公开(公告)号：EE04962B1

公开(公告)日：2008-02-15

申请号：EEP200100318

申请日：1999-12-17

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: A61K31/4709 ,  C07D215/06 ,  A61K31/4365 ,  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：NO318922B1

公开(公告)日：2005-05-23

申请号：NO20013088

申请日：2001-06-21

Applicant: JANSSEN PHARMACEUTICA NV

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

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 ,  A61K31/474

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：SK8732001A3

公开(公告)日：2002-02-05

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 ,  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：CA2716088C

公开(公告)日：2017-03-07

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：AU2008223793B2

公开(公告)日：2012-08-23

申请号：AU2008223793

申请日：2008-03-07

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D215/22 ,  A61K31/4704

Abstract: The present invention provides compounds of Formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds, wherein R, R, R, R, R, R, R, n, m and X have defined meanings.

公开(公告)号：SI2134691T1

公开(公告)日：2012-06-29

申请号：SI200830607

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: C07D215/00 ,  A61K31/00

公开(公告)号：ES2381446T3

公开(公告)日：2012-05-28

申请号：ES08717511

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

Abstract: Compuesto de fórmula (I), las formas de N-óxido, las sales de adición farmacéuticamente aceptables y las formas estereoquímicamente isoméricas del mismo, en los que m es 0, 1 ó 2 y cuando m es 0 entonces se pretende que sea un enlace directo; n es 0, 1, 2, 3 ó 4 y cuando n es 0 entonces se pretende que sea un enlace directo; X es un enlace directo, CR10R11, (C=O)NR8, NR8, O o C≡C; R1 es arilo o Het; en los que arilo es fenilo o naftalenilo; en los que Het es tienilo, pirrolilo, pirrolinilo, oxazolilo, tiazolilo, imidazolilo, pirazolilo, isoxazolilo, isotiazolilo, oxadiazolilo, triazolilo, tetrazolilo, tiadiazolilo, furanilo, piperidinilo, piridinilo, piridazinilo, pirimidinilo, piperazinilo, pirazinilo, triazinilo, indolizinilo, azaindolizinilo, indolilo, indolinilo, benzotienilo, indazolilo, benzoxazolilo, bencimidazolilo, benzofuranilo, benzotiazolilo, benzotriazolilo, cromanilo, purinilo, quinolinilo, cinolinilo, ftalazinilo, quinazolinilo, quinoxazolinilo, naftiridinilo o pteridinilo; dos átomos de carbono en el arilo o Het pueden formar un puente (es decir, formando un resto bi o tricíclico) con un radical bivalente seleccionado de -O-CH2-CH2-O- (a-1), -CH2-O-CH2-O- (a-2), -O-CH2-CH2-CH2- (a-3), -O-CH2-CH2-NR8- (a-4), -O-CR8 2-O- (a-5), -O-CH2-CH2- (a-6), -CH2-N-CH2-CH2- (a-7), -(CH2)3- (a-8), o -(CH2)4- (a-9); cada arilo, Het, arilo en puente o Het en puente puede estar sustituido con uno, dos, tres, cuatro o cinco sustituyentes seleccionados cada uno independientemente de hidrógeno, halo, ciano, nitro, hidroxicarbonilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, aminocicloalquilo C3-6, haloalquilo C1-6, trihaloalquilo C1-6, alquilcarbonilo C1-6, alquiloxicarbonilo C1-6, alquenilcarbonilo C2-6, oxima, alquiloxima C1-6, amidoxima, -CC-CH2O55 CH3, -CC-CH2N(CH3)2, -CC-Si(CH3)3, hidroxialquilo C1-6, hidroxialquenilo C2-6, hidroxialquinilo C2-6, cianoalquilo C1- 6, cianoalquenilo C2-6, aminocarbonilalquilo C1-6, alquilsulfonil C1-6-alquilo C1-6, alquilsulfonil C1-6-alquenilo C2-6, alquilsulfonil C1-6-alquinilo C1-6, -PO(O-alquilo C1-6)2, -B(OH)2, -SCH3, SF5, alquilsulfonilo C1-6, -NR8R9, alquil C1-6- NR8R9, -OR8, -alquil C1-6-OR8, -CONR8R9, piperidinilalquilo C1-6, piperazinilalquilo C1-6, alquil C1-6-piperazinilalquilo C1-6, morfolinilalquilo C1-6, piperidinilo, piperazinilo, alquil C1-6-piperazinilo, morfolinilo, fenilo, tienilo, pirazolilo, pirrolilo, pirrolidinilo, piridinilo, pirimidinilo, oxadiazolilo, imidazolilo, imidazolilalquinilo C2-6, alquil C1-6- imidazolilalquinilo C2-6, cianopiridinilo, fenilalquilo C1-6, fenilalquenilo C2-6, morfolinilalquilo C1-6, alquiloxi C1-6-fenilo, trihaloalquil C1-6-fenilo, metilpirazolilo, halopirimidinilo o dimetilaminopirrolidinilo; R2 es hidrógeno, metilo, etilo, propilo, cicloalquilo C3-6, cicloalquil C3-6-metilo, fluoro, fenilo, cianofenilo o trifluorometilo; R3 es metilo, etilo, propilo, hidroximetilo, halo, trifluorometilo, metiloxilo o alquilcarbonilo C1-6; R4 es hidrógeno, halo, metilo, aminocarbonilo, hidroxiaminocarbonilo, NR8R9-alquilo C1-6-, cianometilo, hidroximetilo o Het; cada R5, R6 y R7 se selecciona independientemente de hidrógeno, halo, alquiloxilo C1-6, ciano, alquilo C1-6, -OCH2CH2NR8R9, -CH2OCH2CH2NR8R9, -OCH2CH2CH2NR8R9 15 o alquiloxi C1-6-alquiloxilo C1-6; cada R8 y R9 se selecciona independientemente de hidrógeno, halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbonilo, alquilsulfonil C1-6-alquilo C1-6, alquiloxi C1-6-alquilo C1-6, hidroxialquilo C1-6, dihidroxialquilo C1-6, cianoalquilo C1-6, trihaloalquilo C1-6, fenilalquilo C1-6, (dialquil C1-6)-aminoalquilo C1-6, alquilsulfonilo C1-6, morfolinilalquilo C1-6, morfolinilcarbonilo, piperazinilalquilo C1-6, alquil C1-6-piperazinilalquilo C1-6, piperidinilalquilo C1-6, tiomorfolinilalquilo C1-6, cicloalquil C3-6-metilo, piridinilo, pirimidinilo, fenilo, halofenilo, oxanilalquilo C1-6, alquilsulfonil C1-6-alquilo C1-6 o alquil C1-6-carbonilaminoalquilo C1-6; cada R10 y R11 se selecciona independientemente de hidrógeno, metilo, hidroxilo, o tomados junto con el átomo de carbono al que están unidos pueden formar un anillo de ciclopropilo o un radical de fórmula C(=O).

