公开(公告)号：WO2005028479A2

公开(公告)日：2005-03-31

申请号：PCT/EP2004/052262

申请日：2004-09-21

Applicant: JANSSEN PHARMACEUTICA N.V. ,  ARTS, Frank, Xavier, Jozef, Herwig ,  LEWI, Paulus, Joannes ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  DAEYAERT, Frederik, Frans, Desiré ,  HEERES, Jan ,  VINKERS, Hendrik, Maarten ,  LEENDERS, Ruben, Gerardus, George ,  VANDENPUT, Dirk, Alfons, Leo

Inventor： LEWI, Paulus, Joannes ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  DAEYAERT, Frederik, Frans, Desiré ,  HEERES, Jan ,  VINKERS, Hendrik, Maarten ,  LEENDERS, Ruben, Gerardus, George ,  VANDENPUT, Dirk, Alfons, Leo

IPC: C07D473/00

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 17 - (c-1); or -NR 17 -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）N-氧化物，其药学上可接受的加成盐，季胺或立体化学异构形式，其中A和B各自代表式（a）或（b）的基团，和 其中-CD-代表式-N = CH-NR 17 - （c-1）的二价基团; 或-NR17-CH = N-（c-2）。 条件是当A代表式（a）的基团时，则B代表式（b）的基团，并且当A代表式（b）的基团时，则B代表式（a）的基团。

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。

公开(公告)号：WO2006035051A1

公开(公告)日：2006-04-06

申请号：PCT/EP2005/054893

申请日：2005-09-28

Applicant: JANSSEN PHARMACEUTICA N.V. ,  ANDRIES, Koenraad, Jozef, Lodewijk, Marcel ,  GÖHLMANN, Hinrich, Wilhelm, Helmut ,  NEEFS, Jean-Marc, Edmond, Fernand, Marie ,  VERHASSELT, Peter, Karel, Maria ,  WINKLER, Johann ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus

Inventor： ANDRIES, Koenraad, Jozef, Lodewijk, Marcel ,  GÖHLMANN, Hinrich, Wilhelm, Helmut ,  NEEFS, Jean-Marc, Edmond, Fernand, Marie ,  VERHASSELT, Peter, Karel, Maria ,  WINKLER, Johann ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus

IPC: C07K14/35 ,  C12N15/31 ,  C12N15/52 ,  G01N33/50 ,  A61K31/00

CPC classification number: C07K14/35 ,  A61K38/00 ,  C12N9/14

Abstract: This invention provides an isolated mutant atpE protein and departing from said mutant atpE protein the identification of an ATPase binding domain. This invention also provides related nucleic acids, vectors, host cells, pharmaceutical compositions and articles of manufacture. This invention further provides methods for determining whether a test compound interacts with an atpE protein, i.e. with the ATPase binding domain of the present invention, as well as pharmaceuticals compositions comprising said test compound, in particular as antimicrobials, more particular as antimycobacterial agent, even more particular for treating tuberculosis in a subject.

Abstract translation: 本发明提供了一种分离的突变型atpE蛋白，并从所述突变型atpE蛋白中脱离鉴定ATP酶结合结构域。 本发明还提供了相关的核酸，载体，宿主细胞，药物组合物和制品。 本发明还提供了用于确定测试化合物是否与atpE蛋白（即与本发明的ATP酶结合结构域）相互作用的方法，以及包含所述测试化合物，特别是作为抗微生物剂的药物组合物，更特别地作为抗分枝杆菌剂，甚至 更具体地用于治疗受试者的结核病。

公开(公告)号：WO03037891A8

公开(公告)日：2003-09-04

申请号：PCT/EP0212077

申请日：2002-10-29

Applicant: JANSSEN PHARMACEUTICA NV ,  FREYNE EDDY JEAN EDGARD ,  BUIJNSTERS PETER JACOBUS JOHAN ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA ,  LOVE CHRISTOPHER JOHN ,  JANSSEN PAUL ADRIAAN JAN ,  LEWI PAULUS JOANNES ,  HEERES JAN ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  VINKERS HENDRIK MAARTEN ,  VAN AKEN KOEN JEANNE ALFONS ,  DIELS GASTON STANISLAS MARCELL

Inventor： FREYNE EDDY JEAN EDGARD ,  BUIJNSTERS PETER JACOBUS JOHAN ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA ,  LOVE CHRISTOPHER JOHN ,  JANSSEN PAUL ADRIAAN JAN ,  LEWI PAULUS JOANNES ,  HEERES JAN ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  VINKERS HENDRIK MAARTEN ,  VAN AKEN KOEN JEANNE ALFONS ,  DIELS GASTON STANISLAS MARCELL

IPC: A61K31/435 ,  A61K31/4406 ,  A61K31/50 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61P3/10 ,  A61P17/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P31/18 ,  A61P35/00 ,  A61P35/02 ,  C07D213/53 ,  C07D213/74 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

CPC classification number: C07D213/74 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  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 is a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxy C1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C1-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C1-6alkyl; R21-O-; R21-S-; R21-C(=0)-; R21-S(=0)p-; R7-S =O R7-S(=O)p-NH-; R21-S(=O)p-NH-; R7-C(=0)-; -NHC(=0)H; -C(=O)NHNH2; R7-C(=O)-NH-; R21-C(=O)-NH-; -C(=NH)R7; -C(=NH)R21; R° is an optionally substituted heterocycle provided that -X-R2 and/or R3 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为6-元杂环; R1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是直接键或连接原子或基团; 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; R3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 1-6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; R21; R21-C 1-6烷基; R21-O-; R21-S-; R21-C（= O） - ; R21-S（= O）p - ; R7-S = O R7-S（= O）p-NH-; R21-S（= O）P-NH-; R7-C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; R7-C（= O）-NH-; R21-C（= O）-NH-; -C（= NH）R 7; -C（= NH）R 21; R°是任选取代的杂环，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：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：WO2003037891A1

