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1. 发明授权

US07615639B2 1-pyridyl-benzofuro[3,2-b]pyridin-2(1H)-ones 失效
标题翻译： 1-吡啶基 - 苯并呋喃并[3,2-b]吡啶-2（1H） - 酮
公开(公告)号：US07615639B2
公开(公告)日：2009-11-10
申请号：US11568845
申请日：2005-05-17
申请人： Bart Rudolf Romanie Kesteleyn , Pierre Jean-Marie Bernard Raboisson , Dominique Louis Nestor Surleraux , Geerwin Yvonne Paul Haché , Sandrine Marie Helene Vendeville , Piet Tom Bert Paul Wigerinck , Annick Ann Peeters
发明人： Bart Rudolf Romanie Kesteleyn , Pierre Jean-Marie Bernard Raboisson , Dominique Louis Nestor Surleraux , Geerwin Yvonne Paul Haché , Sandrine Marie Helene Vendeville , Piet Tom Bert Paul Wigerinck , Annick Ann Peeters
IPC分类号： C07D471/00
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是可被取代的单环或双环芳族杂环体系。

2. 发明授权

US07994187B2 HIV inhibiting 3,4-dihydro-imidazo[4,5-B]pyridin-5-ones 失效
公开(公告)号：US07994187B2
公开(公告)日：2011-08-09
申请号：US12295816
申请日：2007-04-03
申请人： Bart Rudolf Romanie Kesteleyn , Wim Bert Griet Schepens
发明人： Bart Rudolf Romanie Kesteleyn , Wim Bert Griet Schepens
IPC分类号： A61K31/4745 , C07D471/14
CPC分类号： C07D513/14 , C07D471/14
摘要： HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole, triazole, tetrazole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, and thiadiazole; R1 is halo, cyano, nitro, C1-6alkyl, polyhaloC1-6alkyl, —C1-6alkyl-OR4, —C(═O)—R5, —C(═O)—OR4, —C(═O)—NR6R7, —OR4, —O—C(═O)—C1-6alkyl, —O—C1-6alkyl-OR4, —O—C1-6alkyl-NR6R7, —O—C1-6alkyl-O—C(═O)—C1-6alkyl, —O—C1-6alkyl-C(═O)—OR4, —O—C1-6alkyl-C(═O)—NR6R7, —NR6R7, —NR8—C(═O)—R5, —NR8—C(═O)—OR4, —NR8—C(═O)—NR6R7, —NR8—C(═O)—C1-6alkyl-C(═O)—OR4, —NR8—C1-6alkyl-OR4, —NR8—C1-6alkyl-NR6R7, —NR8—C1-6alkyl-imidazolyl, —NR8—SO2R9, —N═CH—NR6R7, —NH—C(═NH)—NH2, —SO2NR6R7, and —O—PO(OR8)2; D forms pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, imidazole, pyrazole, furane, oxazole, isoxazole, thiophene, thiazole, and isothiazole; R2 is C1-6alkyl, polyhaloC1-6alkyl, halo, cyano, —COOR4, —OR4, and —NR6R7; R3 is phenyl, pyridyl, pyrimidinyl, imidazopyridyl, pyrazolopyridyl, triazolopyridyl, quinoline, imidazopyrimidinyl, pyrazolopyrimidinyl, triazolopyrimidinyl, pyridopyrimidinyl; which may optionally be substituted; m is 0, 1, 2 or 3; n is 0, 1, 2 or 3; pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.

