742108-40-3Relevant academic research and scientific papers
MERCAPTOIMIDAZOLES AS CCR2 RECEPTOR ANTAGONISTS
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Page 43, (2008/06/13)
The present invention relates to a compound of formula (I),a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 is hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl or heteroaryl; R2 is halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono-or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 is hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy, C(=O)-O-R5, C(=O)-NR6aR6b, S(=O)2-NR6aR6b, C(=O)-R7; R4 is hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy, C(=O)-O-R5, C(=O)-NR6aR6b, S(=O)2-NR6aR6b, C(=O)-R7; n is 1, 2, 3, 4 or 5;provided that at least one of R3 or R4 is other than hydrogen; and that if R3 represents C(=O)-OH, C(=O)-O-C1-6alkyl or C(=O)-O-C2-6alkenyl, then R4 is other than hydrogen; and that if R3 represents CH2OH and R1 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents C(=O)-NH-C1-4alkyl-NH2 and R1 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents formula (II) and R1 represents hydrogen, then R4 is other than hydrogen; having CCR2 receptor antagonistic properties. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them.
