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1. 发明申请

WO2013068551A1 DISUBSTITUTED TRIAZINE DIMERS FOR TREATMENT AND/OR PREVENTION OF INFECTIOUS DISEASES 审中-公开
标题翻译：用于治疗和/或预防感染性疾病的分离的TRIAZINE二聚体
公开(公告)号：WO2013068551A1
公开(公告)日：2013-05-16
申请号：PCT/EP2012/072308
申请日：2012-11-09
申请人： UNIVERSITEIT ANTWERPEN , HEERES, JAN , SHAKTURANA CV
发明人： HEERES, JAN , AUGUSTYNS, Koen , VAN DER VEKEN, Pieter , JOOSSENS, Jurgen , MUTHUSAMY, Venkatraj , MAES, Louis
IPC分类号： C07D251/52 , C07D251/70 , A61K31/53 , A61P31/00 , A61P31/12 , A61P31/18 , A61P33/00 , A61P33/02 , A61P33/06
CPC分类号： C07D403/12 , C07D251/52 , C07D251/70
摘要： The present invention relates to novel compounds (I) containing two disubstituted triazine rings covalently linked by an organic linker, thereby creating dimers. These compounds show activity against the causative infective agents of infectious diseases such as African trypanosomiasis, Chagas disease, Leishmaniasis, Malaria and HIV. The invention further relates to the prevention and/or treatment of these diseases.
摘要翻译：本发明涉及包含通过有机接头共价连接的两个二取代三嗪环的新化合物（I），从而产生二聚体。这些化合物显示针对感染性疾病如非洲锥虫病，恰加斯病，利什曼病，疟疾和艾滋病毒的致病感染因子的活性。本发明还涉及这些疾病的预防和/或治疗。

2. 发明申请

WO2008152081A3 ANTHELMINTIC BENZO[D]ISOXAZOLYL BENZAMIDE DERIVATIVES 审中-公开
标题翻译：苯乙烯衍生物[D]异辛基苯甲酰衍生物
公开(公告)号：WO2008152081A3
公开(公告)日：2009-05-28
申请号：PCT/EP2008057348
申请日：2008-06-12
申请人： JANSSEN PHARMACEUTICA NV , HEERES JAN , LEWI PAULUS JOANNES
发明人： HEERES JAN , LEWI PAULUS JOANNES
IPC分类号： C07D261/20 , A61K31/423
CPC分类号： C07D261/20
摘要： The present invention is concerned with novel anthelmintic N-benzo[d]isoxazol-6-yl-benzamide derivatives and the pharmaceutically acceptable acid addition salts thereof, compositions comprising said novel Compounds, processes for preparing said Compounds and compositions, and the use thereof as a medicine, in particular in treatment, control and prevention of endo- and ectoparasite infections in warm-blooded animals.
摘要翻译：本发明涉及新的驱虫N-苯并[d]异恶唑-6-基 - 苯甲酰胺衍生物及其药学上可接受的酸加成盐，包含所述新化合物的组合物，制备所述化合物和组合物的方法及其用途为一种药物，特别是治疗，控制和预防温血动物的内寄生虫和外寄生虫感染。

