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1. 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。

2. 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。

5. 发明专利

HRP20080359B1 PIRIMIDINI KOJI INHIBIRAJU REPLIKACIJU HIV-a 未知
公开(公告)号：HRP20080359B1
公开(公告)日：2016-01-01
申请号：HRP20080359
申请日：2008-07-17
申请人： JANSSEN PHARMACEUTICA NV
发明人： DE CORTE BART , DE JONGE MARC RENE , HEERES JAN , HO CHIH YUNG , JANSSEN PAUL ADRIAAN JAN , KAVASH ROBERT W , KOYMANS LUCIEN MARIA HENRICUS , KUKLA MICHAEL JOSEPH , LUDOVICI DONALD WILLIAM , VAN AKEN KOEN JEANNE ALFONS
IPC分类号： C07D239/47 , C07D239/48 , A61K20060101 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/551 , A61K31/5513 , A61K31/675 , A61K31/715 , A61P31/18 , C07D20060101 , C07D239/42 , C07D239/46 , C07D239/50 , C07D239/80 , C07D401/12 , C07D403/12
摘要： Ovaj izum odnosi se na upotrebu spojeva formule (I),njihovih N-oksida, farmaceutski prihvatljivih adicijskih soli, kvaternih amina i njihovih stereokemijski izomernih oblika, u kojoj formuli-a=a-a=a- tvori fenil, piridinil, pirimidinil, piridazinil ili pirazinil s povezanom vinilnom skupinom;n je 0 do 4, i gdje je to moguće 5;Rje vodik, aril, formil, C-alkil karbonil, C-alkil, C-alkiloksikarbonil, supstituirani C-alkil, ili supstituirani C-alkiloksi-C-alkilkarbonil;svaki od Rneovisno predstavlja hidroksi, halogen, prema potrebi supstituirani C-alkil, C-alkenil ili C-alkinil, C-cikloalkil, C-alkiloksi, C-alkiloksi-karbonil, karboksil, cijano, nitro, amino, mono- ili di-(C-alkil)amino, polihalometil, polihalometiloksi, polihalometiltio, -S(=O)R, -NH-S(=O)R, -C(=O)R, -NHC(=O)H, -C(=O)NHNH, -NHC(=O)R, -C=NH) Rili peteročlani heterociklički prsten;p je 1 ili 2;L je prema potrebi supstituirani C-alkil, C-alkenil, C-alkinil, C-cikloalkil; iliL je -X-RgdjeRje prema potrebi supstituirani fenil, piridinil, pirimidinil, pirazinil ili piridazinil;X je -NR-, -NH-NH-, -N=N-, -O-, -C(=O)-, -CHOH-, -S-, -S(=O)- ili -S(=O)-;Q je vodik, C-alkil, halogen, polihalo-C-alkil ili prema potrebi supstituirana amino skupina;Y predstavlja hidroksi, halogen, C-cikloalkil, prema potrebi supstituirani C-alkil, C-alkenil ili C-alkinil, C-alkiloksi, C-alkiloksi-karbonil, karboksil, cijano, nitro, amino, mono- ili di (C-alkil) amino, polihalo-metil, polihalometiloksi, polihalometiltio, -S(=O)R, -NH-S(=O)R, -C(=O)R, -NHC(=O)H, -C(-O)NHNH, -NHC(=O)R, -C(=NH)Rili aril;aril je prema potrebi supstituirani fenil;Het je prema potrebi supstituirani heterociklički radikal;za proizvodnju lijeka za liječenje osoba koje pate od infekcije s HIV-om (virus humane imunodeficijencije).

6. 发明专利

BRPI0817433A2 Moduladores de gama-secretase piperidinila e piperazinila 未知
公开(公告)号：BRPI0817433A2
公开(公告)日：2015-06-16
申请号：BRPI0817433
申请日：2008-10-15
申请人： JANSSEN PHARMACEUTICA NV
发明人： HO CHIH YUNG
IPC分类号： C07D211/18 , A61K31/445 , A61K31/495 , A61P25/28 , C07D211/38 , C07D241/04 , C07D295/155 , C07D401/06 , C07D401/10 , C07D401/12 , C07D417/06

7. 发明专利

BRPI0817424A2 Ácido bifenil carboxílicos e derivados dos mesmos 未知
公开(公告)号：BRPI0817424A2
公开(公告)日：2015-06-16
申请号：BRPI0817424
申请日：2008-09-26
申请人： JANSSEN PHARMACEUTICA NV
发明人： HO CHIH YUNG
IPC分类号： C07C59/68 , A61K31/192 , A61P25/28

8. 发明专利

ES2395083T8 Acidos bifenilcarboxílicos y sus derivados 未知
公开(公告)号：ES2395083T8
公开(公告)日：2014-11-17
申请号：ES08839835
申请日：2008-09-26
申请人： JANSSEN PHARMACEUTICA NV , CELLZOME LTD
发明人： HO CHIH YUNG , MAHAROOF UMAR S M , MAJOR JEREMY , HARRISON JOHN
IPC分类号： C07C59/68 , A61K31/192 , A61P25/28

9. 发明专利

EA018862B1 МОДУЛЯТОРЫ γ-СЕКРЕТАЗЫ 未知
公开(公告)号：EA018862B1
公开(公告)日：2013-11-29
申请号：EA201070498
申请日：2008-10-17
申请人： JANSSEN PHARMACEUTICA NV
发明人： HO CHIH YUNG
IPC分类号： C07C229/34 , A61K31/195 , A61K31/404 , A61K31/435 , A61P25/28 , C07C229/42 , C07C255/58 , C07D209/08 , C07D213/74 , C07D215/06 , C07D215/38 , C07D217/04
摘要： Изобретениеотноситсяк соединениямс общейформулой I, какпоказанониже; определенияА, X, Y, RR, RR, R, R, R, Rи Rприведеныв спецификации. Соединенияформулы I могутприменятьсядлялечениязаболеваний, связанныхс активностьюγ-секретазы, включаяболезньАльцгеймера.

10. 发明专利

AU2008312612B2 Piperidinyl and piperazinyl modulators of gamma-secretase 未知
公开(公告)号：AU2008312612B2
公开(公告)日：2013-11-28
申请号：AU2008312612
申请日：2008-10-15
申请人： JANSSEN PHARMACEUTICA NV
发明人： HO CHIH YUNG
IPC分类号： C07D211/18 , A61K31/445 , A61K31/495 , A61P25/28 , C07D211/38 , C07D241/04 , C07D295/155 , C07D401/06 , C07D401/10 , C07D401/12 , C07D417/06
摘要： The present invention relates to compounds of Formula (I) as shown below, wherein the definitions of Het, R

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