公开(公告)号：WO2003037877A1

公开(公告)日：2003-05-08

申请号：PCT/EP2002/012079

申请日：2002-10-29

Applicant: JANSSEN PHARMACEUTICA N.V. ,  FREYNE, Eddy, Jean, Edgard ,  BUIJNSTERS, Peter, Jacobus, Johannes, Antonius ,  WILLEMS, Marc ,  EMBRECHTS, Werner, Constant, Johan ,  JANSSEN, Paul, Adriaan, Jan ,  LEWI, Paulus, Joannes ,  HEERES, Jan ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  DAEYAERT, Frederik, Frans, Desire ,  KUKLA, Michael, Joseph ,  GEERTS, Hugo, Alfons, Gabriel ,  NUYDENS, Rony, Maria ,  MERCKEN, Marc, Hubert ,  LUDOVICI, Donald, William

Inventor： FREYNE, Eddy, Jean, Edgard ,  BUIJNSTERS, Peter, Jacobus, Johannes, Antonius ,  WILLEMS, Marc ,  EMBRECHTS, Werner, Constant, Johan ,  JANSSEN, Paul, Adriaan, Jan ,  LEWI, Paulus, Joannes ,  HEERES, Jan ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  DAEYAERT, Frederik, Frans, Desire ,  KUKLA, Michael, Joseph ,  GEERTS, Hugo, Alfons, Gabriel ,  NUYDENS, Rony, Maria ,  MERCKEN, Marc, Hubert ,  LUDOVICI, Donald, William

IPC: C07D239/30

CPC classification number: C07D239/42 ,  A61K31/506 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D403/12

Abstract: This invention concerns a compound of formula (I),a N -oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyloxyC 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R 3 is hydrogen; hydroxy; halo; optionally substituted C 1-6 alkyl or C 2-6 alkenyl or C 2-6 alkynyl; C 1-6 alkyloxy; C 1-6 alkylthio; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; polyhaloC 1-6 alkylthio; R 21 ; R 21 -C 1-6 alkyl; R 21 -O-; R 21 -S-; R 21 -C(=O)-; R 21 -S(=O) p -; R 7 -S(=O) p -; R 7 -S(=O) p -NH-; R 21 -S(=O) p -NH-; R 7 -C(=O)-; -NHC(=O)H; -C(=O)NHNH 2 ; R 7 -C(=O)-NH-; R 21 -C(=O)-NH-; -C(=NH)R 7 ; -C(=NH)R 21 ; R 4a or R 4b each independently represent hydrogen, R 8 , -Y 1 -NR 9 -Y 2 -NR 10 R 11 , -Y 1 -NR 9 -Y 1 -R 8 , -Y 1 -NR 9 R 10 ; provided that -X-R 2 and/or R 3 is other than hydrogen;their use, pharmaceutical compositions comprising them and processes for their preparation.

Abstract translation: 本发明涉及式（I）化合物，其中N为氧化物，其药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A为6-元杂环; R 1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是O或S; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 2-6烯基或C 2-6炔基; C1-6烷; C 1-6烷; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; 羧基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; [R <21>; [R <21> -C 1-6烷基; [R <21> -O-; [R <21> -S-; [R <21> C（= O） - ; [R <21> -S（= O）p - ; [R <7> -S（= O）p - ; [R <7> -S（= O）P-NH-; [R <21> S（= O）P-NH-; [R <7> C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; [R <7> C（= O）-NH-; [R <21> C（= O）-NH-; -C（= NH）R <7>; -C（= NH）R 21; R 4a或R 4b各自独立地表示氢，R 8，-Y 1 -NR 9 -Y 2 -NR 10 R 11，-Y 1 -NR 9 -Y 1 -R 8，-Y1-NR 9 R 10; 条件是-X-R 2和/或R 3不是氢;它们的用途，包含它们的药物组合物及其制备方法。

