公开(公告)号：WO2006075023A3

公开(公告)日：2006-09-28

申请号：PCT/EP2006050206

申请日：2006-01-13

Applicant: JANSSEN PHARMACEUTICA NV ,  LOVE CHRISTOPHER JOHN ,  COOYMANS LUDWIG PAUL ,  VANDERMAESEN NELE

Inventor： LOVE CHRISTOPHER JOHN ,  COOYMANS LUDWIG PAUL ,  VANDERMAESEN NELE

IPC: C07D487/04 ,  A61K31/519 ,  A61P3/10

CPC classification number: C07D487/04

Abstract: This invention concerns a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R 1 represents hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 alkyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl or C 1-6 alkylcarbonyloxy; X represents a direct bond; -(CH 2 ) n3 - or -(CH 2 ) n4 -X 1a -X 1b -; R 2 represents an optionally substituted cyclic system; provided that N,3-diphenyl-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-amine is not included ; their use, pharmaceutical compositions comprising them and processes for their preparation.

Abstract translation: 本发明涉及式（I）化合物，其N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A表示苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; R 1代表氢; 芳基; 甲酰基; ç _{1-6 烷基羰基; ç 1-6 烷基; ç 1-6 烷氧基羰基; 被甲酰基取代的C 1-6烷基，C 1-6烷基羰基，C 1-6烷氧基羰基或C 1-6烷基羰基， / SUB>烷基羰基氧基; X代表直接键; - （CH 2 ） n3 < - >或 - （CH 2 ） n4 -X < SUB> -X 图1b - ; R 2代表任选取代的环体系; 条件是不包括N，3-二苯基-3H-1,2,3-三唑并[4,5-d]嘧啶-5-胺; 它们的用途，包含它们的药物组合物以及它们的制备方法。}

公开(公告)号：WO2005012304A3

公开(公告)日：2007-04-26

申请号：PCT/EP2004051457

申请日：2004-07-12

Applicant: JANSSEN PHARMACEUTICA NV ,  FREYNE EDDY JEAN EDGARD ,  LOVE CHRISTOPHER JOHN ,  COOYMANS LUDWIG PAUL ,  VANDERMAESEN NELE ,  BUIJNSTERS PETER JACOBUS JOHAN ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA

Inventor： FREYNE EDDY JEAN EDGARD ,  LOVE CHRISTOPHER JOHN ,  COOYMANS LUDWIG PAUL ,  VANDERMAESEN NELE ,  BUIJNSTERS PETER JACOBUS JOHAN ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA

IPC: C07D487/04 ,  A61K31/519 ,  A61P3/10 ,  A61P25/24 ,  C07D235/00 ,  C07D249/00

CPC classification number: C07D487/04

Abstract: This invention concerns compounds of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochernically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R 1 represents hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 a]kyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonytoxy; or optionally substituted C 1-6 alkyloxyCl-6alkylcarbonyl; X 1 represents a direct bond; -(CH 2 ) n3 - or -(CH 2 ) n4 -X 1a -X 1b -; R 2 represents optionally substituted C 3-7 CYCloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatorn selected from 0, S or N; benzoxazolyl or a radical of formula (a-1); X 2 represents a direct bond; -NR 1 -NR 1 -(CH 2 ) N3 -; -0-; -0-(CH 2 ) n3 -; -C(=O)-; -C(=O)- (CH 2 ) n3 -; -C(=O)-NR 5 -(CH 2 ) n3 -; -C(=S)-; -S-; -S(=O) n1 -; -(CH 2 ) n3 -; -(CH 2 ) n4 -X 1a -X 1b -; -X 1a .-X 1b -(CH 2 ) n4 -; -S(=O) n1 -NR 5 -(CH 2 ) n3 -NR 5 _ or -S(=O) n1 ,-NR 5 -(CH 2 ) n3 -; R 3 represents an optionally substituted 5-or 6-membered monocyclic heterocycle containing at least one heteroatom selected from 0, S or N, or a 9-or 10-membered bicyclic heterocycle containing at least one heteroatom selected from 0, S or N; R 4 represents hydrogen; halo; hydroxy; optionally substituted C 1-4 alkyl; optionally substituted C 2-4 alkenyl or C 2-4 alkynyl; polyhaloC 1-3 alkyl; optionally substituted C 1-4 alkyloxy; polyhaloC 1-3 alkyloxy; C 1-4 alkylthio; polyhaloC 1-3 alkylthio; C 1-4 alkyloxycarbonyl; C 1-4 alkylcarbonyloxy; C 1-4 alkylcarbonyl; polyhaloC 1-4 alkylcarbonyl; nitro; cyano; carboxyl; NR 9 R 10 ; C(=O)NR 9 R 10 ;-NR 5_ C(=O)-NR 9 R 10 ; -NR 5 -C(=O)-R 5 ; -S(=O) n1 ,-R 11 -NR 5 -S(=O) n1 ,-R 11 -S-CN; -NR 5 -CN; their use, pharmaceutical compositions comprising them and processes for their preparation.

