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1.发明授权PROCESS FOR THE PREPARATION OF (3R,3AS,6AR)-HEXAHYDROFURO [2,3-B] FURAN-3-YL (1S,2R)-3-[[(4-AMINOPHENYL) SULFONYL] (ISOBUTYL) AMINO]-1-BENZYL-2-HYDROXYPROPYLCARBAMATE 有权工艺用于制备（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2-HYDROXYPROPYLCARBAMIDSÄURE-（3R，3AS，6AR）六氢呋喃并[2,3-B ]呋喃-3-基酯
公开(公告)号：EP1725566B1
公开(公告)日：2009-06-17
申请号：EP04805020.7
申请日：2004-12-23
发明人： GOYVAERTS, Nicolaas, Martha, Felix , WIGERINCK, Piet, Tom, Bert, Paul , ZINSER, Hartmut, Burghard , EBERT, Birgit, M.
IPC分类号： C07D493/04
CPC分类号： C07D493/04
摘要： The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate as well as intermediates for use in said process. More in particular the invention relates to processes for the preparation of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate which make use of 4-amino-N ((2R,3S)-3-amino-2-hydroxy-4-phenylbutyl)-N-(isobutyl)benzene sulfonamide intermediate, and to processes amenable to industrial scaling up. (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as HIV protease inhibitors.
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2.发明授权HEXAHYDROFURO¬2,3-B FURAN-3-YL-N- 3-¬(1,3-BENZODIOXOL-5-YLSULFONYL)(ISOBUTYL)AMINO -1-BENZYL-2-HYDROXYPROPYL CARBAMATE AS RETROVIRAL PROTEASE INHIBITOR 有权（1,3-苯并二氧戊环-5-基硫烷基）（异丁基）氨基-1-苄基-2-羟基丙基氨基甲酸酯作为逆转录病毒蛋白酶抑制剂
公开(公告)号：EP1222192B8
公开(公告)日：2008-10-01
申请号：EP00966144.8
申请日：2000-10-06
IPC分类号： C07D493/04 , A61K31/34 , A61K31/36 , A61P31/12
CPC分类号： C07D493/04
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3.发明公开6,7,8,9-SUBSTITUTED 1-PHENYL-1,5-DIHYDRO-PYRIDO(3,2-B)INDOL-2-ONES USEFUL AS ANTI-INFECTIVE PHARMACEUTICAL AGENTS 有权取代的1-苯基-1,5-二氢 - 吡啶并[3,2-b]吲哚-2-酮作为药物抗感染药有用的衍生物
公开(公告)号：EP1751156A1
公开(公告)日：2007-02-14
申请号：EP05747918.0
申请日：2005-05-17
发明人： KESTELEYN, Bart, Rudolf, Romanie , VENDEVILLE, Sandrine, Marie, Helene , KINDERMANS, Natalie, Maria, Francisca , SURLERAUX, Dominique, Louis, Nestor, Ghislain , RABOISSON, Pierre Jean-Marie, Bernard , WIGERINCK, Piet, Tom, Bert, Paul , PEETERS, Annick Ann
IPC分类号： C07D471/04 , C07D519/00 , A61K31/475 , A61K31/4741 , A61P31/18
CPC分类号： C07D471/04
摘要： This invention concerns the compounds (I); the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein X is NR2, O, S, SO, SO2; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; n is 1, 2 or 3; R2 is hydrogen, aryl substituted with a radical -COOR4; or R2 is substituted C1-10alkyl, C2-10alkenyl or C3-7cycloalkyl; or R2 is a radical of formula: (b-1); (b-2); -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- (c-5); wherein one of the hydrogen atoms in (c-1) - (c-5) is replaced by particular radicals; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, substituted carbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy- methanimidamidyl or Het1.
