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

Applicant: 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

Inventor： 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: C07D215/22 ,  A61K31/4704

CPC classification number: C07D215/227 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO0039082A3

公开(公告)日：2000-10-26

申请号：PCT/EP9910214

申请日：1999-12-17

Applicant: JANSSEN PHARMACEUTICA NV ,  ANGIBAUD PATRICK RENE ,  VENET MARC GASTON ,  BOURDREZ XAVIER MARC

Inventor： ANGIBAUD PATRICK RENE ,  VENET MARC GASTON ,  BOURDREZ XAVIER MARC

IPC: C07D215/06 ,  A61K31/4365 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  A61P35/00 ,  C07D215/18 ,  C07D401/06 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D401/06 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04

Abstract: This invention concerns compounds of formula (I), the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein =X -X -X - is a trivalent radical; >Y -Y - is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R and R are independently hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)amino, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, aryl, arylC1-6alkyl, aryloxy or arylC1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl; or two R or R on adjacent positions form together a bivalent radical; R is hydrogen, halo, C1-6alkyl, cyano, haloC1-6alkyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, aminoC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1-6alkylthio-C1-6alkyl, aminocarbonylC1-6alkyl, hydroxycarbonyl, hydroxycarbonylC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, C1-6alkylcarbonylC1-6alkyl, C1-6alkyloxycarbonyl, aryl, arylC1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, or a radical of formula -O-R , -S-R or -NR R ; R is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

Abstract translation: 本发明涉及式（I）化合物，其药学上可接受的酸加成盐及其立体化学异构形式，其中= X 1 -X 2 -X 3 - 为三价基团; Y 1 -Y 2 - 为三价基团; r和s各自独立地为0,1,2,3,4或5; t是0,1,2或3; 每个R 1和R 2独立地为羟基，卤素，氰基，C 1-6烷基，三卤甲基，三卤甲氧基，C 2-6烯基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷硫基，C 1-6烷氧基C 1-6烷氧基， 单或二（C1-6烷基）氨基，单或二（C1-6烷基）氨基C1-6烷氧基，芳基，芳基C1-6烷基，芳氧基或芳基C1-6烷氧基，羟基羰基，C1-6烷氧基羰基; 或者在相邻位置上的两个R 1或R 2一起形成二价基团; R 3是氢，卤素，C 1-6烷基，氰基，卤代C 1-6烷基，羟基C 1-6烷基，氰基C 1-6烷基，氨基C 1-6烷基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基-C 1-6烷基，氨基羰基C 1-6烷基， ，羟基羰基C1-6烷基，C1-6烷氧基羰基C1-6烷基，C1-6烷基羰基C1-6烷基，C1-6烷氧基羰基，芳基，芳基C1-6烷氧基C1-6烷基，单或二（C1-6烷基）氨基C1-6烷基， -SR 10或-NR 11 R 12; R 4是任选取代的咪唑基; 芳基是任选取代的苯基或萘基; 具有法尼基转移酶和香叶基香叶基转移酶抑制活性; 它们的制备，含有它们的组合物以及它们作为药物的用途。

公开(公告)号：HU229404B1

公开(公告)日：2013-12-30

申请号：HU0104582

申请日：1999-12-17

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANGIBAUD PATRICK RENE ,  VENET MARC GASTON ,  BOURDREZ XAVIER MARC

IPC: C07D215/06 ,  C07D471/04 ,  A61K31/4365 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  A61P35/00 ,  C07D215/16 ,  C07D215/18 ,  C07D401/06 ,  C07D403/06 ,  C07D487/04

