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1. 发明申请

WO2008096002A1 HCV INHIBITING MACROCYCLIC PHOSPHONATES AND AMIDOPHOSPHATES 审中-公开
标题翻译： HCV抑制大环磷酰胺和氨基磷酸酯
公开(公告)号：WO2008096002A1
公开(公告)日：2008-08-14
申请号：PCT/EP2008/051558
申请日：2008-02-08
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , ANTONOV, Dmitry , NILSSON, Karl, Magnus , RABOISSON, Pierre Jean-Marie Bernard , ROSENQUIST, Asa, Annica, Kristina , SAMUELSSON, Bengt, Bertil , VENDEVILLE, Sandrine, Marie Hélène
发明人： ANTONOV, Dmitry , NILSSON, Karl, Magnus , RABOISSON, Pierre Jean-Marie Bernard , ROSENQUIST, Asa, Annica, Kristina , SAMUELSSON, Bengt, Bertil , VENDEVILLE, Sandrine, Marie Hélène
IPC分类号： C07F9/6561 , A61K31/675 , A61P31/14
CPC分类号： C07F9/6561
摘要： Inhibitors of HCV replication of Formula (I) the /V-oxides, salts, and stcreochcmically isomeric forms thereof; pharmaceutical compositions containing compounds (1) and processes for preparin compounds (I). The side chain R 2 is an amidophosphate or a phosphonate group and X, R 1 , R 3 , E and n are as defined in the application.
摘要翻译：式（I）的HCV复制抑制剂的N-氧化物，盐和其它异构体形式; 含有化合物（1）的药物组合物和制备前体化合物（I）的方法。侧链R 2是酰氨基磷酸酯或膦酸酯基，X，R 1，R 3，E和n如应用。

2. 发明申请

WO2008096001A8 HCV INHIBITING MACROCYCLIC PHENYLCARBAMATES 审中-公开
公开(公告)号：WO2008096001A8
公开(公告)日：2008-08-14
申请号：PCT/EP2008/051556
申请日：2008-02-08
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre Jean-Marie Bernard , ANTONOV, Dmitry , AYESA ALVAREZ, Susana , BELFRAGE, Anna, Karin, Gertrud, Linnea , JÖNSSON, Carl, Erik, Daniel , MC GOWAN, David, Craig , NILSSON, Karl, Magnus , ROSENQUIST, Åsa, Annica, Kristina , SAMUELSSON, Bengt, Bertil
发明人： RABOISSON, Pierre Jean-Marie Bernard , ANTONOV, Dmitry , AYESA ALVAREZ, Susana , BELFRAGE, Anna, Karin, Gertrud, Linnea , JÖNSSON, Carl, Erik, Daniel , MC GOWAN, David, Craig , NILSSON, Karl, Magnus , ROSENQUIST, Åsa, Annica, Kristina , SAMUELSSON, Bengt, Bertil
IPC分类号： C07D245/04 , C07D255/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D498/04 , C07D498/14 , A61K31/538 , A61P31/14
摘要： Compounds of the Formula (I) including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof;usefulas HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.

3. 发明申请

WO2004021969A2 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：非核苷酸逆转录酶抑制剂
公开(公告)号：WO2004021969A2
公开(公告)日：2004-03-18
申请号：PCT/EP2003/009872
申请日：2003-09-05
申请人： MEDIVIR AB , ANTONOV, Dmitry , SUND, Christian , LINDSTRÖM, Stefan , SAHLBERG, Christer
发明人： ANTONOV, Dmitry , SUND, Christian , LINDSTRÖM, Stefan , SAHLBERG, Christer
IPC分类号： A61K
CPC分类号： C07D213/73 , C07D213/65 , C07D307/93 , C07D311/94 , C07D333/78 , C07D335/06 , C07D405/12 , Y02P20/582
摘要： A compound of the formula (Y): where; R 1 is O, S; R 2 is a nitrogen-containing heterocycle; R 3 is H, C l -C 3 alkyl; X is -(CR 8 R 8 ') n -D-(CR 8 R 8 ') m -; D is a bond, -NR 9 -, -O-, -S-, -S(=O)- or -S(=O) 2 -; n and m are independently 0, 1 or 2, R 8 and R 8 ' are independently H, C 1 -C 3 alkyl, haloC 1 -C 3 alkyl, hydroxy, or R 8 and R 8 ' together with their adjacent C atom is -C(=O)-; R 9 is independently H, C 1 -C 3 alkyl; E is CH 2 -, -CHOH-, -C(=O)-, -NR 9 -, -O-, -S-, -S(=O) 2 -; n and m are independently 0, 1 or 2; p and q are independently 0, 1 or 2, where p+q ≤ 2; R 10 is an optionally substituted carbocycle or heterocycle; R 11 is independently H, C 1 -C 3 alkyl, halo substituted C l -C 3 alkyl, hydroxy; have utility as HIV antivirals.
摘要翻译：式（Y）的化合物：其中; R1为O，S; R2是含氮杂环; R3是H，C1-C3烷基; X是 - （CR8R8'）n-D-（CR8R8'）m-; D是键，-NR 9 - ， - O - ， - S - ， - S（= O） - 或-S（= O） n和m独立地为0,1或2，R 8和R 8'独立地为H，C 1 -C 3烷基，卤代C 1 -C 3烷基，羟基或R 8和R 8'与它们相邻的C原子一起为-C（= O） - ; R9独立地为H，C1-C3烷基; E是CH 2 - ， - CHOH - ， - C（= O） - ， - NR 9 - ， - O - ， - S - ， - S（= O） n和m独立地为0,1或2; p和q独立地为0,1或2，其中p + q <= 2; R 10是任选取代的碳环或杂环; R 11独立地为H，C 1 -C 3烷基，卤素取代的C 1 -C 3烷基，羟基; 具有艾滋病毒抗病毒药物的作用。

