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1. 发明申请

WO2008107478A8 QUINOLINONE DERIVATIVES AS PARP AND TANK INHIBITORS 审中-公开
标题翻译：喹诺酮衍生物作为PARP和油墨抑制剂
公开(公告)号：WO2008107478A8
公开(公告)日：2008-10-23
申请号：PCT/EP2008052764
申请日：2008-03-07
申请人： JANSSEN PHARMACEUTICA NV , VIALARD JORGE EDUARDO , ANGIBAUD PATRICK RENE , MEVELLEC LAURENCE ANNE , MEYER CHRISTOPHE , FREYNE EDDY JEAN EDGARD , PILATTE ISABELLE NOELLE CONSTANCE , ROUX BRUNO , PASQUIER ELISABETH THERESE JEANNE , BOURDREZ XAVIER MARC , ADELINET CHRISTOPHE DENIS , MARCONNET-DECRANE LAURENCE FRANCOISE BERNADETTE , MACRITCHIE JACQUELINE ANNE , DUFFY JAMES EDWARD STEWART , OWENS ANDREW PATE , STORCK PIERRE-HENRI , PONCELET VIRGINIE SOPHIE
发明人： VIALARD JORGE EDUARDO , ANGIBAUD PATRICK RENE , MEVELLEC LAURENCE ANNE , MEYER CHRISTOPHE , FREYNE EDDY JEAN EDGARD , PILATTE ISABELLE NOELLE CONSTANCE , ROUX BRUNO , PASQUIER ELISABETH THERESE JEANNE , BOURDREZ XAVIER MARC , ADELINET CHRISTOPHE DENIS , MARCONNET-DECRANE LAURENCE FRACOISE BERNADETTE , MACRITCHIE JACQUELINE ANNE , DUFFY JAMES EDWARD STEWART , OWENS ANDREW PATE , STORCK PIERRE-HENRI , PONCELET VIRGINIE SOPHIE
IPC分类号： C07D215/22 , A61K31/4704
CPC分类号： C07D215/227 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The present invention provides compounds of Formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , n, m and X have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为PARP抑制剂的用途以及包含所述化合物的药物组合物，其中R 1，R 2，R 2， R 4，R 4，R 5，R 6，R 7，n，m和 X已经定义了含义。

2. 发明申请

WO2006061417A3 MACROCYCLIC QUINAZOLE DERIVATIVES AND THEIR USE AS MTKI 审中-公开
标题翻译：大分子喹唑啉衍生物及其作为MTKI的用途
公开(公告)号：WO2006061417A3
公开(公告)日：2006-08-03
申请号：PCT/EP2005056609
申请日：2005-12-08
申请人： JANSSEN PHARMACEUTICA NV , FREYNE EDDY JEAN EDGARD , WILLEMS MARC , TEN HOLTE PETER , PAPANIKOS ALEXANDRA , EMBRECHTS WERNER CONSTANT JOHA , STORCK PIERRE HENRI , PONCELET VIRGINIE SOPHIE
发明人： FREYNE EDDY JEAN EDGARD , WILLEMS MARC , TEN HOLTE PETER , PAPANIKOS ALEXANDRA , EMBRECHTS WERNER CONSTANT JOHA , STORCK PIERRE HENRI , PONCELET VIRGINIE SOPHIE
IPC分类号： C07D498/08 , A61K31/529 , A61P35/00 , C07D239/00 , C07D273/00
CPC分类号： C07D498/06 , C07D498/08
摘要： The present invention concerns kinase inhibitors formula, formula (I), the N-oxide forms, the pharmaceutically isomeric forms thereof, wherein Z represents NH and the other substituents are defined as in the claims.
摘要翻译：本发明涉及激酶抑制剂式（I），N-氧化物形式及其药学上异构体形式，其中Z表示NH且其它取代基如权利要求中所定义。

