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    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
    4.
    发明申请
    MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
    丙型肝炎病毒大肠杆菌抑制剂

    公开(公告)号：US20100240698A1

    公开(公告)日：2010-09-23

    申请号：US11995573

    申请日：2006-07-28

    申请人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Sandrine Marie Helene Vendeville ,  Lili Hu ,  Wim Van De Vreken ,  David Craig McGowan ,  Abdellah Tahri ,  Dominique Louis Nestor Ghislain Surleraux

    发明人： Kenneth Alan Simmen ,  Herman Augustinus De Kock ,  Pierre Jean-Marie Bernard Raboisson ,  Sandrine Marie Helene Vendeville ,  Lili Hu ,  Wim Van De Vreken ,  David Craig McGowan ,  Abdellah Tahri ,  Dominique Louis Nestor Ghislain Surleraux

    IPC分类号： A61K31/427 ,  C07D487/04 ,  A61K31/4709 ,  A61K31/4725 ,  A61P31/12

    CPC分类号： C07D487/04 ,  C07K5/06165

    摘要： Inhibitors of HCV of formula al and the N-oxides, salts, and stereochemically isomeric forms thereof, wherein R1 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—C1-4alkanediyl-, —O—CO—, —O—C(═O)—NR5a— or —O—C(═O)—NR5a—C1-4alkanediyl-; R2 is hydrogen, —OR6, —C(═O)OR6, —C(═O)R7, —C(═O)NR5aR5b, —C(═O)NHR5c, —NR5aR5b, —NHR5c, —NHSOpNR5aR5b, —NR5aSOpR8, or —B(OR6)2; R3 and R4 are hydrogen or C1-6alkyl; or R3 and R4 taken together may form a C3-7cycloalkyl 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A1的HCV的抑制剂及其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8至12元双环杂环体系，其含有一个 氮和任选的一至三个氧，硫或氮，其中所述环系可以任选被取代; L是直接键，-O - ， - O-C 1-4烷二基 - ， - O-CO - ， - O-C（= O）-NR 5a - 或-O-C（= O）-NR 5a -C 1-4烷二基 - ; R2是氢，-OR6，-C（= O）OR6，-C（= O）R7，-C（= O）NR5aR5b，-C（= O）NHR5c，-NR5aR5b，-NHR5c，-NHSOpNR5aR5b，-NR5aSOpR8 ，或-B（OR 6）2; R3和R4是氢或C1-6烷基; 或者R 3和R 4一起形成C 3-7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。

    Macrocyclic inhibitors of hepatitis C virus
    5.
    发明授权
    Macrocyclic inhibitors of hepatitis C virus 有权
    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。

    Derivatives of 1-phenyl-benzofuro[3,2]pyridin-2(1H)-one
    10.
    发明授权
    Derivatives of 1-phenyl-benzofuro[3,2]pyridin-2(1H)-one 失效
    1-苯基 - 苯并呋喃并[3,2]吡啶-2（1H） - 酮的衍生物

    公开(公告)号：US07622582B2

    公开(公告)日：2009-11-24

    申请号：US11569108

    申请日：2005-05-17

    申请人： Bart Rudolf Romanie Kesteleyn ,  Wim Van De Vreken ,  Dominique Louis Nestor Ghislain Surleraux ,  Sandrine Marie Helene Vendeville ,  Pierre Jean-Marie Bernard Raboisson ,  Piet Tom Bert Paul Wigerinck ,  Annick Ann Peeters

    发明人： Bart Rudolf Romanie Kesteleyn ,  Wim Van De Vreken ,  Dominique Louis Nestor Ghislain Surleraux ,  Sandrine Marie Helene Vendeville ,  Pierre Jean-Marie Bernard Raboisson ,  Piet Tom Bert Paul Wigerinck ,  Annick Ann Peeters

    IPC分类号： C07D491/00

    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; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; X is NR2, O, S, SO, SO2; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, which are optionally substituted; R2 is aryl substituted with —COOR4; or R2 is: —CpH2p—CH(OR14)—CqH2q—R15 (b-3); —CH2—CH2—(O—CH2—CH2)m—OR14 (b-4); —CH2—CH2—(O—CH2—CH2)m—NR5aR5b (b-5); -a1=a2-a3=a4- 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; R3 is optionally substituted phenyl or a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted; R21 is halo, hydroxy, amino, carboxyl, C1-6alkyl, C3-7cycloalkyl, arylC1-6alkyl, formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy, —C(═O)—NR13R14; C1-6alkyloxy, arylC1-6alkyloxy, polyhaloC1-6alkyloxy, amino, mono or di(C1-6alkyl)amino, formylamino, C1-6alkylcarbonylamino, C1-6alkylsulfonylamino, mercapto, C1-6alkylthio, arylthio, aryloxy, arylC1-6alkylthio, C1-6alkylsulfynyl, C1-6alkylsulfonyl, aryl, arylamino, Het1, Het2.

    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，甲酰亚胺基，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NR2，O，S，SO，SO2; 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; R2是被-COOR4取代的芳基; 或R2是：-CpH2p-CH（OR14）-CqH2q-R15（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 5 a R 5b（b-5）; -a1 = a2-a3 = a4-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; R3是任选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，一或二（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， C 1-6烷基磺酰基，芳基，芳基氨基，Het1，Het2。