公开(公告)号：US20070021449A1

公开(公告)日：2007-01-25

申请号：US10544735

申请日：2004-02-04

申请人： Jan Heeres ,  Paulus Lewi ,  Paul Janssen ,  Marc de Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Hendrik Vinkers ,  Jerome Guillemont ,  Elisabeth Pasquier ,  Frank Xavier Arts

发明人： Jan Heeres ,  Paulus Lewi ,  Paul Janssen ,  Marc de Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Hendrik Vinkers ,  Jerome Guillemont ,  Elisabeth Pasquier ,  Frank Xavier Arts

IPC分类号： A61K31/513 ,  C07D239/47

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

摘要： 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 -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; and pharmaceutical compositions comprising them.

摘要翻译： 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〜 > 4 - 和 - b 1 - b 2 - b 3 - b 4 - 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：US20050004125A1

公开(公告)日：2005-01-06

申请号：US10493452

申请日：2002-10-29

申请人： Eddy Jean Edgard Freyne ,  Peter Jacobus Buijnsters ,  Marc Willems ,  Werner Embrechts ,  Christopher Love ,  Paul Janssen ,  Paulus Lewi ,  Jan Heeres ,  Marc de Jonge ,  Lucien Koymans ,  Hendrik Vinkers ,  Koen Van Aken ,  Gaston Diels

发明人： Eddy Jean Edgard Freyne ,  Peter Jacobus Buijnsters ,  Marc Willems ,  Werner Embrechts ,  Christopher Love ,  Paul Janssen ,  Paulus Lewi ,  Jan Heeres ,  Marc de Jonge ,  Lucien Koymans ,  Hendrik Vinkers ,  Koen Van Aken ,  Gaston Diels

IPC分类号： 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 ,  A61K31/4965

CPC分类号： C07D213/74 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  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 is 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 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 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; R4 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.

摘要翻译： 本发明涉及式的化合物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，其中环A是6-元杂环; R 1是氢; 芳基; 甲酰基 C 1-6烷基羰基; 任选取代的C 1-6烷基; C 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; 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; C 1-6烷氧基; C 1-6烷硫基; C 1-6烷氧基羰基; C 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C 1-6烷基; 多卤代C 1-6烷氧基; 多卤代C 1-6烷硫基; 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 4是任选取代的杂环，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：US20060293330A1

公开(公告)日：2006-12-28

申请号：US10573364

申请日：2004-09-21

申请人： Paul Janssen ,  Marc De Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Jan Heeres ,  Hendrik Vinkers ,  Ruben Leenders ,  Dirk Vandenput ,  Paul Janssen

发明人： Paul Janssen ,  Marc De Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Jan Heeres ,  Hendrik Vinkers ,  Ruben Leenders ,  Dirk Vandenput ,  Paul Janssen

IPC分类号： A61K31/519 ,  A61K31/525 ,  C07D487/02

CPC分类号： A61K31/52 ,  C07D473/00 ,  C07D473/16 ,  C07D473/18

摘要： 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 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 and wherein —C-D- represents a bivalent radical of formula —N═CH—NR17—  (c-1); or —NR7—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).

摘要翻译： 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，药学上 其中A和B各自表示下式的基团，其中-CD-表示式<β的二价基团。在线式描述=“在线式” - 末端=“铅”→N-CH-NR 17 - （c-1）; 或<？in-line-formula description =“In-line Formulas”end =“tail”？> <？in-line-formula description =“In-line Formulas”end =“lead”？> - NR < 7 -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，并且当A表示基团时，<？in-line-formula description =“In-line Formulas”end =“tail” 式（b）所示的B为式（a）的基团。

公开(公告)号：US20060252764A1

公开(公告)日：2006-11-09

申请号：US11474855

申请日：2006-06-26

申请人： Jerome Guillemont ,  Patrice Palandijian ,  Marc De Jonge ,  Lucien Koymans ,  Hendrik Vinkers ,  Frederik Daeyaert ,  Jan Heeres ,  Koen Van Aken ,  Paulus Lewi ,  Paul Janssen ,  Frank Xavier Arts

发明人： Jerome Guillemont ,  Patrice Palandijian ,  Marc De Jonge ,  Lucien Koymans ,  Hendrik Vinkers ,  Frederik Daeyaert ,  Jan Heeres ,  Koen Van Aken ,  Paulus Lewi ,  Paul Janssen ,  Frank Xavier Arts

IPC分类号： A61K31/506 ,  C07D403/02

CPC分类号： C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07C255/42 ,  C07C257/12 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl;n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(═O)pR6, —NH—S(═O)pR6, —C(═O)R6, —NHC(═O)H, —C(═O)NHNH2, —NHC(═O)R6, —C(═NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N═N—, —O—, —C(═O)—, C1-4alkanediyl, —CHOH—, —S—, —S(═O)p—, —X2—C1-4alkanediyl- or —C1-4alkanediyl-X2—; R3 is NHR13; NR13R14; —C(═O)—NHR13; —C(═O)—NR13R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl; substituted C2-6alkynyl; C1-6alkyl substituted with hydroxy and a second substituent; —C(═N—O—R8)—C1-4alkyl; R7; or —X3—R7; R4 is halo, hydroxy, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxy, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, formyl, amino, mono- or di(C1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

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。

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：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。