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1. 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.

2. 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.

3. 发明申请

US20070265295A1 1-Heterocyclyl-1,5-Dihydro-Pyrido[3,2-B]Indol-2-Ones 失效
标题翻译： 1-杂环基-1,5-二氢吡啶并[3,2-B]吲哚-2-基
公开(公告)号：US20070265295A1
公开(公告)日：2007-11-15
申请号：US11568845
申请日：2005-05-17
申请人： Bart Kesteleyn , Pierre Jean-Marie Raboisson , Dominique Surleraux , Geerwin Hache , Sandrine Vendeville , Piet Tom Wigerinck , Annick Peeters
发明人： Bart Kesteleyn , Pierre Jean-Marie Raboisson , Dominique Surleraux , Geerwin Hache , Sandrine Vendeville , Piet Tom Wigerinck , Annick Peeters
IPC分类号： A61K31/437 , A61P31/18 , C07D471/04
CPC分类号： C07D471/04
摘要： 1-heterocyclyl-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 a monocyclic or bicyclic aromatic heterocyclic ring system that can be substituted.
摘要翻译：式（I）的1-杂环基-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为1,2或3; R 1是氢，氰基，卤素，取代的羰基，甲亚胺酰氨基，N-羟基 - 甲亚氨基亚氨基，单或二（C 1-4烷基）甲亚氨基酰胺基，Het _{1 或Het <2>; X是NR 2，O，S，SO，SO 2; R 2是氢，C 1-10烷基，C 2-10链烯基，C 3-7环烷基，其任选被取代; R 2是被-COOR 4取代的芳基; 或R 2是：<？in-line-formula description =“In-line Formulas”end =“lead”？> - C H 2 p < （b-3）-C（CH 2） - C q H 2 ; -CH 2 CH 2 -CH 2 - （O-CH 2 -CH 2）m - （b-4）; -CH 2 CH 2 -CH 2 - （O-CH 2 -CH 2）m - （b-5）;（b-5）; <？in-line-formula description =“In-line Formulas”end =“tail”？> -a ^{1 = < CH 2 -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; R 3是可被取代的单环或双环芳族杂环体系。}}

4. 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。

5. 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。

6. 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。

7. 发明申请

US20070155716A1 HCV INHIBITING BI-CYCLIC PYRIMIDINES 有权
标题翻译： HCV抑制双循环嘧啶
公开(公告)号：US20070155716A1
公开(公告)日：2007-07-05
申请号：US11684288
申请日：2007-03-09
申请人： Kenneth SIMMEN , Tse-I Lin , Oliver Lenz , Dominique Louis Surleraux , Pierre Jean-Marie Raboisson
发明人： Kenneth SIMMEN , Tse-I Lin , Oliver Lenz , Dominique Louis Surleraux , Pierre Jean-Marie Raboisson
IPC分类号： A61K31/55 , A61K31/519 , A61K31/541 , A61K31/5377
CPC分类号： A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , A61K31/5377 , Y02A50/385 , Y02A50/387
摘要： The present invention relates to the use of bi-cyclic pyrimidines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to processes for preparation of such pharmaceutical compositions. The present invention also concerns combinations of the present bi-cyclic pyrimidines with other anti-HCV agents.
摘要翻译：本发明涉及双环嘧啶作为HCV复制抑制剂的用途，以及它们在旨在治疗或对抗HCV感染的药物组合物中的用途。此外，本发明涉及这种药物组合物的制备方法。本发明还涉及本发明的双环嘧啶与其它抗HCV药物的组合。

