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    3-PHENYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS
    1.
    发明申请
    3-PHENYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS 审中-公开
    吡喹酮作为激酶抑制剂的3-苯基类似物

    公开(公告)号：WO2004007498A2

    公开(公告)日：2004-01-22

    申请号：PCT/EP0350292

    申请日：2003-07-08

    Applicant: JANSSEN PHARMACEUTICA NV ,  LACRAMPE JEAN FERNAND ARMAND ,  CONNORS RICHARD WILLIAM ,  HO CHIH YUNG ,  RICHARDSON ALAN ,  FREYNE EDDY JEAN EDGARD ,  BUIJNSTERS PETER JACOBUS JOHAN ,  BAKKER ANNETTE CORNELIA

    Inventor： LACRAMPE JEAN FERNAND ARMAND ,  CONNORS RICHARD WILLIAM ,  HO CHIH YUNG ,  RICHARDSON ALAN ,  FREYNE EDDY JEAN EDGARD ,  BUIJNSTERS PETER JACOBUS JOHAN ,  BAKKER ANNETTE CORNELIA

    IPC: A61K31/53 ,  A61K31/5377 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04 ,  C07D519/00

    CPC classification number: C07D487/04

    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 n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R represents C I -4alkyl; R represents C I -4alkyl; R represents CI-4alkyl; or R and R taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het wherein said C3-8cycloalkyl or Het each independently may optionally be substituted with C1-4alkyloxycarbonyl; R represents halo or C I -4alkyloxy; R represents C 1-4alkyloxycarbonyl, -O-(mono- or di(C1-4alkyl)aminosulfonyl), CI-4alkyl substituted with one or where possible more substituent being selected from Het or NR R , C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het or NR R ; R and R are each independently selected from hydrogen, C I-4alkyl, C I-4alkyloxyC1-4alkyl, -Het or CI-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het ; R and R are each independently selected from hydrogen, C,1-4alkyl, -Het or mono- or di(C 1-4alkyl)aminosulphonyl; Het represents a heterocycle selected from piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from hydroxy, aminosulfonyl, amino, mono-or di(C 1-4 alkyl)aminosulfonyl, hydroxyC 1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het represents a heterocycle selected from morpholinyl, piperidinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C1-4alkyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl; Het represents a heterocycle selected from pyridinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, or mono- or di(Cl­4alkyl)aminosulfonyl; Het represents piperidinyl.

    Abstract translation: 本发明涉及式（I）化合物的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n表示0,1或2的整数; m表示0或1的整数; R 1表示C 1-4烷基; R 2表示C 1-4烷基; R 3表示C 1-4烷基; 或R 2和R 3与它们所连接的碳原子一起形成C 3-8环烷基或Het 1，其中所述C 3-8环烷基或Het 1各自独立地可以被C1- 4alkyloxycarbonyl; R 4表示卤素或C 1-4烷氧基; R 5表示C 1-4烷氧基羰基，-O-（单或二（C 1-4烷基）氨基磺酰基），被一个或多个可能的更多取代基取代的C 1-4烷基选自Het 3或NR 6 R 被一个或多个可能的更多取代基取代的C 1-4烷氧基选自氨基，Het 4或NR 8 R 9; R 6和R 7各自独立地选自氢，C 1-4烷基，C 1-4烷氧基C 1-4烷基，-Het 5或被一个或多个可能的更多取代基取代的C 1-4烷基，所述取代基选自羟基， 或Het <5>; R 8和R 9各自独立地选自氢，C 1-4烷基，-Het 7或单或二（C 1-4烷基）氨基磺酰基; Het 3表示选自哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可以任选被一个取代，或者如果可能的话，两个或三个取代基各自独立地选自羟基，氨基磺酰基，氨基，单或二（C 1 -4烷基）氨基磺酰基，羟基C 1-4烷氧基C 1-4烷基或C 1-4烷氧基; Het 4表示选自吗啉基，哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可以任选地被一个取代，或者如果可能的话，两个或三个取代基各自独立地选自C 1-4烷基，C 1-4烷氧基羰基或一或二 （C 1-4烷基）氨基磺酰基; Het 5表示选自吡啶基或哌啶基的杂环，其中所述单环杂环各自独立地可以任选地被一个取代，或者两个或三个取代基各自独立地选自氨基磺酰基或单或二（C 1-4烷基）氨基磺酰基; Het 7表示哌啶基。

    3-PHENYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS
    2.
    发明申请
    3-PHENYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS 审中-公开
    作为激酶抑制剂的TOXOFLAVINE的3-苯基类似物

    公开(公告)号：WO2004007498A9

    公开(公告)日：2004-08-12

    申请号：PCT/EP0350292

    申请日：2003-07-08

    Applicant: JANSSEN PHARMACEUTICA NV ,  LACRAMPE JEAN FERNAND ARMAND ,  CONNORS RICHARD WILLIAM ,  HO CHIH YUNG ,  RICHARDSON ALAN ,  FREYNE EDDY JEAN EDGARD ,  BUIJNSTERS PETER JACOBUS JOHAN ,  BAKKER ANNETTE CORNELIA

