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21. 发明申请

WO2004007498A3 3-PHENYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS 审中-公开
公开(公告)号：WO2004007498A3
公开(公告)日：2004-01-22
申请号：PCT/EP2003/050292
申请日：2003-07-08
申请人： JANSSEN PHARMACEUTICA N.V. , LACRAMPE, Jean, Fernand, Armand , CONNORS, Richard, William , HO, Chih, Yung , RICHARDSON, Alan , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes , BAKKER, Annette, Cornelia
发明人： LACRAMPE, Jean, Fernand, Armand , CONNORS, Richard, William , HO, Chih, Yung , RICHARDSON, Alan , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes , BAKKER, Annette, Cornelia
IPC分类号： C07D487/04
摘要： The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereo-chemically isomeric forms thereof, wherein n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R 1 represents C 1-4 alkyl; R 2 represents C 1 - 4 alkyl; R 3 represents C 1-4 alkyl; or R 2 and R 3 taken together with the carbon atom to which they are attached form a C 3-8 cycloalkyl or Het 1 wherein said C 3-8 cycloalkyl or Het 1 each independently may optionally be substituted with C 1-4 alkyloxycarbonyl; R 4 represents halo or C 1-4 alkyloxy; R 5 represents C 1-4 alkyloxycarbonyl, -O-(mono- or di(C 1-4 alkyl)aminosulfonyl), C 1 - 4 alkyl substituted with one or where possible more substituent being selected from Het 3 or NR 6 R 7 , C 1-4 alkyloxy substituted with one or where possible more substituents being selected from amino, Het 4 or NR 8 R 9 ; R 6 and R 7 are each independently selected from hydrogen, C 1-4 alkyl, C 1-4 alkyloxyC 1-4 alkyl, -Het 5 or C 1-4 alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het 5 ; R 8 and R 9 are each independently selected from hydrogen, C 1-4 alkyl, -Het 7 or mono- or di(C 1-4 alkyl)aminosulphonyl; Het 3 represents a heterocycle selected from piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from hydroxy, aminosulfonyl, amino, mono-or di(C 1-4 alkyl)aminosulfonyl, hydroxyC 1-4 alkyloxyC 1-4 alkyl or C 1-4 alkyloxy; Het 4 represents a heterocycle selected from morpholinyl, piperidinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C 1-4 alkyl, C 1-4 alkyloxycarbonyl or mono- or di(C 1-4 alkyl)aminosulfonyl; Het 5 represents a heterocycle selected from pyridinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, or mono- or di(C l4 alkyl)aminosulfonyl; Het 7 represents piperidinyl.

22. 发明申请

WO1993009118A1 1,3-DIHYDRO-2H-IMIDAZO(4,5-B)QUINOLIN-2-ONE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS 审中-公开
标题翻译： 1,3-二氢-2H-咪唑（4,5-B）喹啉-2-酮衍生物作为磷酸二酯酶抑制剂
公开(公告)号：WO1993009118A1
公开(公告)日：1993-05-13
申请号：PCT/EP1992002496
申请日：1992-10-27
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , RAEYMAEKERS, Alfons, Herman, Margaretha , DE CHAFFOY DE COURCELLES, Didier, Robert, Guy, ...
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D471/04
CPC分类号： C07D215/38 , C07D233/76 , C07D233/96 , C07D401/06 , C07D401/10 , C07D471/04
摘要： Novel 1,3-dihydro-2H-imidazo(4,5-b)quinolin-2-one derivatives of formula (I) wherein R is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C1-6alkyloxy, C5-6cycloalkyloxy, C1-6alkyl or trifluoromethyl; pyridinyl; thienyl optionally substituted with halo or C1-6alkyl; and (α) is a radical of formula (a), (b), or (c); the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, said compounds being potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of allergic disorders, atopic diseases and related afflictions. Intermediates in the preparation thereof. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.

