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    TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS
    2.
    发明申请
    TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
    作为糖原合成酶激酶3抑制剂的三唑基嘧啶衍生物

    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。

    CYCLIC ANILINO-PYRIDINOTRIAZINES AS GSK-3 INHIBITORS
    5.
    发明申请
    CYCLIC ANILINO-PYRIDINOTRIAZINES AS GSK-3 INHIBITORS 审中-公开
    作为GSK-3抑制剂的CYCLIC ANILINO-PYRIDINOTRIAZINES

    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。

    2,4-DIAMINOPYRIMIDINE DERIVATES AS DOPAMINE D4 RECEPTOR ANTAGONISTS
    7.
    发明申请
    2,4-DIAMINOPYRIMIDINE DERIVATES AS DOPAMINE D4 RECEPTOR ANTAGONISTS 审中-公开
    2,4-二氨基吡啶衍生物作为DOPAMINE D4受体拮抗剂

    公开(公告)号：WO1997043279A1

    公开(公告)日：1997-11-20

    申请号：PCT/EP1997002506

    申请日：1997-05-02

    Applicant: JANSSEN PHARMACEUTICA N.V. ,  BOSMANS, Jean-Paul, René, Marie, André ,  LOVE, Christopher, John ,  VAN LOMMEN, Guy, Rosalia, Eugène

    Inventor： JANSSEN PHARMACEUTICA N.V.

    IPC: C07D401/12

    CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D405/14

    Abstract: The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl or C3-6alkenediyl; R is hydrogen or C1-4alkyl; R and R each independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; or R and R may also be taken together with the nitrogen atom to which they are attached, thus forming a pyrrolidine, a piperidine or a perhydro azepine ring; R is hydrogen or halo; Q is aryl, aryloxy, di(aryl)methyl or heteroaryl; aryl is naphthyl or phenyl, said naphthyl and phenyl may optionally be substituted; and heteroaryl is quinolinyl, isoquinolinyl, pyridinyl, thienyl, indolyl, 2,3-dihydro-1,4-benzodioxinyl, 2,3-dihydro-benzofuranyl or benzodioxolanyl; said heteroaryls may optionally be substituted; it further relates to processes for their preparation, compositions comprising them as well as their use as a medicine; compounds of formula (I) containing a radioactive isotope; a process of marking dopamine D4 receptor sites; and a process for imaging an organ are disclosed.

    Abstract translation: 本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的酸加成盐和立体化学异构形式，其中Alk是C 1-6烷二基或C 3-6亚烯基; R 1是氢或C 1-4烷基; R 2和R 3各自独立地为氢，C 1-6烷基或C 3-7环烷基; 或R 2和R 3也可以与它们所连接的氮原子一起，从而形成吡咯烷，哌啶或全氢氮杂环; R 4是氢或卤素; Q是芳基，芳氧基，二（芳基）甲基或杂芳基; 芳基是萘基或苯基，所述萘基和苯基可任选被取代; 异喹啉基，吡啶基，噻吩基，吲哚基，2,3-二氢-1,4-苯并二氧杂环己基，2,3-二氢 - 苯并呋喃基或苯并二氧杂环戊烷基; 所述杂芳基可任选被取代; 它还涉及它们的制备方法，包含它们的组合物以及它们作为药物的用途; 含有放射性同位素的式（I）化合物; 标记多巴胺D4受体位点的过程; 并且公开了用于成像器官的方法。

    TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS
    9.
    发明申请
    TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
    三氮唑嘧啶衍生物作为GLYCOGEN SYNTHASE激酶3抑制剂

    公开(公告)号：WO2005012307A1

    公开(公告)日：2005-02-10

    申请号：PCT/EP2004/051455

    申请日：2004-07-12

    Applicant: JANSSEN PHARMACEUTICA N.V. ,  FREYNE, Eddy Jean Edgard ,  LOVE, Christopher John ,  COOYMANS, Ludwig Paul ,  VANDERMAESEN, Nele ,  BUIJNSTERS, Peter Jacobus Johannes Antonius ,  WILLEMS, Marc ,  EMBRECHTS, Werner Constant Johan

