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1. 发明申请

US20050267156A1 Broadspectrum 2-amino-benzothiazole sulfonamide hiv protease inhibitors 审中-公开
标题翻译： Broadspectrum 2-氨基 - 苯并噻唑磺酰胺hiv蛋白酶抑制剂
公开(公告)号：US20050267156A1
公开(公告)日：2005-12-01
申请号：US10523445
申请日：2003-08-04
申请人： Dominique Louis Surleraux , Piet Tom Wigerinck , Daniel Getman
发明人： Dominique Louis Surleraux , Piet Tom Wigerinck , Daniel Getman
IPC分类号： A61K31/425 , A61K31/428 , A61K31/4439 , A61P31/18 , C07D277/82 , C07D417/12 , C07D493/04
CPC分类号： C07D417/12 , A61K31/425 , C07D277/82 , C07D493/04
摘要： The present invention relates to the use of 2-amino-benzothiazoles, having the formula wherein R1 is hexahydrofuro[2,3-b]furanyl, tetrahydrofuranyl, oxazolyl, thiazolyl, pyridinyl, or phenyl optionally substituted with one or more substituents independently selected from C1-6alkyl, hydroxy, amino, halogen, aminoC1-4alkyl and mono- or di(C1-4alkyl)amino; R2 is hydrogen or C1-6alkyl; L is a direct bond, —O—, C1-6alkanediyl-O— or —O—C1-6alkanediyl; R3 is phenylC1-4alkyl; R4 is C1-6alkyl; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; in the manufacture of a medicament useful for inhibiting mutant HIV protease in a mammal infected with said mutant HIV protease. It also relates to novel compounds of formula (I).
摘要翻译：本发明涉及2-氨基 - 苯并噻唑的用途，其具有下式：其中R 1是六氢呋喃并[2,3-b]呋喃基，四氢呋喃基，恶唑基，噻唑基，吡啶基或任选取代的苯基其中一个或多个取代基独立地选自C 1-6烷基，羟基，氨基，卤素，氨基C 1-4烷基和单或二（C 1） -4个烷基）氨基; R 2是氢或C 1-6烷基; L是直链，-O - ， - C 1-6烷二基-O-或-O-C 1-6烷二基; R 3是苯基C 1-4烷基; R 4是C 1-6烷基; R 5是氢或C 1-6烷基; R 6是氢或C 1-6烷基; 在制备用于抑制感染了所述突变HIV蛋白酶的哺乳动物中的突变HIV蛋白酶的药物中。它还涉及新的式（I）化合物。

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.

4. 发明申请

US20050159406A1 Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives 有权
公开(公告)号：US20050159406A1
公开(公告)日：2005-07-21
申请号：US11079606
申请日：2005-03-14
申请人： Marcel De Bruyn , Kristof Van Emelen , Piet Tom Wigerinck , Wim Verschueren
发明人： Marcel De Bruyn , Kristof Van Emelen , Piet Tom Wigerinck , Wim Verschueren
IPC分类号： A61K31/505 , A61K31/513 , A61P1/06 , A61P1/14 , A61P9/00 , C07D405/12 , C07D405/14 , C07D49/02 , A61K31/4015 , A61K31/452 , A61K31/453 , A61K31/496 , A61K31/551 , C07D47/02
CPC分类号： C07D405/12 , C07D405/14
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.

5. 发明申请

US20060058368A1 Broadspectrum substituted oxindole sulfonamide hiv protease inhibitors 有权
标题翻译： Broadspectrum取代羟吲哚磺酰胺hiv蛋白酶抑制剂
公开(公告)号：US20060058368A1
公开(公告)日：2006-03-16
申请号：US10524451
申请日：2003-08-14
申请人： Abdellah Tahri , Piet Tom Wigerinck
发明人： Abdellah Tahri , Piet Tom Wigerinck
IPC分类号： A61K31/404 , C07D405/02
CPC分类号： C07D493/04 , C07D209/34
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; R5a and R5b is C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or C1-6alkyl, optionally substituted on one or more atoms; R5a and R5b may also be hydrogen, aryl, Het1, Het2; R6 is hydrogen or C1-6alkyl optionally substituted on one ore more carbon atoms. 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.
摘要翻译：本发明涉及具有下式的化合物

6. 发明申请

US20050158709A1 Methods for determinging the influence of protein binding on antiretroviral activity 审中-公开
标题翻译：确定蛋白质结合对抗逆转录病毒活性的影响的方法
公开(公告)号：US20050158709A1
公开(公告)日：2005-07-21
申请号：US10504675
申请日：2003-02-21
申请人： Hilde Azijn , Piet Tom Wigerinck , Marie-Pierre De Bethune
发明人： Hilde Azijn , Piet Tom Wigerinck , Marie-Pierre De Bethune
IPC分类号： G01N33/50 , A61K45/00 , A61P31/18 , A61P43/00 , C12Q1/02 , C12Q1/18 , C12Q1/37 , C12Q1/70 , G01N33/15 , G01N33/569 , G01N33/68
CPC分类号： G01N33/56988 , C12Q1/025 , C12Q1/18 , C12Q1/37 , G01N33/68 , G01N2500/10
摘要： The present invention relates to methods for determining the influence of human plasma or serum protein binding on antiretroviral activity at physiologically achieved conditions, by using specific virus strains in a cell-based antiviral assay.
摘要翻译：本发明涉及通过在基于细胞的抗病毒测定中使用特异性病毒株来确定人血浆或血清蛋白结合对生理实现条件下抗逆转录病毒活性的影响的方法。

7. 发明申请

US20090048242A1 (1,10B-DIHYDRO-2-(AMINOALKYL-PHENYL)-5H-PYRAZOLO[1,5 C][1,3]BENZOXAZIN-5-YL)PHENYL METHANONE DERIVATIVES AS HIV VIRAL REPLICATION INHIBITORS 有权
标题翻译：（1,10B-二氢-2-（氨基甲酰基）苯基] -5H-吡唑并[1,5-C] [1,3]苯并恶嗪-5-基）苯甲酮衍生物作为HIV病毒复制抑制剂
公开(公告)号：US20090048242A1
公开(公告)日：2009-02-19
申请号：US12241317
申请日：2008-09-30
申请人： Abdellah TAHRI , Lili Hu , Dominique Louis Nestor Surleraux , Piet Tom Wigerinck
发明人： Abdellah TAHRI , Lili Hu , Dominique Louis Nestor Surleraux , Piet Tom Wigerinck
IPC分类号： C07D498/02 , A61K31/5365 , A61P31/12 , A61P31/18
CPC分类号： C07D498/04
摘要： The present invention relates to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication 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 HIV 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.
摘要翻译：本发明涉及作为HIV病毒的病毒复制的抑制剂的5H-吡唑并[1,5-c] [1,3]苯并恶嗪-5-基）苯基甲酮衍生物，其制备方法以及药物组合物，它们用作药物，以及包括它们的诊断试剂盒。本发明还涉及本发明的HIV抑制剂与其它抗逆转录病毒剂的组合。它还涉及它们在测定中作为参考化合物或作为试剂的用途。本发明的化合物可用于预防或治疗HIV感染和治疗AIDS。

8. 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。}}

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