23. 发明申请

WO2010119284A1 BICYCLIC HETEROCYCLYL DERIVATIVES AS FGFR KINASE INHIBITORS FOR THERAPEUTIC USE 审中-公开
标题翻译：作为用于治疗用途的FGFR激酶抑制剂的双相间苯二酚衍生物
公开(公告)号：WO2010119284A1
公开(公告)日：2010-10-21
申请号：PCT/GB2010/050617
申请日：2010-04-15
申请人： ASTEX THERAPEUTICS LIMITED , SAXTY, Gordon , BERDINI, Valerio , FREYNE, Eddy Jean Edgard , PAPANIKOS, Alexandra , BENDERITTER, Pascal , EMBRECHTS, Werner Constant Johan , WROBLOWSKI, Berthold , AKKARI, Rhalid
发明人： SAXTY, Gordon , BERDINI, Valerio , FREYNE, Eddy Jean Edgard , PAPANIKOS, Alexandra , BENDERITTER, Pascal , EMBRECHTS, Werner Constant Johan , WROBLOWSKI, Berthold , AKKARI, Rhalid
IPC分类号： C07D471/04 , A61P35/00 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译：本发明涉及式（I）的新的双环杂环基衍生物，包含所述化合物的药物组合物和所述化合物在治疗疾病中的用途，例如，癌症。

24. 发明申请

WO2009118370A1 AZA-BICYCLOHEXYL SUBSTITUTED INDOLYL ALKYL AMINO DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译： AZA-BICYCLOHEXYL取代的吲哚基氨基酸衍生物作为HISTONE DEACETYLASE的新型抑制剂
公开(公告)号：WO2009118370A1
公开(公告)日：2009-10-01
申请号：PCT/EP2009/053566
申请日：2009-03-26
申请人： JANSSEN PHARMACEUTICA NV , FREYNE, Eddy, Jean, Edgard , PILATTE, Isabelle,Noëlle, Constance , ANGIBAUD, Patrick, René
发明人： FREYNE, Eddy, Jean, Edgard , PILATTE, Isabelle,Noëlle, Constance , ANGIBAUD, Patrick, René
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D403/14 , C07D401/14 , C07D405/14
摘要： This invention comprises the novel compounds of Formula (I), wherein R 1 , R 2 , R 3 , R 4 , A and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R1，R2，R3，R4，A和X具有定义的含义，具有组蛋白脱乙酰酶抑制酶活性; 其制剂，含有它们的组合物及其作为药物的用途。

25. 发明申请

WO2008006884A2 MTKI QUINAZOLINE DERIVATIVES 审中-公开
标题翻译： MTKI喹唑啉衍生物
公开(公告)号：WO2008006884A2
公开(公告)日：2008-01-17
申请号：PCT/EP2007/057200
申请日：2007-07-12
申请人： JANSSEN PHARMACEUTICA N.V. , PAPANIKOS, Alexandra , FREYNE, Eddy, Jean, Edgard , TEN HOLTE, Peter , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , MEVELLEC, Laurence, Anne , STORCK, Pierre, Henri
发明人： PAPANIKOS, Alexandra , FREYNE, Eddy, Jean, Edgard , TEN HOLTE, Peter , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , MEVELLEC, Laurence, Anne , STORCK, Pierre, Henri
CPC分类号： C07D498/14 , C08K5/544
摘要： The present invention concerns the compounds of formula (I) the N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y represents -C 3-9 alkyl-, -C 1-5 alkyl-NR 6 -C 1-5 alkyl- or -C 1-5 alkyl-NR 7 -CO-C 1-5 alkyl-; X 1 represents -O-; X 2 represents NR 5 -C 1-2 alkyl-; R 1 represents hydrogen, halo or Het 3 -O-; R 2 represents hydrogen; R 3 represents hydroxy, C 1-4 alkyloxy- or C 1-4 alkyloxy subst ituted with one or two substituents each independently selected from Het 4 , hydroxy, C 1-4 alkyloxy-, C 1-4 alkyloxy-C 1-4 alkyloxy and NR 9 R 10 ; R 5 represents hydrogen or C 1-4 alkyl; R 6 represents hydrogen or C 1-4 alkyl; R 7 represents hydrogen; R 9 and R 10 each independently represent hydrogen; C 1-4 alkyl-S(=O) 2 -C 1-4 alkyl-C(=O)-; C 1-4 alkyl or C 1-4 alkyl substituted with hydroxy; Het 3 represents pyridinyl optionally substituted with C 1-4 alkyl; Het 4 represents morpholinyl, piperidinyl or piperazinyl wherein said Het 4 is optionally substituted with hydroxy-C 1-4 alkyl or C 1-4 alkyl-S(=O) 2 -C 1-4 alkyl-.
摘要翻译：本发明涉及式（I）化合物的N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中Y代表-C C 3-5烷基 - ， - C 1-5烷基-NR 6 -C 1-5烷基 - 或 -C <子> 1-5 烷基 - NR ^{7 -CO-C <子> 1-5 烷基 - ; X 1表示-O-; X 2表示NR 5 -C 1-2烷基 - 。 R 1表示氢，卤素或Het 3 -O-; R 2代表氢; R 3代表羟基，C 1-4烷氧基或C 1-4烷氧基，其中各取代基各自独立地选自Het 4，羟基，C 1-4烷氧基，C 1-4烷氧基-C 1-4烷氧基和NR 9 R 10; R 5代表氢或C 1-4烷基; R 6代表氢或C 1-4烷基; R 7代表氢; R 9和R 10各自独立地代表氢; ç<子> 1-4 烷基-S（= O）<子> 2 -C <子> 1-4 烷基-C（= O） - ; 被羟基取代的C 1-4烷基或C 1-4烷基; Het 3 3代表任选被C 1-4烷基取代的吡啶基; Het 4表示吗啉基，哌啶基或哌嗪基，其中所述Het 4任选被羟基-C 1-4烷基或C 1-14 -4 烷基-S（= O）<子> 2 -C <子> 1-4 烷基 - 。}

