14）-C≡H2q-R 15（b-3）; -CH 2 -CH 2 - （O-CH 2 -CH 2）m -OR 14（b-4）; -CH 2 CH 2 - （O-CH2-CH2）M-NR <5A> - [R <5B>（B-5）; -a 1 = a 2 -a 3 = a 4 - 是-CH = CH-CH = CH-; -N = CH-CH = CH-; -CH = N-CH = CH-; -CH = CH-N = CH-; -CH = CH-CH = N-; 其中（c-1） - （c-5）中的氢原子可被某些基团取代; R 3是被取代的苯基或可被取代的单环或双环芳族杂环体系; R 21是卤素，羟基，氨基，羧基，C 1-6烷基，C 3-7环烷基，芳基C 1-6烷基，甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基氧基，-C（= O）-NR 13 > - [R <14>; C 1-6烷氧基，芳基C 1-6烷氧基，多卤代C 1-6烷氧基，氨基，单或二（C 1-6烷基）氨基，甲酰氨基，C 1-6烷基羰基氨基，C 1-6烷基磺酰基氨基，巯基，C 1-6烷硫基，芳硫基，芳氧基，芳基C 1-6烷硫基， -6-烷基亚磺酰基，C 1-6烷基磺酰基，芳基，芳基氨基，Het 1，Het 2。

