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1. 发明申请

US20100034810A1 PYRIMIDINE DERIVATIVES FOR THE PREVENTION OF HIV INFECTION 有权
公开(公告)号：US20100034810A1
公开(公告)日：2010-02-11
申请号：US12567051
申请日：2009-09-25
申请人： Jan HEERES , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts , Marc Rene de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desire Daeyaert , Hendrik Maarten Vinkers , Jerome Emile Georges Gullemont , Elisabeth Theresa Jeanne Pasquier
发明人： Jan HEERES , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts , Marc Rene de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desire Daeyaert , Hendrik Maarten Vinkers , Jerome Emile Georges Gullemont , Elisabeth Theresa Jeanne Pasquier
IPC分类号： A61K31/506 , A61K39/395 , A61K38/00 , A61K31/551 , A61K31/5377 , A61K31/505 , A61P31/18
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 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; 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; and pharmaceutical compositions comprising them.

2. 发明申请

US20090012092A1 Hiv Inhibiting 1,2,4-Triazin-6-One Derivatives 有权
标题翻译： HIF抑制1,2,4-三嗪-6-酮衍生物
公开(公告)号：US20090012092A1
公开(公告)日：2009-01-08
申请号：US11573224
申请日：2005-08-10
申请人： Georges Joseph Cornelius Hoornaert , Amuri Kilonda , Jan Heeres , Paulus Joannes Lewi , Marc Rene de Jonge , Frederik Frans Desire Daeyaert , Hendrik Maarten Vinkers , Lucien Maria Henricus Koymans , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts
发明人： Georges Joseph Cornelius Hoornaert , Amuri Kilonda , Jan Heeres , Paulus Joannes Lewi , Marc Rene de Jonge , Frederik Frans Desire Daeyaert , Hendrik Maarten Vinkers , Lucien Maria Henricus Koymans , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts
IPC分类号： A61K31/53 , C07D253/06 , A61P31/18
CPC分类号： C07D253/075
摘要： The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(═O)pR6; —NH—S(═O)pR6; —C(═O)R6; —NHC(═O)H; —C(═O)NHNH2; NHC(═O)R6; C(═NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14 —C(═O)—NHR13; —C(═O)—NR13 R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 or X2 represents —NR1—; —NH—NH—; —N═N—; —O—; —C(═O)—; —C1-4alkanediyl-; —CHOH—; —S—; —S(═O)p—; —X4—C1-4alkanediyl-; —C1-4alkanediyl-X4—; or —C1-4alkanediyl-X4—C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式N-氧化物的HIV复制抑制剂，其药学上可接受的加成盐，季胺或其立体化学异构形式，其中环A和环B表示苯基，吡啶基，哒嗪基，嘧啶基或吡嗪基; n和m为1〜4; R1表示氢; 芳基; 甲酰基 C 1-6烷基羰基; C 1-6烷氧基羰基; 任选取代的C 1-6烷基; 被C 1-6烷氧基羰基取代的C 1-6烷氧基C 1-6烷基羰基; R2或R4代表氢; 羟基; 光环; 任选取代的C 1-6烷基; 任选取代的C 2-6烯基; 任选取代的C 2-6炔基; C 3-7环烷基; C 1-6烷氧基; 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 1-4烷基; 多卤代1-4烷基氧基; 多卤代 -S（-O）p R 6; -NH-S（-O）p R 6; -C（-O）R 6; -NHC（-O）H; -C（-O）NHNH 2; NHC（-O）R 6; C（-NH）R 6; 或R7; R2a或R3表示氰基; 氨基羰基; 氨基; 光环; NHR13; NR 13 R 14 -C（-O）-NHR 13; -C（ - ） - NR 13 R 14; -C（-O）-R 15; -CH-N-NH-C（-O）-R16; 任选取代的C 1-6烷基; 任选取代的C 1-6烷氧基; 任选取代的C 1-6烷氧基C 1-6烷基; 任选取代的C 2-6烯基; 任选取代的C 2-6炔基; -C（-N-O-R 8）-C 1-4烷基; R7或-X3-R7; X1或X2表示-NR1-; -NH-NH-; -N-N- -O-; -C（-O） - ; -C 1-4烷二基 -CHOH-; -S-; -S（-O）p - ; -X4-C1-4烷二基 -C 1-4烷二基-X4-; 或-C1-4烷二基-X4-C1-4烷二基; 它们作为药物的用途，它们用于制备用于治疗或预防HIV感染的药物的用途; 其制备方法和包含它们的药物组合物。

