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1. 发明申请

WO2008155421A3 INDOLIN-2-ONES AND AZA-INDOLIN-2-ONES 审中-公开
标题翻译：吲哚-2-ONES和AZA-INDOLIN-2-ONES
公开(公告)号：WO2008155421A3
公开(公告)日：2009-02-12
申请号：PCT/EP2008057909
申请日：2008-06-20
申请人： JANSSEN PHARMACEUTICA NV , DIELS GASTON STANISLAS MACELLA , VERDONCK MARC GUSTAAF CELINE , BUIJNSTERS PETER JACOBUS JOHAN , EMELEN KRISTOF VAN
发明人： DIELS GASTON STANISLAS MACELLA , VERDONCK MARC GUSTAAF CELINE , BUIJNSTERS PETER JACOBUS JOHAN , VAN EMELEN KRISTOF
IPC分类号： C07D209/34 , A61K31/404 , A61K31/407 , A61P35/00 , C07D471/04 , C07D487/04
CPC分类号： C07D209/34 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to certain indolin-2-ones and aza-indolin-2-ones which possess anti-tumour activity and are accordingly useful in methods of treatment of the human or animal body, in particular such compounds are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis. Formula (I) a N-oxide form, a quaternary anime or a stereochemically isomeric form thereof, wherein Z represents N or CH.
摘要翻译：本发明涉及其化合物或药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。本发明特别涉及具有抗肿瘤活性的某些二氢吲哚-2-酮和氮杂 - 二氢吲哚-2-酮，因此可用于人或动物体的治疗方法，特别是这些化合物可用于治疗涉及异常细胞增殖的病理过程，例如肿瘤生长，类风湿性关节炎，再狭窄和动脉粥样硬化。式（I）为N-氧化物形式，季铵或其立体化学异构形式，其中Z表示N或CH。

2. 发明申请

WO2007003525A3 CYCLIC ANILINO-PYRIDINOTRIAZINES AS GSK-3 INHIBITORS 审中-公开
标题翻译：作为GSK-3抑制剂的CYCLIC ANILINO-PYRIDINOTRIAZINES
公开(公告)号：WO2007003525A3
公开(公告)日：2008-04-10
申请号：PCT/EP2006063555
申请日：2006-06-26
申请人： JANSSEN PHARMACEUTICA NV , ROMBOUTS FREDERIK JAN RITA , LOVE CHRISTOPHER JOHN , EMELEN KRISTOF VAN , VAN BRANDT SVEN FRANCISCUS ANN , WU TONGFEI
发明人： ROMBOUTS FREDERIK JAN RITA , LOVE CHRISTOPHER JOHN , VAN EMELEN KRISTOF , VAN BRANDT SVEN FRANCISCUS ANN , WU TONGFEI
IPC分类号： C07D251/16 , A61K31/53 , C07D401/04 , C07D471/18 , C07D471/22 , C07D487/08 , C07D487/18
CPC分类号： C07D487/18 , C07D251/16 , C07D401/04 , C07D471/18 , C07D471/22 , C07D487/08
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 m represents 1, n represents 1, Z represents N or C, in particular N; -X 1 - represents C 1-4 alkyl, in particular methyl; -X 2 - represents -C 1-4 alkyl- or -C 1-4 alkyl-NR 7 -, in particular propyl, -ethyl-NR 7 - or -propyl-NR 7 -; -Y- represents-NR 2 -C 1-6 alkyl-CO-NR 4 -, -Het 1 -C 1-6 alkyl-CO-NR 5 - or -Het 2 -CO-NR 6 - and wherein the -C 1-6 alkyl- linker of -NR 2 -C 1-6 alkyl-CO-NR 4 - or -Het 1 -C 1-6 alkyl-CO-NR 5 - is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl; R 1 represents hydrogen, chloro, fluoro or bromo; R 2 represents -C 1-4 alkyl-, in particular ethyl or methyl; R 7 represents hydrogen; R 8 represents hydrogen; R 4 , R 5 and R 6 represent hydrogen; Het 1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het 2 selected from pyrrolidinyl or piperidinyl, in particular pyrrolidinyl wherein said pyrrolidinyl is optionally substituted with hydroxy.
摘要翻译：本发明涉及式（I）化合物，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m表示1，n表示1，Z表示N或C，特别是N; -X 1表示C 1-4烷基，特别是甲基; -X 2 - 表示-C 1-4烷基 - 或-C 1-4 - 烷基-NR 7 - - ，特别是丙基， - 乙基 - NR 7 - 或 - 丙基-NR 7 - 。 -Y-表示-NR 2 -C 1-6烷基-CO-NR 4 - ，-Het 1 SUP / > -C 1-6烷基-CO-NR 5 - 或-Het 2 -CO-NR 6 - - 并且其中-NR 2 -C 1-6烷基-CO-NR的-C 1-6烷基 - 连接基团， 4 - 或-Het 1 -C 1-6烷基-CO-NR 5 - 任选被一个或多个可能的两个或更多个选自羟基，卤素和苯基的取代基; R 1表示氢，氯，氟或溴; R 2表示-C 1-4烷基 - ，特别是乙基或甲基; R 7表示氢; R 8表示氢; R 4，R 5和R 6表示氢; Het 1选自哌嗪基或哌啶基，特别是哌嗪基; Het 2选自吡咯烷基或哌啶基，特别是吡咯烷基，其中所述吡咯烷基任选被羟基取代。