3. 发明申请

WO2008006884A3 MTKI QUINAZOLINE DERIVATIVES 审中-公开
标题翻译： MTKI喹诺酮衍生物
公开(公告)号：WO2008006884A3
公开(公告)日：2008-03-06
申请号：PCT/EP2007057200
申请日：2007-07-12
申请人： JANSSEN PHARMACEUTICA NV , PAPANIKOS ALEXANDRA , FREYNE EDDY JEAN EDGARD , TEN HOLTE PETER , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA , MEVELLEC LAURENCE ANNE , STORCK PIERRE HENRI
发明人： PAPANIKOS ALEXANDRA , FREYNE EDDY JEAN EDGARD , TEN HOLTE PETER , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA , MEVELLEC LAURENCE ANNE , STORCK PIERRE HENRI
IPC分类号： C07D498/14 , A61K31/519 , A61P35/00
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 3-9 - 烷基 - ， - 烷基-C 1-6烷基-C 1-6烷基-C 1-6烷基-C 1-6烷基-C 1-6烷基-C 1-6烷基-C ^{7 -CO-C _{1-5 烷基 - ; X 1表示-O-; X 2表示NR 5 -C 12烷基 - ; R 1表示氢，卤素或Het 3 -O-; R 2表示氢; R 3表示羟基，C 1-4烷基氧基或C 1-4烷氧基，其被一个或两个独立地选自Het的取代基取代羟基，C 1-4烷氧基 - ，C 1-4烷基氧基-C 1-4烷氧基（C 1 -C 4）烷基氧基和NR 9 R 10; R 5表示氢或C 1-4烷基; R 6表示氢或C 1-4烷基; R 7表示氢; R 9和R 10各自独立地表示氢; ç_{1-4 烷基-S（= O）_{2 -C _{1-4 烷基-C（= O） - ; C 1-4烷基或被羟基取代的C 1-4烷基; Het 3表示任选被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〜 -4 烷基-S（= O）_{2 -C _{1-4 烷基 - 。}}}}}}}

4. 发明申请

WO2004007498A2 3-PHENYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS 审中-公开
标题翻译：吡喹酮作为激酶抑制剂的3-苯基类似物
公开(公告)号：WO2004007498A2
公开(公告)日：2004-01-22
申请号：PCT/EP0350292
申请日：2003-07-08
申请人： JANSSEN PHARMACEUTICA NV , LACRAMPE JEAN FERNAND ARMAND , CONNORS RICHARD WILLIAM , HO CHIH YUNG , RICHARDSON ALAN , FREYNE EDDY JEAN EDGARD , BUIJNSTERS PETER JACOBUS JOHAN , 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 JOHAN , BAKKER ANNETTE CORNELIA
IPC分类号： A61K31/53 , A61K31/5377 , A61P9/10 , A61P35/00 , A61P43/00 , C07D487/04 , C07D519/00
CPC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 stereochemically isomeric forms thereof, wherein n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R represents C I -4alkyl; R represents C I -4alkyl; R represents CI-4alkyl; or R and R taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het wherein said C3-8cycloalkyl or Het each independently may optionally be substituted with C1-4alkyloxycarbonyl; R represents halo or C I -4alkyloxy; R represents C 1-4alkyloxycarbonyl, -O-(mono- or di(C1-4alkyl)aminosulfonyl), CI-4alkyl substituted with one or where possible more substituent being selected from Het or NR R , C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het or NR R ; R and R are each independently selected from hydrogen, C I-4alkyl, C I-4alkyloxyC1-4alkyl, -Het or CI-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het ; R and R are each independently selected from hydrogen, C,1-4alkyl, -Het or mono- or di(C 1-4alkyl)aminosulphonyl; Het 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 1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het 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 C1-4alkyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl; Het 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(Cl4alkyl)aminosulfonyl; Het represents piperidinyl.
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n表示0,1或2的整数; m表示0或1的整数; R 1表示C 1-4烷基; R 2表示C 1-4烷基; R 3表示C 1-4烷基; 或R 2和R 3与它们所连接的碳原子一起形成C 3-8环烷基或Het 1，其中所述C 3-8环烷基或Het 1各自独立地可以被C1- 4alkyloxycarbonyl; R 4表示卤素或C 1-4烷氧基; R 5表示C 1-4烷氧基羰基，-O-（单或二（C 1-4烷基）氨基磺酰基），被一个或多个可能的更多取代基取代的C 1-4烷基选自Het 3或NR 6 R 被一个或多个可能的更多取代基取代的C 1-4烷氧基选自氨基，Het 4或NR 8 R 9; R 6和R 7各自独立地选自氢，C 1-4烷基，C 1-4烷氧基C 1-4烷基，-Het 5或被一个或多个可能的更多取代基取代的C 1-4烷基，所述取代基选自羟基，或Het <5>; R 8和R 9各自独立地选自氢，C 1-4烷基，-Het 7或单或二（C 1-4烷基）氨基磺酰基; Het 3表示选自哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可以任选被一个取代，或者如果可能的话，两个或三个取代基各自独立地选自羟基，氨基磺酰基，氨基，单或二（C 1 -4烷基）氨基磺酰基，羟基C 1-4烷氧基C 1-4烷基或C 1-4烷氧基; Het 4表示选自吗啉基，哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可以任选地被一个取代，或者如果可能的话，两个或三个取代基各自独立地选自C 1-4烷基，C 1-4烷氧基羰基或一或二（C 1-4烷基）氨基磺酰基; Het 5表示选自吡啶基或哌啶基的杂环，其中所述单环杂环各自独立地可以任选地被一个取代，或者两个或三个取代基各自独立地选自氨基磺酰基或单或二（C 1-4烷基）氨基磺酰基; Het 7表示哌啶基。

