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公开(公告)号：US20060167055A1
公开(公告)日：2006-07-27
申请号：US10526598
申请日：2003-09-05
IPC分类号： A61K31/4433 , A61K31/4436 , C07D409/02
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; R1 is O, S; R2 is a nitrogen-containing heterocycle; R3 is H, C1-C3 alkyl; X is —(C8R8)n-D-(C8C8′)m—; D is a bond, —NR9—, —O—, —S—, —S(═O)— or —S(═O)2; n and m are independently 0, 1 or 2, R8 and R8′ are independently H, C1-C3 alkyl, haloC1-C3alkyl, hydroxy, or R8 and R8′ together with their adjacent C atom is —C(═O)—; R9 is independently H, C1-C3 alkyl; E is CH2—, —CHOH—, —C(═O)—, —NR9—, —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; R10 is an optionally substituted carbocycle or heterocycle; R11 is independently H, C1-C3 alkyl, halo substituted C1-C3alkyl, hydroxy; have utility as HIV antivirals.
摘要翻译： 式（Y）的化合物：其中; R 1是O，S; R 2是含氮杂环; R 3是H，C 1 -C 3烷基; X是 - （C 8 R 8） - - - - （C 8 C 8） / SUB>'） D是键，-NR 9 - ， - O - ， - S - ， - S（-O） - 或-S（-O）2。 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原子一起是-C（-O） - ; R 9独立地是H，C 1 -C 3烷基; E是CH 2 - ， - CHOH - ， - C（-O） - ， - NR 9 - ， - O - ， - S - ， - S（-O ）＆lt; 2＆gt; - ; 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独立地是H，C 1 -C 3烷基，卤素取代的C 1 -C 3烷基， 3烷基，羟基; 具有艾滋病毒抗病毒药物的作用。
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公开(公告)号：US07915295B2
公开(公告)日：2011-03-29
申请号：US10584933
申请日：2004-12-30
申请人： Christian Sund , Nathalie Roue , Stefan Lindstrom , Dmitry Antonov , Christer Sahlberg , Katarina Jansson
发明人： Christian Sund , Nathalie Roue , Stefan Lindstrom , Dmitry Antonov , Christer Sahlberg , Katarina Jansson
IPC分类号： A61K31/453 , C07D405/12
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; R1 is a substituent to a carbon atom in the ring containing A selected from —S(═O)pRa, where Ra is —C1-C4 alkyl, —ORx, —NRxRx, —NHNRxRx, —NHNHC(═O)ORx, —NRxOH; —C(═O)—Rb, where Rb is —CT-C4-alkyl, ORx, —NRxRx, —NHNRxRx, —NHC1-C3-alkyl-C(═O)Orx —NRxRc, where Rc is H, C1-C4 alkyl, —NRxRx; —C(=0)Rd, —CN, S(═O)pRx, where Rd is Rd is C1-C4-alkyl, —ORx, —NRxRx C1-C3-alkyl-O—C1-C3-alkylC(═O)ORx, —C1-C3-alkyl-COORx; —C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O—C1-C3alkyl)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, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is -0-, —S(═O)—, or —CH2—, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is —(CR8R8′)n-D-(CR8R8′)m-; D is a bond, —NR9—, -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，-NHNHC（= O）OR x， NR x OH; -C（= O）-R b，其中R b是-CT-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 ）ORx，-C1-C3-烷基-COORx; -C 1 -C 3烷基-OH或C 1 -C 4烷基醚或其酯（O-C 1 -C 3烷基）q-O-R 1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。
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公开(公告)号：US20080070951A1
公开(公告)日：2008-03-20
申请号：US10584933
申请日：2004-12-30
申请人： Christian Sund , Nathalie Roue , Stefan Lindstrom , Dmitry Antonov , Christer Sahlberg , Katarina Jansson
发明人： Christian Sund , Nathalie Roue , Stefan Lindstrom , Dmitry Antonov , Christer Sahlberg , Katarina Jansson
IPC分类号： A61K31/44 , A61P31/18 , C07D211/00
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; R1 is a substituent to a carbon atom in the ring containing A selected from —S(═O)pRa, where Ra is —C1-C4 alkyl, —ORx, —NRxRx, —NHNRxRx, —NHNHC(═O)ORx, —NRxOH; —C(═O)—Rb, where Rb is —CT-C4-alkyl, ORx, —NRxRx, —NHNRxRx, —NHC1-C3-alkyl-C(═O)Orx —NRxRc, where Rc is H, C1-C4 alkyl, —NRxRx; —C(=0)Rd, —CN, S(═O)pRx, where Rd is Rd is C1-C4-alkyl, —ORx, —NRxRx C1-C3-alkyl-O—C1-C3-alkylC(═O)ORx, —C1-C3-alkyl-COORx; —C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O—C1-C3alkyl)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, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is —O —, —S(═O)—, or —CH2—, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is —(CR8R8′)n-D-(CR8R8′)m-; D is a bond, —NR9—, —O—, —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）n R a的A的环中的碳原子的取代基，其中R a是-C 1 - -O - ， - NR x R x，-NHNR x R x，-NHNHC（-O）OR x，-NR x OH; -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，C 1 -C 4烷基，-NR x R x; -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-COOR x; -C 1 -C 3烷基-OH或C 1 -C 4烷基醚或其酯（OC 烷基）qO-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; R 3 -R 7是说明书中定义的取代基; X是 - （CR 8 R 8 8）n-D-（CR 8 R 8）m - ; D是键，-NR 9 - ， - O - ， - S - ， - S（= O） - 或-S（= O）2 - 其药学上可接受的盐和前药具有作为HIV抗病毒剂的效用。