4. 发明申请

WO2003020705A1 UREA AND THIOUREA DERIVATIVES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：尿素和硫脲衍生物作为非核苷酸逆转录酶抑制剂
公开(公告)号：WO2003020705A1
公开(公告)日：2003-03-13
申请号：PCT/EP2002/002346
申请日：2002-03-04
申请人： MEDIVIR AB
发明人： SAHLBERG, Christer , ANTONOV, Dmitry , WALLBERG, Hans , NOREEN, Rolf
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , C07D213/85
摘要： Compounds of the formula (I): where R 1 is O, S; R 2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R 3 is H, C 1 -C 3 alkyl, R 4 -R 7 are independently selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, haloC 1 -C 6 alkyl, C 1 -C 6 alkanoyl, haloC 1 -C 6 alkanoyl, C 1 -C 6 alkoxy, haloC 1 -C 6 alkoxy, C 1 -C 6 alkyloxy-C 1 -C 6 alkyl, haloC 1 -C 6 alkyloxy-C 1 -C 6 alkyl hydroxy-C 1 -C 6 alkyl, amino-C 1 -C 6 alkyl, carboxy-C 1 -C 6 alkyl, cyano-C 1 -C 6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is -(CR 8 R 9 ) n -, R 8 and R 9 are independently H, C 1 -C 3 alkyl, OH or R 8 and R 9 together are =0, n is 1, 2 or 3, and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.
摘要翻译：式（I）的化合物：其中R 1是O，S; R2是任选取代的含氮杂环，其中氮位于相对于（硫）脲键的2位; R3是H，C1-C3烷基，R4-R7独立地选自H，C1-C6烷基，C2-C6烯基，C2-C6炔基，卤代C 1 -C 6烷基，C 1 -C 6烷酰基，卤代C 1 -C 6烷酰基， C6烷氧基，卤代C 1 -C 6烷氧基，C 1 -C 6烷氧基-C 1 -C 6烷基，卤代C 1 -C 6烷氧基-C 1 -C 6烷基羟基-C 1 -C 6烷基，氨基-C 1 -C 6烷基，羧基-C 1 -C 6烷基， C 1 -C 6烷基，氨基，羧基，氨基甲酰基，氰基，卤素，羟基，酮基; X是 - （CR 8 R 9）n - ， - R 8和R 9独立地为H，C 1 -C 3烷基，OH或R 8和R 9一起为= 0，n为1,2或3，并且其前药和药学上可接受的盐可用作 HIV-1逆转录酶的抑制剂，特别是药物逃逸突变体。