    Inventor： FREYNE, Eddy Jean Edgard ,  LOVE, Christopher John ,  COOYMANS, Ludwig Paul ,  VANDERMAESEN, Nele ,  BUIJNSTERS, Peter Jacobus Johannes Antonius ,  WILLEMS, Marc ,  EMBRECHTS, Werner Constant Johan

    IPC: C07D487/04

    CPC classification number: C07D487/04

    Abstract: This invention concerns a compound of formula (I), a N -oxide, a pharmaceutically acceptable addition salt, a quaternary arnine and a stereochernic ally isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R 1 represents hydrogen; aryl; formyI; C l . 6 alkylcarbonyl, C 1-6 alkyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylearbonyl, C 1-­6 alkyloxycarbonyl, C 1 - 6 alkylcarbonyloxy; or C 1 - 6 alkyloxyC 1-6 alkylcarbonyl optionally substituted with C 1-6 alkyloxycarbonyl; X represents a direct bond; -(CH 2 ) n3 ­or -(CH 2 ) m4 -X 1a -X 1b -; R 2 represents C 3-7 cycloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatom. selected from 0, S or N; benzoxazolyl or a radical of formula (a-1), wherein said R 2 substituent may optionally be substituted; R 3 represents halo; hydroxy; optionally substituted C 1-.6 alkyl; C 2-6 a]kenyl or C 2-6 alkynyl, each optionally substituted; optionally substituted polyhaloC 1-6 alkyl; optionally substituted C 1-6 alkyloxy; optionally substituted polyhaloC 1-­6 alkyloxy; C 1-6 alkylthio; polyhaloC 1-6 a]kylthio; C 1-6 a]kyloxycarbonyl; C 1-6 alkylcarbonyloxy; C 1-6 alkylearbonyl; polyhaloC 1-6 alkylcarbonyl; cyano; carboxyl; aryloxy; arylthio; arylcarbonyl; NR 6b R 7b ; C(=O)-NR 6b R 7b ; -NR 5 -C(=O)R 5 ;'-S(=O) nl -R 8a ; -NR 5 S(=O) nl -R 8a ;-NR 5 -S(=O) nl -R 8a ; -S-CN; -NR 5 -CN;R 4 represents hydrogen; halo; hydroxy; optionally substituted C 1-4 alkyl; C 2-4 alkenyl or C 2-4 alkynyl, each optionally substituted; polyha]oC 1-3 alkyl; optionally substituted C 1-4 alkyloxy; polyhalo-C 1-3 alkyloxy; C 1-4 alkylthio; polyhaloC 1-3 alkylthio­ C 1-4 alkyloxycarbonyl; C 1-4 alkylcarbonyloxy; C 1-4 alkylcarbonyl; polyhatoC 1-4 alkyl­carbonyl; nitro; cyano; carboxyl; NR 10 R 11 ; C(=O)NR 10 -R 11 ;NR 5 -C(=O)-NR 10 R 11 ;-NR 5 -C(=O)-R 5 ; -S(=O) nl ,-R 12 -NR 5 -S(=O) nI -R 12 ; -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）化合物，N-氧化物，药学上可接受的加成盐，季铵和其立体异构体异构体形式，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烷基; C1-6alkyloxycarbonyl; 被甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰氧基取代的C 1-6烷基; 或任选被C 1-6烷氧基羰基取代的C 1-6烷氧基C 1-6烷基羰基; X表示直接键; - （CH2）n3or - （CH2）m4-X1a-X1b-; R 2表示C 3-7环烷基; 苯基; 含有至少一个杂原子的4,5,6-或7-元单环杂环。 选自0，S或N; 苯并恶唑基或式（a-1）的基团，其中所述R 2取代基可任选被取代; R 3表示卤素; 羟基; 任选取代的C 1-6烷基; C 2-6烯基或C 2-6炔基，各自任选取代; 任选取代的多卤代C 1-6烷基; 任选取代的C 1-6烷氧基; 任选取代的多卤代C 1-6烷氧基; C 1-6烷; polyhaloC1-6a]烷硫基; C1-6a] kyloxycarbonyl; C1-6alkylcarbonyloxy; C1-6alkylearbonyl; polyhaloC1-6alkylcarbonyl; 氰基; 羧基; 芳; 芳; 基羰基; NR 6b; R 7b; C（= O）-NR 6b R 7b; -NR <5> -C（= O）R <5>;' - S（= O）NL-R <8A>; -NR 5 S（= O）n -R 8 8a; -NR 5 -S（= O）n -R 8 8a; -S-CN; -NR 5 -CN; R 4表示氢; 光环; 羟基; 任选取代的C 1-4烷基; C2-4烯基或C2-4炔基，各自任选取代; polyha] OC 1-3烷基; 任选取代的C 1-4烷氧基; 多卤代C1-3alkyloxy; C1-4alkylthio; 多卤代C 1-3烷硫基C 1-4烷氧基羰基; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhatoC1-4alkylcarbonyl; 硝基; 氰基; 羧基; NR 10 R 11; C（= O）NR 10 -R 11; NR 5 -C（= O）-NR 10 R 11; -NR 5 -C（= O）-R 5 >; -S（= O）n1，-R 12 -NR 5 -S（= O）n I -R 12; -S-CN; -NR 5 -CN; 其用途，包含它们的药物组合物及其制备方法。

    TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS
    10.
    发明申请
    TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
    三氮唑嘧啶衍生物作为GLYCOGEN SYNTHASE激酶3抑制剂

    公开(公告)号：WO2005012304A2

    公开(公告)日：2005-02-10

    申请号：PCT/EP2004/051457

    申请日：2004-07-12

    Applicant: JANSSEN PHARMACEUTICA N.V. ,  FREYNE, Eddy, Jean, Edgard ,  LOVE, Christopher, John ,  COOYMANS, Ludwig, Paul ,  VANDERMAESEN, Nele ,  BUIJNSTERS, Peter, Jacobus, Johannes, Antonius ,  WILLEMS, Marc ,  EMBRECHTS, Werner, Constant, Johan

    Inventor： FREYNE, Eddy, Jean, Edgard ,  LOVE, Christopher, John ,  COOYMANS, Ludwig, Paul ,  VANDERMAESEN, Nele ,  BUIJNSTERS, Peter, Jacobus, Johannes, Antonius ,  WILLEMS, Marc ,  EMBRECHTS, Werner, Constant, Johan

    IPC: C07D487/00

    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烷基羰基氧基取代的C 1-6烷基; 或任选取代的C 1-6烷氧基C 1-6烷基羰基; X1表示直接键; - （CH 2）n3-或 - （CH 2）n4-X1a-X1b-; R 2表示任选取代的C 3-7C环烷基; 苯基; 含有至少一个选自0，S或N的杂化剂的4,5,6-或7-元单环杂环; 苯并恶唑基或式（a-1）基团; X2表示直接键; -NR 1 -NR 1 - （CH 2）N 3 - ; -0-; -O-（CH 2）N 3 - ; -C（= O） - ; -C（= O） - （CH 2）n3-; -C（= O）-NR <5> - （CH2）N3-; -C（= S） - ; -S-; -S（= O）N 1 - ; - （CH2）N3-; - （CH 2）N 4 - X1A-X1b-; -X1a.-X1b-（CH2）N4-; -S（= O）n1-NR5 - （CH2）n3-NR5或-S（= O）n1，-NR5 - （CH2）n3-; 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选自O，S或S的杂原子的9元或10元双环杂环的任选取代的5元或6元单环杂环， 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; polyhaloC1-3alkyl; 任选取代的C 1-4烷氧基; polyhaloC1-3alkyloxy; C1-4alkylthio; polyhaloC1-3alkylthio; C1-4alkyloxycarbonyl; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhaloC1-4alkylcarbonyl; 硝基; 氰基; 羧基; 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; 其用途，包含它们的药物组合物及其制备方法。

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