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31. 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。

32. 发明申请

US20060167253A1 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-2pyrimidinyl]amino]benzonitrile 有权
标题翻译：制备4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基]氨基] -2-2嘧啶基]氨基]苄腈的方法
公开(公告)号：US20060167253A1
公开(公告)日：2006-07-27
申请号：US10523753
申请日：2003-08-07
申请人： Didier Philippe Schils , Joannes Josephus Willems , Bart Petrus Anna Medaer , Elisabeth Pasquier , Paul Janssen , Jan Heeres , Ruben Gerardus Leenders , Jerome Guillemont
发明人： Didier Philippe Schils , Joannes Josephus Willems , Bart Petrus Anna Medaer , Elisabeth Pasquier , Paul Janssen , Jan Heeres , Ruben Gerardus Leenders , Jerome Guillemont
IPC分类号： 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。

33. 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。

34. 发明授权

US07563922B2 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile 有权
标题翻译：制备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
公开(公告)号：US07563922B2
公开(公告)日：2009-07-21
申请号：US11738688
申请日：2007-04-23
申请人： Didier Philippe Robert Schils , Joannes Josephus Maria Willems , Bart Petrus Anna Maria Jozef Medaer , Elisabeth Therese Jeanne Pasquier , Paul Adriaan Jan Janssen , Jan Heeres , Ruben Gerardus George Leenders , Jérôme Emile Georges Guillemont
发明人： Didier Philippe Robert Schils , Joannes Josephus Maria Willems , Bart Petrus Anna Maria Jozef Medaer , Elisabeth Therese Jeanne Pasquier , Paul Adriaan Jan Janssen , Jan Heeres , Ruben Gerardus George Leenders , Jérôme Emile Georges Guillemont
IPC分类号： C07C255/42 , C07C253/30 , C07C253/20 , C07D239/48 , A61K31/505 , A61P31/18
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。

35. 发明授权

US07531548B2 HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines 有权
标题翻译： HIV抑制5-碳环或杂环取代的嘧啶
公开(公告)号：US07531548B2
公开(公告)日：2009-05-12
申请号：US11576068
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 , C07D239/50 , C07D239/34 , C07D239/38 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , A61K31/505 , A61P31/18
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; polyhalomethylthio; —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.
摘要翻译：式（I）的HIV复制抑制剂N-氧化物，药学上可接受的加成盐，季胺或其立体异构形式，其中-a1 = a2-a3 = a4-是-CH-CH-CH-CH-，-N -CH-CH-CH-，-N-CH-N-CH-，-N-CH-CH-N - ，-NN-CH-CH-; -b1 = b2-b3 = b4-是-CH-CH-CH-CH-，-N-CH-CH-CH-，-N-CH-N-CH-，-N-CH-CH-N-， -NN-CH-CH-; 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; R2是OH; 光环; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; 取代的羰基; 羧基; CN; 硝基氨基; 取代氨基; 多卤甲基多卤甲硫基 -S（-O）r R 6; C（-NH）R 6; R2a为CN; 氨基; 取代氨基; 任选取代的C 1-6烷基; 光环; 任选取代的C 2-6烷氧基; 取代的羰基; -CH-N-NH-C（-O）-R16; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6炔基; -C（-N-O-R 8）-C 1-4烷基; R7或-X3-R7; X 1是-NR 1 - ， - O - ， - C（-O） - ，CH 2，-CHOH - ， - S - ， - S（-O） R3为CN; 氨基; C 1-6烷基; 光环; 任选取代的C 1-6烷氧基; 取代的羰基; -CH-N-NH-C（-O）-R16; 取代的C 1-6烷基; 任选取代的C 1-6烷氧基C 1-6烷基; 取代的C 2-6烯基或C 2-6炔基; -C（-N-O-R 8）-C 1-4烷基; R7; -X3-R7; R4是卤素; 哦; 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; CN; 硝基多卤代C1-6烷基; 多卤C 1-6烷氧基; 取代的羰基; 甲酰基氨基; 单或二（C 1-4烷基）氨基或R 7; R5是-Y-CqH2q-L或-CqH2q-Y-CrH2r-L; L是芳基或Het; 制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物以及这些化合物用于预防或治疗HIV感染的用途。

