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1. 发明授权

US08012939B2 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：US08012939B2
公开(公告)日：2011-09-06
申请号：US11995714
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 , Abdellah Tahri , Dominique Louis Nestor Ghislain Surleraux , Wim Van De Vreken , Ismet Dorange , Yvan Simonnet , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Hans Kristian Wallberg
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Sandrine Marie Helene Vendeville , Lili Hu , Abdellah Tahri , Dominique Louis Nestor Ghislain Surleraux , Wim Van De Vreken , Ismet Dorange , Yvan Simonnet , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Hans Kristian Wallberg
IPC分类号： A61K38/05 , C07D245/00
CPC分类号： C07D401/14 , C07D401/12 , C07D417/14 , C07D487/04 , C07K5/06191
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein each variable has specific definitions. Pharmaceutical compositions containing compounds (I) and process for preparing compounds (I) are also provided. 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，盐和立体异构体，其中每个变量具有特定定义。还提供了含有化合物（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。

2. 发明申请

US20090281141A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
标题翻译：丙型肝炎病毒大肠杆菌抑制剂
公开(公告)号：US20090281141A1
公开(公告)日：2009-11-12
申请号：US11995714
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 , Abdellah Tahri , Dominique Louis nestor Ghislain Surleraux , Wim Van De Vreken , Ismet Dorange , Yvan Simonnet , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Hans Kristian Wallberg
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Bernard Raboisson , Sandrine Marie Helene Vendeville , Lili Hu , Abdellah Tahri , Dominique Louis nestor Ghislain Surleraux , Wim Van De Vreken , Ismet Dorange , Yvan Simonnet , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Åsa Annica Kristina Rosenquist , Hans Kristian Wallberg
IPC分类号： A61K31/4709 , C07D245/00 , A61P31/12
CPC分类号： C07D401/14 , C07D401/12 , C07D417/14 , C07D487/04 , C07K5/06191
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein X is N, CH and where X bears a double bond it is C; R1 is —OR1, —NH—SO2R6; 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; R4 is isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halo, polyhaloC1-6alkyl, polyhaloC1-6alkoxy, amino, mono- or diC1-6alkylamino, mono- or diC1-6alkylaminocarbonyl, C1-6alkylcarbonyl-amino, aryl, and Het; n is 3, 4, 5, or 6; each dashed line (represented by - - - - - ) represents an optional double bond; R5 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R6 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; each aryl is phenyl optionally substituted with one, two or three substituents; and each 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, and being 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复制抑制剂及其N-氧化物，盐和立体异构体，其中X为N，CH，X为双键时为C; R1为-OR1，-NH-SO2R6; 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; R 4是任选被一个，两个或三个独立地选自C 1-6烷基，C 1-6烷氧基，羟基，卤素，多卤代C 1-6烷基，多卤代C 1-6烷氧基，氨基，单或二C 1-6烷基氨基，单或二-C 1-6烷基， C 1-6烷基氨基羰基，C 1-6烷基羰基 - 氨基，芳基和Het; n为3,4,5或6; 每个虚线（由 - - - - 表示）表示可选的双键; R5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; R6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; 每个芳基是任选被一个，两个或三个取代基取代的苯基; 并且每个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，并且任选地被一个，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。

3. 发明授权

US07989471B2 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：US07989471B2
公开(公告)日：2011-08-02
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： A61K31/47 , C07D245/00
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 the terms R1, L, R2, R3, R4, and n have specific definitions; pharmaceutical compositions containing compounds of formula (I), and processes for preparing compounds of formula (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，其中术语R1，L，R2，R3，R4和n具有特定的定义; 含有式（I）化合物的药物组合物，以及制备式（I）化合物的方法。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

US20100240698A1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 有权
标题翻译：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。

5. 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。

6. 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。

7. 发明申请

US20080262058A1 Macrocylic Inhibitors of Hepatitis C Virus 有权
标题翻译：丙型肝炎病毒的大胆抑制剂
公开(公告)号：US20080262058A1
公开(公告)日：2008-10-23
申请号：US11995560
申请日：2006-07-28
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： A61K31/41 , C07D487/04 , A61P31/12
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。

8. 发明申请

US20120202859A1 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：US20120202859A1
公开(公告)日：2012-08-09
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： A61K31/41 , A61K31/427 , A61P31/14 , C07D403/08
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。

9. 发明授权

US08183277B2 Macrocylic inhibitors of hepatitis C virus 有权
标题翻译：丙型肝炎病毒的大肠杆菌抑制剂
公开(公告)号：US08183277B2
公开(公告)日：2012-05-22
申请号：US11995560
申请日：2006-07-28
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。

10. 发明授权

US07622582B2 Derivatives of 1-phenyl-benzofuro[3,2]pyridin-2(1H)-one 失效
标题翻译： 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。

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