5. 发明申请

WO2007014918A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014918A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064812
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , DE KOCK, Herman, Augustinus , RABOISSON, Pierre, Jean-Marie, Bernard , SIMMEN, Kenneth, Alan , LINDSTRÖM, Mats, Stefan , KAHNBERG, Pia, Cecilia , ANTONOV, Dmitry , NILSSON, Karl, Magnus , SAMUELSSON, Bengt, Bertil , ROSENQUIST, Åsa, Annica, Kristina
发明人： DE KOCK, Herman, Augustinus , RABOISSON, Pierre, Jean-Marie, Bernard , SIMMEN, Kenneth, Alan , LINDSTRÖM, Mats, Stefan , KAHNBERG, Pia, Cecilia , ANTONOV, Dmitry , NILSSON, Karl, Magnus , SAMUELSSON, Bengt, Bertil , ROSENQUIST, Åsa, Annica, Kristina
IPC分类号： C07K5/078 , A61K31/4709 , A61P31/14 , C07K5/06
CPC分类号： A61K31/4709 , C07K5/06165 , Y02A50/385 , Y02A50/387
摘要： Inhibitors of HCV of formula (I), and the N -oxides, salts, and stereoisomers thereof, wherein the dashed line represents an optional double bond between atoms C7 and C8; R 1 is hydrogen or C 1-6 alkyl; R 2 is hydrogen or C 1-6 alkyl; and n is 3, 4, 5, or 6; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I) are provided. 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，盐和立体异构体，其中虚线表示原子C7和C8之间任选的双键; R 1是氢或C 1-6烷基; R 2是氢或C 1-6烷基; n为3,4,5或6; 提供含有化合物（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。

6. 发明申请

WO2005066131A1 NON-NUCLEOTIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：非核苷酸逆转录酶抑制剂
公开(公告)号：WO2005066131A1
公开(公告)日：2005-07-21
申请号：PCT/SE2004/002034
申请日：2004-12-30
申请人： MEDIVIR AB , SUND, Christian , ROUE, Nathalie , LINDSTRÖM, Stefan , ANTONOV, Dmitry , SAHLBERG, Christer , JANSSON, Katarina
发明人： SUND, Christian , ROUE, Nathalie , LINDSTRÖM, Stefan , ANTONOV, Dmitry , SAHLBERG, Christer , JANSSON, Katarina
IPC分类号： C07D213/75
CPC分类号： C07D409/12 , C07D405/12 , C07D405/14 , C07D409/14
摘要： Compounds of the formula Z: where; A is CH or N; R 1 is a substituent to a carbon atom in the ring containing A selected from -S(=O) p Ra, where Ra is -C 1 -C 4 alkyl, -ORx, -NRxRx, -NHNRxRx, - NHNHC(=O)ORx, -NRxOH; -C(=O)-Rb, where Rb is -CT-C4-alkyl, ORx, -NRxRx, -NHNRxRx, -NHC 1 -C 3 -alkyl-C(=O)Orx -NRxRc, where Rc is H, C 1 -C 4 alkyl, -NRxRx; -C(=0)Rd, -CN, S(=O)pRx where Rd is Rd is C1-C4-alkyl, -ORx, -NRxRx C 1 -C 3 -alkyl-O-Cl-C3alkylC(=O)ORx, -C 1 -C 3 -alkyl-COORx; -C 1 -C 3 alkyl-OH or C 1 -C 4 alkyl ethers or esters thereof (O-C l -C 3 alkyl)q-O-Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C 1 -C 4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is -0-, -S(=O),- or -CH 2 -, where r is 0, 1 or 2; R 3 -R 7 are substituents as defined in the specification; X is -(CR 8 R 8 ')n-D-(CR 8 R 8 ')m-; D is a bond, -NR 9 -, -0-, -S-, -S(=0)- or -S(=0) 2 -; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.
摘要翻译：式Z的化合物：其中; A是CH或N; R 1是含有选自-S（= O）p R a的A的环中的碳原子的取代基，其中R a是-C 1 -C 4烷基，-OR x，-NR x R x，-NHNR x R x，-NH NH（= O）OR x， NRxOH; -C（= O）-R b，其中R b是-C 1 -C 4 - 烷基，OR x，-NR x R x，-NHNR x R x，-NHC 1 -C 3 - 烷基-C（= O）OR x -NR x R c，其中R c是H， C4烷基，-NRxRx; -C（= O）R d，-CN，S（= O）p R x其中Rd是Rd是C 1 -C 4 - 烷基，-OR x，-NR x R x C 1 -C 3烷基-O-C 1 -C 3烷基C（= O）OR x， -C 1 -C 3 - 烷基 - COORx; -C 1 -C 3烷基-OH或C 1 -C 4烷基醚或其酯（O-Cl-C 3烷基）q-O-Rx具有1-3个杂原子的5或6元芳环p为1或2; R x独立地选自H，C 1 -C 4烷基或乙酰基; 或一对Rx可与相邻的N原子一起形成环; L是-O - ， - S（= O）， - 或-CH 2 - ，其中r是0,1或2; R3-R7是说明书中定义的取代基; X是 - （CR8R8'）n-D-（CR8R8'）m-; D是键，-NR 9 - ， - O - ， - S - ， - S（= O） - 或-S（= O）其药学上可接受的盐和前药具有作为HIV抗病毒剂的效用。

