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1. 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。

2. 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.

3. 发明授权

US07585861B2 HIV inhibiting 1,2,4-triazines 有权
标题翻译： HIV抑制1,2,4-三嗪
公开(公告)号：US07585861B2
公开(公告)日：2009-09-08
申请号：US10544584
申请日：2004-02-05
申请人： Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Jozef Herwig Arts, legal representative , Marc René de Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Ruben Gerardus George Leenders , Georges Joseph Cornelius Hoomaert , Amuri Kilonda , Donald William Ludovici
发明人： Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Marc René de Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Ruben Gerardus George Leenders , Georges Joseph Cornelius Hoomaert , Amuri Kilonda , Donald William Ludovici
IPC分类号： C07D253/075 , A61K31/53 , A61P31/18 , C07D403/12 , 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。

4. 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.

5. 发明授权

US07514445B2 Heteroaryl amines as glycogen synthase kinase 3β inhibitors (GSK3 inhibitors) 有权
标题翻译：杂芳基胺作为糖原合酶激酶3β抑制剂（GSK3抑制剂）
公开(公告)号：US07514445B2
公开(公告)日：2009-04-07
申请号：US10493452
申请日：2002-10-29
申请人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts , Christopher John Love , Paul Adriaan Jan Janssen , Paulus Joannes Lewi , Jan Heeres , Marc René de Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Koen Jeanne Alfons Van Aken , Gaston Stanislas Marcella Diels
发明人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts , Christopher John Love , Paul Adriaan Jan Janssen , Paulus Joannes Lewi , Jan Heeres , Marc René de Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Koen Jeanne Alfons Van Aken , Gaston Stanislas Marcella Diels
IPC分类号： A61K31/506 , A61P3/10 , A61P25/28 , A61P25/02 , C07D403/06 , C07D403/12 , C07D403/14
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; R1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; R3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; R21; R21-C1-6烷基; 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）NHNH 2; R7-C（-O）-NH-; R 21 -C（-O）-NH-; -C（ - NH）R 7 -C（-NH）R 21; R4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。

6. 发明授权

US08003789B2 HIV replication inhibiting pyrimidines 有权
标题翻译： HIV复制抑制嘧啶
公开(公告)号：US08003789B2
公开(公告)日：2011-08-23
申请号：US11930835
申请日：2007-10-31
申请人： Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries
发明人： Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries
IPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61P31/18
CPC分类号： A61K31/505 , A61K31/5513
摘要： This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, 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, 5-membered heterocyclic ring; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or —X—R3; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl, optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or 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, 13 NHC(═O)R6,—C(═NH)R6, aryl; for the treatment of subjects suffering from HIV infection.
摘要翻译：本发明涉及式I化合物的N-氧化物，药学上可接受的加成盐，季胺，其立体化学异构体形式的用途，其中-a1 = a2-a3 = a4形成苯基，吡啶基，嘧啶基，哒嗪基，吡嗪基，乙烯基; n为0〜5; R 1是氢，芳基，甲酰基，C 1-6烷基羰基，C 1-6烷基，C 1-6烷氧基羰基，取代的C 1-6烷基，取代的C 1-6烷氧基C 1-6烷基羰基; R2是羟基，卤素，任选取代的C 1-6烷基，C 2-6烯基或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，羧基，氰基，硝基，氨基，单或二（C 1-6烷基）氨基，多卤代甲基，多卤代甲氧基，多卤甲硫基，-S（= O）pR 6，-NH-S（= O）pR 6，-C（= O）R 6，-NHC（= O）H，-C（= O）NHNH 2， NHC（= O）R 6，-C（= NH）R 6，5元杂环; L是任选取代的C 1-10烷基，C 2-10烯基，C 2-10炔基或C 3-7环烷基; 或-X-R 3; Q是氢，C 1-6烷基，卤素，多卤代-C 1-6烷基，任选取代的氨基; Y表示羟基，卤素，C 3-7环烷基，任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基，C 1-6烷氧基，C 1-6烷氧基羰基，羧基，氰基，硝基，氨基，单 - 或二（C 1-6烷基）氨基，多卤甲基，多卤代甲氧基，多卤甲硫基，-S（= O）pR 6，-NH-S（= O）pR 6，-C（= O）R 6，-NHC（= O）H，-C（= O）NHNH 2， NHC（= O）R 6，-C（= NH）R 6，芳基; 用于治疗患有艾滋病毒感染的受试者。