Abstract: This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein -X 1 -X 2 -X 3 - is a trivalent radical,; >Y 1 -Y 2 - is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R 1 and R 2 are independently hydroxy, halo, cyano, C 1-6 alkyl, trihalomethyl, trihalomethoxy, C 2-6 alkenyl, C 1-6 alkyloxy, hydroxyC 1-6 alkyloxy, C 1-6 alkylthio, C 1-6 alkyloxyC 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, aminoC 1-6 alkyloxy, mono- or di(C 1-6 alkyl)amino, mono- or di(C 1-6 alkylaminoC 1-6 alkyloxy, aryl, arylC 1-6 alkyl, aryloxy or arylC 1-6 alkyloxy, hydroxycarbonyl, C 1-6 alkyloxycarbonyl; or two R 1 or R 2 on adjacent positions form together a bivalent radical; R 3 is hydrogen, halo, C 1-6 alkyl, cyano, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, cyanoC 1-6 alkyl, aminoC 1-6 alkyl, C 1-6 alkyloxyC 1-6 alkyl, C 1-6 alkylthio-C 1-6 alkyl, aminocarbonylC 1-6 alkyl, hydroxycarbonyl, hydroxycarbonylC 1-6 alkyl, C 1-6 alkyoxycarbonylC 1-6 alkyl, C 1-6 alkylcarbonylC 1-6 alkyl, C 1-6 alkyloxycarbonyl, aryl, arylC 1-6 alkyloxyC 1-6 alkyl, mono- or di(C 1-6 alkyl)aminoC 1-6 alkyl, or a radical of formula -O-R 10 , -S-R 10 or -NR 11 R 12 ; R 4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

公开(公告)号：AU2009228945A1

公开(公告)日：2009-10-01

申请号：AU2009228945

申请日：2009-03-26

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MEYER CHRISTOPHE ,  FREYNE EDDY JEAN EDGARD ,  BOURDREZ XAVIER MARC ,  PASQUIER ELISABETH THERESE JEANNE ,  MEVELLEC LAURENCE ANNE ,  ANGIBAUD PATRICK RENE ,  VIALARD JORGE EDUARDO

IPC: C07D239/80 ,  A61K31/517 ,  A61P35/00 ,  C07D401/06 ,  C07D417/06

Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, n, m and X have defined meanings.

公开(公告)号：AU765437B2

公开(公告)日：2003-09-18

申请号：AU2795300

申请日：1999-12-17

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANGIBAUD PATRICK RENE ,  VENET MARC GASTON ,  BOURDREZ XAVIER MARC

IPC: C07D215/06 ,  A61K31/4365 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  A61P35/00 ,  C07D215/18 ,  C07D401/06 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04

Abstract: This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein -X 1 -X 2 -X 3 - is a trivalent radical,; >Y 1 -Y 2 - is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R 1 and R 2 are independently hydroxy, halo, cyano, C 1-6 alkyl, trihalomethyl, trihalomethoxy, C 2-6 alkenyl, C 1-6 alkyloxy, hydroxyC 1-6 alkyloxy, C 1-6 alkylthio, C 1-6 alkyloxyC 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, aminoC 1-6 alkyloxy, mono- or di(C 1-6 alkyl)amino, mono- or di(C 1-6 alkylaminoC 1-6 alkyloxy, aryl, arylC 1-6 alkyl, aryloxy or arylC 1-6 alkyloxy, hydroxycarbonyl, C 1-6 alkyloxycarbonyl; or two R 1 or R 2 on adjacent positions form together a bivalent radical; R 3 is hydrogen, halo, C 1-6 alkyl, cyano, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, cyanoC 1-6 alkyl, aminoC 1-6 alkyl, C 1-6 alkyloxyC 1-6 alkyl, C 1-6 alkylthio-C 1-6 alkyl, aminocarbonylC 1-6 alkyl, hydroxycarbonyl, hydroxycarbonylC 1-6 alkyl, C 1-6 alkyoxycarbonylC 1-6 alkyl, C 1-6 alkylcarbonylC 1-6 alkyl, C 1-6 alkyloxycarbonyl, aryl, arylC 1-6 alkyloxyC 1-6 alkyl, mono- or di(C 1-6 alkyl)aminoC 1-6 alkyl, or a radical of formula -O-R 10 , -S-R 10 or -NR 11 R 12 ; R 4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