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

WO2005012304A3 TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
标题翻译：三氮唑嘧啶衍生物作为GLYCOGEN SYNTHASE激酶3抑制剂
公开(公告)号：WO2005012304A3
公开(公告)日：2007-04-26
申请号：PCT/EP2004051457
申请日：2004-07-12
申请人： JANSSEN PHARMACEUTICA NV , FREYNE EDDY JEAN EDGARD , LOVE CHRISTOPHER JOHN , COOYMANS LUDWIG PAUL , VANDERMAESEN NELE , BUIJNSTERS PETER JACOBUS JOHAN , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA
发明人： FREYNE EDDY JEAN EDGARD , LOVE CHRISTOPHER JOHN , COOYMANS LUDWIG PAUL , VANDERMAESEN NELE , BUIJNSTERS PETER JACOBUS JOHAN , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA
IPC分类号： C07D487/04 , A61K31/519 , A61P3/10 , A61P25/24 , C07D235/00 , C07D249/00
CPC分类号： C07D487/04
摘要： This invention concerns compounds of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochernically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R 1 represents hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 a]kyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonytoxy; or optionally substituted C 1-6 alkyloxyCl-6alkylcarbonyl; X 1 represents a direct bond; -(CH 2 ) n3 - or -(CH 2 ) n4 -X 1a -X 1b -; R 2 represents optionally substituted C 3-7 CYCloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatorn selected from 0, S or N; benzoxazolyl or a radical of formula (a-1); X 2 represents a direct bond; -NR 1 -NR 1 -(CH 2 ) N3 -; -0-; -0-(CH 2 ) n3 -; -C(=O)-; -C(=O)- (CH 2 ) n3 -; -C(=O)-NR 5 -(CH 2 ) n3 -; -C(=S)-; -S-; -S(=O) n1 -; -(CH 2 ) n3 -; -(CH 2 ) n4 -X 1a -X 1b -; -X 1a .-X 1b -(CH 2 ) n4 -; -S(=O) n1 -NR 5 -(CH 2 ) n3 -NR 5 _ or -S(=O) n1 ,-NR 5 -(CH 2 ) n3 -; R 3 represents an optionally substituted 5-or 6-membered monocyclic heterocycle containing at least one heteroatom selected from 0, S or N, or a 9-or 10-membered bicyclic heterocycle containing at least one heteroatom selected from 