| 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; R1 represents hydrogen; aryl; formyl; C1-6 alkylcarbonyl; C1-6 a]kyl; C1-6 alkyloxycarbonyl; C1-6 alkyl substituted with formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonytoxy; or optionally substituted C1-6 alkyloxyCl-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 heteroatorn selected from 0, S or N; benzoxazolyl or a radical of formula (a-1); X2 represents a direct bond; -NR1-NR1-(CH2)N3 -; -0-; -0-(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 0, S or N, or a 9-or 10-membered bicyclic heterocycle containing at least one heteroatom selected from 0, 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)-R5; -S(=O) n1,-R11 -NR5-S(=O)n1,-R11 -S-CN; -NR5 -CN; their use, pharmaceutical compositions comprising them and processes for their preparation. |