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

US20090170855A1 HIV INHIBITING 3,4-DIHYDRO-IMIDAZO[4,5-B]PYRIDIN-5-ONES 失效
标题翻译： HIV抑制3,4-二氢-1H-咪唑并[4,5-B]吡啶-5-ONES
公开(公告)号：US20090170855A1
公开(公告)日：2009-07-02
申请号：US12295816
申请日：2007-04-03
申请人： Bart Rudolf Romanie Kesteleyn , Wim Bert Griet Schepens
发明人： Bart Rudolf Romanie Kesteleyn , Wim Bert Griet Schepens
IPC分类号： A61K31/5025 , C07D471/22 , A61P31/18 , A61K31/4375
CPC分类号： C07D513/14 , C07D471/14
摘要： HIV inhibitory compounds of formula: salts, hydrates, solvates, N-oxides, or stereoisomers thereof, wherein A forms pyridine, pyrimidine, pyrazine, pyridazine, triazine, imidazole, pyrazole, triazole, tetrazole, oxazole, isoxazole, oxadiazole, thiazole, isothiazole, and thiadiazole; R1 is halo, cyano, nitro, C1-6alkyl, polyhaloC1-6alkyl, —C1-6alkyl-OR4, —C(═O)—R5, —C(═O)—OR4, —C(═O)—NR6R7, —OR4, —O—C(═O)—C1-6alkyl, —O—C1-6alkyl-OR4, —O—C1-6alkyl-NR6R7, —O—C1-6alkyl-O—C(═O)—C1-6alkyl, —O—C1-6alkyl-C(═O)—OR4, —O—C1-6alkyl-C(═O)—NR6R7, —NR6R7, —NR8—C(═O)—R5, —NR8—C(═O)—OR4, —NR8—C(═O)—NR6R7, —NR8—C(═O)—C1-6alkyl-C(═O)—OR4, —NR8—C1-6alkyl-OR4, —NR8—C1-6alkyl-NR6R7, —NR8—C1-6alkyl-imidazolyl, —NR8—SO2R9, —N═CH—NR6R7, —NH—C(═NH)—NH2, —SO2NR6R7, and —O—PO(OR8)2; D forms pyridine, pyrimidine, pyrazine, pyridazine, pyrrole, imidazole, pyrazole, furane, oxazole, isoxazole, thiophene, thiazole, and isothiazole; R2 is C1-C6alkyl, polyhaloC1-C6alkyl, halo, cyano, —COOR4, —OR4, and —NR6R7; R3 is phenyl, pyridyl, pyrimidinyl, imidazopyridyl, pyrazolopyridyl, triazolopyridyl, quinoline, imidazopyrimidinyl, pyrazolopyrimidinyl, triazolopyrimidinyl, pyridopyrimidinyl; which may optionally be substituted; m is 0, 1, 2 or 3; n is 0, 1, 2 or 3; pharmaceutical compositions containing these compounds, methods for preparing these compounds and compositions.
摘要翻译：其中A形成吡啶，嘧啶，吡嗪，哒嗪，三嗪，咪唑，吡唑，三唑，四唑，恶唑，异恶唑，恶二唑，噻唑，异噻唑和噻二唑; R 1是卤素，氰基，硝基，C 1-6烷基，多卤代C 1-6烷基，-C 1-6烷基-OR 4，-C（-O）-R 5，-C（-O）-OR 4，-C（ - ） - NR 6 R 7， -OR4，-OC（-O）-C 1-6烷基，-O-C 1-6烷基-OR 4，-O-C 1-6烷基-NR 6 R 7，-O-C 1-6烷基-C 0（-O）-C 1-6烷基， - O-C 1-6烷基-C（-O）-OR 4，-O-C 1-6烷基-C（-O）-NR 6 R 7，-NR 6 R 7，-NR 8 -C（-O）-R 5，-NR 8 -C（-O ）-OR4，-NR8-C（-O）-NR6R7，-NR8-C（-O）-C 1-6烷基-C（ - ） - OR4，-NR8-C1-6烷基-OR4，-NR8-C1- 烷基-NR6R7，-NR8-C1-6烷基 - 咪唑基，-NR8-SO2R9，-N-CH-NR6R7，-NH-C（-NH）-NH2，-SO2NR6R7和-O-PO（OR8）2; D形成吡啶，嘧啶，吡嗪，哒嗪，吡咯，咪唑，吡唑，呋喃，恶唑，异恶唑，噻吩，噻唑和异噻唑; R2是C1-C6烷基，多卤代C 1 -C 6烷基，卤素，氰基，-COOR 4，-OR 4和-NR 6 R 7; 吡唑基，嘧啶基，咪唑并吡啶基，吡唑并吡啶基，三唑并吡啶基，喹啉，咪唑并嘧啶基，吡唑并嘧啶基，三唑并嘧啶基，吡啶并嘧啶基; 其可任选地被取代; m为0,1,2或3; n为0,1,2或3; 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。