公开(公告)号：WO2003037869A1

公开(公告)日：2003-05-08

申请号：PCT/EP2002/012067

申请日：2002-10-29

Applicant: JANSSEN PHARMACEUTICA N.V. ,  FREYNE, Eddy, Jean, Edgard ,  BUIJNSTERS, Peter, Jacobus, Johannes, Antonius ,  WILLEMS, Marc ,  EMBRECHTS, Werner, Constant, Johan ,  LACRAMPE, Jean, Fernand, Armand ,  JANSSEN, Paul, Adriaan, Jan ,  LEWI, Paulus, Joannes ,  HEERES, Jan ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  DAEYAERT, Frederik, Frans, Desire ,  KUKLA, Michael, Joseph ,  GEERTS, Hugo, Alfons, Gabriel ,  NUYDENS, Rony, Maria ,  MERCKEN, Marc, Hubert ,  LUDOVICI, Donald, William

Inventor： FREYNE, Eddy, Jean, Edgard ,  BUIJNSTERS, Peter, Jacobus, Johannes, Antonius ,  WILLEMS, Marc ,  EMBRECHTS, Werner, Constant, Johan ,  LACRAMPE, Jean, Fernand, Armand ,  JANSSEN, Paul, Adriaan, Jan ,  LEWI, Paulus, Joannes ,  HEERES, Jan ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  DAEYAERT, Frederik, Frans, Desire ,  KUKLA, Michael, Joseph ,  GEERTS, Hugo, Alfons, Gabriel ,  NUYDENS, Rony, Maria ,  MERCKEN, Marc, Hubert ,  LUDOVICI, Donald, William

IPC: C07D213/82

CPC classification number: C07D213/81 ,  C07D213/82 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: This invention concerns a compound of formula (I' ),a N -oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyloxyC 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R 3 is hydrogen; hydroxy; halo; optionally substituted C 1-6 alkyl or C 2-6 alkenyl or C 2-6 alkynyl; C 1-6 alkyloxy; C 1-6 alkylthio; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; polyhaloC 1-6 alkylthio; R 21 ; R 21 -C 1-6 alkyl; R 21 -O-; R 21 -S-; R 21 -C(=O)-; R 21 -S(=O) p -; R 7 -S(=O) p -; R 7 -S(=O) p -NH-; R 21 -S(=O) p -NH-; R 7 -C(=O)-; -NHC(=O)H;-C(=O)NHNH 2 ; R 7 -C(=O)-NH-; R 21 -C(=O)-NH-; -C(=NH)R 7 ; -C(=NH)R 21 ; R 4a or R 4b each independently represent hydrogen, R 8 , -Y 1 -NR 9 -Y 2 -NR 10 R 11 , -Y 1 -NR 9 -Y 1 -R 8 , -Y 1 -NR 9 R 10 ; provided that -X-R 2 and/or R 3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.

Abstract translation: 本发明涉及式（I'）化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A表示6-元杂环; R 1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是O或S; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 2-6烯基或C 2-6炔基; C1-6烷; C 1-6烷; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; 羧基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; [R <21>; [R <21> -C 1-6烷基; [R <21> -O-; [R <21> -S-; [R <21> C（= O） - ; [R <21> -S（= O）p - ; [R <7> -S（= O）p - ; [R <7> -S（= O）P-NH-; [R <21> S（= O）P-NH-; [R <7> C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; [R <7> C（= O）-NH-; [R <21> C（= O）-NH-; -C（= NH）R <7>; -C（= NH）R 21; R 4a或R 4b各自独立地表示氢，R 8，-Y 1 -NR 9 -Y 2 -NR 10 R 11，-Y 1 -NR 9 -Y 1 -R 8，-Y1-NR 9 R 10; 条件是-X-R 2和/或R 3不是氢; 其用途，包含它们的药物组合物及其制备方法。

公开(公告)号：WO2004096807A2

公开(公告)日：2004-11-11

申请号：PCT/EP2004050621

申请日：2004-04-27

Applicant: TIBOTEC PHARM LTD ,  VERSCHUEREN WIM GASTON ,  DIERYNCK INGE ,  SURLERAUX DOMINIQUE LOUIS NEST ,  DAEYAERT FREDERIK FRANS DESIRE