3. 发明申请

WO2006010749A3 SUBSTITUTED PROPENYL PIPERAZINE DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译：取代的丙烯酰胆碱衍生物作为HISTONE脱乙酰壳多糖的新型抑制剂
公开(公告)号：WO2006010749A3
公开(公告)日：2006-06-08
申请号：PCT/EP2005053611
申请日：2005-07-25
申请人： JANSSEN PHARMACEUTICA NV , VAN BRANDT SVEN FRANCISCUS ANN , EMELEN KRISTOF VAN , ANGIBAUD PATRICK RENE , MARCONNET-DECRANE LAURENCE FRA , ARTS JANINE
发明人： VAN BRANDT SVEN FRANCISCUS ANN , VAN EMELEN KRISTOF , ANGIBAUD PATRICK RENE , MARCONNET-DECRANE LAURENCE FRA , ARTS JANINE
IPC分类号： C07D403/12 , A61K31/505 , A61P35/00 , C07D239/42 , C07D239/54
CPC分类号： C07D239/42 , C07D239/54 , C07D403/12
摘要： This invention comprises the novel compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 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R 1，R 2，R 3，R 4， > X定义含有组蛋白脱乙酰酶抑制酶活性的含义; 其制剂，含有它们的组合物及其作为药物的用途。

4. 发明专利

CY1112914T1 ΥΠΟΚΑΤΕΣΤΗΜΕΝΑ ΠΑΡΑΓΩΓΑ ΙΝΔΟΛΥΛ ΑΛΚΥΛ ΑΜΙΝΗΣ ΩΣ ΝΕΟΙ ΑΝΑΣΤΟΛΕΙΣ ΤΩΝ ΑΠΟΑΚΕΤΥΛΑΣΩΝ ΙΣΤΟΝΗΣ 未知
公开(公告)号：CY1112914T1
公开(公告)日：2016-04-13
申请号：CY121100387
申请日：2012-04-25
申请人： JANSSEN PHARMACEUTICA NV
发明人： VERDONCK MARC GUSTAAF C , ANGIBAUD PATRICK RENÉ , ROUX BRUNO , PILATTE ISABELLE NOËLLE CONSTANCE , TEN HOLTE PETER , ARTS JANINE , VAN EMELEN KRISTOF
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00 , C07D405/14 , C07D409/14
摘要： Ηπαρούσαεφεύρεσηπεριέχειτιςνέεςενώσειςτουτύπου (Ι)