8. 发明申请

US20090062311A1 MACROCYLIC INHIBITORS OF HEPATITIS C VIRUS 有权
标题翻译： HEPATITIS C病毒的大肠抑制剂
公开(公告)号：US20090062311A1
公开(公告)日：2009-03-05
申请号：US11995835
申请日：2008-01-16
申请人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Raboisson , Lili Hu , Dominique Louis Surleraux , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Lourdes Salvador Oden
发明人： Kenneth Alan Simmen , Herman Augustinus De Kock , Pierre Jean-Marie Raboisson , Lili Hu , Dominique Louis Surleraux , Karl Magnus Nilsson , Bengt Bertil Samuelsson , Asa Annica Kristina Rosenquist , Lourdes Salvador Oden
IPC分类号： A61K31/517 , C07D255/04 , C07D245/04 , A61P31/12 , A61K31/4709
CPC分类号： C07D487/04 , C07D245/04 , C07K5/06139
摘要： Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1a and R1b are hydrogen, C3-7cycloalkyl, aryl, Het, C1-6alkoxy, C1-6alkyl optionally substituted with halo, C1-6alkoxy, cyano, polyhaloC1-6alkoxy, C3-7cycloalkyl, aryl, or with Het; or R1a and R1b together with the nitrogen to which they are attached form a 4 to 6 membered heterocyclic ring which 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, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl, amino, mono- or diC1-6alkylamino; R4 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 O, S and N, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted; 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; and Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S, being optionally condensed with a benzene ring, and wherein Het may be optionally substituted with one, two or three substituents; 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N-氧化物，盐和立体异构体，其中每个虚线表示任选的双键; X为N，CH，X为双键，为C; R 1a和R 1b是氢，C 3-7环烷基，芳基，Het，C 1-6烷氧基，任选被卤素，C 1-6烷氧基，氰基，多卤代C 1-6烷氧基，C 3-7环烷基，芳基或与Het取代的C 1-6烷基; 或R 1a和R 1b与它们所连接的氮一起形成可任选被取代的4至6元杂环; 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，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，C 3-7环烷基，氨基，单或二C 1-6烷基氨基; R4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，以及任选地一至三个选自O，S和N的杂原子，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被取代; 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; 并且Het是含有1至4个选自N，O和S的杂原子的5或6元饱和的，部分不饱和的或完全不饱和的杂环，任选地与苯环稠合，并且其中Het可以任选被一个，两个或三个取代基; 含有化合物（I）的药物组合物和制备化合物（I）的方法。

9. 发明授权

US08481510B2 Uracyl spirooxetane nucleosides 有权
标题翻译：尿嘧啶螺吡啶核苷
公开(公告)号：US08481510B2
公开(公告)日：2013-07-09
申请号：US13319735
申请日：2010-05-11
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Raboisson , Koen Vandyck , Steven Maurice Van Hoof , Lili Hu , Abdellah Tahri
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Raboisson , Koen Vandyck , Steven Maurice Van Hoof , Lili Hu , Abdellah Tahri
IPC分类号： A01N43/04 , A61K31/70 , C07H1/00
CPC分类号： C07H19/10 , C07D493/10 , C07H15/04 , C07H15/18 , C07H19/067
摘要： Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8′ are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8′ form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.
摘要翻译：式I化合物：包括其任何可能的立体异构体，其中：R4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 4为R 7为任选取代的苯基，任选取代的萘基或任选取代的吲哚基; R8和R8'是氢，C1-C6烷基，苄基或苯基; 或R 8和R 8'形成C 3 -C 7环烷基; R 9为C 1 -C 10烷基，C 3 -C 7环烷基，苯基或苯基-C 1 -C 6烷基，其中苯基或苯基-C 1 -C 6烷基中的苯基部分任选被取代; 或其药学上可接受的盐或溶剂化物; 药物制剂和化合物I用作HCV抑制剂。

10. 发明申请

US20120065156A1 Uracyl Spirooxetane Nucleosides 有权
标题翻译：尿嘧啶螺吡喃核苷
公开(公告)号：US20120065156A1
公开(公告)日：2012-03-15
申请号：US13319735
申请日：2010-05-11
申请人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Raboisson , Koen Vandyck , Steven Maurice Van Hoof , Lili Hu , Abdellah Tahri
发明人： Tim Hugo Maria Jonckers , Pierre Jean-Marie Raboisson , Koen Vandyck , Steven Maurice Van Hoof , Lili Hu , Abdellah Tahri
IPC分类号： A61K31/7072 , A61P31/12 , A61P31/14 , C07H19/06 , C07H19/10
CPC分类号： C07H19/10 , C07D493/10 , C07H15/04 , C07H15/18 , C07H19/067
摘要： Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8′ are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8′ form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.
摘要翻译：式I化合物：包括其任何可能的立体异构体，其中：R4是单磷酸酯，二磷酸酯或三磷酸酯; 或R 4为R 7为任选取代的苯基，任选取代的萘基或任选取代的吲哚基; R8和R8'是氢，C1-C6烷基，苄基或苯基; 或R 8和R 8'形成C 3 -C 7环烷基; R 9为C 1 -C 10烷基，C 3 -C 7环烷基，苯基或苯基-C 1 -C 6烷基，其中苯基或苯基-C 1 -C 6烷基中的苯基部分任选被取代; 或其药学上可接受的盐或溶剂化物; 药物制剂和化合物I用作HCV抑制剂。

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