Abstract translation: 本发明涉及式（I）的化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体异构体形式，其中环A表示苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; R 1表示氢; 芳基; 甲酰基; C 1-6烷基羰基; C 1-6 a] kyl; C 1-6烷氧基羰基; 被甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基取代的C 1-6烷基， / SUB> alkylcarbonytoxy; 或任选取代的C 1-6烷氧基C 1-6烷基羰基; X 1表示直接键; - （CH 2 2）n3 - 或 - （CH 2）n4 - - - - - SUB> -X _{图1b - ; R 2表示任选取代的C 3-7环烷基; 苯基; 含有至少一个选自0，S或N的杂化子的4,5,6-或7-元单环杂环; 苯并恶唑基或式（a-1）基团; X 2代表直接键; -NR 1 - （CH 2）N 3 - ;（CH 2）N 3 - 。 -0-; -O-（CH 2 ） N3 - ; -C（= O） - ; -C（= O） - （CH 2）n3 - ; -C（= O）-NR ^{5 - （CH 2 ） N3 - ; -C（= S） - ; -S-; -S（= O） N1 - ; - （CH 2 ） N3 - ; - （CH 2 ） N4 -X 1A -X 图1b - ; -X 1A .- X 图1b - （CH 2 ） N4 - ; -S（= O） N1 -NR 5 - （CH 2 ） N3 -NR 5 n =（CH 2）n或-S（= O）n1， - NR 5 - （CH 2）n 3 - ; R 3表示含有至少一个选自O，S或N的杂原子或含有至少一个杂原子的9元或10元双环杂环的任选取代的5元或6元单环杂环 从0，S或N; R 4表示氢; 光环; 羟基; 任选取代的C 1-4烷基; 任选取代的C 2-4 - 烯基或C 2-4 - 炔基; 多卤代 1-3 烷基; 任选取代的C 1-4烷氧基; 多卤代 1-3 烷氧基; ç 1-4 烷硫基; 多卤代 1-3 烷硫基; ç 1-4 烷氧基羰基; ç 1-4 烷基羰基氧基; ç 1-4 烷基羰基; 多卤代 1-4 烷基羰基; 硝基; 氰基; 羧基; NR 9 - [R 10 ; C（= O）NR 9 - [R 10 ; - NR 5 _ C（= O）-NR 9 ř 10 ; -NR 5 C（= O）-R 5 ; -S（= O）n1， - R 11 -NR 5 -S（= O）n1， -R 11 -S-CN; -NR 5 -CN; 其用途，包含它们的药物组合物及其制备方法。}}

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

Applicant: JANSSEN PHARMACEUTICA NV ,  ROMBOUTS FREDERIK JAN RITA ,  LOVE CHRISTOPHER JOHN ,  EMELEN KRISTOF VAN ,  VAN BRANDT SVEN FRANCISCUS ANN ,  WU TONGFEI

Inventor： ROMBOUTS FREDERIK JAN RITA ,  LOVE CHRISTOPHER JOHN ,  VAN EMELEN KRISTOF ,  VAN BRANDT SVEN FRANCISCUS ANN ,  WU TONGFEI

IPC: C07D251/16 ,  A61K31/53 ,  C07D401/04 ,  C07D471/18 ,  C07D471/22 ,  C07D487/08 ,  C07D487/18

CPC classification number: C07D487/18 ,  C07D251/16 ,  C07D401/04 ,  C07D471/18 ,  C07D471/22 ,  C07D487/08

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO03037891A8

公开(公告)日：2003-09-04

申请号：PCT/EP0212077

申请日：2002-10-29

Applicant: JANSSEN PHARMACEUTICA NV ,  FREYNE EDDY JEAN EDGARD ,  BUIJNSTERS PETER JACOBUS JOHAN ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA ,  LOVE CHRISTOPHER JOHN ,  JANSSEN PAUL ADRIAAN JAN ,  LEWI PAULUS JOANNES ,  HEERES JAN ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  VINKERS HENDRIK MAARTEN ,  VAN AKEN KOEN JEANNE ALFONS ,  DIELS GASTON STANISLAS MARCELL