    Inventor： LACRAMPE JEAN FERNAND ARMAND ,  CONNORS RICHARD WILLIAM ,  HO CHIH YUNG ,  RICHARDSON ALAN ,  FREYNE EDDY JEAN EDGARD ,  BUIJNSTERS PETER JACOBUS JOHAN ,  BAKKER ANNETTE CORNELIA

    IPC: A61K31/53 ,  A61K31/5377 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04 ,  C07D519/00

    CPC classification number: C07D487/04

    Abstract: The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereo-chemically isomeric forms thereof, wherein n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R represents C1-4alkyl; R represents C1-4alkyl; R represents C1-4alkyl; or R and R taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het wherein said C3-8cycloalkyl or Het each independently may optionally be substituted with C1-4alkyloxycarbonyl; R represents halo or C1-4alkyloxy; R represents C1-4alkyloxycarbonyl, -O-(mono- or di(C1-4alkyl)aminosulfonyl), C1-4alkyl substituted with one or where possible more substituent being selected from Het or NR R , C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het or NR R ; R and R are each independently selected from hydrogen, C1-4alkyl, C1-4alkyloxyC1-4alkyl, -Het or C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het ; R and R are each independently selected from hydrogen, C1-4alkyl, -Het or mono- or di(C1-4alkyl)aminosulphonyl; Het represents a heterocycle selected from piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from hydroxy, aminosulfonyl, amino, mono-or di(C1-4 alkyl)aminosulfonyl, hydroxyC1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het represents a heterocycle selected from morpholinyl, piperidinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C1-4alkyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl; Het represents a heterocycle selected from pyridinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, or mono- or di(Cl­4alkyl)aminosulfonyl; Het represents piperidinyl.

    Abstract translation: 本发明涉及式（I）的N-氧化物形式的化合物，其药学上可接受的加成盐和立体化学异构形式，其中n表示0,1或2的整数; m表示0或1的整数; R 1表示C 1-4烷基; R 2表示C 1-4烷基; R 3代表C 1-4烷基; 或R 2和R 3与它们所连接的碳原子一起形成C 3-8环烷基或Het 1，其中所述C 3-8环烷基或Het 1各自独立地可任选被C 1 -C 8 - 4alkyloxycarbonyl; R 4代表卤素或C 1-4烷氧基; R 5表示C 1-4烷氧基羰基，-O-（一或二（C 1-4烷基）氨基磺酰基），被一个或可能的更多取代基取代的C 1-4烷基，所述取代基选自Het 3或NR 6 R 6; 被一个或在可能的情况下被选自氨基，Het 4或NR 8 R 9的更多取代基取代的C 1-4烷氧基; R 6和R 7各自独立地选自氢，C 1-4烷基，C 1-4烷氧基C 1-4烷基，-Het 5或被一个或可能的更多取代基取代的C 1-4烷基，所述取代基选自羟基或Het <5>; R 8和R 9各自独立地选自氢，C 1-4烷基，-Het 7或单 - 或二（C 1-4烷基）氨基磺酰基; Het 3代表选自哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可任选被一个或任选地两个或三个取代基取代，所述取代基各自独立地选自羟基，氨基磺酰基，氨基，单或二（C1- 4烷基）氨基磺酰基，羟基C1-4烷氧基C1-4烷基或C1-4烷氧基; Het 4代表选自吗啉基，哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可任选被一个或在可能的情况下被两个或三个取代基取代，所述取代基各自独立地选自C 1-4烷基，C 1-4烷氧基羰基或一或二 （C 1-4烷基）氨基磺酰基; Het 5代表选自吡啶基或哌啶基的杂环，其中所述单环杂环各自独立地可任选地被一个或任选地两个或三个取代基取代，所述取代基各自独立地选自氨基磺酰基或单或二（C 1-4烷基）氨基磺酰基; Het 7代表哌啶基。

    RESPIRATORY SYNCYTIAL VIRUS REPLICATION INHIBITORS
    3.
    发明申请
    RESPIRATORY SYNCYTIAL VIRUS REPLICATION INHIBITORS 审中-公开
    呼吸道同种病毒复制抑制剂

    公开(公告)号：WO0100615A8

    公开(公告)日：2002-01-10

    申请号：PCT/EP0005677

    申请日：2000-06-20

    Applicant: JANSSEN PHARMACEUTICA NV ,  JANSSENS FRANS EDUARD ,  LACRAMPE JEAN FERNAND ARMAND ,  GUILLEMONT JEROME EMILE GEORGE ,  VENET MARC GASTON ,  ANDRIES KOENRAAD JOZEF LODEWIJ

