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1. 发明授权

US07514427B2 1,5,6,-substituted-2-oxo-3-cyano-1,6a-diaza-tetrahydro-fluoranthenes as anti-inflective agents 失效
标题翻译： 1,5,6， - 取代-2-氧代-3-氰基-1,6a-二氮杂 - 四氢 - 荧蒽作为抗反应剂
公开(公告)号：US07514427B2
公开(公告)日：2009-04-07
申请号：US11722951
申请日：2006-01-10
申请人： Bart Rudolf Romanie Kesteleyn , Pierre Jean-Marie Raboisson , Wim Van De Vreken , Maxime Francis Jean-Marie Ghislain Canard
发明人： Bart Rudolf Romanie Kesteleyn , Pierre Jean-Marie Raboisson , Wim Van De Vreken , Maxime Francis Jean-Marie Ghislain Canard
IPC分类号： C07D498/22 , C07D487/22 , A61K31/5365 , A61K31/4985
CPC分类号： C07D471/16 , C07D498/16
摘要： HIV inhibitory compounds of formula: salts and stereoisomers thereof, wherein R1 and R2 are hydrogen or optionally substituted C1-10alkyl; R3 is n is 1, 2 or 3; R3a is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, aminocarbonyl, C 1-4alkyloxycarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C1-4alkylcarbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het; or R3 is a monocyclic or bicyclic aromatic heterocyclic ring system, wherein one, two, three or four ring members are nitrogen, oxygen and sulfur, and wherein the remaining ring members are carbon atoms; and wherein each of said heterocyclic ring systems may optionally be substituted; X is —NR7—, —O— or —S—; pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.
摘要翻译： HIV抑制化合物：其盐和立体异构体，其中R 1和R 2是氢或任选取代的C 1-10烷基; R3为n为1,2或3; R3a是硝基，氰基，氨基，卤素，羟基，C1-4烷氧基，羟基羰基，氨基羰基，C 1-4烷氧基羰基，一或二（C 1-4烷基）氨基羰基，C 1-4烷基羰基，甲亚氨基甲酰基，单 - 或二（C 1-4烷基）甲酰亚胺酰氨基，N-羟基 - 甲亚胺酰氨基或Het; 或R 3是单环或双环芳族杂环体系，其中一个，两个，三个或四个环成员是氮，氧和硫，其中剩余的环成员是碳原子; 并且其中每个所述杂环体系可任选地被取代; X是-NR 7 - ， - O-或-S-; 含有这些化合物的药物组合物，制备这些化合物和组合物的方法。

2. 发明申请

US20080167296A1 1,5,6,-Substituted-2-Oxo-3-Cyano-1,6a-Diaza-Tetrahydro-Fluoranthenes as Anti-Infective Agents 失效
标题翻译： 1,5,6， - 取代-2-氧代-3-氰基-1,6a-二氮杂 - 四氢 - 氟化物作为抗感染剂
公开(公告)号：US20080167296A1
公开(公告)日：2008-07-10
申请号：US11722951
申请日：2006-01-10
申请人： Bart Rudolf Romanie Kesteleyn , Pierre Jean-Marie Raboisson , Wim Van De Vreken , Maxime Francis Jean-Marie Ghislain Canard
发明人： Bart Rudolf Romanie Kesteleyn , Pierre Jean-Marie Raboisson , Wim Van De Vreken , Maxime Francis Jean-Marie Ghislain Canard
IPC分类号： C07D498/22 , A61K31/5365 , A61K31/4985 , C07D487/22 , A61P31/12
CPC分类号： C07D471/16 , C07D498/16
摘要： HIV inhibitory compounds of formula: salts and stereoisomers thereof, whereinR1 and R2 are hydrogen or optionally substituted C1-10alkyl;R3 is n is 1, 2 or 3;R3a is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, aminocarbonyl, CI 4alkyloxycarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C1-4alkylcarbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het; orR3 is a monocyclic or bicyclic aromatic heterocyclic ring system, wherein one, two, three or four ring members are nitrogen, oxygen and sulfur, and wherein the remaining ring members are carbon atoms; and wherein each of said heterocyclic ring systems may optionally be substituted;X is —NR7—, —0— or —S—;pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.
摘要翻译：下式的HIV抑制化合物：其盐和立体异构体，其中R 1和R 2是氢或任选取代的C 1-10烷基; R 3是n是1,2或3; R 3a是硝基，氰基，氨基，卤素，羟基，C 1-4烷氧基，羟基羰基，氨基羰基，C 1-4烷氧基羰基，或二（C 1-4烷基）氨基羰基，C 1-4烷基羰基，甲亚磺酰氨基，单或二（C 1-4烷基））甲酰亚胺酰氨基，N-羟基 - 甲亚胺酰氨基或Het; 或R 3是单环或双环芳族杂环体系，其中一个，两个，三个或四个环成员是氮，氧和硫，其中剩余的环成员是碳原子; 并且其中每个所述杂环体系可任选地被取代; X是-NR 7 - ， - O-或-S-; 含有这些化合物的药物组合物，制备这些化合物和组合物的方法。