7. 发明申请

WO2007014922A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014922A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064816
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , SIMMEN, Kenneth Alan , JÖNSSON, Carl Erik Daniel , NILSSON, Karl Magnus , ROSENQUIST, Åsa Annica Kristina , SAMUELSSON, Bengt Bertil , ANTONOV, Dmitry , SALVADOR ODÉN, Lourdes , AYESA ALVAREZ, Susana , CLASSON, Björn Olof
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , SIMMEN, Kenneth Alan , JÖNSSON, Carl Erik Daniel , NILSSON, Karl Magnus , ROSENQUIST, Åsa Annica Kristina , SAMUELSSON, Bengt Bertil , ANTONOV, Dmitry , SALVADOR ODÉN, Lourdes , AYESA ALVAREZ, Susana , CLASSON, Björn Olof
IPC分类号： C07D401/12 , C07D403/12 , C07D245/04 , A61K31/4523 , A61P31/14
CPC分类号： C07D401/12 , C07D225/04 , C07D245/04 , C07D403/12 , C07D413/12 , C07D417/12 , C07D487/04
摘要： Inhibitors of HCV replication of formula (I) and the N -oxides, salts, or 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; R 1 is -OR 6 , -NH-SO 2 R 7 ; R 2 is hydrogen, and where X is C or CH, R 2 may also be C 1-6 alkyl; R 3 is hydrogen, C 1-6 alkyl, C 1-6 alkoxyC 1-6 alkyl, or C 3-7 cycloalkyl; n is 3, 4, 5, or 6; R 4 and R 5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 alkylcarbonyl, C 1-6 alkoxy- carbonyl, amino, azido, mercapto, C 1-6 alkylthio, polyhaloC 1-6 alkyl, aryl or Het; W is aryl or Het; R 6 is hydrogen; aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; R 7 is aryl; Het; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl; or C 1-6 alkyl optionally substituted with C 3-7 cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 - 4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1 -3 substituents; 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复制抑制剂及其N-氧化物，盐或立体异构体，其中每个虚线（由 - 表示）表示任选的双键; X为N，CH，X为双键，C为C; R 1是-OR 6，-NH-SO 2 R 7， 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，或 ç_{3-7 环烷基; n为3,4,5或6; R 4和R 5彼此独立地是氢，卤素，羟基，硝基，氰基，羧基，C 1-6烷基，C C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，C 1-6烷基羰基，C 烷基 - 羰基，氨基，叠氮基，巯基，C 1-6烷基硫基，多卤代C 1-6烷基，芳基或Het; W是芳基或Het; R 6是氢; 芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; R 7是芳基; HET; 任选被C 1-6烷基取代的C 3-7环烷基; 或任选被C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 芳基是苯基或萘基，各自任选被1-3个取代基取代; Het是含有1-4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，各自独立地选自N，O或S，并且任选被1-3取代基取代; 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。}