3. 发明申请

WO2006035068A3 HIV INHIBITING 5-CARBO- OR HETEROCYCLIC SUBSTITUTED PYRIMIDINES 审中-公开
标题翻译：艾滋病毒抑制5-碳环或杂环取代的吡咯啉
公开(公告)号：WO2006035068A3
公开(公告)日：2006-08-31
申请号：PCT/EP2005054931
申请日：2005-09-29
申请人： TIBOTEC PHARM LTD , GUILLEMONT JEROME EMILE GEORGE , HEERES JAN , LEWI PAULUS JOANNES
发明人： GUILLEMONT JEROME EMILE GEORGE , HEERES JAN , LEWI PAULUS JOANNES
IPC分类号： C07D239/48 , A61K31/505 , A61P31/18 , C07D239/50 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/14 , C07D417/12
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 -a 1 =a 2 -a 3 =a 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH- CH=N-, -N=N-CH=CH-; -b 1 =b 2 -b 3 =b 4 - is -CH=CH-CH=CH-, -N=CH-CH=CH-, -N=CH-N=CH-, -N=CH-CH=N-, -N=N-CH=CH-; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally subst ituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; R 2 is OH; halo; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalo methylt hio; -S(=O)rR 6 ; C(=NH)R 6 ; R 2a is CN; amino; substituted amino; optionally subst ituted C 1-6 alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R 16 ; optionally substituted C 1-6 alkyloxy C 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 or -X 3 -R 7 ; X 1 is -NR 1 -, -O-, -C(=O)-, CH 2 , -CHOH-, -S-, -S(=O) r -; R 3 is CN; amino; C 1-6 alkyl; halo; optionally substituted C 1-6 alkyloxy; substituted carbonyl; -CH=N-NH-C(=O)-R 16 ; substituted C 1-6 alkyl; optionally substituted C 1-6 alkyloxy C 1-6 alkyl; substituted C 2-6 alkenyl or C 2-6 alkynyl; -C(=N-O-R 8 )-C 1-4 alkyl; R 7 ; -X 3 -R 7 ; R 4 is halo; OH; optionally substituted C 1-6 alkyl, C 2-6 alkenyl or C 2-6 alkynyl; C 3-7 cycloalkyl; C 1-6 alkyloxy; CN; nitro; polyhalo C 1-6 alkyl; polyhalo C 1-6 alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C 1-4 alkyl)amino or R 7 ; R 5 is-Y-C q H2 q -L or -C q H 2q -Y-C r H 2r -L; L is aryl or Het; processes for the preparation of these compounds, pharmaceut ical 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-a-1-a-2 -a 是-CH = CH-CH = CH-，-N = CH-CH = CH-，-N = CH-N = CH-， -N = CH-CH = N-，-N = N-CH = CH-; b = 1〜3 = b 4 - 是-CH = CH-CH = CH - ，-N = CH-CH = CH-，-N = CH-N = CH-，-N = CH-CH = N-，-N = N-CH = CH-; R 1是氢; 芳基; 甲酰基; ç_{1-6 烷基羰基; 任选地取代C 1-6烷基; ç_{1-6 烷氧基羰基; R 2是OH; 光环; 任选取代的C 1-6烷基，C 2-6 - 烯基或C 2-6 - 亚炔基; 取代的羰基; 羧基; CN; 硝基; 氨基; 取代氨基; 多卤代; 多卤代甲基 -S（= O）RR ^{6 ; C（= NH）R ^{6 ; R 2a是CN; 氨基; 取代氨基; 任选地取代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）-R ^{16 ; 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亚炔基; -C（= N-O-R ^{8 ） - c _{1-4 烷基; R 7或-X 3 -R 7; X 1是-NR 1 - ， - O - ， - C（= O） - ，CH 2，-CHOH - ，-S - ， - （= O） - ， - R 3是CN; 氨基; ç_{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）-R ^{16 ; 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亚炔基; -C（= N-O-R ^{8 ） - c _{1-4 烷基; [R ^{7 ; -X _{3 -R ^{7 ; R 4是卤素; 哦; 任选取代的C 1-6烷基，C 2-6 - 烯基或C 2-6 - 亚炔基; ç_{3-7 环烷基; ç_{1-6 烷氧基; CN; 硝基; 多卤C 1-6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; R 5是-Y C q H 2 q -L或-C Q 2 H 2 q / SUB > -YC _{- [R ħ_{2R -L; L是芳基或Het; 这些化合物的制备方法，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。}}}}}}}}}}}}}}}}}}