公开(公告)号：PL199080B1

公开(公告)日：2008-08-29

申请号：PL34950499

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 ,  A61K31/435 ,  A61K31/4365 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/498 ,  A61K31/519 ,  A61P35/00 ,  C07D215/18 ,  C07D401/06 ,  C07D403/06 ,  C07D487/04

公开(公告)号：EA004542B1

公开(公告)日：2004-06-24

申请号：EA200100708

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: Данноеизобретениеотноситсяк соединениямформулы (I), ихфармацевтическиприемлемымсолямприсоединениякислотыи стереохимическиизомернымформам, где =Х-Х-Х- представляетсобойтривалентныйрадикал; >Y-Y- представляетсобойтривалентныйрадикал; r и s представляютсобой, каждыйнезависимо, 0, 1, 2, 3, 4 или 5; t равно 0, 1, 2 или 3; каждый Rи Rнезависимопредставляетсобойгидрокси, галоген, циано, Cалкил, тригалогенметил, тригалогенметокси, Салкенил, Cалкилокси, гидрокси Cалкилокси, Cалкилтио, СалкилоксиСалкилокси, Салкилоксикарбонил, аминоСалкилокси, моно- илиди(Салкил)амино, моно- илиди (Cалкил)аминоСалкилокси, арил, арилСалкил, арилоксиилиарилСалкилокси, гидроксикарбонил, Салкилоксикарбонил; оба Rили Rзаместителя, соседниедругс другом, образуютбивалентныйрадикал; Rпредставляетсобойводород, галоген, Салкил, циано, галоген Cалкил, гидроксиСалкил, цианоСалкил, аминоСалкил, CалкилоксиСалкил, СалкилтиоСалкил, аминокарбонилСалкил, гидроксикарбонил, гидроксикарбонилСалкил, СалкилоксикарбонилСалкил, СалкилкарбонилСалкил, Салкилоксикарбонил, арил, арилСалкилоксиСалкил, моно- илиди(Салкил)аминоСалкилилирадикалформулы -O-R, -S-Rили -NRR; Rпредставляетсобойнеобязательнозамещенныйимидазолил; арилпредставляетсобойнеобязательнозамещенныйфенилилинафталенил; имеющимфарнезилтрансферазнуюи геранилгеранилтрансферазнуюингибирующуюактивность; кихполучению, ихсодержащимкомпозициями ихиспользованиюв медицине.

公开(公告)号：DE69907964T2

公开(公告)日：2004-02-19

申请号：DE69907964

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.