Inventor： VERSCHUEREN WIM GASTON ,  DIERYNCK INGE ,  SURLERAUX DOMINIQUE LOUIS NEST ,  DAEYAERT FREDERIK FRANS DESIRE

IPC: A61P31/18 ,  C07D487/04 ,  C07D487/00

CPC classification number: C07D487/04

Abstract: The present invention concerns the compounds having the formula (1), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof wherein (a) or (b); A, together with the two carbons of the phenyl ring to which it is attached forms a monocyclic aryl or a monocyclic Het ; R is hydrogen, halo, nitro, cyano, sultam, sulltim, C3-7cycloalkyl, C(=O)-R , S(=O)y-R , OR , NR R , C(=NR )-R , optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl; R is hydrogen, C3-7cycloalkyl, aryl, Het , Het , C(=O)-R , S(=O)Y-R OR , NR R , C=NR )-R , or optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl. It further relates to their use as HIV integrase inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with other anti-retroviral agents, and to their use in assays as reference compounds or as reagents.

Abstract translation: 本发明涉及具有式（1），N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物的化合物，其中（a）或（b）; A与连接的苯环的两个碳一起形成单环芳基或单环Het 2; R 1是氢，卤素，硝基，氰基，苏丹，苏利坦，C 3-7环烷基，C（= O）-R 5，S（= O）y R 6，OR 7，NR 8 R 9，C（= NR 8）-R 5，任选多取代的C 1-6烷基，任选多取代的C 2-6烯基或任选多取代的C 2-6炔基; R 2是氢，C 3-7环烷基，芳基，Het 1，Het 2，C（= O）-R 5，S（= O）Y R 6 OR 7， 或任选多取代的C 1-6烷基，任选多取代的C 2-6烯基或任选多取代的C 2-6炔基。 它还涉及它们作为HIV整合酶抑制剂的用途，其制备方法以及包含它们的药物组合物和诊断试剂盒。 它还涉及与其它抗逆转录病毒剂的组合，以及它们在测定中作为参考化合物或作为试剂的用途。

公开(公告)号：WO2002078708A1

公开(公告)日：2002-10-10

申请号：PCT/EP2002/002806

申请日：2002-03-13

Applicant: JANSSEN PHARMACEUTICA N.V. ,  JANSSEN, Paul, Adriaan, Jan ,  VAN AKEN, Koen, Jeanne, Alfons ,  LEWI, Paulus, Joannes ,  KOYMANS, Lucien, Maria, Henricus ,  DE JONGE, Marc, René ,  HEERES, Jan ,  DAEYAERT, Frederik, Frans, Desire ,  HOORNAERT, Georges, Joseph, Cornelius ,  COMPERNOLLE, Frans, Josef, Cornelius ,  KILONDA, Amuri

Inventor： JANSSEN, Paul, Adriaan, Jan ,  VAN AKEN, Koen, Jeanne, Alfons ,  LEWI, Paulus, Joannes ,  KOYMANS, Lucien, Maria, Henricus ,  DE JONGE, Marc, René ,  HEERES, Jan ,  DAEYAERT, Frederik, Frans, Desire ,  HOORNAERT, Georges, Joseph, Cornelius ,  COMPERNOLLE, Frans, Josef, Cornelius ,  KILONDA, Amuri

IPC: A61K31/4965

CPC classification number: C07D241/20

Abstract: This invention concerns compounds of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R 1-4 and X are as defined in the claims; their use as a medicine for inhibiting HIV replication, their processes for preparation and pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及式（I）的化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中R 1-4和X如权利要求中所定义; 它们用作抑制HIV复制的药物，其制备方法和包含它们的药物组合物。

公开(公告)号：WO2005028479A3

公开(公告)日：2005-06-16

申请号：PCT/EP2004052262

申请日：2004-09-21

Applicant: JANSSEN PHARMACEUTICA NV ,  ARTS FRANK XAVIER JOZEF HERWIG ,  LEWI PAULUS JOANNES ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  DAEYAERT FREDERIK FRANS DESIRE ,  HEERES JAN ,  VINKERS HENDRIK MAARTEN ,  LEENDERS RUBEN GERARDUS GEORGE ,  VANDENPUT DIRK ALFONS LEO