7. 发明申请

WO2003076413A1 BROADSPECTRUM SUBSTITUTED BENZIMIDAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS 审中-公开
标题翻译： BROADSPECTRUM取代苯并咪唑磺酰胺艾滋病毒蛋白酶抑制剂
公开(公告)号：WO2003076413A1
公开(公告)日：2003-09-18
申请号：PCT/EP2003/050057
申请日：2003-03-12
申请人： TIBOTEC PHARMACEUTICALS LTD , SURLERAUX, Dominique, Louis, Nestor, Ghislain , WIGERINCK, Piet, Tom, Bert, Paul , VOETS, Marieke, Christiane, Johanna , VENDEVILLE, Sandrine, Marie, Helene , DE KOCK, Herman, Augustinus , VERGOUWEN, Bernhard, Joanna, Bernard
发明人： SURLERAUX, Dominique, Louis, Nestor, Ghislain , WIGERINCK, Piet, Tom, Bert, Paul , VOETS, Marieke, Christiane, Johanna , VENDEVILLE, Sandrine, Marie, Helene , DE KOCK, Herman, Augustinus , VERGOUWEN, Bernhard, Joanna, Bernard
IPC分类号： C07D235/32
CPC分类号： C07D401/12 , A61K31/415 , C07D235/30 , C07D235/32 , C07D405/12 , C07D413/12 , C07D417/12 , C07D493/04
摘要： The present invention concerns the compounds having the formula (I), wherein N -oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R 1 and R 8 each are H, optionally substituted C 1-6 alkyl, C 2-6 alkenyl, C 3-7 cycloalkyl, aryl, Het 1 , Het 2 ; R 1 may also be a radical of formula (R 11a R 11b )NC(R 10a R l0b )CR 9 -; t is 0, 1 or 2; R 2 is H or C 1-6 alkyl; L is -C(=O)-, -O-C(=O)-, -NR 8 -C(=O)-, -O-C 1-6 alkanediyl-C(=O)-, -NR 8 -C 1-6 alkanediyl-C(=O)-, -S(=O) 2 -, -O-S(=O) 2 -, -NR 8 -S(=O) 2 ; R 3 is C 1-6 alkyl, aryl, C 3-7 cycloalkyl, C 3-7 cycloalkylC 1-4 alkyl, or arylC 1-4 alkyl; R 4 is H, C 1-4 alkylOC(=O), carboxyl, aminoC(=O), mono- or di(C 1-4 alkyl)aminoC(=O), C 3-7 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl or optionally substituted C 1-6 alkyl; A is C 1-6 alkanediyl, -C(=O)-, -C(=S)-, -S(=O) 2 -, C 1-6 alkanediyl-C(=O)-, C 1-6 alkanediyl-C(=S)- or C 1-6 alkanediyl-S(=O) 2 -; R 5 is H, OH, C 1-6 alkyl, Het 1 C 1-6 alkyl, Het 2 C 1-6 alkyl, optionally substituted amino-C 1-6 alkyl; R 6 is C 1-6 alkylO, Het 1 , Het 1 O, Het 2 , Het 2 O, aryl, arylO, C 1-6 alkyloxycarbonylamino or amino; and in case _ A- is other than C 1-6 alkanediyl then R 6 may also be C 1-6 alkyl, Het 1 C 1-4 alkyl, Het 1 OC 1-4 alkyl, Het 2 C 1-4 alkyl, Het 2 OC 1-4 alkyl, arylC 1-4 alkyl, arylOC 1-4 alkyl or aminoC 1-4 alkyl; whereby each of the amino groups in the definition of R 6 may optionally be substituted; R 5 and _ A-R 6 taken together with the nitrogen atom to which they are attached may also form Het 1 or Het 2 , R 12 , is H, - NH 2 , _ NR 5 AR 6 , - C 1-6 alkyl or alkyl-W-R 14 , wherein said alkyl is optionally substituted with halogen, hydroxy, aryl, heteroaryl, Het 1 , Het 2 , or amino wherein said amino is optionally mono- or di-substituted with C 1-4 alkyl and R 13 is H, C 1-6 -alkyl, optionally substituted by aryl, Het 1 , Het 2 , hydroxy, halogen, amino whereby the amino group may be optionally be mono- or di-substituted with C 1-4 alkyl.
摘要翻译：本发明涉及具有式（I）的化合物，其中N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物，其中R 1和R 8各自为H，任选取代的C 1-6烷基，C 2-6烯基，C 3-7环烷基，芳基，Het1，Het2; R1也可以是式（R11aR11b）NC（R10aR10b）CR9-的基团; t为0,1或2; R2是H或C1-6烷基; L是-C（= O） - ， - OC（= O） - ， - NR 8 -C（= O） - ， - O-C 1-6烷二基-C（= O） - ， - NR 8 -C 1-6烷二基-C （= O） - ， - S（= O）2 - ， - OS（= O）2 - ， - NR 8 -S（= O）2; R 3是C 1-6烷基，芳基，C 3-7环烷基，C 3-7环烷基C 1-4烷基或芳基C 1-4烷基; R 4是H，C 1-4烷基OC（= O），羧基，氨基C（= O），单或二（C 1-4烷基）氨基C（= O），C 3-7环烷基，C 2-6烯基，C 2-6炔基或任选取代的C 1 1-6; A是C 1-6烷二基，-C（= O） - ， - C（= S） - ， - S（= O）2 - ，C 1-6烷二基-C（= O） - ，C 1-6烷二基-C S） - 或C 1-6烷二基-S（= O）2 - ; R5是H，OH，C1-6烷基，Het1C1-6烷基，Het2C1-6烷基，任选取代的氨基-C 1-6烷基; R 6是C 1-6烷基O，Het 1，Het 10，Het 2，Het 2 O，芳基，芳基O，C 1-6烷氧基羰基氨基或氨基; 并且在_A-不是C 1-6烷二基的情况下，R 6还可以是C 1-6烷基，Het 1 C 1-4烷基，Het 1 OC 1-4烷基，Het 2 C 1-4烷基，Het 2 OC 1-4烷基，芳基C 1-4烷基，芳基OC 1-4烷基或氨基C 1-4烷基; 其中R6的定义中的每个氨基可任选被取代; R5和_A-R6与它们所连接的氮原子一起也可以形成Het1或Het2，R12，是H，-NH2，_NR5AR6，C1-6烷基或烷基-W-R14，其中所述烷基任选被取代卤素，羟基，芳基，杂芳基，Het1，Het2或氨基，其中所述氨基任选被C 1-4烷基单取代或二取代，R 13为H，任选被芳基，Het1，Het2，羟基，卤素，氨基，其中氨基可以任选被C 1-4烷基单取代或二取代。