4. 发明申请

WO2004016581A1 PROCESSES FOR THE PREPARATION OF 4-[[4-[[4-(2-CYANOETHENYL)-2,6-DIMETHYLPHENYL]AMINO]-2-PYRIMIDINYL]AMINO]BENZONITRILE 审中-公开
标题翻译：制备4 - [[4 - [[4-（2-氰基乙基）-2,6-二甲基苯基]氨基] -2-吡啶基]氨基]苯并噻唑的方法
公开(公告)号：WO2004016581A1
公开(公告)日：2004-02-26
申请号：PCT/EP2003/050366
申请日：2003-08-07
申请人： JANSSEN PHARMACEUTICA N.V. , GUILLEMONT, Jérôme, Emile, Georges , SCHILS, Didier, Philippe, Robert , WILLEMS, Joannes, Josephus, Maria , MEDAER, Bart, Petrus, Anna, Maria, Jozef , PASQUIER, Elisabeth, Therese, Jeanne , JANSSEN, Paul, Adriaan, Jan , HEERES, Jan , LEENDERS, Ruben, Gerardus, George
发明人： SCHILS, Didier, Philippe, Robert , WILLEMS, Joannes, Josephus, Maria , MEDAER, Bart, Petrus, Anna, Maria, Jozef , PASQUIER, Elisabeth, Therese, Jeanne , JANSSEN, Paul, Adriaan, Jan , HEERES, Jan , LEENDERS, Ruben, Gerardus, George
IPC分类号： C07C255/42
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，N-氧化物，提供了可接受的酸加成盐，季胺或其立体化学异构形式，所述方法包括a）在合适的存在下，使4-（2-氰基乙烯基）-2,6-二甲基苯胺与式（III）的中间体反应溶剂; 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。

5. 发明申请

WO03037891A8 HETEROARYL AMINES AS GLYCOGEN SYNTHASE KINASE 3BETA INHIBITORS (GSK3 INHIBITORS) 审中-公开
标题翻译：作为GLYCOGEN SYNTHASE KINASE 3BETA抑制剂（GSK3抑制剂）的HETEROARYL AMINES
公开(公告)号：WO03037891A8
公开(公告)日：2003-09-04
申请号：PCT/EP0212077
申请日：2002-10-29
申请人： JANSSEN PHARMACEUTICA NV , FREYNE EDDY JEAN EDGARD , BUIJNSTERS PETER JACOBUS JOHAN , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA , LOVE CHRISTOPHER JOHN , JANSSEN PAUL ADRIAAN JAN , LEWI PAULUS JOANNES , HEERES JAN , DE JONGE MARC RENE , KOYMANS LUCIEN MARIA HENRICUS , VINKERS HENDRIK MAARTEN , VAN AKEN KOEN JEANNE ALFONS , DIELS GASTON STANISLAS MARCELL
发明人： FREYNE EDDY JEAN EDGARD , BUIJNSTERS PETER JACOBUS JOHAN , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA , LOVE CHRISTOPHER JOHN , JANSSEN PAUL ADRIAAN JAN , LEWI PAULUS JOANNES , HEERES JAN , DE JONGE MARC RENE , KOYMANS LUCIEN MARIA HENRICUS , VINKERS HENDRIK MAARTEN , VAN AKEN KOEN JEANNE ALFONS , DIELS GASTON STANISLAS MARCELL
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
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 (I), 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 C1-6alkyloxy C1-6alkylcarbonyl; 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 C1-6alkenyl 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(=0)-; R21-S(=0)p-; R7-S =O R7-S(=O)p-NH-; R21-S(=O)p-NH-; R7-C(=0)-; -NHC(=0)H; -C(=O)NHNH2; R7-C(=O)-NH-; R21-C(=O)-NH-; -C(=NH)R7; -C(=NH)R21; R° 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（I）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为6-元杂环; R1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 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 1-6烯基或C 2-6炔基; C1-6烷; C 1-6烷; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; 羧基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C 1-6烷基; R21-O-; R21-S-; R21-C（= O） - ; R21-S（= O）p - ; R7-S = O R7-S（= O）p-NH-; R21-S（= O）P-NH-; R7-C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; R7-C（= O）-NH-; R21-C（= O）-NH-; -C（= NH）R 7; -C（= NH）R 21; R°是任选取代的杂环，条件是-X-R 2和/或R 3不是氢;它们的用途，包含它们的药物组合物及其制备方法。