0, S or N; R 4 represents hydrogen; halo; hydroxy; optionally substituted C 1-4 alkyl; optionally substituted C 2-4 alkenyl or C 2-4 alkynyl; polyhaloC 1-3 alkyl; optionally substituted C 1-4 alkyloxy; polyhaloC 1-3 alkyloxy; C 1-4 alkylthio; polyhaloC 1-3 alkylthio; C 1-4 alkyloxycarbonyl; C 1-4 alkylcarbonyloxy; C 1-4 alkylcarbonyl; polyhaloC 1-4 alkylcarbonyl; nitro; cyano; carboxyl; NR 9 R 10 ; C(=O)NR 9 R 10 ;-NR 5_ C(=O)-NR 9 R 10 ; -NR 5 -C(=O)-R 5 ; -S(=O) n1 ,-R 11 -NR 5 -S(=O) n1 ,-R 11 -S-CN; -NR 5 -CN; their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式（I）的化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体异构体形式，其中环A表示苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; R 1表示氢; 芳基; 甲酰基; C 1-6烷基羰基; C 1-6 a] kyl; C 1-6烷氧基羰基; 被甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基取代的C 1-6烷基， / SUB> alkylcarbonytoxy; 或任选取代的C 1-6烷氧基C 1-6烷基羰基; X 1表示直接键; - （CH 2 2）n3 - 或 - （CH 2）n4 - - - - - SUB> -X _{图1b - ; R 2表示任选取代的C 3-7环烷基; 苯基; 含有至少一个选自0，S或N的杂化子的4,5,6-或7-元单环杂环; 苯并恶唑基或式（a-1）基团; X 2代表直接键; -NR 1 - （CH 2）N 3 - ;（CH 2）N 3 - 。 -0-; -O-（CH _{2 ）_{N3 - ; -C（= O） - ; -C（= O） - （CH 2）n3 - ; -C（= O）-NR ^{5 - （CH _{2 ）_{N3 - ; -C（= S） - ; -S-; -S（= O）_{N1 - ; - （CH _{2 ）_{N3 - ; - （CH _{2 ）_{N4 -X _{1A -X _{图1b - ; -X _{1A .- X _{图1b - （CH _{2 ）_{N4 - ; -S（= O）_{N1 -NR ^{5 - （CH _{2 ）_{N3 -NR ^{5 n =（CH 2）n或-S（= O）n1， - NR 5 - （CH 2）n 3 - ; R 3表示含有至少一个选自O，S或N的杂原子或含有至少一个杂原子的9元或10元双环杂环的任选取代的5元或6元单环杂环从0，S或N; R 4表示氢; 光环; 羟基; 任选取代的C 1-4烷基; 任选取代的C 2-4 - 烯基或C 2-4 - 炔基; 多卤代_{1-3 烷基; 任选取代的C 1-4烷氧基; 多卤代_{1-3 烷氧基; ç_{1-4 烷硫基; 多卤代_{1-3 烷硫基; ç_{1-4 烷氧基羰基; ç_{1-4 烷基羰基氧基; ç_{1-4 烷基羰基; 多卤代_{1-4 烷基羰基; 硝基; 氰基; 羧基; NR ^{9 - [R ^{10 ; C（= O）NR ^{9 - [R ^{10 ; - NR ^{5 _ C（= O）-NR ^{9 ř ^{10 ; -NR ^{5 C（= O）-R ^{5 ; -S（= O）n1， - R 11 -NR 5 -S（= O）n1， -R 11 -S-CN; -NR 5 -CN; 其用途，包含它们的药物组合物及其制备方法。}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}