3. 发明授权

US07608726B2 Substituted indolepyridinium as anti-infective compounds 失效
标题翻译：取代的吲哚吡啶作为抗感染性化合物
公开(公告)号：US07608726B2
公开(公告)日：2009-10-27
申请号：US10535007
申请日：2003-11-14
申请人： Bart Rudolf Romanie Kesteleyn , Wim Van De Vreken , Natalie Maria Francisca Kindermans , Maxime Francis Jean-Marie Ghislain Canard , Kurt Hertogs , Eva Bettens , Veronique Corine Paul De Vroey , Dirk Edward Désiré Jochmans
发明人： Bart Rudolf Romanie Kesteleyn , Wim Van De Vreken , Natalie Maria Francisca Kindermans , Maxime Francis Jean-Marie Ghislain Canard , Kurt Hertogs , Eva Bettens , Veronique Corine Paul De Vroey , Dirk Edward Désiré Jochmans
IPC分类号： C07D491/00
CPC分类号： C07D471/04
摘要： The present invention concerns the compounds of formula (I) their N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites, wherein n is 1, 2 or 3; R1is H, CN, halo, aminoC(═O), C(═O)OH, C1-4alkyloxyC(═O), C1-4alkylC(═O), mono- or di(C1-4alkyl)aminoC(═O), arylaminoC(═O), N-(aryl)-N—(C1-4alkyl)aminoC(═O), methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; R2 is H, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, wherein said C1-10alkyl, C2-10alkenyl and C3-7cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxyC(═O), aminoC(═O), C1-4alkyloxyC(═O), mono- or di(C1-4alkyl)aminoC(═O), C1-4alkylC(═O), methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1; for use as a medicine. The invention further relates to a novel subgroup of the compounds of formula (I), and to compositions comprising compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物的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为1,2或3; R 1是H，CN，卤素，氨基C（-O），C（-O）OH，C 1-4烷氧基C（-O），C 1-4烷基C（-O），单或二（C 1-4烷基）氨基C ，芳基氨基C（-O），N-（芳基）-N-（C 1-4烷基）氨基C（O），甲亚氨基甲酰胺基，N-羟基 - 甲亚氨基甲酰胺基，单或二（C 1-4烷基）甲酰亚胺基，Het1或Het2; R 2是H，C 1-10烷基，C 2-10烯基，C 3-7环烷基，其中所述C 1-10烷基，C 2-10烯基和C 3-7环烷基可以任选被取代; R3是硝基，氰基，氨基，卤素，羟基，C1-4烷氧基，羟基C（-O），氨基C（-O），C1-4烷氧基C（-O），单或二（C1-4烷基）氨基C（-O），C 1-4烷基C（-O），甲亚氨基甲酰胺基，单或二（C 1-4烷基）甲亚氨基酰胺基，N-羟基 - 甲亚胺酰氨基或Het1; 用作药物。本发明还涉及式（I）化合物的新亚组和包含式（I）化合物的组合物。