公开(公告)日：2003-05-08

申请号：PCT/EP2002/012077

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 ,  LOVE, Christopher, John ,  JANSSEN, Paul, Adriaan, Jan ,  LEWI, Paulus, Joannes ,  HEERES, Jan ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  VINKERS, Hendrik, Maarten ,  VAN AKEN, Koen, Jeanne, Alfons ,  DIELS, Gaston, Stanislas, Marcella

Inventor： FREYNE, Eddy, Jean, Edgard ,  BUIJNSTERS, Peter, Jacobus, Johannes, Antonius ,  WILLEMS, Marc ,  EMBRECHTS, Werner, Constant, Johan ,  LOVE, Christopher, John ,  JANSSEN, Paul, Adriaan, Jan ,  LEWI, Paulus, Joannes ,  HEERES, Jan ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  VINKERS, Hendrik, Maarten ,  VAN AKEN, Koen, Jeanne, Alfons ,  DIELS, Gaston, Stanislas, Marcella

IPC: C07D403/12

CPC classification number: C07D213/74 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  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 is 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 alkyloxy C 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; 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 1-6 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(=0)-; R 21 -S(=0)p-; R 7 -S =O R 7 -S(=O)p-NH-; R 21 -S(=O)p-NH-; R 7 -C(=0)-; -NHC(=0)H; -C(=O)NHNH2; R 7 -C(=O)-NH-; R 21 -C(=O)-NH-; -C(=NH)R 7 ; -C(=NH)R 21 ; R° is an optionally substituted heterocycle 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为6-元杂环; R 1是氢; 芳基; 甲酰基; ç<子> 1-6 烷基羰基; 任选取代的C 1-6烷基; ç<子> 1-6 烷氧基羰基; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接基原子或基团; Z是直接键或连接基原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基 ，碳环或杂环，每个所述基团可以任选被取代; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 1-6链烯基或C 2-6炔基; ç<子> 1-6 烷氧基; ç<子> 1-6 烷硫基; ç<子> 1-6 烷氧基羰基; ç<子> 1-6 烷基羰基氧基; 羧基; 氰基; 硝基; 氨基; 单 - 或二（C 1-6烷基）氨基; 多卤代<子> 1-6 烷基; 多卤代<子> 1-6 烷氧基; 多卤代<子> 1-6 烷硫基; [R ^{21 ; [R 21 -C <子> 1-6 烷基; [R 21 -O-; [R 21 -S-; [R 21 -C（= O） - ; [R 21 -S（= O）p - ; R 7 -S = O 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＆度; 是任选取代的杂环，条件是-XR 2和/或R 3不为氢;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：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：WO2004074266A1

公开(公告)日：2004-09-02

申请号：PCT/EP2004/050084

申请日：2004-02-05

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 ,  LEWI, Paulus, Joannes ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  VINKERS, Hendrik, Maarten ,  DAEYAERT, Frederik, Frans, Desiré ,  HEERES, Jan ,  LEENDERS, Ruben, Gerardus, George ,  HOORNAERT, Georges, Joseph, Cornelius ,  KILONDA, Amuri ,  LUDOVICI, Donald, William

Inventor： LEWI, Paulus, Joannes ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  VINKERS, Hendrik, Maarten ,  DAEYAERT, Frederik, Frans, Desiré ,  HEERES, Jan ,  LEENDERS, Ruben, Gerardus, George ,  HOORNAERT, Georges, Joseph, Cornelius ,  KILONDA, Amuri ,  LUDOVICI, Donald, William

IPC: C07D253/06

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: 本发明涉及如本说明书中定义的式（I）的HIV复制抑制剂，其用作药物，其制备方法和包含它们的药物组合物。

公开(公告)号：WO2004074262A1

公开(公告)日：2004-09-02

申请号：PCT/EP2004/050177

申请日：2004-02-20

Applicant: TIBOTEC PHARMACEUTICALS Ltd. ,  ARTS, Frank, Xavier, Jozef, Herwig ,  ARTS, Theodora ,  GUILLEMONT, Jerôme, Emile, Georges ,  PASQUIER, Elisabeth, Thérese, Jeanne ,  HEERES, Jan ,  HERTOGS, Kurt ,  BETTENS, Eva ,  LEWI, Paulus, Joannes ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  DAEYAERT, Frederik, Frans, Desiré ,  VINKERS, Hendrik, Maarten

Inventor： GUILLEMONT, Jerôme, Emile, Georges ,  PASQUIER, Elisabeth, Thérese, Jeanne ,  HEERES, Jan ,  HERTOGS, Kurt ,  BETTENS, Eva ,  LEWI, Paulus, Joannes ,  DE JONGE, Marc, René ,  KOYMANS, Lucien, Maria, Henricus ,  DAEYAERT, Frederik, Frans, Desiré ,  VINKERS, Hendrik, Maarten

IPC: C07D239/47

CPC classification number: C07D239/47 ,  C07D239/48 ,  C07D413/12

Abstract: This invention concerns HIV replication inhibitors of formula (I), The N -oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及式（I）的N-复制抑制剂，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，它们作为药物的用途，其制备方法和包含它们的药物组合物。