7. 发明申请

WO2004007498A9 3-PHENYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的TOXOFLAVINE的3-苯基类似物
公开(公告)号：WO2004007498A9
公开(公告)日：2004-08-12
申请号：PCT/EP0350292
申请日：2003-07-08
申请人： JANSSEN PHARMACEUTICA NV , LACRAMPE JEAN FERNAND ARMAND , CONNORS RICHARD WILLIAM , HO CHIH YUNG , RICHARDSON ALAN , FREYNE EDDY JEAN EDGARD , BUIJNSTERS PETER JACOBUS JOHAN , 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 JOHAN , BAKKER ANNETTE CORNELIA
IPC分类号： A61K31/53 , A61K31/5377 , A61P9/10 , A61P35/00 , A61P43/00 , C07D487/04 , C07D519/00
CPC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 represents C1-4alkyl; R represents C1-4alkyl; R represents C1-4alkyl; or R and R taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het wherein said C3-8cycloalkyl or Het each independently may optionally be substituted with C1-4alkyloxycarbonyl; R represents halo or C1-4alkyloxy; R represents C1-4alkyloxycarbonyl, -O-(mono- or di(C1-4alkyl)aminosulfonyl), C1-4alkyl substituted with one or where possible more substituent being selected from Het or NR R , C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het or NR R ; R and R are each independently selected from hydrogen, C1-4alkyl, C1-4alkyloxyC1-4alkyl, -Het or C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het ; R and R are each independently selected from hydrogen, C1-4alkyl, -Het or mono- or di(C1-4alkyl)aminosulphonyl; Het 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(C1-4 alkyl)aminosulfonyl, hydroxyC1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het 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 C1-4alkyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl; Het 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(Cl4alkyl)aminosulfonyl; Het represents piperidinyl.
摘要翻译：本发明涉及式（I）的N-氧化物形式的化合物，其药学上可接受的加成盐和立体化学异构形式，其中n表示0,1或2的整数; m表示0或1的整数; R 1表示C 1-4烷基; R 2表示C 1-4烷基; R 3代表C 1-4烷基; 或R 2和R 3与它们所连接的碳原子一起形成C 3-8环烷基或Het 1，其中所述C 3-8环烷基或Het 1各自独立地可任选被C 1 -C 8 - 4alkyloxycarbonyl; R 4代表卤素或C 1-4烷氧基; R 5表示C 1-4烷氧基羰基，-O-（一或二（C 1-4烷基）氨基磺酰基），被一个或可能的更多取代基取代的C 1-4烷基，所述取代基选自Het 3或NR 6 R 6; 被一个或在可能的情况下被选自氨基，Het 4或NR 8 R 9的更多取代基取代的C 1-4烷氧基; R 6和R 7各自独立地选自氢，C 1-4烷基，C 1-4烷氧基C 1-4烷基，-Het 5或被一个或可能的更多取代基取代的C 1-4烷基，所述取代基选自羟基或Het <5>; R 8和R 9各自独立地选自氢，C 1-4烷基，-Het 7或单 - 或二（C 1-4烷基）氨基磺酰基; Het 3代表选自哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可任选被一个或任选地两个或三个取代基取代，所述取代基各自独立地选自羟基，氨基磺酰基，氨基，单或二（C1- 4烷基）氨基磺酰基，羟基C1-4烷氧基C1-4烷基或C1-4烷氧基; Het 4代表选自吗啉基，哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可任选被一个或在可能的情况下被两个或三个取代基取代，所述取代基各自独立地选自C 1-4烷基，C 1-4烷氧基羰基或一或二（C 1-4烷基）氨基磺酰基; Het 5代表选自吡啶基或哌啶基的杂环，其中所述单环杂环各自独立地可任选地被一个或任选地两个或三个取代基取代，所述取代基各自独立地选自氨基磺酰基或单或二（C 1-4烷基）氨基磺酰基; Het 7代表哌啶基。