36. 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。

37. 发明授权

US07399856B2 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-2pyrimidinyl]amino]benzonitrile 有权
标题翻译：制备4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基]氨基] -2-2嘧啶基]氨基]苄腈的方法
公开(公告)号：US07399856B2
公开(公告)日：2008-07-15
申请号：US10523753
申请日：2003-08-07
申请人： Didier Philippe Robert Schils , Joannes Josephus Maria Willems , Bart Petrus Anna Maria Jozef Medaer , Elisabeth Therese Jeanne Pasquier , Paul Adriaan Jan Janssen , Jan Heeres , Ruben Gerardus George Leenders , Jérôme Emile Georges Guillemont
发明人： Didier Philippe Robert Schils , Joannes Josephus Maria Willems , Bart Petrus Anna Maria Jozef Medaer , Elisabeth Therese Jeanne Pasquier , Paul Adriaan Jan Janssen , Jan Heeres , Ruben Gerardus George Leenders , Jérôme Emile Georges Guillemont
IPC分类号： C07D239/48 , C07C255/42 , C07C253/30 , C07C253/20 , A61K31/505 , A61P31/18
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。

38. 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.

39. 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}}

40. 发明授权

US06197972B1 Triazolones as apolipoprotein-B synthesis inhibitors 失效
标题翻译：新型三唑酮作为载脂蛋白-B合成抑制剂
公开(公告)号：US06197972B1
公开(公告)日：2001-03-06
申请号：US09251989
申请日：1999-02-17
申请人： Jan Heeres , Leo Jacobus Jozef Backx , Paul August Clement Luyts
发明人： Jan Heeres , Leo Jacobus Jozef Backx , Paul August Clement Luyts
IPC分类号： C07D40506
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： The present invention concerns novel compounds of formula (I). wherein R1 is C1-10alkyl, C3-7cycloalkyl or C1-6alkyl substituted with C3-7cycloalkyl; R2 is hydrogen or C1-6alkyl; Alk represents C1-3alkanediyl; —A— represents a bivalent radical of formula —CH═CH—N═CH— (a), —N═CH—N═CH— (b), —CH═N—N═CH— (c), —CH═CH—CH═N— (d); in said bivalent radicals a hydrogen atom may be replaced by C1-6alkyl; and Ar is unsubstituted phenyl; phenyl substituted with up to two substituents selected from halo, C1-6alkyl or C1—6alkyloxy; unsubstituted naphthyl; or naphthyl substituted with up to two substituents selected from halo, C1-6alkyl or C1-6alkyloxy; the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof. The present invention further comprises the pharmaceutical compositions comprising compounds of formula (I), the preparation thereof as well as the use as a medicine in the treatment of hyperlipidemia.
摘要翻译：本发明涉及新的式（I）化合物，其中R 1是C 1-10烷基，C 3-7环烷基或被C 3-7环烷基取代的C 1-6烷基; R2是氢或C1-6烷基; Alk表示C1-3烷二基; -A-表示式-CH = CH-N = CH-（a），-N = CH-N = CH-（b），-CH = NN = CH-（c），-CH = CH -CH = N-（d）; 在所述二价基团中，氢原子可被C 1-6烷基取代; 和Ar是未取代的苯基; 被至多两个选自卤素，C 1-6烷基或C 1-6烷氧基的取代基取代的苯基; 未取代的萘基; 或被至多两个选自卤素，C 1-6烷基或C 1-6烷氧基的取代基取代的萘基; 其立体化学异构形式及其药学上可接受的酸加成盐。本发明还包含包含式（I）化合物，其制备方法以及用作治疗高脂血症药物的药物组合物。

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