4. 发明申请

US20100048563A1 SUBSTITUTED INDOLEPYRIDINIUM AS ANTI-INFECTIVE COMPOUNDS 审中-公开
标题翻译：替代吲哚美辛作为抗感染性化合物
公开(公告)号：US20100048563A1
公开(公告)日：2010-02-25
申请号：US12547151
申请日：2009-08-25
申请人： Bart Rudolf Romanie KESTELEYN , Wim Van De Vreken , Natalie Maria Francisca Kindermans , Maxime Francis Jean-Marie Ghislain Canard , Kurt Hertogs , Eva Bettens , Veronique Corine Paul De Vroey , Dirk Edward Désiré Jochmans
发明人： Bart Rudolf Romanie KESTELEYN , Wim Van De Vreken , Natalie Maria Francisca Kindermans , Maxime Francis Jean-Marie Ghislain Canard , Kurt Hertogs , Eva Bettens , Veronique Corine Paul De Vroey , Dirk Edward Désiré Jochmans
IPC分类号： A61K31/5377 , A61K31/437 , A61P31/04 , A61P31/12
CPC分类号： C07D471/04
摘要： The present invention concerns the compounds of formula (I) their N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites, wherein n is 1, 2 or 3; R1 is H, CN, halo, aminoC(═O), C(═O)OH, C1-4alkyloxyC(═O), C1-4alkylC(═O), mono- or di(C1-4alkyl)aminoC(═O), arylaminoC(═O), N-(aryl)-N—(C1-4alkyl)aminoC(═O), methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; R2 is H, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, wherein said C1-10alkyl, C2-10alkenyl and C3-7cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxyC(═O), aminoC(═O), C1-4alkyloxyC(═O), mono- or di(C1-4alkyl)aminoC(═O), C1-4alkylC(═O), methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1; for use as a medicine. The invention further relates to a novel subgroup of the compounds of formula (I), and to compositions comprising compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物的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为1,2或3; R 1是H，CN，卤素，氨基C（= O），C（= O）OH，C 1-4烷氧基C（= O），C 1-4烷基C（= O），单或二（C 1-4烷基）氨基C ），芳基氨基C（= O），N-（芳基）-N-（C 1-4烷基）氨基C（= O），甲亚氨基亚氨基，N-羟基 - 甲亚磺酰氨基，单或二（C 1-4烷基）甲酰亚胺基，Het1或Het2; R 2是H，C 1-10烷基，C 2-10烯基，C 3-7环烷基，其中所述C 1-10烷基，C 2-10烯基和C 3-7环烷基可以任选被取代; R3是硝基，氰基，氨基，卤素，羟基，C1-4烷氧基，羟基C（= O），氨基C（= O），C1-4烷氧基C（= O），单或二（C1-4烷基）氨基C（= ，C 1-4烷基C（= O），甲亚氨基酰胺基，单或二（C 1-4烷基）甲亚氨基酰胺基，N-羟基 - 甲酰亚胺基或Het1; 用作药物。本发明还涉及式（I）化合物的新亚组和包含式（I）化合物的组合物。

5. 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。

6. 发明申请

US20070213320A1 4-SUBSTITUTED-1,5-DIHYDRO-PYRIDO[3,2-B]INDOL-2-ONES 失效
公开(公告)号：US20070213320A1
公开(公告)日：2007-09-13
申请号：US11569108
申请日：2005-05-17
申请人： Bart Kesteleyn , Wim Van De Vreken , Dominique Louis Surleraux , Sandrine Vendeville , Pierre Jean-Marie Raboisson , Piet Tom Wigerinck , Annick Peeters
发明人： Bart Kesteleyn , Wim Van De Vreken , Dominique Louis Surleraux , Sandrine Vendeville , Pierre Jean-Marie Raboisson , Piet Tom Wigerinck , Annick Peeters
IPC分类号： A61K31/55 , A61K31/541 , A61K31/5377 , A61K31/506 , A61K31/501 , A61K31/497 , A61K31/496 , A61K31/4745 , C07D498/02 , C07D491/02 , C07D471/02
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.

7. 发明申请

US20100022578A1 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：US20100022578A1
公开(公告)日：2010-01-28
申请号：US12441812
申请日：2007-11-16
申请人： Pierre Jean-Marie Raboisson , Herman Augustinus De Kock , David Craig Mc Gowan , Wim Van De Vreken , Abdellah Tahri , Sandrine Marie Helene Vendeville
发明人： Pierre Jean-Marie Raboisson , Herman Augustinus De Kock , David Craig Mc Gowan , Wim Van De Vreken , Abdellah Tahri , Sandrine Marie Helene Vendeville
IPC分类号： A61K31/4709 , C07D245/04 , A61K31/4741 , A61P31/12
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（由表示可选的双键; X是N，CH，其中X具有双键，它是C; R1是-OR7， -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; R 8是任选取代的C 3-7环烷基取代C 1-6烷基; 任选被C 3-7环烷基取代的C 1-6烷基; 或-NR8aR8b; R8a和R8b是C1-6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。