8. 发明申请

WO2008049904A3 USE OF MTKI 1 FOR TREATING OR PREVENTING BONE CANCER 审中-公开
标题翻译：使用MTKI 1治疗或预防骨癌
公开(公告)号：WO2008049904A3
公开(公告)日：2009-01-15
申请号：PCT/EP2007061501
申请日：2007-10-25
申请人： JANSSEN PHARMACEUTICA NV , PERERA TIMOTHY PIETRO SUREN , JANICOT MICHEL MARIE FRANCOIS , MEERT THEO FRANS , FREYNE EDDY JEAN EDGARD
发明人： PERERA TIMOTHY PIETRO SUREN , JANICOT MICHEL MARIE FRANCOIS , MEERT THEO FRANS , FREYNE EDDY JEAN EDGARD
IPC分类号： A61K31/529 , A61P35/00 , A61P35/04
CPC分类号： A61K31/529
摘要： The present invention is concerned with the finding that the macrocyclic quinazoline derivative 4,6-ethanediylidenepyrimido[4,5-b][6,1,12]benzoxadiazacyclo-pentadecine, 17-bromo-8,9,10,11,12,13, 14,19-octahydro-20-methoxy-13-methyl-, described as compound 22 in PCT publication WO2004/105765, is useful in the manufacture of a medicament for the treatment or prevention of bone cancers and methods for killing bone cancer cells, including osteosarcomas, chondrosarcomas, myeloma bone disease and osteolytic bone metastases from other primary sites. It accordingly provides methods for treating, preventing, delaying or mitigating bone cancer, or for preventing and treating of bone loss associated with cancer metastases.
摘要翻译：本发明涉及大环喹唑啉衍生物4,6-乙二亚甲基嘧啶并[4,5-b] [6,1,12]苯并恶二氮杂环十五碳烯，17-溴-8,9,10,11,12，在PCT公开WO2004 / 105765中描述为化合物22的13,14,19-八氢-20-甲氧基-13-甲基可用于制备用于治疗或预防骨癌的药物和用于杀死骨癌的方法细胞，包括骨肉瘤，软骨肉瘤，骨髓瘤骨病和其他原发部位的骨溶解性骨转移。因此，它提供了治疗，预防，延缓或减轻骨癌或预防和治疗与癌症转移相关的骨丢失的方法。

9. 发明专利

JP2013249307A Mtki quinazoline derivative 有权
标题翻译： MTKI喹诺酮衍生物
公开(公告)号：JP2013249307A
公开(公告)日：2013-12-12
申请号：JP2013167044
申请日：2013-08-09
申请人： Janssen Pharmaceutica Nv , ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap
发明人： PAPANIKOS ALEXANDRA , FREYNE EDDY JEAN EDGARD , TEN HOLTE PETER , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHAN , MEVELLEC LAURENCE ANNE , STORCK PIERRE HENRI
IPC分类号： C07D498/18 , A61K31/519 , A61K31/541 , A61P9/00 , A61P9/10 , A61P35/00 , A61P43/00
CPC分类号： C07D498/14 , C08K5/544
摘要： PROBLEM TO BE SOLVED: To provide a certain kind of new quinazoline derivative, having an antitumor activity and useful in a treating method for a human body or an animal body.SOLUTION: A quinazoline derivative is expressed by formula (I) (wherein, Y, X, X, R, Rand Rare each optionally a halogen atom or an organic group) or its N-oxy form, pharmaceutically acceptable addition salt or stereochemically isomeric form.
摘要翻译：要解决的问题：提供一种具有抗肿瘤活性并可用于人体或动物体的治疗方法的新型喹唑啉衍生物。解决方案：喹唑啉衍生物由式（I）表示（其中Y为，X，X，R，R 3各自任选是卤素原子或有机基团）或其N-氧基形式，药学上可接受的加成盐或立体化学异构形式。