8. 发明申请

WO2012080449A1 AZABENZIMIDAZOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS 审中-公开
标题翻译：作为呼吸道同源病毒抗病毒药物的AZABENZIMIDAZOLES
公开(公告)号：WO2012080449A1
公开(公告)日：2012-06-21
申请号：PCT/EP2011/073014
申请日：2011-12-16
申请人： JANSSEN R&D IRELAND , COOYMANS, Ludwig Paul , DEMIN, Samuël Dominique , HU, Lili , JONCKERS, Tim Hugo Maria , RABOISSON, Pierre Jean-Marie Bernard , TAHRI, Abdellah , VENDEVILLE, Sandrine Marie Helene
发明人： COOYMANS, Ludwig Paul , DEMIN, Samuël Dominique , HU, Lili , JONCKERS, Tim Hugo Maria , RABOISSON, Pierre Jean-Marie Bernard , TAHRI, Abdellah , VENDEVILLE, Sandrine Marie Helene
IPC分类号： C07D471/04 , A61K31/437 , A61P31/12
CPC分类号： C07D519/00 , C07D471/04 , C07F5/025
摘要： A compound satisfying formula I, a prodrug, N -oxide, addition salt, quaternary metal complex, or a stereochemically isomeric form thereof; (formula I) 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，四元金属络合物或其立体化学异构形式的化合物; （式I）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。

9. 发明申请

WO2010018233A1 MACROCYCLIC INDOLE DERIVATIVES USEFUL AS HEPATITIS C VIRUS INHIBITORS 审中-公开
标题翻译：大环内酯衍生物作为丙型肝炎病毒抑制剂有用
公开(公告)号：WO2010018233A1
公开(公告)日：2010-02-18
申请号：PCT/EP2009/060580
申请日：2009-08-14
申请人： TIBOTEC PHARMACEUTICALS , MC GOWAN, David, Craig , VENDEVILLE, Sandrine, Marie, Helene , RABOISSON, Pierre, Jean-Marie, Bernard
发明人： MC GOWAN, David, Craig , VENDEVILLE, Sandrine, Marie, Helene , RABOISSON, Pierre, Jean-Marie, Bernard
IPC分类号： C07D515/08 , A61K31/407 , A61P31/14
CPC分类号： C07D515/08
摘要： Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein Y, R 1 , R 2 , R 4 and n 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 in HCV therapy.
摘要翻译：包含立体化学异构体形式的式（I）的HCV复制抑制剂及其盐，水合物，溶剂化物，其中Y，R1，R2，R4和n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在HCV治疗中的用途。

10. 发明申请

WO2008099020A1 1,1-DIOXO-1-THIA-5,10-DIAZADIBENZOCYCLOHEPTENES USEFUL AS HEPATITIS C VIRUS INHIBITORS 审中-公开
标题翻译： 1-DIOXO-1-THIA-5,10-DIAZADIBENZOCYCLOHEPTENES有用的丙型肝炎病毒抑制剂
公开(公告)号：WO2008099020A1
公开(公告)日：2008-08-21
申请号：PCT/EP2008/051903
申请日：2008-02-15
申请人： TIBOTEC PHARMACEUTICALS LTD. , RABOISSON, Pierre Jean-Marie Bernard , VANDYCK, Koen , NYANGUILE, Origène , MC GOWAN, David Craig , VENDEVILLE, Sandrine Marie Helene , AMSSOMS, Katie Ingrid Eduard , BOUTTON, Carlo Willy Maurice , LORY, Pedro Miguel Jales , HU, Lili , VAN DEN BROECK, Walter Marcel Mathilde , CUMMINGS, Maxwell David , ROMBAUTS, Klara , LAST, Stefaan Julien , TAHRI, Abdellah
发明人： RABOISSON, Pierre Jean-Marie Bernard , VANDYCK, Koen , NYANGUILE, Origène , MC GOWAN, David Craig , VENDEVILLE, Sandrine Marie Helene , AMSSOMS, Katie Ingrid Eduard , BOUTTON, Carlo Willy Maurice , LORY, Pedro Miguel Jales , HU, Lili , VAN DEN BROECK, Walter Marcel Mathilde , CUMMINGS, Maxwell David , ROMBAUTS, Klara , LAST, Stefaan Julien , TAHRI, Abdellah
IPC分类号： C07D495/04 , A61K31/55 , A61P31/00
CPC分类号： C07D495/04
摘要： Inhibitors of HCV replication of formula (I) the stereoisomers, prodrugs, tautomers, racemics, salts, hydrates or solvates thereof wherein R 1a ; R 1b R 2 ; R 3 ; R 4a and R 4b 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 in HCV therapy.
摘要翻译：式（I）的HCV复制抑制剂其立体异构体，前体药物，互变异构体，外消旋物，盐，水合物或溶剂合物，其中R 1a是 R 1b，R 2，R 2， [R ^{3 ; R 4a和R 4b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在HCV治疗中的用途。}

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