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4 条记录 (耗时 0.053 秒)

    Macrocyclic quinazoline derivatives as antiproliferative agents
    2.
    发明申请
    Macrocyclic quinazoline derivatives as antiproliferative agents 有权

    公开(公告)号：US20060247237A1

    公开(公告)日：2006-11-02

    申请号：US10558007

    申请日：2004-05-25

    申请人： Eddy Jean Freyne ,  Timothy Perera ,  Peter Jacobus Buijnsters ,  Marc Willems ,  Gaston Diels ,  Werner Embrechts

    发明人： Eddy Jean Freyne ,  Timothy Perera ,  Peter Jacobus Buijnsters ,  Marc Willems ,  Gaston Diels ,  Werner Embrechts

    IPC分类号： A61K31/5377 ,  A61K31/519 ,  C07D487/22

    CPC分类号： C07D498/06 ,  C07C229/16 ,  C07C229/40 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94

    摘要： 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 Z represents O, CH2, NH or S; in particular Z represents NH; Y represents —C3-9alkyl-, —C3-9alkenyl-, —C3-9alkynyl-, —C3-7alkyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4 alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-oxy-C1-5alkyl-, —C1-5alkyl NR13—, —C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-6alkyl-NH—CO—, —C1-3alkyl-NH—CS-Het20-, —C1-3alkyl-NH—CO-Het20, —C1-2alkyl-CO-Het21-CO—, -Het22-CH2—CO—NH—C1-3alkyl-, —CO—NH—C1-6alkyl-, —NH—CO—C1-6alkyl-, —CO—C1-7alkyl-, —C1-7alkyl-CO—, —C1-6alkyl-CO—C1-6alkyl-, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, C1-2alkyl-NR21—CH2—CO—NH—C1-3alkyl-, or NR22—CO—C1-3alkyl-NH—, X1 represents a direct bond, O or —O—C1-2alkyl-, CO, —CO—C1-2alkyl-, NR11, —NR11—C1-2alkyl-, —CH2—, —O—N═CH— or —C1-2alkyl-; X2 represents a direct bond, O, —O—C1-2alkyl-, CO, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —CH2—, —O—N═CH— or —C1-2alkyl-. The growth inhibitory effect anti-tumour activity of the present compounds has been demonstrated in vitro, in enzymatic on the receptor tyrosine kinase EGFR.

    Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
    3.
    发明申请
    Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors 有权

    公开(公告)号：US20060183747A1

    公开(公告)日：2006-08-17

    申请号：US10565065

    申请日：2004-07-12

    申请人： Eddy Freyne ,  Christopher Love ,  Ludwig Cooymans ,  Nele Vandermaesen ,  Peter Jacobus Buijnsters ,  Marc Willems ,  Werner Embrechts

    发明人： Eddy Freyne ,  Christopher Love ,  Ludwig Cooymans ,  Nele Vandermaesen ,  Peter Jacobus Buijnsters ,  Marc Willems ,  Werner Embrechts

    IPC分类号： A61K31/519 ,  C07D487/02

    CPC分类号： C07D487/04

    摘要： This invention concerns compounds of formula 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; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; C1-6alkyl substituted with formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; or optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X1 represents a direct bond; —(CH2)n3— or —(CH2)n4—X1a—X1b—; R2 represents optionally substituted C3-7cycloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one hetetoatom selected from O, S or N; benzoxazolyl or a radical of formula X2 represents a direct bond; —NR1—; —NR1—(CH2)n3—; —O—; —O—(CH2)n3—; —C(═O)—; —C(═O)—(CH2)n3—; —C(═O)—NR5—(CH2)n3—; —C(═S)—; —S—; —S(═O)n1—; —(CH2)n3—; —(CH2)n4—X1a—X1b—; —X1a—X1b—(CH2)n4—; —S(═O)n1—NR5—(CH2)n3—NR5— or —S(═O)n1—NR5—(CH2)n3—; R3 represents an optionally substituted 5- or 6-membered monocyclic heterocycle containing at least one heteroatom selected from O, S or N, or a 9- or 10-membered bicyclic heterocycle containing at least one heteroatom selected from O, S or N; R4 represents hydrogen; halo; hydroxy; optionally substituted C1-4alkyl; optionally substituted C2-4alkenyl or C2-4alkynyl; polyhaloC1-3alkyl; optionally substituted C1-4alkyloxy; polyhaloC1-3alkyloxy; C1-4alkylthio; polyhaloC1-3alkylthio; C1-4alkyloxycarbonyl; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhaloC1-4alkylcarbonyl; nitro; cyano; carboxyl; NR9R10; C(═O)NR9R10; —NR5—C(═O)—NR9R10; —NR5—C(═O)—R11; —S(═O)n1—R11; —NR5—S(═O)n1—R11; —S—CN; —NR5—CN; their use, pharmaceutical compositions comprising them and processes for their preparation.

    3-Phenyl analogs of toxoflavine as kinase inhibitors
    4.
    发明申请
    3-Phenyl analogs of toxoflavine as kinase inhibitors 审中-公开

    公开(公告)号：US20050239784A1

    公开(公告)日：2005-10-27

    申请号：US10520768

    申请日：2003-07-08

    申请人： Jean LaCrampe ,  Richard Connors ,  Chih Ho ,  Alan Ricardson ,  Eddy Freyne ,  Peter Jacobus Buijnsters ,  Annette Bakker

    发明人： Jean LaCrampe ,  Richard Connors ,  Chih Ho ,  Alan Ricardson ,  Eddy Freyne ,  Peter Jacobus Buijnsters ,  Annette Bakker

    IPC分类号： A61K31/53 ,  A61K31/5377 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04 ,  C07D519/00 ,  C07D487/02

    CPC分类号： C07D487/04

    摘要： The present invention concerns the compounds of formula 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; R3 represents C1-4alkyl; or R2 and R3 taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het1 wherein said C3-8cycloalkyl or Het1 each independently may optionally be substituted with C1-4alkyloxycarbonyl; R4 represents halo or C1-4alkyloxy; R5 represents C1-4alkyloxycarbonyl, —O-(mono- or di(C1-4alkyl)aminosulfonyl), C1-4alkyl substituted with one or where possible more substituent being selected from Het3 or NR6R7, C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het4 or NR8R9; R6 and R7 are each independently selected from hydrogen, C1-4alkyl, C1-4alkyloxyC1-4alkyl, -Het5 or C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het5; R8 and R9 are each independently selected from hydrogen, C1-4alkyl, -Het7 or mono- or di(C1-4alkyl)aminosulphonyl; Het3 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(C1-4alkyl)aminosulfonyl, hydroxyC1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het4 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; Het5 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(C1-4alkyl)aminosulfonyl; Het7 represents piperidinyl.