3. 发明申请

US20120076835A1 HIV INHIBITING PYRIMIDINES DERIVATIVES 审中-公开
标题翻译：艾滋病毒抑制吡啶衍生物
公开(公告)号：US20120076835A1
公开(公告)日：2012-03-29
申请号：US13249796
申请日：2011-09-30
申请人： Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts
发明人： Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts
IPC分类号： A61K9/14 , A61K31/505 , C07D405/12 , A61K31/506 , C07D417/12 , A61K31/541 , C07D401/12 , C07D409/12 , C07D413/12 , A61K31/5377 , C07D403/12 , A61K31/551 , C07D401/14 , C07D403/14 , C07D239/47 , A61P31/18 , C07D239/48 , B82Y5/00
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; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及具有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的式II的HIV复制抑制剂; 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。

4. 发明授权

US08026245B2 HIV replication inhibiting purine derivatives 有权
标题翻译： HIV复制抑制嘌呤衍生物
公开(公告)号：US08026245B2
公开(公告)日：2011-09-27
申请号：US10573364
申请日：2004-09-21
申请人： Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative , Paulus Joannes Lewi , Marc René de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Jan Heeres , Hendrik Maarten Vinkers , Ruben Gerardus George Leenders , Dirk Alfons Leo Vandenput
发明人： Paul Adriaan Jan Janssen , Paulus Joannes Lewi , Marc René de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Jan Heeres , Hendrik Maarten Vinkers , Ruben Gerardus George Leenders , Dirk Alfons Leo Vandenput
IPC分类号： C07D473/16 , C07D473/18 , A61K31/52 , A61K31/522 , A61P31/18 , C07D473/40
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 —NR17—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各自表示式的基团，其中-CD-表示式-N = CH-NR 17 - （c-1）的二价基团; 或-NR17-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表示式（b）的基团时，B表示式（a）的基团。

5. 发明授权

US08080551B2 HIV inhibiting pyrimidines derivatives 有权
标题翻译： HIV抑制嘧啶衍生物
公开(公告)号：US08080551B2
公开(公告)日：2011-12-20
申请号：US11474855
申请日：2006-06-26
申请人： Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative
发明人： Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen
IPC分类号： A61K31/501 , A61K31/497 , C07D417/12 , C07D417/14 , C07D417/06 , C07D401/12 , C07D401/14 , C07D401/06 , C07D403/12 , C07D403/14 , C07D403/06 , C07D405/12 , C07D405/14 , C07D405/06 , C07D409/14 , C07D409/12 , C07D409/06 , C07D237/20 , C07F9/02 , C07D413/06 , C07D413/12 , C07D413/14 , C07C257/06 , C07C211/40 , C07C233/03 , C07C235/06 , C07C237/20 , C07C239/08 , C07C229/34 , C07C255/49 , C07C207/02
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： HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.
摘要翻译：公开了具有本文定义的式（I）的HIV复制抑制剂。含有HIV复制抑制剂的药物组合物; 使用HIV复制抑制剂治疗艾滋病毒; 还公开了制备HIV复制抑制剂的方法。

6. 发明授权

US07923554B2 HIV inhibiting 1,2,4-triazin-6-one derivatives 有权
公开(公告)号：US07923554B2
公开(公告)日：2011-04-12
申请号：US11573224
申请日：2005-08-10
申请人： Georges Joseph Cornelius Hoornaert , Amuri Kilonda , Jan Heeres , Paulus Joannes Lewi , Marc René de Jonge , Frederik Frans Desiré Daeyaert , Hendrik Maarten Vinkers , Lucien Maria Henricus Koymans , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative
发明人： Georges Joseph Cornelius Hoornaert , Amuri Kilonda , Jan Heeres , Paulus Joannes Lewi , Marc René de Jonge , Frederik Frans Desiré Daeyaert , Hendrik Maarten Vinkers , Lucien Maria Henricus Koymans , Paul Adriaan Jan Janssen
IPC分类号： C07D253/07 , C07D253/065 , A61K31/53 , A61P31/18
CPC分类号： C07D253/075
摘要： The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(═O)pR6; —NH—S(═O)pR6; —C(═O)R6; —NHC(═O)H; —C(═O)NHNH2; NHC(═O)R6; C(═NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14; —C(═O)—NHR13; —C(═O)—NR13R14; —C(═O)—R15; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted C1-6alkyloxyC1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 or X2 represents —NR1—; —NH—NH—; —N═N—; —O—; —C(═O)—; —C1-4alkanediyl-; —CHOH—; —S—; —S(═O)p—; —X4—C1-4alkanediyl-; —C1-4alkanediyl-X4—; or —C1-4alkanediyl-X4—C1-4alkanediyl-; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.