5. 发明专利

ES2562218T3 Pirrolopirimidinas útiles para el tratamiento de enfermedades proliferativas 未知
公开(公告)号：ES2562218T3
公开(公告)日：2016-03-03
申请号：ES08775359
申请日：2008-07-25
申请人： JANSSEN PHARMACEUTICA NV
发明人： DIELS GASTON STANISLAS MARCELLA , TEN HOLTE PETER , FREYNE EDDY JEAN EDGARD , GRAND-PERRET THIERRY ANDRE REGIS , VAN EMELEN KRISTOF , EMBRECHTS WERNER CONSTANT JOHAN , BONNET PASCAL GHISLAIN ANDRÉ
IPC分类号： C07D487/08 , A61K31/529 , A61P35/02 , C07D498/08
摘要： Un compuesto de fórmula:**Fórmula** las formas de N-óxido, las sales de adición farmacéuticamente aceptables, las aminas cuaternarias y las formas estereoquímicamente isoméricas de los mismos, en la que Y representa -alquilo de C1-6-NR3-CO-alquilo de C1-6-; -alquilo de C1-6-CO-Het1-alquilo de C1-6-; -alquilo de C1-6- Het2-CO-NR4-alquilo de C1-6-; o -alquilo de C1-6-NR3-CO-alquilo de C1-6-NR4-CO-alquilo de C1-6-; en los que cada -alquilo de C1-6- en cualquiera de -alquilo de C1-6-NR3-CO-alquilo de C1-6-; -alquilo de C1-6-CO-Het1-alquilo de C1- 6-; -alquilo de C1-6-Het2-CO-NR4-alquilo de C1-6-; o -alquilo de C1-6-NR3-CO-alquilo de C1-6-NR4-CO-alquilo de C1- 6- está opcional e independientemente sustituido con un sustituyente seleccionado de hidroxi, fenilo o Het3; X1 representa un enlace directo, -O-; -NR5- o -alquilo de C1-4-NR6-, en el que el resto de -alquilo de C1-4- está directamente unido al anillo de fenilo; X2 representa un enlace directo o -alquilo de C1-4-NR7-, en el que el resto de -alquilo de C1-4- está directamente unido al sistema anular de pirrolopidimidina Q representa hidrógeno, halógeno, alquilo de C1-6, cicloalquilo de C3-6, Het5, -NR9R10, alquilo de C1-4-O-, cicloalquilo de C3-6-O-, Het6-O-, Ar1-O, alquilo de C1-4-S(O)1-2-, cicloalquilo de C3-6-S(O)1-2-, Het7-S(O)1-2-, Ar2- S(O)1-2, alquilo de C1-4-S- o cicloalquilo de C3-6-S-; R1 y R2 representan cada uno independientemente hidrógeno; halo; hidroxi; alquilo de C1-6; cicloalquilo de C3-6; alquilo de C1-4-O-; cicloalquilo de C3-6-O-; Het4; ciano; alquilo de C1-6 sustituido con uno o, cuando sea posible, dos, tres o más sustituyentes seleccionados de halo, hidroxi o alquilo de C1-4-O-; alquilo de C1-4-O- sustituido con uno o, cuando sea posible, dos, tres o más sustituyentes seleccionados de halo, hidroxi, alquilo de C1-4-O-, alquilo de C1-4-O-alquilo de C1-4-O-, fenilo, cicloalquilo de C3-6, cicloalquilo de C3-6-O-, cicloalquilo de C3-6-NH-CO- , Het8-O-, Het9-CO-, Ar3-O-, Ar6-S-, HetAr1-S-, tiazolil-NR11-, piridinil-NR12-, pirazinil-NH-, alquilo de C1-4-O-alquilo de C1-4-NR13-, Ar7-NH-, HetAr2-NH-; cicloalquilo de C3-6-O- sustituido con uno o, cuando sea posible, dos, tres o más sustituyentes seleccionados de halo, hidroxi o alquilo de C1-4-O-; piranil-O-; tetrahidrofuran-O-; Ar8-NH-CONH-; alquilo de C1-6-NH-CO-NH-; cicloalquilo de C3-6-NH-CO-NH-; cicloalquilo de C3-6-alquilo de C1-4-NH-CONR14-; alquilo de C1-4-O-NR15-; Ar5-NH-; R3 y R4 representan cada uno independientemente hidrógeno, alquilo de C1-4, alquilo de C1-4 sustituido con alquilo de C1-4-O-, morfonilino o piperazinilo; o cicloalquilo de C3-6; R5, R6 y R7 representan cada uno independientemente hidrógeno, alquilo de C1-4, cicloalquilo de C3-6 o alquilo de C1-4 sustituido con alquilo de C1-4-O-, cicloalquilo de C3-6, fenilo o piridilo; R8 representa hidrógeno, alquilo de C1-6 o cicloalquilo de C3-6; R9, R10, R11, R12 y R13 representan cada uno independientemente hidrógeno, alquilo de C1-6, cicloalquilo de C3-6; R14 y R15 representan cada uno independientemente hidrógeno, alquilo de C1-4, cicloalquilo de C3-6 o bencilo; Ar1, Ar2, Ar3, Ar5, Ar6, Ar7 y Ar8 representan cada uno independientemente fenilo opcionalmente sustituido con uno o, cuando sea posible, dos o más sustituyentes seleccionados de halo, ciano, amino, alquilo de C1-4, alquilo de C1-4-O-, halo-alquilo de C1-4, polihalo-alquilo de C1-4, cicloalquilo de C3-6, hidroxi-alquilo de C1-4, alquilo de C1-4- oxi-alquilo de C1-4 o polihidroxi-alquilo de C1-4; Het1 y Het2 representan cada uno independientemente piperidinilo, piperazinilo, pirrolidinilo o azetidinilo; Het3, Het4, Het5, Het6, Het7, Het8 y Het9 representan cada uno independientemente morfolinilo, pirrolidinilo, piperazinilo o piperidinilo, en el que dichos Het3, Het4, Het5, Het6, Het7, Het8 y Het9 están independiente y opcionalmente sustituidos con uno o, cuando sea posible, dos o más sustituyentes seleccionados de halo, ciano, amino, alquilo de C1-4, halo-alquilo de C1-4, polihalo-alquilo de C1-4, cicloalquilo de C3-6, fenilo, hidroxi-alquilo de C1-4, alquilo de C1-4-oxi-alquilo de C1-4 o polihidroxi-alquilo de C1-4; HetAr1 y HetAr2 representan cada uno independientemente un sistema anular arílico o heteroarílico seleccionado del grupo que consiste en fenilo, naftilo, quinolinilo, benzoxazolilo, piridilo, pirazinilo, furanilo, tienilo, pirimidinilo, isoxazolilo, isotiazolilo, oxazolilo, tiazolilo, pirrolilo, pirazolilo, indolilo, piridazinilo, bencimidazolilo, benzotienilo y benzotiazolilo.

