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 n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R<1> represents C I -4alkyl; R<2 >represents C I -4alkyl; R<3 >represents CI-4alkyl; or R<2 >and R<3 >taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het<1> wherein said C3-8cycloalkyl or Het<1> each independently may optionally be substituted with C1-4alkyloxycarbonyl; R<4 >represents halo or C I -4alkyloxy; R<5> 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<3> or NR<6>R<7>, C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het<4 >or NR<8>R<9>; R<6> and R<7 >are each independently selected from hydrogen, C I-4alkyl, C I-4alkyloxyC1-4alkyl, -Het<5> or CI-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het<5>; R<8> and R<9> are each independently selected from hydrogen, C,1-4alkyl, -Het<7> or mono- or di(C 1-4alkyl)aminosulphonyl; Het<3 >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<4 >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<5> 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<7> represents piperidinyl. |
申请人 |
JANSSEN PHARMACEUTICA N.V.;LACRAMPE, JEAN, FERNAND, ARMAND;CONNORS, RICHARD, WILLIAM;HO, CHIH, YUNG;RICHARDSON, ALAN;FREYNE, EDDY, JEAN, EDGARD;BUIJNSTERS, PETER, JACOBUS, JOHANNES;BAKKER, ANNETTE, CORNELIA |
发明人 |
LACRAMPE, JEAN, FERNAND, ARMAND;CONNORS, RICHARD, WILLIAM;HO, CHIH, YUNG;RICHARDSON, ALAN;FREYNE, EDDY, JEAN, EDGARD;BUIJNSTERS, PETER, JACOBUS, JOHANNES;BAKKER, ANNETTE, CORNELIA |