7. 发明授权

US07585870B2 HIV replication inhibiting pyrimidines and triazines 有权
标题翻译： HIV复制抑制嘧啶和三嗪
公开(公告)号：US07585870B2
公开(公告)日：2009-09-08
申请号：US10545719
申请日：2004-02-20
申请人： Jerôme Emile Georges Guillemont , Elisabeth Thérese Jeanne Pasquier , Jan Heeres , Kurt Hertogs , Eva Bettens , Paulus Joannes Lewi , Marc René De Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Hendrik Maarten Vinkers , Frank Xavier Jozef Herwig Arts
发明人： Jerôme Emile Georges Guillemont , Elisabeth Thérese Jeanne Pasquier , Jan Heeres , Kurt Hertogs , Eva Bettens , Paulus Joannes Lewi , Marc René De Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Hendrik Maarten Vinkers , Frank Xavier Jozef Herwig Arts
IPC分类号： C07D239/47 , C07D239/48 , C07D407/12 , A61K31/505 , A61P31/18
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。

8. 发明授权

US08828982B2 Pyrimidine derivatives for the prevention of HIV infection 有权
公开(公告)号：US08828982B2
公开(公告)日：2014-09-09
申请号：US12567051
申请日：2009-09-25
申请人： Jan Heeres , Paulus Joannes Lewi , Marc René de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Hendrik Maarten Vinkers , Jéròme Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier , Frank Xavier Jozef Herwig Arts
发明人： Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Marc René de Jonge , Lucien Maria Henricus Koymans , Frederik Frans Desiré Daeyaert , Hendrik Maarten Vinkers , Jéròme Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier
IPC分类号： A01N43/00 , A61K31/33 , A61K39/395
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 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; 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; and pharmaceutical compositions comprising them.

9. 发明授权

US07105522B2 HIV inhibiting pyrazinone derivatives 有权
公开(公告)号：US07105522B2
公开(公告)日：2006-09-12
申请号：US10468447
申请日：2002-03-13
申请人： Paul Adriaan Jan Janssen , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Lucien Maria Henricus Koymans , Marc René de Jonge , Jan Heeres , Frederik Frans Desire Daeyaert , Georges Joseph Cornelius Hoornaert , Frans Josef Cornelius Compernolle , Amuri Kilonda
发明人： Paul Adriaan Jan Janssen , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Lucien Maria Henricus Koymans , Marc René de Jonge , Jan Heeres , Frederik Frans Desire Daeyaert , Georges Joseph Cornelius Hoornaert , Frans Josef Cornelius Compernolle , Amuri Kilonda
IPC分类号： A61K31/4965 , C07D401/00 , C07D403/00 , C07D405/00 , C07D241/02
CPC分类号： C07D241/20
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 R1 is hydrogen, hydroxy, cyano, amino, mono-or di(C1-4alkyl)amino, formyl, carboxyl, C1-6alkyl, hydroxyC1-6alkyl, polyhaloC1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkylcarbonyl, aminocarbonyl, —S(═O)m—NH2, mono-or di(C1-4alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy, aryl, arylC1-6alkyl or aryloxy; R2 is hydrogen; halo; mercapto; formyl; cyano; carboxy; azido; hydroxy; oxiranyl; amino; mono- or di(C1-4alkyl)amino; formylamino; R5R6N—C(═O)—; R7—N═C(R8)—; C1-6alkyl-S(═O)m; aryl-S(═O)m; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C1-6alkyloxy; hydroxyC1-6alkyloxy; aminoC1-6alkyloxy; mono- or di(C1-4alkyl)amino-C1-6alkyloxy; C1-6alkylcarbonyl; arylcarbonyl; Het1carbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aryl; aryloxy; arylC1-6alkyloxy; arylthio; arylC1-6alkylthio; mono- or di(aryl)amino; Het1; Het1oxy; Het1thio; Het1C1-6alkyloxy; Het1C1-6alkylthio; mono- or di(Het1)amino; C3-7cycloalkyl; C3-7cycloalkyloxy; C3-7cycloalkylthio; C1-6alkylthio; hydroxyC1-6alkylthio; aminoC1-6alkylthio; mono- or di(C1-4alkyl)aminoC1-6alkylthio; optionally substituted C1-6alkyl; R3 or R4 each independently represent optionally be substituted phenyl, pyridyl, pyrimidinyl, pyrazinyl or pyridazinyl; —X— is a bivalent radical selected from —NR14—, —NH—NH—, —N═N—, —O—, —C1-6alkanediyl-, —C(═O)—, —CHOH—, —S—, —S(═O)m—; aryl is optionally substituted phenyl; Het1, Het2 or Het3 represent an optionally substituted monocyclic or bicyclic heterocycle; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