6. 发明专利

CA2687909C INDOLIN-2-ONES AND AZA-INDOLIN-2-ONES 未知
公开(公告)号：CA2687909C
公开(公告)日：2015-09-15
申请号：CA2687909
申请日：2008-06-20
申请人： JANSSEN PHARMACEUTICA NV
发明人： DIELS GASTON STANISLAS MARCELLA , VERDONCK MARC GUSTAAF CELINE , BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS , VAN EMELEN KRISTOF
IPC分类号： C07D498/18 , A61K31/529 , A61P15/16 , A61P35/00 , C07D487/18 , C07D487/22 , C07D498/22 , C07D513/08 , C07D513/18 , C07D513/22
摘要： The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to certain indolin-2-ones and aza-indolin-2-ones which possess anti-tumour activity and are accordingly useful in methods of treatment of the human or animal body, in particular such compounds are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis. Formula (I) a N-oxide form, a quaternary anime or a stereochemically isomeric form thereof, wherein Z represents N or CH.

7. 发明专利

ES2442458T3 Derivados de 2,4 (4,6)-pirimidina 未知
公开(公告)号：ES2442458T3
公开(公告)日：2014-02-11
申请号：ES05819148
申请日：2005-12-08
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN E , WILLEMS MARC , EMBRECHTS WERNER C J , VAN EMELEN KRISTOF , VAN BRANDT SVEN F A , ROMBOUTS FREDERIK J R
IPC分类号： C07D487/08 , A61K31/505 , A61P35/00 , C07D209/00 , C07D221/00 , C07D239/00 , C07D241/00 , C07D259/00 , C07D273/00 , C07D487/22 , C07D498/18
摘要： Un compuesto que tiene la fórmula (I).**Fórmula** las formas N-óxido, las sales de adición farmacéuticamente aceptables y las formas estereoquímicamenteisoméricas del mismo, en la que: Z1 y Z2 representan cada uno independientemente NR22 ; Y representa -alquilo C3-9-, -alquenilo C3-9-, -alquinilo C3-9-, -alquil C3-7-CO-NH- opcionalmente sustituido con amino,mono- o di(alquil C1-4)amino, aminosulfonilo, mono- o di(alquil C1-4)aminosulfonilo, (alquil C1-4)sulfuro, (alquil C1-4)sulfóxido, o alquil C1-4-oxicarbonilamino-, -alquenil C3-7-CO-NH- opcionalmente sustituido con amino, mono- odi(alquil C1-4)amino, aminosulfonilo, mono- o di(alquil C1-4)aminosulfonilo, (alquil C1-4)sulfuro, (alquil C1-4)sulfóxido, oalquil C1-4-oxicarbonilamino-, -alquinil C3-7-CO-NH- opcionalmente sustituido con amino, mono- o di(alquil C1-4)amino,aminosulfonilo, mono- o di(alquil C1-4)aminosulfonilo, (alquil C1-4)sulfuro, (alquil C1-4)sulfóxido, o alquil C1-4-oxicarbonilamino-, -alquil C1-5-oxi-alquilo C1-5-, -alquil C1-5-NR6-alquilo C1-5-, -alquil C1-5-NR7-CO-alquilo C1-5-, -alquilC1-6-CO-NH-, -alquil C1-6-NH-CO-, -alquil C1-3-NH-CS-Het9-, -alquil C1-3-NH-CO-Het3-, -alquil C1-2-CO-Het10-CO-, -Het4-alquil C1-3-CO-NH-alquilo C1-3-, -alquil