Inventor： LEWI PAULUS JOANNES ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  DAEYAERT FREDERIK FRANS DESIRE ,  HEERES JAN ,  VINKERS HENDRIK MAARTEN ,  LEENDERS RUBEN GERARDUS GEORGE ,  VANDENPUT DIRK ALFONS LEO ,  JANSSEN PAUL ADRIAAN JAN DI

IPC: A61K31/52 ,  C07D473/00 ,  C07D473/16 ,  C07D473/18 ,  A61P31/18

CPC classification number: A61K31/52 ,  C07D473/00 ,  C07D473/16 ,  C07D473/18

Abstract: The present invention relates to the use of a compound of formula (I) for the manufacture of a medicament for the prevention or the treatment of HIV infection wherein the compound of formula (I) is a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A and B each represents a radical of formula (a) or (b) and wherein -C-D- represents a bivalent radical of formula -N=CH-NR - (c-1); or -NR -CH=N- (c-2); provided that when A represents a radical of formula (a) then B represents a radical of formula (b) and when A represents a radical of formula (b) then B represents a radical of formula (a).

Abstract translation: 本发明涉及式（I）化合物在制备用于预防或治疗HIV感染的药物中的用途，其中式（I）化合物为式（I）化合物，N-氧化物 ，其药学上可接受的加成盐，季胺或其立体化学异构形式，其中A和B各自表示式（a）或（b）的基团，其中-CD-表示式-N = CH- NR 17 - （c-1）; 或-NR 17 -CH = N-（C-2）; 条件是当A表示式（a）的基团时，B表示式（b）的基团，当A表示式（b）的基团时，B表示式（a）的基团。

公开(公告)号：WO2004069812A1

公开(公告)日：2004-08-19

申请号：PCT/EP2004/001011

申请日：2004-02-04

Applicant: JANSSEN PHARMACEUTICA N.V. ,  ARTS, Theodora, Joanna, Francisca ,  JANSSEN, Graziella, Maria, Constantina ,  JANSSEN, Herwig, Josephus, Margareta ,  JANSSEN, Jasmine, Josée, Werner ,  JANSSEN, Paul, Peter, Maria ,  JANSSEN, Maroussia, Godelieve, Frank ,  GUILLEMONT, Jérôme, Emile, Georges ,  PASQUIER, Elisabeth, Therese, Jeanne ,  HEERES, Jan ,  LEWI, Paulus, Joannes ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  DAEYAERT, Frederik, Frans, Desire ,  VINKERS, Hendrik, Maarten

Inventor： HEERES, Jan ,  LEWI, Paulus, Joannes ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  DAEYAERT, Frederik, Frans, Desire ,  VINKERS, Hendrik, Maarten

IPC: C07D239/47

CPC classification number: A61K31/513 ,  C07D239/47 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: This invention concerns the use of a compound for the manufacture of a medicament for the prevention of HIV infection via sexual intercourse and related intimate contact between partners, wherein the compound is a compound of formula (I) a N -oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein the ring containing -a 1 =a 2 -a 3 =a 4 - and -b 1 =b 2 -b 3 =b 4 - represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; and pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及化合物在制备药物中的用途，所述药物通过性交和伴侣之间的相关紧密接触来预防HIV感染，其中所述化合物是式（I）的化合物，N-氧化物，药学上可接受的添加剂 盐，季胺及其立体化学异构形式，其中含-a 1 = a 2 -a 3 = a 4 - 和-b 1 = b 2 -b的环 3 =表示苯基，吡啶基，嘧啶基，吡嗪基，哒嗪基; 和包含它们的药物组合物。

公开(公告)号：WO2004096807A8

公开(公告)日：2005-09-22

申请号：PCT/EP2004050621

申请日：2004-04-27

Applicant: TIBOTEC PHARM LTD ,  VERSCHUEREN WIM GASTON ,  DIERYNCK INGE ,  SURLERAUX DOMINIQUE LOUIS NEST ,  DAEYAERT FREDERIK FRANS DESIRE

