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1. 发明申请

US20050176713A1 Amide derivatives as glycogen synthase kinase 3-beta inhibitors 有权
公开(公告)号：US20050176713A1
公开(公告)日：2005-08-11
申请号：US10493454
申请日：2002-10-29
申请人： Eddy Jean Freyne , Peter Jacobus Johannes Buijnsters , Marc Willems , Werner Constant Embrechts , Jean Fernand Lacrampe , Paul Adriaan Janssen , Herwig Josephus Janssen , Paul Janssen , Graziella Janssen , Jasmine Janssen , Maroussia Godelieve Janssen , Theodora Joanna Arts , Paulus Lewi , Jan Heeres , Marc de Jonge , Lucien Maria Koymans , Frederik Frans Daeyaert , Rony Nuydens , Marc Mercken
发明人： Eddy Jean Freyne , Peter Jacobus Johannes Buijnsters , Marc Willems , Werner Constant Embrechts , Jean Fernand Lacrampe , Paul Adriaan Janssen , Herwig Josephus Janssen , Paul Janssen , Graziella Janssen , Jasmine Janssen , Maroussia Godelieve Janssen , Theodora Joanna Arts , Paulus Lewi , Jan Heeres , Marc de Jonge , Lucien Maria Koymans , Frederik Frans Daeyaert , Rony Nuydens , Marc Mercken
IPC分类号： A61K31/44 , A61K31/4409 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P7/00 , A61P17/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D213/81 , C07D213/82 , C07D239/42 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D407/12 , C07D413/12 , C07D413/14 , C07D417/12 , A61K31/655 , A61K31/4965
CPC分类号： C07D213/81 , C07D213/82 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , 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 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.

2. 发明申请

US20060142571A1 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：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。

3. 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。

4. 发明申请

US20050004125A1 Heteroaryl amines as glycogen synthase kinase 3beta 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：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。

5. 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。

6. 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。

7. 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.

8. 发明申请

US20080085907A1 Hiv Inhibiting Bicyclic Pyrimdine Derivatives 有权
公开(公告)号：US20080085907A1
公开(公告)日：2008-04-10
申请号：US11718181
申请日：2005-10-27
申请人： Jerome Guillemont , Mikael Paugam , Bruno Delest , Jan Heeres , Paulus Lewi , Paul Adriaan Janssen , Frank Javier Arts
发明人： Jerome Guillemont , Mikael Paugam , Bruno Delest , Jan Heeres , Paulus Lewi , Paul Adriaan Janssen , Frank Javier Arts
IPC分类号： C07D473/36 , A61K31/519 , A61K31/52 , A61P31/18 , C07D487/04 , C07D239/70 , C07D473/32
CPC分类号： C07D487/04 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/34
摘要： HIV replication inhibitors of formula (1) 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—; n and m is 0, 1, 2, 3 and in certain cases also 4; 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)—R16; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4 alkyl; R7 or —X—R4; 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)—C1-4 alkyl; R7; —X—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; -A-B— is —CR5═N—, —N═N—, —CH2—CH2—, —CS—NH—, —CO—NH—, —CH═CH—; pharmaceutical compositions comprising these; methods for the preparation of these compounds and compositions; the use of these compounds for the prevention or the treatment of HIV infection.

9. 发明申请

US20070208022A1 HIV INHIBITING 5-CARBO- OR HETEROCYCLYL SUBSTITUTED PYRIMIDINES 有权
公开(公告)号：US20070208022A1
公开(公告)日：2007-09-06
申请号：US11576068
申请日：2005-09-29
申请人： Jerome Guillemont , Jan Heeres , Paulus Lewi
发明人： Jerome Guillemont , Jan Heeres , Paulus Lewi
IPC分类号： A61K31/5377 , A61K31/53 , A61K31/506 , C07D403/02 , C07D413/02
CPC分类号： C07D403/12 , C07D239/48 , C07D239/50 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/14 , C07D417/12
摘要： HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a 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; polyhalo methylthio; —S(═O)rR6; C(═NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C2-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 is —NR1—, —O—, —C(═O)—, CH2, —CHOH—, —S—, —S(═O)r—; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxy C1-6alkyl; 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; polyhalo C1-6alkyl; polyhalo C1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; R5 is —Y—CqH2q-L or —CqH2q—Y—CrH2r-L; L is aryl or Het; processes for the preparation of these compounds, pharmaceutical compositions comprising these compounds as active ingredient and the use of these compounds for the prevention or the treatment of HIV infection.

10. 发明申请

US20050084832A1 Stereotypy test apparatus and methods 审中-公开
标题翻译：定型检验仪器及方法
公开(公告)号：US20050084832A1
公开(公告)日：2005-04-21
申请号：US10499385
申请日：2002-12-19
申请人： Paul Janssen , Paulus Lewi , Roger Rosiers
发明人： Paul Janssen , Paulus Lewi , Roger Rosiers
IPC分类号： A61B5/16 , G06F19/00 , G09B19/00
CPC分类号： A61B5/16 , A61B5/168
摘要： A stereotypy test apparatus 10 is disclosed, which is suitable for interactive use in the diagnosis of a psychiatric disorder. The apparatus comprises an input means in the form of a keypad 14 adapted for physical entry of input signals to the apparatus 10 and a control means 28 which is adapted to prompt a candidate to enter during a test session a succession of said input signals. The control means 28 analyses entered said input signals in order to derive and output from said analysis one or more output signals indicative of at least one value RC, RS which is used in the diagnosis of the presence or absence in said candidate of at least one predetermined psychiatric disorder or of the candidate's predisposition theretowards. The input signals comprise a succession of choices (1-9) selected freely by said candidate from a plurality of mutually independent choices (1-9) and a said output signal RC, RS is indicative of repetitive patterns among said candidate choices.
摘要翻译：公开了一种定型测试装置10，其适用于精神障碍诊断中的互动使用。该装置包括适于将输入信号物理地输入到装置10的小键盘14形式的输入装置和控制装置28，该控制装置28适于提示候选者在测试会话期间输入一系列所述输入信号。控制装置28分析输入的所述输入信号，以便从所述分析中导出和输出表示至少一个值RC，RS的一个或多个输出信号，所述值用于诊断所述候选者是否存在至少一个预期的精神障碍或候选人的倾向。所述输入信号包括由多个相互独立的选择（1-9）中所述候选者自由选择的一系列选择（1-9），并且所述输出信号RC，RS表示所述候选选择中的重复模式。

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