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4.发明公开5-SUBSTITUTED 1-PHENYL-1,5-DIHYDRO-PYRIDO[3,2-B] INDOL-2-ONES AND ANALOGS AS ANTI-VIRALS 审中-公开5-取代的1-苯基-1,5-二氢 - 吡啶并[3,2-b]吲哚-2-酮及其类似物作为抗病毒剂的
公开(公告)号：EP1751154A1
公开(公告)日：2007-02-14
申请号：EP05742818.7
申请日：2005-05-17
发明人： KESTELEYN, Bart Rudolf Romanie , CANARD, Maxime Francis Jean-Marie Ghislain , VAN DE VREKEN, Wim , RABOISSON, Pierre Jean-Marie Bernard , SURLERAUX, Dominique, Louis, Nestor, Ghislain , WIGERINCK, Piet, Tom, Bert, Paul
IPC分类号： C07D471/04 , A61K31/437 , A61P31/12
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)-NR 5cR5d, -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-NR17aR 17b; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, a carbonyl derivative, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1.
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5.发明公开PROCESS FOR THE PREPARATION OF (3R,3AS,6AR)-HEXAHYDROFURO [2,3-B] FURAN-3-YL (1S,2R)-3-[[(4-AMINOPHENYL) SULFONYL] (ISOBUTYL) AMINO]-1-BENZYL-2-HYDROXYPROPYLCARBAMATE 有权工艺用于制备（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2-HYDROXYPROPYLCARBAMIDSÄURE-（3R，3AS，6AR）六氢呋喃并[2,3-B ]呋喃-3-基酯
公开(公告)号：EP1725566A1
公开(公告)日：2006-11-29
申请号：EP04805020.7
申请日：2004-12-23
发明人： GOYVAERTS, Nicolaas, Martha, Felix , WIGERINCK, Piet, Tom, Bert, Paul , ZINSER, Hartmut, Burghard , EBERT, Birgit, M.
IPC分类号： C07D493/04
CPC分类号： C07D493/04
摘要： The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate as well as intermediates for use in said process. More in particular the invention relates to processes for the preparation of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate which make use of 4-amino-N ((2R,3S)-3-amino-2-hydroxy-4-phenylbutyl)-N-(isobutyl)benzene sulfonamide intermediate, and to processes amenable to industrial scaling up. (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as HIV protease inhibitors.
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公开(公告)号：EP1667675A1
公开(公告)日：2006-06-14
申请号：EP04766768.8
申请日：2004-09-10
发明人： VAN ACKER, Koenraad, Lodewijk, August , WIGERINCK, Piet, Tom, Bert, Paul , MICHIELS, Lieve, Emma, Jan , TAHRI, Abdellah
IPC分类号： A61K31/34 , A61K31/472 , C07D307/68 , C07D217/02 , C07D403/14 , C07D207/06 , C07D215/24
CPC分类号： C07C233/29 , C07C233/73 , C07C233/75 , C07C235/16 , C07C235/24 , C07C235/56 , C07C237/04 , C07C311/21 , C07C311/29 , C07D207/06 , C07D215/08 , C07D217/02 , C07D217/06 , C07D295/13 , C07D295/15 , C07D307/68 , C07D317/68 , C07D405/12 , C07D405/14
摘要： The present invention relates to small molecules as entry inhibitors of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present entry inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS. The compounds of formula (I) have the following structure: (I).
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7.发明授权HEXAHYDROFURO¬2,3-B FURAN-3-YL-N- 3-¬(1,3-BENZODIOXOL-5-YLSULFONYL)(ISOBUTYL)AMINO -1-BENZYL-2-HYDROXYPROPYL CARBAMATE AS RETROVIRAL PROTEASE INHIBITOR 有权六氢呋喃并[2,3-b]呋喃-3-基-L-N-3-（1,3-苯并二氧杂环戊烯-5-基磺酰基）（异丁基）氨基] - 苯甲酰基-2-羟基丙酸甲酯ALS RETROVIRUSPROTEASEHEMMER
公开(公告)号：EP1222192B1
公开(公告)日：2008-06-18
申请号：EP00966144.8
申请日：2000-10-06
IPC分类号： C07D493/04 , A61K31/34 , A61K31/36 , A61P31/12
CPC分类号： C07D493/04
摘要： The present invention relates to novel bis-tetrahydrofuran benzodioxolyl sulfonamide compounds which are surprisingly effective protease inhibitors. The invention also relates to pharmaceutical compositions, methods of inhibiting retrovirus proteases, in particular multidrug resistant retrovirus proteases, methods of treating or combating infection or disease associated with retrovirus infection in a mammal, and methods of inhibiting viral replication.
