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1. 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.

2. 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.

3. 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.

4. 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。

5. 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。

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

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。

9. 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。

10. 发明申请

US20070191407A1 PROCESSES FOR THE PREPARATION OF 4-[[4-[[4-(2-CYANOETHENYL)-2,6-DIMETHYLPHENYL]-2-PYRIMIDINYL]AMINO]BENZONITRILE 有权
标题翻译：制备4 - [[4 - [[4-（2-氰基乙基）-2,6-二甲基苯基] -2-吡啶基]氨基]苯并噻唑的方法
公开(公告)号：US20070191407A1
公开(公告)日：2007-08-16
申请号：US11738688
申请日：2007-04-23
申请人： Didier Schils , Joannes Willems , Bart Petrus Anna Medaer , Elisabeth Therese Pasquier , Paul Janssen , Jan Heeres , Ruben Gerardus Leenders , Jerome Guillemont
发明人： Didier Schils , Joannes Willems , Bart Petrus Anna Medaer , Elisabeth Therese Pasquier , Paul Janssen , Jan Heeres , Ruben Gerardus Leenders , Jerome Guillemont
IPC分类号： A61K31/505 , C07D239/48
CPC分类号： C07D239/48 , C07C253/20 , C07C253/30 , C07C255/42
摘要： Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
摘要翻译：用于制备式（I）的4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基] - 氨基] -2-嘧啶基]氨基]苄腈的方法，N-氧化物，提供药学上可接受的酸加成盐，季胺或其立体化学异构形式，所述方法包括：a）使4-（2-氰基乙烯基）-2,6-二甲基苯胺与式（III）的中间体在合适的溶剂; b）在合适的钯催化剂，合适的碱和合适的溶剂的存在下使式（Ⅳ）的中间体与丙烯腈反应; c）使相应的式（I）化合物的酰胺脱水。

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