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1. 发明申请

US20070021449A1 Pyrimidine derivatives for the prevention of hiv infection 审中-公开
标题翻译：嘧啶衍生物用于预防HIV感染
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。

2. 发明申请

US20060252764A1 HIV inhibiting pyrimidines derivatives 有权
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.

3. 发明申请

US20060194804A1 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：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。

4. 发明申请

US20060293330A1 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：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。

5. 发明申请

US20070037811A1 Hiv inhibiting 1,2,4-triazines 有权
标题翻译：抑制1,2,4-三嗪
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。

6. 发明申请

US20060063789A1 Aminobenzamide derivatives as glycogen synthase kinase 3 beta inhibitors 审中-公开
标题翻译：氨基苯甲酰胺衍生物作为糖原合酶激酶3β抑制剂
公开(公告)号：US20060063789A1
公开(公告)日：2006-03-23
申请号：US10493446
申请日：2002-10-29
申请人： Eddy Jean Freyne , Peter Antonius , Marc Willems , Werner Johan , Paul Janssen , Paulus Joannes , Jan Heeres , Marc de Jonge , Lucien Koymans , Frederik Daeyaert , Michael Kukla , Hugo Gabriel , Bony Nuydens , Marc Mercken , Donald Ludovici , Herwig Janssen , Paul Maria , Graziella Janssen , Jasmine Werner , Maroussia Janssen , Theodora Arts
发明人： Eddy Jean Freyne , Peter Antonius , Marc Willems , Werner Johan , Paul Janssen , Paulus Joannes , Jan Heeres , Marc de Jonge , Lucien Koymans , Frederik Daeyaert , Michael Kukla , Hugo Gabriel , Bony Nuydens , Marc Mercken , Donald Ludovici , Herwig Janssen , Paul Maria , Graziella Janssen , Jasmine Werner , Maroussia Janssen , Theodora Arts
IPC分类号： A61K31/655 , A61K31/50 , A61K31/4965 , A61K31/513 , C07D241/18 , C07D239/47
CPC分类号： C07D239/42 , A61K31/506 , C07D239/47 , C07D239/48 , C07D239/50 , C07D403/12
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.
摘要翻译：本发明涉及式的化合物

7. 发明申请

US20060211724A1 Hiv integrase inhibitors 审中-公开
标题翻译： Hiv整合酶抑制剂
公开(公告)号：US20060211724A1
公开(公告)日：2006-09-21
申请号：US10554712
申请日：2004-04-27
申请人： Gaston Verschueren , Inge Dierynck , Dominique Louis Nestor Surleraux , Frederik Daeyaert
发明人： Gaston Verschueren , Inge Dierynck , Dominique Louis Nestor Surleraux , Frederik Daeyaert
IPC分类号： C07D471/02 , C07D491/02 , A61K31/4745 , A61K31/407
CPC分类号： C07D487/04
摘要： The present invention concerns the compounds having the formula (1), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof wherein (a) or (b); A, together with the two carbons of the phenyl ring to which it is attached forms a monocyclic aryl or a monocyclic Het2; R1 is hydrogen, halo, nitro, cyano, sultam, sultim, C3-7cycloalkyl, C(═O)—R5, S(═O)y—R6, OR7, NR8R9, C(═NR8)—R5, optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl; R2 is hydrogen, C3-7cycloalkyl, aryl, Het1, Het2, C(═O)—R5, S(═)y—R6OR7, NR8R9, C═NR8)—R5, or optionally polysubstituted C1-6alkyl, optionally polysubstituted C2-6alkenyl or optionally polysubstituted C2-6alkynyl. It further relates to their use as HIV integrase inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with other anti-retroviral agents, and to their use in assays as reference compounds or as reagents.
摘要翻译：本发明涉及具有式（1），N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物的化合物，其中（a）或（b）; A与连接的苯环的两个碳一起形成单环芳基或单环Het 2; R 1是氢，卤素，硝基，氰基，苏丹，仲胺，C 3-7环烷基，C（-O）-R 5 ，S（-O） - ， - - - - - - - - - - - - - - - - - - - - - 任选多取代的C 1-6烷基，任选多取代的C 2 - 烷基，任选多取代的C 1-6烷基，任选多取代的C 1-6烷基， -6个链烯基或任选多取代的C 2-6炔基; R 2是氢，C 3-7环烷基，芳基，Het 1，Het 2，C（ - O）-R 5，S（ - ） - - - - - - - - - - - - - - - - - - - - - - 或者任选多取代的C 1-6烷基，或任选多取代的C 1-6烷基，烷基，任选多取代的C 2-6链烯基或任选多取代的C 2-6 - 炔基。它还涉及它们作为HIV整合酶抑制剂的用途，其制备方法以及包含它们的药物组合物和诊断试剂盒。它还涉及与其它抗逆转录病毒剂的组合，以及它们在测定中作为参考化合物或作为试剂的用途。

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