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公开(公告)号：US07517992B2
公开(公告)日：2009-04-14
申请号：US10526598
申请日：2003-09-05
IPC分类号： C07D401/12 , A61K31/444
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; R1 is O, S; R2 is a nitrogen-containing heterocycle; R3 is H, C1-C3 alkyl; X is —(CR8R8′)n-D-(CR8R8′)m—; D is a bond, —NR9—, —O—, —S—, —S(═O)— or —S(═O)2—; n and m are independently 0, 1 or 2, R8 and R8′ are independently H, C1-C3 alkyl, haloC1-C3alkyl, hydroxy, or R8 and R8′ together with their adjacent C atom is —C(═O)—; R9 is independently H, C1-C3 alkyl; E is CH2—, —CHOH—, —C(═O)—, —NR9—, —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; R10 is an optionally substituted carbocycle or heterocycle; R11 is independently H, C1-C3 alkyl, halo substituted C1-C3alkyl, 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独立地是0,1或2，R 8和R 8'独立地是H，C 1 -C 3烷基，卤代C 1 -C 3烷基，羟基或R 8和R 8'连同它们相邻的C原子是-C（ - ） - 。 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。
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公开(公告)号：US06610714B2
公开(公告)日：2003-08-26
申请号：US10093112
申请日：2002-03-05
申请人： Christer Sahlberg , Dmitry Antonov , Hans Wallberg , Rolf Noréen
发明人： Christer Sahlberg , Dmitry Antonov , Hans Wallberg , Rolf Noréen
IPC分类号： C07D21302
CPC分类号： C07D213/75 , C07D213/85
摘要： Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CR8R9)n— R8 and R9 are independently H, C1-C3 alkyl, OH or R8 and R9 together are ═O 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化合物：其中R 1为O，S; R 2为任选取代的含氮杂环，其中氮位于相对于（硫）脲键的2位; R 3为H，C 1 -C 3烷基 ，R 4 -R 7独立地选自H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6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，C 1 -C 6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，氰基-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 - （CR8R9）n-R8和R9独立地是H，C1-C3烷基，OH或R8和R9一起= On是1,2或3，前药和药学上可接受的 其盐可用作HIV-1逆转录酶的抑制剂，特别是药物逃避突变体。
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公开(公告)号：US20080200503A1
公开(公告)日：2008-08-21
申请号：US11995888
申请日：2006-07-27
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Mats Stefan Lindstrom , Pia Cecilia Kahnberg , Dmitry Antonov , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Mats Stefan Lindstrom , Pia Cecilia Kahnberg , Dmitry Antonov , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist
IPC分类号： A61K31/4709 , C07D401/14
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。 和其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为氢或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。
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公开(公告)号：US20110237621A1
公开(公告)日：2011-09-29
申请号：US13109395
申请日：2011-05-17
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Dmitry Antonov
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Abdellah Tahri , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Dmitry Antonov
IPC分类号： A61K31/4725 , C07D498/04 , C07D401/12 , A61K31/4709 , A61P31/14
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; R1 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—C1-4alkanediyl-, —O—C(═O)—, —O—C(═O)—NR4a— or —O—C(═O)—NR4aC1-4 alkanediyl-; R2 is hydrogen, —OR5, —C(═O)OR5, —C(═O)R6, —C(═O)NR4aR4b, —C(═O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and where X is C or CH, R3 may also be C1-6alkyl; 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.