6. 发明申请

WO2003037877A1 AMINOBENZAMIDE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3β INHIBITORS 审中-公开
标题翻译：氨基苯甲酸衍生物作为GLYCOGEN SYNTHASE KINASE 3β抑制剂
公开(公告)号：WO2003037877A1
公开(公告)日：2003-05-08
申请号：PCT/EP2002/012079
申请日：2002-10-29
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desire , KUKLA, Michael, Joseph , GEERTS, Hugo, Alfons, Gabriel , NUYDENS, Rony, Maria , MERCKEN, Marc, Hubert , LUDOVICI, Donald, William
发明人： FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desire , KUKLA, Michael, Joseph , GEERTS, Hugo, Alfons, Gabriel , NUYDENS, Rony, Maria , MERCKEN, Marc, Hubert , LUDOVICI, Donald, William
IPC分类号： C07D239/30
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 (I),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; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyloxyC 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R 3 is hydrogen; hydroxy; halo; optionally substituted C 1-6 alkyl or C 2-6 alkenyl or C 2-6 alkynyl; C 1-6 alkyloxy; C 1-6 alkylthio; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; polyhaloC 1-6 alkylthio; R 21 ; R 21 -C 1-6 alkyl; 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 4a or R 4b each independently represent hydrogen, R 8 , -Y 1 -NR 9 -Y 2 -NR 10 R 11 , -Y 1 -NR 9 -Y 1 -R 8 , -Y 1 -NR 9 R 10 ; provided that -X-R 2 and/or R 3 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（I）化合物，其中N为氧化物，其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为6-元杂环; R 1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 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O或S; 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; C1-6烷; C 1-6烷; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; 羧基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; [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 4a或R 4b各自独立地表示氢，R 8，-Y 1 -NR 9 -Y 2 -NR 10 R 11，-Y 1 -NR 9 -Y 1 -R 8，-Y1-NR 9 R 10; 条件是-X-R 2和/或R 3不是氢;它们的用途，包含它们的药物组合物及其制备方法。

7. 发明申请

WO2003037869A1 AMIDE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3-BETA INHIBITORS 审中-公开
标题翻译：作为GLYCOGEN SYNTHASE KINASE 3-BETA抑制剂的酰胺衍生物
公开(公告)号：WO2003037869A1
公开(公告)日：2003-05-08
申请号：PCT/EP2002/012067
申请日：2002-10-29
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LACRAMPE, Jean, Fernand, Armand , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desire , KUKLA, Michael, Joseph , GEERTS, Hugo, Alfons, Gabriel , NUYDENS, Rony, Maria , MERCKEN, Marc, Hubert , LUDOVICI, Donald, William
发明人： FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LACRAMPE, Jean, Fernand, Armand , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , DAEYAERT, Frederik, Frans, Desire , KUKLA, Michael, Joseph , GEERTS, Hugo, Alfons, Gabriel , NUYDENS, Rony, Maria , MERCKEN, Marc, Hubert , LUDOVICI, Donald, William
IPC分类号： C07D213/82
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 (I' ),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; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyloxyC 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R 3 is hydrogen; hydroxy; halo; optionally substituted C 1-6 alkyl or C 2-6 alkenyl or C 2-6 alkynyl; C 1-6 alkyloxy; C 1-6 alkylthio; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; polyhaloC 1-6 alkylthio; R 21 ; R 21 -C 1-6 alkyl; 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 4a or R 4b each independently represent hydrogen, R 8 , -Y 1 -NR 9 -Y 2 -NR 10 R 11 , -Y 1 -NR 9 -Y 1 -R 8 , -Y 1 -NR 9 R 10 ; provided that -X-R 2 and/or R 3 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（I'）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表示6-元杂环; R 1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 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O或S; 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; C1-6烷; C 1-6烷; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; 羧基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; [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 4a或R 4b各自独立地表示氢，R 8，-Y 1 -NR 9 -Y 2 -NR 10 R 11，-Y 1 -NR 9 -Y 1 -R 8，-Y1-NR 9 R 10; 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。