    Inventor： JANSSENS FRANS EDUARD ,  LACRAMPE JEAN FERNAND ARMAND ,  GUILLEMONT JEROME EMILE GEORGE ,  VENET MARC GASTON ,  ANDRIES KOENRAAD JOZEF LODEWIJ

    IPC: C07D491/056 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61P11/00 ,  A61P31/12 ,  A61P43/00 ,  C07B61/00 ,  C07D401/06 ,  C07D401/14 ,  C07D409/14 ,  C07D413/00 ,  C07D417/14 ,  C07D471/04 ,  A61K31/436 ,  A61K31/4375 ,  A61K31/4409 ,  C07D413/14

    CPC classification number: C07D401/14 ,  C07D409/14 ,  C07D471/04 ,  Y02P20/55

    Abstract: The present invention concerns compounds of formula (I), prodrugs, N -oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a =a -a =a - represents a radical of formula -CH=CH-CH=CH-; -N=CH-CH=CH-; -CH=N-CH=CH-; -CH=CH-N=CH-; -CH=CH-CH=N-; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y is a bivalent radical of formula -NR - or -CH(NR R )-; X is NR , S, S(=O), S(=O)2, O, CH2, C(=O), CH(=CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR R ), CH2-NR or NR -CH2; X is a direct bond, CH2, C(=O), NR , C1-4alkyl-NR , NR -C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R ; provided that when R is hydroxy or C1-6alkyloxy, then R cannot replace a hydrogen atom in the alpha position relative to a nitrogen atom; G is a direct bond or optionally substituted C1-10alkanediyl; R is an optionally substituted bicyclic heterocycle; R is hydrogen, formyl, C1-6alkylcarbonyl, Hetcarbonyl, pyrrolidinyl, piperidinyl, homopiperidinyl, C3-7cycloalkyl or C1-10alkyl substituted with N(R )2 and optionally with another substituent; R is hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy, arylC1-6alkyl or arylC1-6alkyloxy, R is hydrogen, C1-6alkyl or arylC1-6alkyl; R , R , R and R are hydrogen or C1-6alkyl; or R and R , or R and R taken together from a bivalent radical of formula -(CH2)s- wherein S is 4 or 5; R is hydrogen, C1-4alkyl, formyl, hydroxyC1-6alkyl, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; aryl is optionally substituted phenyl; Het is pyridyl, pyrimidinyl, pyryzinyl, pyridazinyl; as respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and their use as a medicine.

    Abstract translation: 本发明涉及式（I）的化合物，前药，N，N-氧化物，加成盐，季胺，金属配合物及其立体化学异构形式，其中-a 1 = a 2 -a <3> = a 4 - 表示式-CH = CH-CH = CH-的基团; -N = CH-CH = CH-; -CH = N-CH = CH-; -CH = CH-N = CH-; -CH = CH-CH = N-; 其中每个氢原子可以任选被取代; Q是式（b-1），（b-2），（b-3），（b-4），（b-5），（b-6），（b-7）和 -8），其中Alk是C 1-6烷二基; Y 1是式-NR 2 - 或-CH（NR 2 R 4） - 的二价基团。 X 1是NR 4，S，S（= O），S（= O）2，O，CH 2，C（= O），CH（= CH 2），CH（OH） CH（OCH 3），CH（SCH 3），CH（NR 5a R 5b），CH 2 -NR 4或NR 4 -CH 2; X 2是直接键，CH 2，C（= O），NR 4，C 1-4烷基-NR 4，NR 4 -C 1-4烷基，t是2至5; 你是1到5; v为2或3; 并且其中Alk和（b-3），（b-4），（b-5），（b-6），（b-7）和（b-8）中的每个氢可以任选地被R <3>; 条件是当R 3为羟基或C 1-6烷氧基时，R 3不能代替相对于氮原子的α位氢原子; G是直接键或任选取代的C 1-10烷二基; R 1是任选取代的双环杂环; R 2是氢，甲酰基，C 1-6烷基羰基，Het羰基，吡咯烷基，哌啶基，高哌啶基，C 3-7环烷基或被N（R 6）2取代的C 1-10烷基，任选地与另外的取代基取代; R 3是氢，羟基，C 1-6烷基，C 1-6烷氧基，芳基C 1-6烷基或芳基C 1-6烷氧基，R 4是氢，C 1-6烷基或芳基C 1-6烷基; R 5a，R 5b，R 5c和R 5d是氢或C 1-6烷基; 或R 5a和R 5b，或R 5c和R 5一起来自式 - （CH 2）s - 的二价基团，其中S为4或5; R 6是氢，C 1-4烷基，甲酰基，羟基C 1-6烷基，C 1-6烷基羰基或C 1-6烷氧基羰基; 芳基是任选取代的苯基; Het是吡啶基，嘧啶基，吡嗪基，哒嗪基; 作为呼吸道合胞病毒复制抑制剂; 其制剂，含有它们的组合物及其作为药物的用途。

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