公开(公告)号：ES2200591T3

公开(公告)日：2004-03-01

申请号：ES99969220

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：PT1140935E

公开(公告)日：2003-10-31

申请号：PT99969220

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：HU0104582A2

公开(公告)日：2002-04-29

申请号：HU0104582

申请日：1999-12-17

Applicant: JANSSEN PHARMACEUTICA NV

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

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：CZ20012142A3

公开(公告)日：2002-01-16

申请号：CZ20012142

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：BR9916827A

公开(公告)日：2001-10-16

申请号：BR9916827

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：DK2134691T3

公开(公告)日：2012-05-07

申请号：DK08717511

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 BERNADETTE ,  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：CA2355717C

公开(公告)日：2011-02-08

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

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, hydroxyC1-6alkyloxy, C1-6alkylthio, C1-6alkyloxyC1-6alkyloxy, C1-4alkyloxycarbonyl, 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, hydroxy-carbonylC1-6alkyl, 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-R10, -S-R10 or -NR11R12; R4 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：CA2716088A1

公开(公告)日：2009-10-01

申请号：CA2716088

申请日：2009-03-26

Applicant: JANSSEN PHARMACEUTICA NV

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

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：CA2678248A1

公开(公告)日：2008-09-12

申请号：CA2678248

申请日：2008-03-07

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ROUX BRUNO ,  PASQUIER ELISABETH THERESE JEANNE ,  PILATTE ISABELLE NOELLE CONSTANCE ,  MEYER CHRISTOPHE ,  FREYNE EDDY JEAN EDGARD ,  BOURDREZ XAVIER MARC ,  ADELINET CHRISTOPHE DENIS ,  DUFFY JAMES EDWARD STEWART ,  ANGIBAUD PATRICK RENE ,  MEVELLEC LAURENCE ANNE ,  PONCELET VIRGINIE SOPHIE ,  STORCK PIERRE-HENRI ,  OWENS ANDREW PATE ,  VIALARD JORGE EDUARDO ,  MARCONNET-DECRANE LAURENCE FRANCOISE BERNADETTE ,  MACRITCHIE JACQUELINE ANNE

IPC: C07D215/22 ,  A61K31/4704

Abstract: The present invention provides compounds of Formula (I), their use as PAR P inhibitors as well as pharmaceutical compositions comprising said compound s, wherein R1, R2, R3, R4, R5, R6, R7, n, m and X have defined meanings.

公开(公告)号：SI1140935T1

公开(公告)日：2003-10-31

申请号：SI9930350

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.