公开(公告)号：NO20013088L

公开(公告)日：2001-06-21

申请号：NO20013088

申请日：2001-06-21

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANGIBAUD PATRICK RENE ,  VENET MARC GASTON ,  BOURDREZ XAVIER MARC

IPC: C07D215/06 ,  A61K31/4365 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  A61P35/00 ,  C07D215/18 ,  C07D401/06 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04

Abstract: This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein -X 1 -X 2 -X 3 - is a trivalent radical,; >Y 1 -Y 2 - is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R 1 and R 2 are independently hydroxy, halo, cyano, C 1-6 alkyl, trihalomethyl, trihalomethoxy, C 2-6 alkenyl, C 1-6 alkyloxy, hydroxyC 1-6 alkyloxy, C 1-6 alkylthio, C 1-6 alkyloxyC 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, aminoC 1-6 alkyloxy, mono- or di(C 1-6 alkyl)amino, mono- or di(C 1-6 alkylaminoC 1-6 alkyloxy, aryl, arylC 1-6 alkyl, aryloxy or arylC 1-6 alkyloxy, hydroxycarbonyl, C 1-6 alkyloxycarbonyl; or two R 1 or R 2 on adjacent positions form together a bivalent radical; R 3 is hydrogen, halo, C 1-6 alkyl, cyano, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, cyanoC 1-6 alkyl, aminoC 1-6 alkyl, C 1-6 alkyloxyC 1-6 alkyl, C 1-6 alkylthio-C 1-6 alkyl, aminocarbonylC 1-6 alkyl, hydroxycarbonyl, hydroxycarbonylC 1-6 alkyl, C 1-6 alkyoxycarbonylC 1-6 alkyl, C 1-6 alkylcarbonylC 1-6 alkyl, C 1-6 alkyloxycarbonyl, aryl, arylC 1-6 alkyloxyC 1-6 alkyl, mono- or di(C 1-6 alkyl)aminoC 1-6 alkyl, or a radical of formula -O-R 10 , -S-R 10 or -NR 11 R 12 ; R 4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

公开(公告)号：NO20013088D0

公开(公告)日：2001-06-21

申请号：NO20013088

申请日：2001-06-21

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANGIBAUD PATRICK RENE ,  VENET MARC GASTON ,  BOURDREZ XAVIER MARC

IPC: C07D215/06 ,  A61K31/4365 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  A61P35/00 ,  C07D215/18 ,  C07D401/06 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04 ,  C07D

Abstract: This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein -X 1 -X 2 -X 3 - is a trivalent radical,; >Y 1 -Y 2 - is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R 1 and R 2 are independently hydroxy, halo, cyano, C 1-6 alkyl, trihalomethyl, trihalomethoxy, C 2-6 alkenyl, C 1-6 alkyloxy, hydroxyC 1-6 alkyloxy, C 1-6 alkylthio, C 1-6 alkyloxyC 1-6 alkyloxy, C 1-6 alkyloxycarbonyl, aminoC 1-6 alkyloxy, mono- or di(C 1-6 alkyl)amino, mono- or di(C 1-6 alkylaminoC 1-6 alkyloxy, aryl, arylC 1-6 alkyl, aryloxy or arylC 1-6 alkyloxy, hydroxycarbonyl, C 1-6 alkyloxycarbonyl; or two R 1 or R 2 on adjacent positions form together a bivalent radical; R 3 is hydrogen, halo, C 1-6 alkyl, cyano, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, cyanoC 1-6 alkyl, aminoC 1-6 alkyl, C 1-6 alkyloxyC 1-6 alkyl, C 1-6 alkylthio-C 1-6 alkyl, aminocarbonylC 1-6 alkyl, hydroxycarbonyl, hydroxycarbonylC 1-6 alkyl, C 1-6 alkyoxycarbonylC 1-6 alkyl, C 1-6 alkylcarbonylC 1-6 alkyl, C 1-6 alkyloxycarbonyl, aryl, arylC 1-6 alkyloxyC 1-6 alkyl, mono- or di(C 1-6 alkyl)aminoC 1-6 alkyl, or a radical of formula -O-R 10 , -S-R 10 or -NR 11 R 12 ; R 4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