26. 发明申请

WO2005058913A1 PYRIDO- AND PYRIMIDOPYRIMIDINE DERIVATIVES AS ANTI- PROLIFERATIVE AGENTS 审中-公开
标题翻译：作为抗增生剂的吡咯并吡啶并吡啶衍生物
公开(公告)号：WO2005058913A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/053501
申请日：2004-12-15
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , WILLEMS, Marc , STORCK, Pierre, Henri , PONCELET, Virginie, Sophie , VAN EMELEN, Kristof , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , EMBRECHTS, Werner, Constant, Johan , PERERA, Timothy, Pietro, Suren
发明人： FREYNE, Eddy, Jean, Edgard , WILLEMS, Marc , STORCK, Pierre, Henri , PONCELET, Virginie, Sophie , VAN EMELEN, Kristof , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , EMBRECHTS, Werner, Constant, Johan , PERERA, Timothy, Pietro, Suren
IPC分类号： C07D498/18
CPC分类号： C07D498/16 , C07D471/04 , C07D487/04 , C07D487/16 , C07D487/22
摘要： The present invention concerns the compounds of formula (I) the N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a 1 -a 2 =a 3 -a 4 represents a divalent radical selected from N-CH=CH-CH, N-CH N-CH or CH-CH=N-CH; Z represents NH; Y represents -C 3-9 alkyl-, -C l-5 alkyl-NR 13 -C l-5 alkyl-,-C 1 - 6 alkyl-NH-CO- or -CO-NH -C 1-6 alkyl- ; X 1 represents -O- or -NR 11 -; X 2 represents -C 1-2 alkyl-, -O-C 1-2 alkyl, -O- or -O-CH 2 -;R 1 represents hydrogen or halo; R 2 represents hydrogen, cyano, halo, hydroxycarbonyl-C l-4 alkyloxycarbonyl-, Het 16 -carbonyl- or Ar 5 ; R 3 represents hydrogen; R 4 represents hydroxy, C 1-4 alkyloxy-, Ar 4 -C 1-4 alkyloxy or R 4 represents C l-4 alkyloxy substituted with one or where possible two or more substituents selected from C 1-4 alkyloxy- or Het 2 -; R 11 represents hydrogen; R 12 represents hydrogen, C l-4 alkyl- or C l-4 alkyl-oxy-carbonyl-; R 13 represents Het 14 -C l-4 alkyl, in particular morpholinyl-C l-4 alkyl; Het 2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C 1-4 alkyl-, preferably methyl; Het 14 represents morpholinyl; Het 16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar 4 represents phenyl; Ar 5 represents phenyl optionally substituted with cyano.
摘要翻译：本发明涉及式（I）化合物的N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中a 1 -a 2 = a 3 -a 4表示选自N-CH = CH-CH，N-CHN-CH或CH-CH = N-CH的二价基团; Z表示NH; Y表示-C3-9烷基 - ， - C1-5烷基-NR13-C1-5烷基 - ，C1-6烷基-NH-CO-或-CO-NH-C 1-6烷基 - ; X 1表示-O-或-NR 11 - ; X 2表示-C 1-2烷基 - ， - O-C 1-2烷基，-O-或-O-CH 2 - ; R 1表示氢或卤素; R 2代表氢，氰基，卤素，羟基羰基-C 1-4烷基氧基羰基，Het 16 - 羰基 - 或Ar 5。 R 3表示氢; R 4表示羟基，C 1-4烷氧基 - ，Ar 4 -C 1-4烷氧基或R 4表示被一个或多个可能的两个或多个选自C 1-4烷氧基或Het 2的取代基取代的C 1-4烷氧基。 - ; R 11表示氢; R 12表示氢，C 1-4烷基 - 或C 1-4烷基 - 氧 - 羰基 - ; R 13代表Het 14 -Cl-4烷基，特别是吗啉基-C 1-4烷基; Het 2表示选自被C 1-4烷基，优选甲基取代的吗啉基或哌啶基的杂环; Het <14>代表吗啉基; Het 16表示选自吗啉基或吡咯烷基的杂环; Ar 4表示苯基; Ar 5表示任选被氰基取代的苯基。