C1-7-CO-, -alquil C1-6-CO-alquilo C1-6-, -alquil C1-2-NH-CO-L1 -NH-, -NHCO-L2-NH-, -alquil C1-2-CO-NH-L3-CO-, -alquil C1-2-NH-CO-L1-NH-CO-alquilo C1-3-, -alquil C1-2-NH-CO-L1-NH-CO-, -CO-NH-L2-CO-, -alquil C1-2-CO-NH-L3-CO-NH-alquilo C1-3-, -alquil C1-2-CO-NH-L3-CO-NH-, -alquil C1-2-CO-NR10-alquil C1-3-CO-, -alquil C1-2-NR11-CH2-CO-NH-alquilo C1-3-, -NR12-CO-alquil C1-3-NH-, Het5-CO-alquilo C1-2-, -alquil C1-5-CO-NH-alquil C1-3-CO-NH-, -alquil C1-5-NR13-CO-alquil C1-3-NH-, -Het6-CO-Het7-, -Het8-NH-alquil C1-3-CO-NH-, -alquil C1-3-NH-CO-Het32-CO-, o-alquil C1-3-CO-Het33 -CO-NH-.

8. 发明专利

CA2611438C CYCLIC ANILINO-PYRIDINOTRIAZINES 未知
公开(公告)号：CA2611438C
公开(公告)日：2014-01-07
申请号：CA2611438
申请日：2006-06-26
申请人： JANSSEN PHARMACEUTICA NV
发明人： ROMBOUTS FREDERIK JAN RITA , LOVE CHRISTOPHER JOHN , VAN EMELEN KRISTOF , VAN BRANDT SVEN FRANCISCUS ANNA , WU TONGFEI
IPC分类号： C07D487/18 , A61K31/53 , C07D251/42 , C07D471/18 , C07D471/22 , C07D487/08
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 m represents 1, n represents 1, Z represents N or C, in particular N; -X1- represents C1-4alkyl, in particular methyl; -X2-represents -C1-4alkyl- or -C1-4alkyl-NR7-, in particular propyl, -ethyl-NR7-or -propyl-NR7-; -Y- represents-NR2-C1-6alkyl-CO-NR4-, -Het1-C1-6alkyl-CO-NR5-or -Het2-CO-NR6- and wherein the -C1-6alkyl- linker of -NR2-C1-6alkyl-CO-NR4-or -Het1-C1-6alkyl-CO-NR5- is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl; R1 represents hydrogen, chloro, fluoro or bromo; R2 represents -C1-4alkyl-, in particular ethyl or methyl; R7 represents hydrogen; R8 represents hydrogen; R4, R5 and R6 represent hydrogen; Het1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het2 selected from pyrrolidinyl or piperidinyl, in particular pyrrolidinyl wherein said pyrrolidinyl is optionally substituted with hydroxy.

10. 发明专利

AU2008265104B2 Indolin-2-ones and aza-indolin-2-ones 未知
公开(公告)号：AU2008265104B2
公开(公告)日：2013-09-12
申请号：AU2008265104
申请日：2008-06-20
申请人： JANSSEN PHARMACEUTICA NV
发明人： DIELS GASTON STANISLAS MARCELLA , VAN EMELEN KRISTOF , VERDONCK MARC GUSTAAF CELINE , BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS
IPC分类号： C07D209/34 , A61K31/404 , A61K31/407 , A61P35/00 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to certain indolin- 2-ones and aza-indolin-2-ones which possess anti-tumour activity and are accordingly useful in methods of treatment of the human or animal body, in particular such compounds are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.

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