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公开(公告)号：US07666834B2
公开(公告)日：2010-02-23
申请号：US11995827
申请日：2006-07-28
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Carl Erik Daniel Jönsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Dmitry Antonov , Lourdes Salvador Odén , Susana Ayesa Alvarez , Björn Olof Classon
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Carl Erik Daniel Jönsson , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Dmitry Antonov , Lourdes Salvador Odén , Susana Ayesa Alvarez , Björn Olof Classon
IPC分类号： A61K38/00
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.
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; R1是-OR6，-NH-SO2R7; R2是氢，并且其中X是C或CH，R2也可以是C1-6烷基; R 3是氢，C 1-6烷基，C 1-6烷氧基C 1-6烷基或C 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 1-6烷氧基，C 1-6烷氧基C 1-6烷基，C 1-6烷基羰基，C 1-6烷氧基羰基，氨基，叠氮基，巯基， C 1-6烷硫基，多卤代C 1-6烷基，芳基或Het; W是芳基或Het; R6为氢; 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; R7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元饱和的，部分不饱和的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。
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公开(公告)号：US08754105B2
公开(公告)日：2014-06-17
申请号：US13109395
申请日：2011-05-17
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Rabiosson , Abdellah Tahri , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Dmitry Antonov
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Rabiosson , Abdellah Tahri , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Dmitry Antonov
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; R1 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—C1-4alkanediyl-, —O—C(═O)—, —O—C(═O)—NR4a— or —O—C(═O)—NR4aC1-4 alkanediyl-; R2 is hydrogen, —OR5, —C(═O)OR5, —C(═O)R6, —C(═O)NR4aR4b, —C(═O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and where X is C or CH, R3 may also be C1-6alkyl; 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.
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公开(公告)号：US08383584B2
公开(公告)日：2013-02-26
申请号：US12526085
申请日：2008-02-08
申请人： Dmitry Antonov , Susana Ayesa Alvarez , Anna Karin Gertrud Linnea Belfrage , Carl Erik Daniel Jönsson , David Craig McGowan , Karl Magnus Nilsson , Pierre Jean-Marie Bernard Raboisson , Åsa Annica Kristina Rosenquist , Bengt Bertil Samuelsson
发明人： Dmitry Antonov , Susana Ayesa Alvarez , Anna Karin Gertrud Linnea Belfrage , Carl Erik Daniel Jönsson , David Craig McGowan , Karl Magnus Nilsson , Pierre Jean-Marie Bernard Raboisson , Åsa Annica Kristina Rosenquist , Bengt Bertil Samuelsson
CPC分类号： C07D245/04 , C07D255/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D498/04 , C07D498/14
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; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
摘要翻译： 式I化合物：包括其立体异构体或N-氧化物，药学上可接受的加成盐或其药学上可接受的加成溶剂合物; 用作HCV抑制剂; 制备这些化合物的方法以及包含这些化合物作为活性成分的药物组合物。
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