8. 发明申请

US20070238727A1 5-Substituted 1-Phenyl-1,5-Dihydro-Pyrido[3,2-B]Indol-2-Ones and Analogs as Anti-Virals 审中-公开
公开(公告)号：US20070238727A1
公开(公告)日：2007-10-11
申请号：US11568838
申请日：2005-05-17
申请人： Bart Kesteleyn , Maxime Francis Canard , Wim Van De Vreken , Pierre Jean-Marie Raboisson , Dominique Louis Surleraux , Piet Tom Wigerinck
发明人： Bart Kesteleyn , Maxime Francis Canard , Wim Van De Vreken , Pierre Jean-Marie Raboisson , Dominique Louis Surleraux , Piet Tom Wigerinck
IPC分类号： A61K31/4355 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P31/12 , C07D401/14 , C07D413/14 , C07D417/14 , C07D491/044
CPC分类号： C07D471/04
摘要： Compounds of formula (I) the N-oxides, salts, stereoisomeric forms, prodrugs, esters and metabolites thereof, wherein X is NR2, O, S, SO, SO2; R1 is hydrogen, cyano, halo, a carbonyl derivative, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)-methanimidamidyl, Het1 or Het2; n is 1, 2 or 3; R2 is (i) aryl substituted with a radical —COOR4; (ii) C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, substituted with aryl which is substituted with a radical —COOR4; (iii) C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, substituted with —NR5a—C(═NR5b)—NR5cR5d, —O—NR5a—C(═NR5b)—NR5cR5d, -sulfonyl-R6, —NR7R8, —NR9R10, a radical (a-1), (a-2), (a-3), (a-4), (a-5); or (iv) a radical of formula: (a-6), (b-2), —CpH2p—CH(OR14)—CqH2q—R15; —CH2—CH2—(O—CH2—CH2)m—OR14; —CH2—CH2—(O—CH2—CH2)m—NR17aR17b; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, a carbonyl derivative, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1.

9. 发明申请

US20060173000A1 Substituted indolepyridinium as anti-infective compounds 失效
标题翻译：取代的吲哚吡啶作为抗感染性化合物
公开(公告)号：US20060173000A1
公开(公告)日：2006-08-03
申请号：US10535007
申请日：2003-11-14
申请人： Bart Kesteleyn , Wim Van De Vreken , Natalie Kindermans , Maxime Francis Canard , Kurt Hertogs , Eva Bettens , Veronique Corine De Vroey , Dirk Jochmans
发明人： Bart Kesteleyn , Wim Van De Vreken , Natalie Kindermans , Maxime Francis Canard , Kurt Hertogs , Eva Bettens , Veronique Corine De Vroey , Dirk Jochmans
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/501 , A61K31/53 , A61K31/497 , A61K31/496 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention concerns the compounds of formula (I) their N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites, wherein n is 1, 2 or 3; R1 is H, CN, halo, aminoC(═O), C(═O)OH, C1-4alkyloxyC(═O), C1-4alkylC(═O), mono- or di(C1-4alkyl)aminoC(═O), arylaminoC(═O), N-(aryl)-N—(C1-4alkyl)aminoC(═O), methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het, or Het2; R2 is H, C1-10alkyl, C2-10alkenyl, C3-7cycloalkyl, wherein said C1-10alkyl, C2-10alkenyl and C3-7cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxyC(═O), aminoC(═O), C1-4alkyloxyC(═O), mono- or di(C1-4alkyl)aminoC(═O), C1-4alkylC(═O), methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1; for use as a medicine. The invention further relates to a novel subgroup of the compounds of formula (I), and to compositions comprising compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物的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为1,2或3; R 1是H，CN，卤素，氨基C（-O），C（-O）OH，C 1-4烷氧基C（-O），C 1-4烷基C（-O），单或二（C 1-4烷基）氨基C（-O），芳基氨基C（-O），N-（芳基）-N - （C 1-4烷基）氨基C（-O），甲亚氨基亚氨基，N-羟基 - 甲亚磺酰氨基，一或二（C 1-4烷基）甲酰胺基，Het ，或Het 2; R 2是H，C 1-10烷基，C 2-10链烯基，C 3-7环烷基，其中所述C 1-10烷基，C 2-10链烯基和C 3-7环烷基可以是任选取代的; R 3是硝基，氰基，氨基，卤素，羟基，C 1-4烷氧基，羟基C（-O），氨基C（-O），C 1 -4烷氧基C（-O），单 - 或二（C 1-4烷基）氨基C（-O），C 1-4烷基C（ - 甲氧基亚氨基甲酰胺基或甲基亚氨基甲酰胺基，甲基亚氨基甲酰胺基或甲基亚氨基甲酰胺基; 用作药物。本发明还涉及式（I）化合物的新亚组和包含式（I）化合物的组合物。

10. 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。

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