Inventor： VERSCHUEREN WIM GASTON ,  DIERYNCK INGE ,  SURLERAUX DOMINIQUE LOUIS NEST ,  DAEYAERT FREDERIK FRANS DESIRE

IPC: A61P31/18 ,  C07D487/04 ,  A61K31/4985 ,  C07D471/04

CPC classification number: C07D487/04

Abstract: The present invention concerns the compounds having the formula (I), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof wherein (a) or (b); A, together with the two carbons of the phenyl ring to which it is attached forms a monocyclic aryl or a monocyclic Het ; R is hydrogen, halo, nitro, cyano, sultam, sulltim, C3-7cycloalkyl, C(=O)-R , S(=O)y-R , OR , NR R , C(=NR )-R , optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl; R is hydrogen, C3-7cycloalkyl, aryl, Het , Het , C(=O)-R , S(=O)Y-R OR , NR R , C=NR )-R , or optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl. It further relates to their use as HIV integrase inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with other anti-retroviral agents, and to their use in assays as reference compounds or as reagents.

Abstract translation: 本发明涉及具有式（I）的化合物，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（a）或（b）; A与连接的苯环的两个碳一起形成单环芳基或单环Het 2; R 1是氢，卤素，硝基，氰基，苏丹，苏利坦，C 3-7环烷基，C（= O）-R 5，S（= O）y R 6，OR 7，NR 8 R 9，C（= NR 8）-R 5，任选多取代的C 1-6烷基，任选多取代的C 2-6烯基或任选多取代的C 2-6炔基; R 2是氢，C 3-7环烷基，芳基，Het 1，Het 2，C（= O）-R 5，S（= O）Y R 6 OR 7， 或任选多取代的C 1-6烷基，任选多取代的C 2-6烯基或任选多取代的C 2-6炔基。 它还涉及它们作为HIV整合酶抑制剂的用途，其制备方法以及包含它们的药物组合物和诊断试剂盒。 它还涉及与其它抗逆转录病毒剂的组合，以及它们在测定中作为参考化合物或作为试剂的用途。

公开(公告)号：WO2004074266A8

公开(公告)日：2004-11-11

申请号：PCT/EP2004050084

申请日：2004-02-05

Applicant: JANSSEN PHARMACEUTICA NV ,  LEWI PAULUS JOANNES ,  ARTS THEODORA JOANNA FRANCISCA ,  JANSSEN GRAZIELLA MARIA CONSTA ,  JANSSEN HERWIG JOSEPHUS MARGAR ,  JANSSEN JASMINE JOSEE WERNER H ,  JANSSEN PAUL PETER MARIA HM ,  JANSSEN MAROUSSIA GODELIEVE FR ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  VINKERS HENDRIK MAARTEN ,  DAEYAERT FREDERIK FRANS DESIRE ,  HEERES JAN ,  LEENDERS RUBEN GERARDUS GEORGE ,  HOORNAERT GEORGES JOSEPH CORNE ,  KILONDA AMURI ,  LUDOVICI DONALD WILLIAM

Inventor： LEWI PAULUS JOANNES ,  JANSSEN PAUL ADRIAAN JAN DI ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  VINKERS HENDRIK MAARTEN ,  DAEYAERT FREDERIK FRANS DESIRE ,  HEERES JAN ,  LEENDERS RUBEN GERARDUS GEORGE ,  HOORNAERT GEORGES JOSEPH CORNE ,  KILONDA AMURI ,  LUDOVICI DONALD WILLIAM

IPC: A61K31/53 ,  C07D253/06 ,  C07D253/07 ,  C07D253/075

CPC classification number: A61K31/53 ,  C07D253/07 ,  C07D253/075

Abstract: The present invention relates to HIV replication inhibitors of formula (I) as defined in the specification their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及如说明书中所定义的式（I）的HIV复制抑制剂作为药物的用途，它们的制备方法和包含它们的药物组合物。