6. 发明授权

US08592429B2 5-amino-4-hydroxypentoyl amides 有权
标题翻译： 5-氨基-4-羟基戊酰基酰胺
公开(公告)号：US08592429B2
公开(公告)日：2013-11-26
申请号：US13515187
申请日：2010-12-10
申请人： Genadiy Kalayanov , Bart Rudolf Romanie Kesteleyn , Kevin Parkes , Bengt Bertil Samuelsson , Wim Bert Griet Schepens , Johannes Wilhelmus J. Thuring , Hans Kristian Wallberg , Jörg Kurt Wegner
发明人： Genadiy Kalayanov , Bart Rudolf Romanie Kesteleyn , Kevin Parkes , Bengt Bertil Samuelsson , Wim Bert Griet Schepens , Johannes Wilhelmus J. Thuring , Hans Kristian Wallberg , Jörg Kurt Wegner
IPC分类号： A61K31/18 , A61K31/17 , A61K31/325 , A61K31/38 , A61K31/42 , A61K31/44 , A61K31/495
CPC分类号： C07D213/64 , C07D213/74 , C07D277/30 , C07D401/12 , C07D405/12 , C07D417/12 , C07D493/04
摘要： HIV inhibitors of formula (I) wherein R1 is halo, C1-4 alkoxy, trifluoromethoxy; R2 is a group of formula (A); R3 is a group of formula (B); R4 is a group of formula (C); n is 0 or 1; A is CH or N; R5 and R6 are hydrogen, C1-4 allyl, halo; R7 and R8 are C1-4 allyl or C1-4 alkoxy-C1-4 alkyl; R9 is C1-4 allyl, cyclopropyl, trifluoromethyl, C1-4 alkoxy, or dimethylamino; R10 is hydrogen, C1-4 alkyl, cyclopropyl, trifluoromethyl, C1-4 alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.
摘要翻译：式（I）的HIV抑制剂，其中R 1是卤素，C 1-4烷氧基，三氟甲氧基; R2是式（A）的基团; R3是式（B）的基团; R4是式（C）的基团; n为0或1; A是CH或N; R5和R6是氢，C1-4烷基，卤素; R 7和R 8是C 1-4烯丙基或C 1-4烷氧基-C 1-4烷基; R 9为C 1-4烯丙基，环丙基，三氟甲基，C 1-4烷氧基或二甲基氨基; R 10是氢，C 1-4烷基，环丙基，三氟甲基，C 1-4烷氧基或二甲基氨基; 其药学上可接受的加成盐和溶剂合物; 含有这些化合物作为活性成分的药物组合物和制备所述化合物的方法。