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公开(公告)号：EP1848816A1
公开(公告)日：2007-10-31
申请号：EP06708054.9
申请日：2006-02-06
IPC分类号： C12Q1/48
CPC分类号： C12Q1/48
摘要： The present invention is directed to methods for identifying a specific class of inhibitors of HIV reverse transcriptase that act differently from known reverse transcriptase inhibitors. In particular, the invention is based on identifying inhibitors which have higher inhibitory activity in presence of a nucleoside triphosphate or pyrophosphate .
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公开(公告)号：EP1751165A1
公开(公告)日：2007-02-14
申请号：EP05752659.2
申请日：2005-05-17
发明人： KESTELEYN, Bart, Rudolf, Romanie , VAN DE VREKEN, Wim , SURLERAUX, Dominique, Louis, Nestor, Ghislain , VENDEVILLE, Sandrine, Marie, Helene , RABOISSON, Pierre, Jean-Marie, Bernard , WIGERINCK, Piet, Tom, Bert, Paul , PEETERS, Annick, Ann
IPC分类号： C07D491/04 , C07D491/14 , C07D471/04 , A61K31/4355 , A61K31/437 , A61K31/4353 , A61P31/18 , C07D307/00 , C07D221/00
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-hydroxymethanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; X is NR 2, O, S, SO, SO2; R2 is hydrogen, C 1-10alkyl, C2-10alkenyl, C 3-7cycloalkyl, which are optionally substituted; R2 is aryl substituted with -COOR4 ; or R2 is: (b-1); (b-2); -CpH2p-CH(OR14 )-CqH 2q-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 obtionally 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, C1-6alkylcarbonylo xy, -C(=O)-NR13R14; C1-6alkyloxy, arylC1-6alkyloxy, polyhaloC1-6alkyloxy, amino, mono or di(C1-6alkyl)amino, formylamino, C1-6alkylcarbonylamino, C1-6alkylsulfo nylamino, mercapto, C1-6alkylthio, arylthio, aryloxy, arylC1-6alkylthio, C1-6alkylsulfynyl, C1-6alkylsulfo nyl, aryl, arylamino, Het1, Het2.
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10.发明公开HEXAHYDROFURO[2,3-B]FURAN-3-YL-N- 3-[(1,3-BENZODIOXOL-5-YLSULFONYL)(ISOBUTYL)AMINO]-1-BENZYL-2-HYDROXYPROPYL CARBAMATE AS RETROVIRAL PROTEASE INHIBITOR 有权HEXAHYDROFURO¬2,3-B呋喃-3- YL-N- 3-¬（1,3-苯并二氧戊环-5-基磺酰基）（异丁基）氨基-1-苄基-2-羟基丙基氨基甲酸叔丁酯作为逆转录病毒蛋白酶抑制剂
公开(公告)号：EP1222192A1
公开(公告)日：2002-07-17
申请号：EP00966144.8
申请日：2000-10-06
IPC分类号： C07D493/04 , A61K31/34 , A61K31/36 , A61P31/12
CPC分类号： C07D493/04
摘要： The present invention relates to novel bis-tetrahydrofuran benzodioxolyl sulfonamide compounds which are surprisingly effective protease inhibitors. The invention also relates to pharmaceutical compositions, methods of inhibiting retrovirus proteases, in particular multidrug resistant retrovirus proteases, methods of treating or combating infection or disease associated with retrovirus infection in a mammal, and methods of inhibiting viral replication.
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