公开(公告)号：US20060142571A1

公开(公告)日：2006-06-29

申请号：US10545719

申请日：2004-02-20

申请人： Jerome Guillemont ,  Elisabeth Therese Pasquier ,  Jan Heeres ,  Kurt Hertogs ,  Eva Bettens ,  Paulus Lewi ,  Marc De Jonge ,  Lucien Maria Koymans ,  Frederik Frans Daeyaert ,  Hendrik Vinkers ,  Frank Xavier Jozef Arts

发明人： Jerome Guillemont ,  Elisabeth Therese Pasquier ,  Jan Heeres ,  Kurt Hertogs ,  Eva Bettens ,  Paulus Lewi ,  Marc De Jonge ,  Lucien Maria Koymans ,  Frederik Frans Daeyaert ,  Hendrik Vinkers ,  Frank Xavier Jozef Arts

IPC分类号： C07D403/02

CPC分类号： C07D239/47 ,  C07D239/48 ,  C07D413/12

摘要： 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.

摘要翻译： 本发明涉及式（I）的HIV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，其作为药物的用途，其制备方法和包含它们的药物组合物。

公开(公告)号：US20060194804A1

公开(公告)日：2006-08-31

申请号：US10545358

申请日：2004-02-20

申请人： Jerome Guillemont ,  Elisabeth Pasquier ,  Jan Heeres ,  Kurt Hertogs ,  Eva Bettens ,  Paulus Lewi ,  Marc De Jonge ,  Lucien Maria Koymans ,  Frederik Daeyaert ,  Hendrik Vinkers ,  Adriaan Janssen ,  Frank Zavier Jozef Arts

发明人： Jerome Guillemont ,  Elisabeth Pasquier ,  Jan Heeres ,  Kurt Hertogs ,  Eva Bettens ,  Paulus Lewi ,  Marc De Jonge ,  Lucien Maria Koymans ,  Frederik Daeyaert ,  Hendrik Vinkers ,  Adriaan Janssen ,  Frank Zavier Jozef Arts

IPC分类号： A61K31/53 ,  A61K31/506 ,  C07D405/14

CPC分类号： C07D239/47 ,  C07D239/48 ,  C07D413/12

摘要： 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.

摘要翻译： 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。

公开(公告)号：US20050176713A1

公开(公告)日：2005-08-11

申请号：US10493454

申请日：2002-10-29

申请人： Eddy Jean Freyne ,  Peter Jacobus Johannes Buijnsters ,  Marc Willems ,  Werner Constant Embrechts ,  Jean Fernand Lacrampe ,  Paul Adriaan Janssen ,  Herwig Josephus Janssen ,  Paul Janssen ,  Graziella Janssen ,  Jasmine Janssen ,  Maroussia Godelieve Janssen ,  Theodora Joanna Arts ,  Paulus Lewi ,  Jan Heeres ,  Marc de Jonge ,  Lucien Maria Koymans ,  Frederik Frans Daeyaert ,  Rony Nuydens ,  Marc Mercken

发明人： Eddy Jean Freyne ,  Peter Jacobus Johannes Buijnsters ,  Marc Willems ,  Werner Constant Embrechts ,  Jean Fernand Lacrampe ,  Paul Adriaan Janssen ,  Herwig Josephus Janssen ,  Paul Janssen ,  Graziella Janssen ,  Jasmine Janssen ,  Maroussia Godelieve Janssen ,  Theodora Joanna Arts ,  Paulus Lewi ,  Jan Heeres ,  Marc de Jonge ,  Lucien Maria Koymans ,  Frederik Frans Daeyaert ,  Rony Nuydens ,  Marc Mercken

IPC分类号： A61K31/44 ,  A61K31/4409 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61P3/10 ,  A61P7/00 ,  A61P17/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D213/81 ,  C07D213/82 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  A61K31/655 ,  A61K31/4965

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

摘要： This invention concerns a compound of formula 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; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; 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 C2-6alkenyl 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(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7; —C(═NH)R21; R4a or R4b each independently represent hydrogen, R8, —Y1—NR9—Y2—NR10R11, —Y1—NR9—Y1—R8, —Y1—NR9R10; provided that —X—R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.

公开(公告)号：US20070037811A1

公开(公告)日：2007-02-15

申请号：US10544584

申请日：2004-02-05

申请人： Paulus Lewi ,  Paul Janssen ,  Marc de Jonge ,  Lucien Maria Koymans ,  Hendrik Vinkers ,  Frederik Daeyaert ,  Jan Heeres ,  Ruben Leenders ,  Georges Hoomaert ,  Amuri Kilonda ,  Donald Ludovici

发明人： Paulus Lewi ,  Paul Janssen ,  Marc de Jonge ,  Lucien Maria Koymans ,  Hendrik Vinkers ,  Frederik Daeyaert ,  Jan Heeres ,  Ruben Leenders ,  Georges Hoomaert ,  Amuri Kilonda ,  Donald Ludovici

IPC分类号： A61K31/53 ,  C07D403/14

CPC分类号： A61K31/53 ,  C07D253/07 ,  C07D253/075

摘要： 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.

摘要翻译： 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。