27. 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。

28. 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。

29. 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。

30. 发明申请

WO1996031486A1 1,3-DIHYDRO-1-(PHENYLALKENYL)-2H-IMIDAZOL-2-ONE DERIVATIVES HAVING PDE IV AND CYTOKINE INHIBITING ACTIVITY 审中-公开
标题翻译：具有PDE IV和细胞因子抑制活性的1,3-二氢-1-（苯乙烯基）-2H-咪唑-2-酮衍生物
公开(公告)号：WO1996031486A1
公开(公告)日：1996-10-10
申请号：PCT/EP1996001395
申请日：1996-03-28
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , DIELS, Gaston, Stanislas, Marcella , ANDRES-GIL, José Ignacio , FERNANDEZ-GADEA, Francisco Javier
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D233/32
CPC分类号： C07D233/32 , C07D233/70
摘要： The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceuticlaly acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R and R each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; R is hydrogen, halo or C1-6alkyloxy; R is hydrogen; cyano; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl or aryl; R is hydrogen; cyano; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl or aryl; Y is a direct bond or C1-3alkanediyl; -A-B- is a bivalent radical of formula -CR =CR - or -CHR -CHR -; L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl; -furanyl or -thienyl; having PDE IV and cytokine inhibiting acitivity. Further, pharmaceutical compositions, preparations and use as a medicine are described.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，药学上可接受的酸或碱加成盐及其立体化学异构形式，其中R 1和R 2各自独立地为氢; C1-6烷基; 二氟; 三氟甲基; 3-6环; 含有一个或两个选自氧，硫或氮的杂原子的饱和的5-，6-或7-元杂环; 二氢化茚基; 二环[2.2.1] -2-庚烯基; 二环[2.2.1]庚烷基; C1-6alkylsulfonyl; 芳基磺酰基; 或取代的C 1-10烷基; R 3是氢，卤素或C 1-6烷氧基; R 4是氢; 氰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基或芳基; R 5是氢; 氰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基或芳基; Y是直接键或C1-3烷二基; -A-B-是式-CR 6 = CR 7 - 或-CHR 6 -CHR 7 - 的二价基团; L是氢; 任选取代的C 1-6烷基; C1-6烷基; C1-6alkyloxycarbonyl; C 1-6烷基磺酰基或芳基磺酰基; 芳基是任选取代的苯基; Het是吗啉基或任选取代的哌啶基，哌嗪基， - 吡啶基; - 呋喃基或 - 噻吩基; 具有PDE IV和细胞因子抑制活性。此外，描述了作为药物的药物组合物，制剂和用途。

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