7. 发明申请

US20120295920A1 5-AMINO-4-HYDROXYPENTOYL AMIDES 有权
标题翻译： 5-氨基-4-羟基戊酸
公开(公告)号：US20120295920A1
公开(公告)日：2012-11-22
申请号：US13515187
申请日：2010-12-10
申请人： Genadiy Kalayanov , Bart Rudolf Romanie Kesteleyn , Kevin Parkes , Bengt Bertil Samuelsson , Wim Bert Griet Schepens , Johannes Wilhelmus J. Thuring , Hans Kristian Wallberg , Jörg Kurt Wegner
发明人： Genadiy Kalayanov , Bart Rudolf Romanie Kesteleyn , Kevin Parkes , Bengt Bertil Samuelsson , Wim Bert Griet Schepens , Johannes Wilhelmus J. Thuring , Hans Kristian Wallberg , Jörg Kurt Wegner
IPC分类号： A61K31/4433 , C07D213/64 , A61K31/4418 , C07D409/12 , A61K31/4436 , C07D417/12 , A61K31/427 , C07D405/14 , A61K31/4439 , A61K31/497 , A61K31/506 , C07D493/04 , A61K31/443 , A61P31/18 , C07D405/12
CPC分类号： C07D213/64 , C07D213/74 , C07D277/30 , C07D401/12 , C07D405/12 , C07D417/12 , C07D493/04
摘要： HIV inhibitors of formula wherein R1 is halo, C1-4alkoxy, trifluoromethoxy; n is 0 or 1; A is CH or N; R5 and R6 are hydrogen, C1-4alkyl, halo; R7 and R8 are C1-4alkyl or C1-4alkoxyC1-4alkyl; R9 is C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; R10 is hydrogen, C1-4alkyl, cyclopropyl, trifluoromethyl, C1-4alkoxy, or dimethylamino; pharmaceutically acceptable addition salts and solvates thereof; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds.
摘要翻译：下式的HIV抑制剂其中R1是卤素，C1-4烷氧基，三氟甲氧基; n为0或1; A是CH或N; R5和R6是氢，C1-4烷基，卤素; R 7和R 8是C 1-4烷基或C 1-4烷氧基C 1-4烷基; R 9为C 1-4烷基，环丙基，三氟甲基，C 1-4烷氧基或二甲基氨基; R 10是氢，C 1-4烷基，环丙基，三氟甲基，C 1-4烷氧基或二甲基氨基; 其药学上可接受的加成盐和溶剂合物; 含有这些化合物作为活性成分的药物组合物和制备所述化合物的方法。

8. 发明申请

US20100087649A1 QUINOLINONE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：US20100087649A1
公开(公告)日：2010-04-08
申请号：US12442753
申请日：2007-09-28
申请人： Bart Rudolf Romanie Kesteleyn , Dominique Louis Nestor Ghislain Surleraux , Geerwin Yvonne Paul Haché
发明人： Bart Rudolf Romanie Kesteleyn , Dominique Louis Nestor Ghislain Surleraux , Geerwin Yvonne Paul Haché
IPC分类号： C07D471/04 , C07D215/02
CPC分类号： C07D215/54 , C07D221/12 , C07D401/04 , C07D401/12 , C07D409/04 , C07D413/04 , C07D417/04 , C07F9/60 , C07F9/65685
摘要： HIV inhibitory compounds of formula (I) including the stereoisomeric forms thereof, the pharmaceutically acceptable salts, and pharmaceutically acceptable solvates thereof; wherein R1 is cyano; R2 is H, C1-6alkyl, trifluoromethyl, amino, mono- or di-C1-6alkylamino, C1-6alkylamino wherein the C1-6alkyl group can be substituted; X1 is CH or N; R3 is phenyl or pyridyl, each unsubstituted or substituted; R4 is H, C1-6alkyl, (C1-6alkylcarbonylamino)C1-6alkyl-, Ar, potionally substituted thienyl, furanyl, pyridyl, pyrimidyl, pyrazinyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, oxazolyl, thiazolyl, halo, trifluoromethyl, hydroxy, C1-6alkyloxy, —OPO(OH)2, amino, aminocarbonyl, cyano, —Y1—R6, —Y1-Alk-R6, or —Y1-Alk-Y2—R7; R3 is H, halo, hydroxy or C1-6alkyloxy; or R4 and R5 form —O—CH2—O—; Y1 is O or NR8; Y2 is O or NR9; Alk is bivalent C1-6alkyl; R6 is pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, 4-C1-6alkylpiperazinyl, 4-(C1-6alkylcarbonyl)piperazinyl, pyridyl, or imidazolyl; R7 is H, C1-6alkyl, hydroxyC1-6alkyl, C1-6alkylcarbonyl; R8 and R9 are H or C1-6alkyl; Ar is optionally substituted phenyl; pharmaceutical compositions comprising the above compounds (I) as active ingredient.
摘要翻译：包括其立体异构形式的式（I）的HIV抑制化合物，其药学上可接受的盐和药学上可接受的溶剂合物; 其中R1是氰基; R2是H，C1-6烷基，三氟甲基，氨基，单或二C1-6烷基氨基，C1-6烷基氨基，其中C1-6烷基可以被取代; X1是CH或N; R3是苯基或吡啶基，各自未取代或取代; R 4是H，C 1-6烷基，（C 1-6烷基羰基氨基）C 1-6烷基 - ，Ar，有取代的噻吩基，呋喃基，吡啶基，嘧啶基，吡嗪基，吡咯基，吡唑基，咪唑基，三唑基，恶唑基，噻唑基， C1-6烷氧基，-OPO（OH）2，氨基，氨基羰基，氰基，-Y1-R6，-Y1-Alk-R6或-Y1-Alk-Y2-R7; R3是H，卤素，羟基或C1-6烷氧基; 或R 4和R 5形成-O-CH 2 -O-; Y1是O或NR8; Y2为O或NR9; Alk是二价C 1-6烷基; R6是吡咯烷基，哌啶基，吗啉基，哌嗪基，4-C 1-6烷基哌嗪基，4-（C 1-6烷基羰基）哌嗪基，吡啶基或咪唑基; R7是H，C1-6烷基，羟基C1-6烷基，C1-6烷基羰基; R8和R9是H或C1-6烷基; Ar是任选取代的苯基; 包含上述化合物（I）作为活性成分的药物组合物。