Inventor： FREYNE EDDY JEAN EDGARD ,  BUIJNSTERS PETER JACOBUS JOHAN ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA ,  LOVE CHRISTOPHER JOHN ,  JANSSEN PAUL ADRIAAN JAN ,  LEWI PAULUS JOANNES ,  HEERES JAN ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  VINKERS HENDRIK MAARTEN ,  VAN AKEN KOEN JEANNE ALFONS ,  DIELS GASTON STANISLAS MARCELL

IPC: A61K31/435 ,  A61K31/4406 ,  A61K31/50 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61P3/10 ,  A61P17/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P31/18 ,  A61P35/00 ,  A61P35/02 ,  C07D213/53 ,  C07D213/74 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

CPC classification number: C07D213/74 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

Abstract: This invention concerns a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxy C1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C1-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C1-6alkyl; R21-O-; R21-S-; R21-C(=0)-; R21-S(=0)p-; R7-S =O R7-S(=O)p-NH-; R21-S(=O)p-NH-; R7-C(=0)-; -NHC(=0)H; -C(=O)NHNH2; R7-C(=O)-NH-; R21-C(=O)-NH-; -C(=NH)R7; -C(=NH)R21; R° is an optionally substituted heterocycle provided that -X-R2 and/or R3 is other than hydrogen;their use, pharmaceutical compositions comprising them and processes for their preparation.

Abstract translation: 本发明涉及式（I）化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A为6-元杂环; R1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是直接键或连接原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 1-6烯基或C 2-6炔基; C1-6烷; C 1-6烷; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; 羧基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C 1-6烷基; R21-O-; R21-S-; R21-C（= O） - ; R21-S（= O）p - ; R7-S = O R7-S（= O）p-NH-; R21-S（= O）P-NH-; R7-C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; R7-C（= O）-NH-; R21-C（= O）-NH-; -C（= NH）R 7; -C（= NH）R 21; R°是任选取代的杂环，条件是-X-R 2和/或R 3不是氢;它们的用途，包含它们的药物组合物及其制备方法。

公开(公告)号：CA2611438C

公开(公告)日：2014-01-07

申请号：CA2611438

申请日：2006-06-26

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ROMBOUTS FREDERIK JAN RITA ,  LOVE CHRISTOPHER JOHN ,  VAN EMELEN KRISTOF ,  VAN BRANDT SVEN FRANCISCUS ANNA ,  WU TONGFEI

IPC: C07D487/18 ,  A61K31/53 ,  C07D251/42 ,  C07D471/18 ,  C07D471/22 ,  C07D487/08

Abstract: 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.

公开(公告)号：ES2407807T3

公开(公告)日：2013-06-14

申请号：ES02758455

申请日：2002-08-09

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： LOVE CHRISTOPHER JOHN ,  VAN LOMMEN GUY ROSALIA EUGEEN ,  DOYON JULIEN GEORGESPIERRE-OLIVIER ,  BONGARTZ JEAN-PIERRE ANDRE MARC ,  VAN DER AA MARCEL JOZEF MARIA ,  HENDRICKX ROBERT JOZEF MARIA ,  BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS ,  COOYMANS LUDWIG PAUL ,  VANDERMAESEN NELE ,  COESEMANS ERWIN ,  BOECKX GUSTAAF MARIA

IPC: A61K31/425 ,  A61K31/429 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/5377 ,  A61P29/00 ,  A61P33/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D221/00 ,  C07D235/00 ,  C07D277/00 ,  C07D277/42 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04