10. 发明授权

US6150360A Trisubstituted 1,3,5-Triazine Derivatives 失效
标题翻译：三取代1,3,5-三嗪衍生物
公开(公告)号：US6150360A
公开(公告)日：2000-11-21
申请号：US276362
申请日：1999-03-25
申请人： Frederik Frans Desire Daeyaert , Bart De Corte , Marc Rene De Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici
发明人： Frederik Frans Desire Daeyaert , Bart De Corte , Marc Rene De Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici
IPC分类号： A61K31/53 , A61P31/18 , C07D251/42 , C07D251/50 , C07D251/52 , C07D251/66 , C07D251/70 , C07D401/12 , C07D403/12 , C07D413/14 , C07D31/54
CPC分类号： C07D251/42 , C07D251/50 , C07D251/52 , C07D251/66 , C07D251/70 , C07D403/12
摘要： This invention concerns the use of the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR.sup.4 or N; n is 0, 1, 2, 3 or 4; R.sup.1 and R.sup.2 are each independently selected from hydrogen, hydroxy, C.sub.1-12 alkyl, C.sub.1-12 alkyloxy, C.sub.1-12 alkylcarbonyl, C.sub.1-12 -alkyloxycarbonyl, aryl, amino, mono- or di(C.sub.1-12 alkyl)amino, mono- or di(C.sub.1-12 alkyl)aminocarbonyl wherein each of the aforementioned C.sub.1-12 alkyl groups may optionally and each individually be substituted; or R.sup.1 and R.sup.2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C.sub.1-12 alkyl)aminoC.sub.1-4 alkylidene; R.sup.3 is hydrogen, aryl, C.sub.1-6 alkylcarbonyl, optionally substituted C.sub.1-6 alkyl; and each R.sup.4 independently is hydroxy, halo, C.sub.1-6 alkyl, C.sub.1-6 -alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is --X--R.sup.5 or --X--Alk--R.sup.6 ; wherein R.sup.5 and R.sup.6 each independently are indanyl, indolyl or phenyl; each of said indanyl, indolyl or phenyl may be substituted; and X is --NR.sup.3 --, --NH--NH--, --N.dbd.N--, --O--, --S--, --S(.dbd.O)-- or --S(.dbd.O).sub.2 --; aryl is optionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I化合物在N-氧化物，其药学上可接受的加成盐和立体化学异构形式中的用途，其中A是CH，CR 4或N; n为0,1,2,3或4; R 1和R 2各自独立地选自氢，羟基，C 1-12烷基，C 1-12烷氧基，C 1-12烷基羰基，C 1-12烷氧基羰基，芳基，氨基，单或二（C 1-12烷基）氨基，单或二 C 1-12烷基）氨基羰基，其中每个上述C 1-12烷基可以任选地和各自独立地被取代; 或R 1和R 2可以一起形成吡咯烷基，哌啶基，吗啉基，叠氮基或单或二（C 1-12烷基）氨基C 1-4亚烷基; R3是氢，芳基，C1-6烷基羰基，任选取代的C 1-6烷基; 并且每个R 4独立地是羟基，卤素，C 1-6烷基，C 1-6 - 烷氧基，氰基，氨基羰基，硝基，氨基，三卤代甲基或三卤代甲氧基; L是-X-R5或-X-Alk-R6; 其中R 5和R 6各自独立地为茚满基，吲哚基或苯基; 所述二氢化茚基，吲哚基或苯基中的每一个可以被取代; 并且X是-NR 3 - ， - NH-NH - ， - N = N - ， - O - ， - S - ， - S（= O） - 或-S（= O）芳基是任选取代的苯基; Het是任选取代的脂族或芳族杂环基; 用于制造用于治疗患有HIV（人类免疫缺陷病毒）感染的受试者的药物。它还涉及作为式（I）化合物的亚组的新化合物，其制备方法和包含它们的药物组合物。

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