9. 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。

10. 发明授权

US07595408B2 Methods for the preparation of (3R,3aS,6aR) hexahydro-furo[2,3-b]furan-3-ol 有权
标题翻译：制备（3R，3aS，6aR）六氢 - 呋喃并[2,3-b]呋喃-3-醇的方法
公开(公告)号：US07595408B2
公开(公告)日：2009-09-29
申请号：US10599497
申请日：2005-03-31
申请人： Peter Jan Leonard Mario Quaedflieg , Bart Rudolf Romanie Kesteleyn , Robert Jan Vijn , Constantinus Simon Maria Liebregts , Jacob Hermanus Matheus Hero Kooistra , Franciscus Alphons Marie Lommen
发明人： Peter Jan Leonard Mario Quaedflieg , Bart Rudolf Romanie Kesteleyn , Robert Jan Vijn , Constantinus Simon Maria Liebregts , Jacob Hermanus Matheus Hero Kooistra , Franciscus Alphons Marie Lommen
IPC分类号： C07D307/93 , C07D493/00
CPC分类号： C07D493/04 , C07D307/20
摘要： The present invention relates to methods for the preparation of diastereomerically pure (3R,3aS,6aR) hexahydro-furo[2,3-b]furan-3-ol as well as a novel intermediate, (3aR,4S,6aS) 4-methoxy-tetrahydro-furo[3,4-b]furan-2-one for use in said methods. More in particular the invention relates to a stereoselective method for the preparation of diastereomerically pure (3R,3aS,6aR) hexahydro-furo[2,3-b]furan-3-ol, as well as methods for the crystallization of (3aR,4S,6aS) 4-methoxy-tetrahydro-furo[3,4-b]furan-2-one and for the epimerization of (3aR,4R,6aS) 4-methoxy-tetrahydro-furo[3,4-b]-furan-2-one to (3aR,4S,6aS) 4-methoxy-tetrahydro-furo[3,4-b]furan-2-one.
摘要翻译：本发明涉及制备非对映体纯的（3R，3aS，6aR）六氢 - 呋喃并[2,3-b]呋喃-3-醇以及新的中间体（3aR，4S，6aS）-4- 甲氧基 - 四氢 - 呋喃并[3,4-b]呋喃-2-酮。更具体地，本发明涉及用于制备非对映体纯（3R，3aS，6aR）六氢 - 呋喃并[2,3-b]呋喃-3-醇的立体选择性方法，以及（3aR， 4S，6aS）4-甲氧基 - 四氢 - 呋喃并[3,4-b]呋喃-2-酮，并用于（3aR，4R，6aS）4-甲氧基 - 四氢 - 呋喃并[3,4-b] 呋喃-2-酮与（3aR，4S，6aS）-4-甲氧基 - 四氢 - 呋喃并[3,4-b]呋喃-2-酮。

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