Abstract: Uso de un compuesto para la fabricación de un medicamento para la prevención o el tratamiento deenfermedades autoinmunitarias mediadas por TNF-a (factor de necrosis tumoral alfa) y/o IL-12 (interleucina 12), enel que el compuesto es un compuesto de fórmula **Fórmula** un N-óxido, una sal de adición farmacéuticamente aceptable, una amina cuaternaria y una formaestereoquímicamente isomérica del mismo, en la que Z es halo; alquilo C1-6; alquilcarbonilo C1-6; aminocarbonilo; alquilo C1-6 sustituido con hidroxilo, carboxilo, ciano,amino, amino sustituido con piperidinilo, amino sustituido con piperidinilo sustituido con alquilo C1-4, mono o di(alquilC1-6)amino, aminocarbonilo, mono o di(alquil C1-6)aminocarbonilo, alquiloxicarbonilo C1-6, alquiloxilo C1-6, piperidinilo,piperazinilo, morfolinilo o tiomorfolinilo; polihaloalquilo C1-4; ciano; amino; mono o di(alquil C1-6)aminocarbonilo;alquiloxicarbonilo C1-6; alquilcarboniloxilo C1-6; amino-S(>=O)2-; mono o di(alquil C1-6)amino-S(>=O)2 o -C(>=N-Rx)NRyRz;Rx es hidrógeno, alquilo C1-6, ciano, nitro o -S(>=O)2-NH2; Ry es hidrógeno, alquilo C1-6, alquenilo C2-6 o alquinilo C2-6; Rz es hidrógeno o alquilo C1-6; Q es cicloalquilo C3-6, fenilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, benzotiazolilo, benzoxazolilo, bencimidazolilo,indazolilo o imidazopiridilo, estando cada uno de dichos anillos opcionalmente sustituido con hasta tressustituyentes, seleccionado cada uno independientemente de halo; hidroxilo; ciano; carboxilo; azido; amino; mono odi(alquil C1-6)amino; alquilcarbonilamino C1-6; alquilo C1-6; alquenilo C2-6; alquinilo C2-6; cicloalquilo C3-6; alquilo C1-6sustituido con hidroxilo, alquiloxilo C1-6, amino o mono o di(alquil C1-4)amino; alquiloxilo C1-6; alquiltio C1-6;alquilcarbonilo C1-6; alquiloxicarbonilo C1-6; arilalquiloxilo C1-6; ariloxilo; polihaloalquilo C1-6; polihaloalquiloxilo C1-6;polihaloalquilcarbonilo C1-6; Het; (alquil C1-4)-S(>=O)n- o R1HN-S(>=O)n-.

公开(公告)号：AU2009239471B2

公开(公告)日：2013-01-24

申请号：AU2009239471

申请日：2009-04-21

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： WIENER DANIELLE ,  LEBSACK ALEC DONALD ,  LEENAERTS JOSEPH ELISABETH ,  RECH JASON CHRISTOPHER ,  VENABLE JENNIFER DIANE ,  COOYMANS LUDWIG PAUL ,  SMITH DEBORAH MARGARET ,  BREITENBUCHER JAMES GUY ,  LOVE CHRISTOPHER JOHN ,  GLEASON ELIZABETH ANN ,  BRANSTETTER BRYAN JAMES

IPC: C07D401/14 ,  A61K31/4427 ,  C07D405/14 ,  C07D413/14

Abstract: The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I)

公开(公告)号：CA2451981C

公开(公告)日：2012-02-21

申请号：CA2451981

申请日：2002-08-09

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： LOVE CHRISTOPHER JOHN ,  VAN WAUWE JEAN PIERRE FRANS ,  DE BRABANDER MARC J ,  MOSES ROGER CLIVE ,  COOYMANS LUDWIG PAUL ,  VANDERMAESEN NELE ,  DIELS GASTON STANISLAS MARCELLA ,  SIBLEY ANTHONY WILLIAM ,  NOULA CATERINA ,  GONCHARENKO MYKHAYLO

IPC: C07D277/24 ,  A61K31/426 ,  A61K31/427 ,  A61K31/497 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/16 ,  A61P5/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P25/16 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/22 ,  A61P33/14 ,  A61P35/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P39/02 ,  C07D277/28 ,  C07D417/04 ,  C07D417/14

Abstract: This invention concerns the use of a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, mono -or di(C1-6alkyl)amino, aminocarbonyl, mono -or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl or C1-6alkyloxy; polyhaloC1-4alkyl; C1-4alkyloxy; cyano; amino; aminocarbonyl; mono -or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; H2N-S(=O)2-; mono -or di(C1-6alkyl)amino-S(=O)2; -C(=N-Rx)NRyRz; Q is an optionally substituted carbocycle or an optionally substituted heterocycle; L is substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through TNF-.alpha. and/or IL-12.

公开(公告)号：HK1128086A1

公开(公告)日：2009-10-16

申请号：HK09105680

申请日：2009-06-24

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ROMBOUTS FREDERIK JAN RITA ,  LOVE CHRISTOPHER JOHN ,  EMELEN KRISTOF VAN ,  BRANDT SVEN FRANCISCUS ANNA VAN ,  WU TONGFEI

IPC: C07D20060101 ,  A61K20060101

Abstract: 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.

公开(公告)号：AT439349T

公开(公告)日：2009-08-15

申请号：AT06777463

申请日：2006-06-26

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： ROMBOUTS FREDERIK JAN RITA ,  LOVE CHRISTOPHER JOHN ,  VAN EMELEN ,  VAN BRANDT SVEN FRANCISCUS ANNA ,  WU TONGFEI

IPC: C07D251/16 ,  A61K31/53 ,  C07D401/04 ,  C07D471/18 ,  C07D471/22 ,  C07D487/08 ,  C07D487/18

Abstract: 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.