8. 发明申请

WO1996001821A1 ANTI-HELICOBACTER HETEROCYCLIC DERIVATIVES OF AZOLONES 审中-公开
标题翻译：丙二醇的抗真菌剂杂环衍生物
公开(公告)号：WO1996001821A1
公开(公告)日：1996-01-25
申请号：PCT/EP1995002616
申请日：1995-07-05
申请人： JANSSEN PHARMACEUTICA N.V. , HEERES, Jan , STOKBROEKX, Raymond, Antoine , WILLEMS, Marc , HENDRICKX, Robert, Jozef, Maria
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D403/12
CPC分类号： C07D401/14 , C07D403/12 , C07D413/12 , C07D417/14
摘要： The invention is concerned with the compounds having formula (I), the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y is CH or N; R , R and R each independently are hydrogen or C1-4alkyl; R and R each independently are hydrogen, halo, C1-4alkyl, C1-4alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R is pyridinyl optionally substituted with up to two C1-4alkyl groups; di(C1-4alkyl)hydroxypyridinyl; di(C1-4alkyl)C1-4alkyloxypyridinyl; pyridazinyl optionally substituted with C1-4alkyloxy; pyrimidinyl optionally substituted with hydroxy or C1-4alkyloxy; thiazolyl optionally substituted with C1-4alkyl; thiadiazolyl optionally substituted with C1-4alkyl; benzoxazolyl or benzothiazolyl; or R is pyrazinyl or pyridazinyl substituted with C1-4alkyl; Z is C=O or CHOH; and (a) is a radical of formula (a-1), (a-2), (a-3), (a-4), (a-5), (a-6), or (a-7). Compositions comprising said compounds, processes for preparing the same and the use of these compounds as a medicine.
摘要翻译：本发明涉及具有式（I）的化合物，其药学上可接受的加成盐和立体化学异构形式，其中Y是CH或N; R 1，R 2和R 3各自独立地是氢或C 1-4烷基; R 4和R 5各自独立地为氢，卤素，C 1-4烷基，C 1-4烷氧基，羟基，三氟甲基，三氟甲氧基或二氟甲氧基; R 6是任选被至多两个C 1-4烷基取代的吡啶基; 二（C 1-4烷基）羟基吡啶基; 二（C 1-4烷基）C1-4alkyloxypyridinyl; 任选被C 1-4烷氧基取代的哒嗪基; 任选被羟基或C 1-4烷氧基取代的嘧啶基; 任选被C 1-4烷基取代的噻唑基; 任选被C 1-4烷基取代的噻二唑基; 苯并恶唑基或苯并噻唑基; 或R 6是被C 1-4烷基取代的吡嗪基或哒嗪基; Z是C = O或CHOH; 和（a）是式（a-1），（a-2），（a-3），（a-4），（a-5），（a-6）或（a-7））。包含所述化合物的组合物，其制备方法以及这些化合物作为药物的用途。