8. 发明申请

WO2007014920A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 审中-公开
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：WO2007014920A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064814
申请日：2006-07-28
申请人： TIBOTEC PHARMACEUTICALS LTD. , MEDIVIR AB , DE KOCK, Herman, Augustinus , RABOISSON, Pierre, Jean-Marie, Bernard , TAHRI, Abdellah , SIMMEN, Kenneth, Alan , NILSSON, Karl, Magnus , SAMUELSSON, Bengt, Bertil , ROSENQUIST, Åsa, Annica, Kristina , ANTONOV, Dmitry
发明人： DE KOCK, Herman, Augustinus , RABOISSON, Pierre, Jean-Marie, Bernard , TAHRI, Abdellah , SIMMEN, Kenneth, Alan , NILSSON, Karl, Magnus , SAMUELSSON, Bengt, Bertil , ROSENQUIST, Åsa, Annica, Kristina , ANTONOV, Dmitry
IPC分类号： C07D487/04 , C07K5/078 , A61K38/05 , A61K31/33 , A61P31/14 , C07D413/12
CPC分类号： C07D487/04 , C07D413/12
摘要： Inhibitors of HCV replication of formula (I), the N -oxides, salts, and stereochemically isomeric forms 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; R 1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituents; L is a direct bond, -O-. -O-C 1-4 alkanediyl-, -O-C(=O)-, -O-C(=O)-NR 4a - or -O-C(=O)-NR 4a C 1-4 alkanediyl-; R 2 is hydrogen, -OR 5 , -C(O)OR 5 , -C(=O)R 6 , -C(=O)NR 4a R 4b , -C(=O)NHR 4c ,-NR 4a R 4b , -NHR 4c , -NR 4a SO p NR 4a R 4b , -NR 4a SO p R 7 , or B(OR 5 ) 2 ; R 3 is hydrogen, and where X is C or CH, R 3 may also be C 1-6 alkyl; 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 with one, two or three substituents ; 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 with one, two or three substituents; 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复制抑制剂，其N-氧化物，盐和立体化学异构形式，其中每个虚线（由 - 表示）表示任选的双键; X为N，CH，X为双键，C为C; R 1是芳基或饱和的，部分不饱和的或完全不饱和的5或6元单环或9至12元双环杂环体系，其中所述环体系含有一个氮，以及任选的一至三个另外的杂原子选自氧，硫和氮，并且其中剩余的环成员是碳原子; 其中所述环系可以任选地在任何碳或氮环原子上被一个，两个，三个或四个取代基取代; L是直接键，-O-。 -OC 1-4烷基 - ， - OC（= O） - ， - OC（= O）-NR 4a - 或-OC（= O） SUP>图4a C _{1-4 烷二; R 2是氢，-OR 5，-C（O）OR 5，-C（= O）R 6， -C（= O）NR 4a R 4b，-C（= O）NHR 4c， - NR 4a，4b，4b，4b，4b，4a，4a，4b，4b，或者B（OR）4，其中R 4，R 4，R 4， 5 ）_{2 ; R 3是氢，并且其中X是C或CH，R 3也可以是C 1-6烷基; 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，其各自可以任选地被一个，两个或三个取代基取代; Het是含有1至4个各自独立地选自氮，氧和硫的杂原子的5或6元饱和，部分不饱和或完全不饱和的杂环，任选地与苯环稠合，并且其中基团Het作为整体可以是任选的被一个，两个或三个取代基取代; 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。}}

9. 发明公开

EP1913014A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
标题翻译：丙型肝炎病毒的大环内酯类抑制剂
公开(公告)号：EP1913014A1
公开(公告)日：2008-04-23
申请号：EP06764263.7
申请日：2006-07-28
申请人： Tibotec Pharmaceuticals Ltd. , MEDIVIR AB
发明人： DE KOCK, Herman, Augustinus , RABOISSON, Pierre, Jean-Marie, Bernard , SIMMEN, Kenneth, Alan , LINDSTRÖM, Mats Stefan , KAHNBERG, Pia Cecilia , ANTONOV, Dmitry , NILSSON, Karl Magnus , SAMUELSSON, Bengt Bertil , ROSENQUIST, Åsa Annica, Kristina
IPC分类号： C07K5/078 , A61K31/4709 , A61P31/14 , C07K5/06
CPC分类号： A61K31/4709 , C07K5/06165 , Y02A50/385 , Y02A50/387
摘要： Inhibitors of HCV of formula (I). and the N-oxides, salts, and stereoisomers thereof, wherein the dashed line represents an optional double bond between atoms C7 and C8; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; and n is 3, 4, 5, or 6; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I) are provided. 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，盐和立体异构体，其中虚线代表原子C7和C8之间的任选双键; R1是氢或C1-6烷基; R2是氢或C1-6烷基; 并且n是3,4,5或6; 提供了含有化合物（I）的药物组合物和用于制备化合物（I）的方法。还提供了式（I）的HCV抑制剂与利托那韦的生物可用组合。

10. 发明授权

EP1919898B1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
公开(公告)号：EP1919898B1
公开(公告)日：2011-01-26
申请号：EP06778069.2
申请日：2006-07-28
申请人： Tibotec Pharmaceuticals , MEDIVIR AB
发明人： RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , SIMMEN, Kenneth Alan , JÖNSSON, Carl Erik Daniel , NILSSON, Karl Magnus , ROSENQUIST, Åsa Annica Kristina , SAMUELSSON, Bengt Bertil , ANTONOV, Dmitry , SALVADOR ODÉN, Lourdes , AYESA ALVAREZ, Susana , CLASSON, Björn Olof
IPC分类号： C07D401/12 , C07D403/12 , C07D245/04 , A61K31/4523 , A61P31/14
CPC分类号： C07D401/12 , C07D225/04 , C07D245/04 , C07D403/12 , C07D413/12 , C07D417/12 , C07D487/04
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or 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 -OR6, -NH-SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy- carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 - 4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1 -3 substituents; 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.

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