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    3-Furanyl analogs of toxoflavine as kinase inhibitors
    1.
    发明申请
    3-Furanyl analogs of toxoflavine as kinase inhibitors 失效

    公开(公告)号：US20060040943A1

    公开(公告)日：2006-02-23

    申请号：US10520641

    申请日：2003-07-08

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

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

    IPC分类号： C07D487/04 ,  A61K31/53

    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 stereochemically isomeric forms thereof, wherein m represents an integer being 0 or 1; n represents an integer being 0, 1 or 2; R1 represents C1-4alkyl, C1-4alkyl substituted with pyridinyl, phenyl, piperidinyl or piperidinyl substituted with C1-4alkyloxycarbonyl; R2 represents hydrogen or C1-4alkyl; R3 represents hydrogen or C1-4alkyl; or R2 and R3 taken together with the carbon atom to which they are attached form cyclopentyl or piperidinyl wherein said cyclopentyl or piperidinyl each independently may optionally be substituted with one, or where possible, two or three substituents each independently selected from C1-4alkyloxycarbonyl, phenylcarbonyl or —C(═NH)—NH2; R4 represents halo or C1-4alkyloxy; R5 represents Het2, C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy, halo, Het3 or NR6R7, or C1-4alkyloxy substituted with one or where possible more substituents being selected from Het4 or —C(═O)-Het4; R6 and R7 are each independently selected from hydrogen, C1-4alkyl, Het5 or C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy or Het5; Het2 represents piperazinyl; Het3 represents a heterocycle selected from morpholinyl, pyrrolidinyl, 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 preferably methyl, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, hydroxyC1-4alkyloxyC1-4alkyl, C1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het4 represents a heterocycle selected from morpholinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three C1-4alkyl substituents, preferably methyl; Het5 represents a heterocycle selected from pyridinyl, pyrrolidinyl 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, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl.

    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

    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.