9. 发明申请

WO1996001818A1 SULFONAMIDE DERIVATIVES OF AZOLONES ANTI-HELICOBACTER AGENTS 审中-公开
标题翻译：阿洛莫隆抗真菌剂的磺酰胺衍生物
公开(公告)号：WO1996001818A1
公开(公告)日：1996-01-25
申请号：PCT/EP1995002619
申请日：1995-07-05
申请人： JANSSEN PHARMACEUTICA N.V. , HEERES, Jan , STOKBROEKX, Raymond, Antoine , MOSTMANS, Joseph, Hector , VAN DER VEKEN, Louis, Jozef, Elisabeth
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D249/12
摘要： The invention is concerned with the compounds having formula (I) the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y is CH or N; R , R and R each independently are hydrogen or C1-4alkyl; R and R each independently are hydrogen, halo, C1-4alkyl, C1-4alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R is C1-4alkyl; or phenyl optionally substituted with halo, C1-4alkylcarbonylamino, C1-4alkyloxy, C1-4alkyl or nitro; Z is C=O or CHOH; and (1) is a radical of formula ((a-1), (a-2), (a-3), (a-4), (a-5), (a-6), or (a-7). Compositions comprising said compounds, processes for preparing the same and the use of these compounds as a medicine.
摘要翻译：本发明涉及具有式（I）的药学上可接受的加成盐及其立体化学异构形式的化合物，其中Y是CH或N; R 1，R 2和R 3各自独立地是氢或C 1-4烷基; R 4和R 5各自独立地为氢，卤素，C 1-4烷基，C 1-4烷氧基，羟基，三氟甲基，三氟甲氧基或二氟甲氧基; R 6是C 1-4烷基; 或任选被卤素，C 1-4烷基羰基氨基，C 1-4烷氧基，C 1-4烷基或硝基取代的苯基; Z是C = O或CHOH; 和（1）是式（a-1），（a-2），（a-3），（a-4），（a-5），（a-6） 7）。包含所述化合物的组合物，其制备方法以及这些化合物作为药物的用途。

10. 发明申请

WO1995019983A1 WATERSOLUBLE AZOLE ANTIFUNGALS 审中-公开
标题翻译：水溶性氨基酸反义词
公开(公告)号：WO1995019983A1
公开(公告)日：1995-07-27
申请号：PCT/EP1995000174
申请日：1995-01-17
申请人： JANSSEN PHARMACEUTICA N.V. , HEERES, Jan , BACKX, Leo, Jacobus, Jozef , VAN DER EYCKEN, Luc, Alfons, Leo , ODDS, Frank, Christopher , MESENS, Jean, Louis
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07F09/6558
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07F9/65586
摘要： A compound of formula (I), an acid or base addition salt thereof or a stereochemically isomeric form thereof, wherein A and B taken together form -N=CH-, -CH=N-, -CH2-CH2, CH=CH-, -C(=O)-CH2-, -CH2-C(=O); D is a radical of formula (D1), (D2), (D3); L is a radical of formula (L1), (L2); Alk is a C1-4alkanediyl radical; R is halo; R is hydrogen or halo; R is hydrogen, C1-6alkyl, phenyl or halophenyl; R is hydrogen, C1-6alkyl, phenyl or halophenyl; R is hydrogen or C1-6alkyl; R is hydrogen, C1-6alkyl, C1-6alkyloxycarbonyl, or R and R taken together with the nitrogen atom to which they are attached form a heterocyclic ring. Active intermediates, compositions and methods of preparing compounds, compositions are described.
摘要翻译：式（I）化合物，其酸或碱加成盐或其立体化学异构形式，其中A和B一起形成-N = CH-，-CH = N-，-CH 2 -CH 2，CH = CH- ，-C（= O）-CH 2 - ， - CH 2 -C（= O）; D是式（D1），（D2），（D3）; L是式（L1），（L2）的基团; Alk是C1-4烷二基; R 1是卤素; R 2是氢或卤素; R 3是氢，C 1-6烷基，苯基或卤代苯基; R 4是氢，C 1-6烷基，苯基或卤代苯基; R 5是氢或C 1-6烷基; R 6是氢，C 1-6烷基，C 1-6烷氧基羰基或R 5和R 6与它们所连接的氮原子一起形成杂环。描述了制备化合物的活性中间体，组合物和方法，组合物。

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