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1. 发明授权

US09487518B2 HIV inhibiting bicyclic pyrimidine derivatives 有权
标题翻译： HIV抑制双环嘧啶衍生物
公开(公告)号：US09487518B2
公开(公告)日：2016-11-08
申请号：US13410779
申请日：2012-03-02
申请人： Jerôme Emile Georges Guillemont , Mikaël Paugam , Bruno Francois Marie Delest , Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts
发明人： Jerôme Emile Georges Guillemont , Mikaël Paugam , Bruno Francois Marie Delest , Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen
IPC分类号： C07D487/04 , A61K31/519 , C07D473/00 , C07D473/34 , A61P31/18 , A61K31/52
CPC分类号： C07D487/04 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/34
摘要： HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(═O)pR6; C(═NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH═N—NH—C(═O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; -A-B— is —CR5═N—, —N═N—, —CH2—CH2—, —CS—NH—, —CO—NH—, —CH═CH—; and the use of these compounds for the prevention or the treatment of HIV infection.

2. 发明授权

US08946248B2 HIV inhibiting 5-substituted pyrimidines 有权
标题翻译： HIV抑制5-取代嘧啶
公开(公告)号：US08946248B2
公开(公告)日：2015-02-03
申请号：US11576315
申请日：2005-09-29
申请人： Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
发明人： Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
IPC分类号： C07D239/48 , A61K31/505 , C07D239/50
CPC分类号： C07D239/48 , C07D239/50
摘要： HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A is —CH2—CH2—, —CH═CH—, —C≡C—; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, R2 hydroxy, halo, C1-6alkyl, carboxyl, cyano, —C(═O)R6, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl; X1 is —NR1—, —O—, —S—, —S(═O)p—; R3 is H, C1-6alkyl, halo; R4 is H, C1-6alkyl, halo; R5 is nitro, amino, mono- and diC1-4alkylamino, aryl, halo, —CHO, —CO—R6, —COOR7, —NH—C(═O)H, —NH—C(═O)R6, —CH═N—O—R8; R6 is C1-4alkyl, amino, mono- or di(C1-4alkyl)amino or polyhaloC1-4alkyl; R7 is hydrogen, C1-6alkyl, arylC1-6alkyl; R8 is hydrogen, C1-6alkyl, aryl; p is 1 or 2; aryl is optionally substituted phenyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.
摘要翻译：其中A是-CH 2 -CH 2 - ， - CH = CH - ， - C≡C-;其中A是-CH 2 -CH 2 - ， - CH = CH - ， - C≡C-; R1是氢，芳基，甲酰基，C1-6烷基羰基，C1-6烷基，C1-6烷氧基羰基，R2羟基，卤素，C1-6烷基，羧基，氰基，-C（= O）R6，硝基，氨基，单或二 C 1-6烷基）氨基，多卤甲基; X 1是-NR 1 - ， - O - ， - S - ， - S（= O）p - ; R 3是H，C 1-6烷基，卤素; R4是H，C1-6烷基，卤素; R 5是硝基，氨基，单和二C 1-4烷基氨基，芳基，卤素，-CHO，-CO-R 6，-COOR 7，-NH-C（= O）H，-NH-C（= = N-O-R8; R 6是C 1-4烷基，氨基，单或二（C 1-4烷基）氨基或多卤代C 1-4烷基; R 7是氢，C 1-6烷基，芳基C 1-6烷基; R8是氢，C1-6烷基，芳基; p为1或2; 芳基是任选取代的苯基; 含有这些化合物作为活性成分的药物组合物及其制备方法。

3. 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。

4. 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.

5. 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。

6. 发明申请

US20090181993A1 HIV INHIBITING 5-HETEROCYCLYL PYRIMIDINES 有权
公开(公告)号：US20090181993A1
公开(公告)日：2009-07-16
申请号：US11575818
申请日：2005-09-29
申请人： Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
发明人： Jerôme Emile Georges Guillemont , Jan Heeres , Paulus Joannes Lewi
IPC分类号： A61K31/506 , C07D403/04 , C07D401/04 , C07D405/04 , C07D413/14 , C07D417/04 , A61P31/12
CPC分类号： C07D405/04 , C07D401/04 , C07D403/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04
摘要： HIV replication inhibitors of formula (I), N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; S(═O)pR6; C(═NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(O)—R10; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C1-6alkenyl or C2-6 alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R3; X1 is —NR1—, —O—, —C(═O)—, —CH2—, —CHOH—, —S—, —S(═O)p—R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X3—R7; R4 is halo; OH; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; R5 is a 5- or 6-membered completely unsaturated ring system wherein 1-4 ring members are nitrogen, oxygen or sulfur; which ring may optionally be substituted and may optionally be annelated with a benzene ring; methods for their preparation and pharmaceutical compositions comprising them. The invention also relates to the use of these compounds for the prevention or the treatment of HIV infection.

7. 发明申请

US20090124644A1 HIV INHIBITING 2-(4-CYANOPHENYLAMINO) PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：艾滋病毒抑制2-（4-氰基苯胺）吡嗪衍生物
公开(公告)号：US20090124644A1
公开(公告)日：2009-05-14
申请号：US11813772
申请日：2006-01-27
申请人： Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts , Rudolf Leemans , Luc Jozef Raphael Moens
发明人： Jan Heeres , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts , Rudolf Leemans , Luc Jozef Raphael Moens
IPC分类号： A61K31/505 , C07D239/24 , A61P31/18
CPC分类号： C07D239/50 , C07D239/48
摘要： HIV replication inhibitors of formula pharmaceutically acceptable addition salts or stereochemically isomeric forms thereof, wherein X is NR4, S, SO or SO2; the preparation of these compounds as well as pharmaceutical compositions comprising these compounds; the use of these compounds for the prevention or the treatment of HIV infection.
摘要翻译：其药学上可接受的加成盐或立体化学异构形式的HIV复制抑制剂，其中X为NR4，S，SO或SO2; 这些化合物的制备以及包含这些化合物的药物组合物; 使用这些化合物预防或治疗艾滋病毒感染。

8. 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。

9. 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。

10. 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.

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