10. 发明专利

MY169441A 2,4, (4,6) PYRIMIDINE DERIVATIVES 未知
公开(公告)号：MY169441A
公开(公告)日：2019-04-11
申请号：MYPI20055703
申请日：2005-12-06
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN EDGARD , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHAN , VAN BRANDT SVEN FRANCISCUS ANNA , VAN EMELEN KRISTOF , ROMBOUTS FREDERIK JAN RITA
摘要： The present invention concerns the compounds of formula (I), the N-oxide fonns, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z1 and Z2 represent NH; Y represents -C3_9alkyl-, -C3_9alkenyl-, -C1 -salkyl-NR 6- C1 -salkyl-, -C1_5alkyl-NR 7- CO-C1 _ 5alkyl-, -C1-6alkyl-CO-NH-, -C1-6alkyl-NH-CO-, -C1 _2a lkyl-CO-H et10-CO-, -C1 _ 3alkyl-NH-CO-H et3-, -Het4-C1_3alkyl-CO-NH-C 1 _3alkyl-, -C1-2alkyl-NH-CO-L1- NH-, -NH-CO-L2-NH-, -C1-2 alkyl-CO-NH-L 3-CO-, -C1_2alkyl-NH-CO-L 1 -NH-CO- C1_3alkyl-, -C1 -2alkyl-CO-NH-L 3-CO-NH-C 1_3alkyl-, -C 1-2alkyl-NR 11 -CH2- CO-NH-C1_3alkyl-, Het5-CO-C1 -2alkyl-, -C1 _5alkyl-CO-NH-C 1 _3alkyl-CO-NH-, -C1 _5alkyl-NR 1 3-CO-C1 _3alkyl-NH-, -C1 _3alkyl-NH-CO-Het27- CO-, or -C1 _3alkyl-CO- Het28-CO-NH-?, X1 represents a direct bond, 0, -O-C1 _2alkyl-, -CO-C1 _2alkyl-, -NR16-C1 _2alkyl-, -CO- NR17-, Het23- C1 _2alkyl- or C1-2alkyl; X2 represents a direct bond, 0, -O-C1 _2alkyl-, -CO-C1 _2alkyl-, -NR18 -C1 _2alkyl-, -CO- NR19-, Het24-C1-2alkyl- or C1-2alkyl; R1 and R5 each independently represent hydrogen, halo, C1_6alkyloxy- or C1 _6alkyloxy- substituted with Het1 or C1-4alkyloxy-; R2 and R4 each independently represent hydrogen or halo; R3 represents hydrogen or cyano; R6, R7, R1 3, R17 and R19 represent hydrogen; R11 represents hydrogen or C14 alkyl; R16 and R18 represent hydrogen, C14 a lkyl or Het17 -C14 alkyl-; L1 , L2 and L3 each independently represents C1 _8al kyl optionally substituted with one or where possible two or more substituents selected from phenyl, methylsulfide, cyano, polyhaloC1-4alkyl-phenyl-, C1-4alkyloxy, pyridinyl, mono- or di(C14 a lkyl)- amino- or C3_6cycloalkyl; Het1 , Het 2, Het 17 each independently represent morpholinyl, oxazolyl, isoxazolyl, or piperazinyl; Het3, Het 4, Het5 each independently represent morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl; Het 1 0 represents piperazinyl, piperidinyl, pyrrolidinyl or azetidinyl; Het22 represents morpholinyl, oxazolyl, isoxazolyl or piperazinyl wherein said Het22 is optionally substituted with C14 a lkyl; Het23 and He t24 each independently represent a heterocycle selected from pyrrolidinyl, piperazinyl or piperidinyl wherein said Het23 or Het24 are optionally substituted with Het 22-carbonyl; Het 27 and Het28 each independently represent a heterocycle selected from morpholinyl, piperazinyl, piperidinyl or pyrrolidinyl.

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