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1. 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。}}

2. 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.

3. 发明授权

US07659404B2 Broad spectrum 2-(substituted-amino)-benzothiazole sulfonamide HIV protease inhibitors 失效
公开(公告)号：US07659404B2
公开(公告)日：2010-02-09
申请号：US10467609
申请日：2002-02-14
申请人： Dominique Louis Nestor Ghislain Surleraux , Piet Tom Bert Paul Wigerinck , Daniel Getman , Wim Gaston Verschueren , Sandrine Vendeville , Marie-Pierre De Bethune , Jan Octaaf Antoon De Kerpel , Samuel Leo Christiaan Moors , Herman Augustinus De Kock , Marieke Christiane Johanna Voets
发明人： Dominique Louis Nestor Ghislain Surleraux , Piet Tom Bert Paul Wigerinck , Daniel Getman , Wim Gaston Verschueren , Sandrine Vendeville , Marie-Pierre De Bethune , Jan Octaaf Antoon De Kerpel , Samuel Leo Christiaan Moors , Herman Augustinus De Kock , Marieke Christiane Johanna Voets
IPC分类号： A61K31/428 , C07D417/12
CPC分类号： C07D417/12 , C07D277/82
摘要： The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(═O)—, —O—C(═O)—, —NR8—C(═O)—, —O—C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR8—S(═O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C1-4alkyl)aminoC(═O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(═O)—, —C(═S)—, —S(═O)2—, C1-6alkanediyl-C(═O)—, C1-6alkanediyl-C(═S)— or C1-6alkanediyl-S(═O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6alkyloxycarbonylamino or amino; and in case —A— is other than C1-6alkanediyl then R6 may also be C1-6alkyl, Het1C1-4alkyl, Het1OC1-4alkyl, Het2C1-4alkyl, Het2OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R6 may optionally be substituted; R5 and —A—R6 taken together with the nitrogen atom to which they are attached may also form Het1 or Het2. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

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