公开(公告)号：CA2355717A1

公开(公告)日：2000-07-06

申请号：CA2355717

申请日：1999-12-17

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANGIBAUD PATRICK RENE ,  VENET MARC GASTON ,  BOURDREZ XAVIER MARC

IPC: C07D215/06 ,  A61K31/4365 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  A61P35/00 ,  C07D215/18 ,  C07D401/06 ,  C07D403/06 ,  C07D471/04 ,  C07D487/04 ,  C07D221/00 ,  C07D235/00 ,  C07D239/00 ,  C07D249/00 ,  C07D257/00

Abstract: This invention concerns compounds of formula (I), the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein =X1-X2-X3- is a trivalent radical; ~Y1-Y2- is a trivalent radical; r and s are each independently 0, 1, 2, 3, 4 or 5; t is 0, 1, 2 or 3; each R1 and R2 are independently hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkylox y, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1- 6alkyloxy, mono- or di(C1-6alkyl)amino, mono- or di(C1-6alkyl)aminoC1- 6alkyloxy, aryl, arylC1-6alkyl, aryloxy or arylC1-6alkyloxy, hydroxycarbonyl , C1-6alkyloxycarbonyl; or two R1 or R2 on adjacent positions form together a bivalent radical; R3 is hydrogen, halo, C1-6alkyl, cyano, haloC1-6alkyl, hydroxyC1-6alkyl, cyanoC1-6alkyl, aminoC1-6alkyl, C1-6alkyloxyC1-6alkyl, C1- 6alkylthio-C1-6alkyl, aminocarbonylC1-6alkyl, hydroxycarbonyl, hydroxycarbonylC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, C1-6alkylcarbonylC1 - 6alkyl, C1-6alkyloxycarbonyl, aryl, arylC1-6alkyloxyC1-6alkyl, mono- or di(C 1- 6alkyl)aminoC1-6alkyl, or a radical of formula -O-R10, -S-R10 or -NR11R12; R 4 is an optionally substituted imidazolyl; aryl is an optionally substituted phenyl or naphthalenyl; having farnesyl transferase and geranylgeranyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

公开(公告)号：AT542799T

公开(公告)日：2012-02-15

申请号：AT08717511

申请日：2008-03-07

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： 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 ,  MACRITCHIE JACQUELINE ANNE ,  DUFFY JAMES EDWARD STEWART ,  OWENS ANDREW PATE ,  STORCK PIERRE-HENRI ,  PONCELET VIRGINIE SOPHIE

IPC: C07D215/22 ,  A61K31/4704

公开(公告)号：SK286072B6

公开(公告)日：2008-02-05

申请号：SK8732001

申请日：1999-12-17

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ANGIBAUD PATRICK RENE ,  VENET MARC GASTON ,  BOURDREZ XAVIER MARC

IPC: C07D215/06 ,  C07D471/00 ,  A61K31/00 ,  A61K31/4365 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  A61P35/00 ,  C07D215/18 ,  C07D401/00 ,  C07D401/06 ,  C07D403/00 ,  C07D403/06 ,  C07D471/04 ,  C07D487/00 ,  C07D487/04

Abstract: The invention concerns quinoline derivatives of general formula (I), their pharmaceutically acceptable acid addition salt or a stereo chemically isomeric form thereof, method for their preparation, its intermediates, pharmaceutical composition comprising them and their use as a medicine. The compounds of formula (I) have farnesyl transferase and geranylgeranyl transferase inhibiting activity.