7. 发明授权

US07276510B2 HIV replication inhibitors 有权
标题翻译： HIV复制抑制剂
公开(公告)号：US07276510B2
公开(公告)日：2007-10-02
申请号：US10275931
申请日：2001-05-03
申请人： Michael Joseph Kukla , Donald William Ludovici , Robert William Kavash , Bart Lieven Daniel De Corte , Jan Heeres , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Marc René de Jonge , Koen Jeanne Alfons Van Aken , Alain Krief , Ruben Gerardus George Leenders
发明人： Michael Joseph Kukla , Donald William Ludovici , Robert William Kavash , Bart Lieven Daniel De Corte , Jan Heeres , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Marc René de Jonge , Koen Jeanne Alfons Van Aken , Alain Krief , Ruben Gerardus George Leenders
IPC分类号： C07D239/46 , C07D239/48 , A61K31/505 , C07D401/12
CPC分类号： C07D239/47 , C07D239/48 , C07D251/16 , C07D251/50 , C07D401/12
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, provided that when Q is halo then Z is N; or when Q is polyhaloC1-6alkyl then Y is hydrogen or C1-6alkyl; 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的HIV复制抑制剂，条件是当Q为卤素时，Z为N; 或当Q为多卤C 1-6烷基时，则Y为氢或C 1-6烷基; 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。

8. 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.

9. 发明授权

US07034019B2 Prodrugs of HIV replication inhibiting pyrimidines 有权
标题翻译： HIV复制抑制嘧啶的药物
公开(公告)号：US07034019B2
公开(公告)日：2006-04-25
申请号：US10275333
申请日：2001-05-03
申请人： Michael Joseph Kukla , Donald William Ludovici , Robert William Kavash , Bart Lieven Daniel De Corte , Jan Heeres , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Marc René de Jonge , Koen Jeanne Alfons Van Aken , Alain Krief
发明人： Michael Joseph Kukla , Donald William Ludovici , Robert William Kavash , Bart Lieven Daniel De Corte , Jan Heeres , Paul Adriaan Jan Janssen , Lucien Maria Henricus Koymans , Marc René de Jonge , Koen Jeanne Alfons Van Aken , Alain Krief
IPC分类号： C07D239/46 , C07D239/48 , C07D401/12 , A61K31/505
CPC分类号： C07D239/47 , C07D239/48 , C07D401/12
摘要： The present invention concerns compounds of formula (A1)(A2)N—R1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is substituted C1-6alkyl; —S(═O)—R8; —S(═O)2—R8; C7-12alkylcarbonyl; optionally substituted C1-6alkyloxycarbonylC1-6alkylcarbonyl; with R8 being C1-6alkyl, aryl1 or Het1; (A1)(A2)N— is the covalently bonded form of the corresponding intermediate of formula (A1)(A2)N—H, which is a HIV replication inhibiting pyrimidine of formula
摘要翻译：本发明涉及式（A 1 _{1）（A 2 N）NR 1（I）的化合物，N-氧化物形式，药学上可接受的加成盐，季胺和其立体化学异构形式，其中R 1是取代的C 1-6烷基; -S（-O）-R 8; -S（-O）2 -R 8; C 12-12烷基羰基; 任选取代的C 1-6烷氧基羰基C 1-6烷基羰基; 其中R 8是C 1-6烷基，芳基1或Het 1; （A 1 N 2）（A 2 N）N-是式（A 1 SUB）的相应中间体的共价键合形式（A _{2）NH，其是具有下式的HIV复制抑制性嘧啶}}

10. 发明申请

US20110263625A1 HIV REPLICATION INHIBITING PYRIMIDINES 有权
公开(公告)号：US20110263625A1
公开(公告)日：2011-10-27
申请号：US13177188
申请日：2011-07-06
申请人： Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries , Frank Xavier Jozef Herwig Arts
发明人： Bart De Corte , Marc René de Jonge , Jan Heeres , Chih Yung Ho , Paul Adriaan Jan Janssen , Robert W. Kavash , Lucien Maria Henricus Koymans , Michael Joseph Kukla , Donald William Ludovici , Koen Jeanne Alfons Van Aken , Koenraad Jozef Lodewijk Marcel Andries , Frank Xavier Jozef Herwig Arts
IPC分类号： A61K31/505 , A61P31/18 , C07D239/50 , C07D239/48 , C07D239/47
CPC分类号： A61K31/505 , A61K31/5513
摘要： This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a1=a2-a3=a4- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, substituted C1-6alkyl, or substituted C1-6alkyloxyC1-6alkylcarbonyl; each R2 independently is hydroxy, halo, optionally substituted C3-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkylamino, 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 heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is —X—R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is —NR1—, —NH—NH—, —N═N—, —O—, —C(═O)—, —CHOH—, —S—, —S(═O)— or —S(═O)2—; Q is hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or an optionally substituted amino group; Y represents hydroxy, halo, C3-7cycloalkyl, optionally substituted C1-6alkyl, C2-6alkenyl or 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 aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

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