871313-07-4

Upstream product

• 40023-89-0 3,4-dichloro-α-ethylbenzenemethanamine 
• 107-14-2 chloroacetonitrile 
• 90650-06-9 1-(3,4-dichloro-phenyl)-propan-1-one oxime 
• 6582-42-9 1-(3,4-dichlorophenyl)propan-1-one 
• 742107-61-5 (R)-1-(3,4-Dichloro-phenyl)-propylamine 

Downstream Products

• 847448-26-4 N-cyanomethyl-N-[1-(3,4-dichloro-phenyl)-propyl]-formamide 

Relevant academic research and scientific papers

MERCAPTOIMIDAZOLES AS CCR2 RECEPTOR ANTAGONISTS

The present invention relates to a compound of formula (I), aN-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7

2-Mercaptoimidazoles, a new class of potent CCR2 antagonists

We describe the synthesis and SAR of a new class of CCR2 antagonists based on a 2-mercaptoimidazole scaffold. The initial lead 1a was optimized to the 3,4-disubstituted analogues 1p-(S) and 1q-(S), which have IC50 values in the MCP-1 induced Ca

MERCAPTOIMIDAZOLES AS CCR2 RECEPTOR ANTAGONISTS

The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine, a polymorphic form or a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalky

MERCAPTOIMIDAZOLES AS CCR2 RECEPTOR ANTAGONISTS

The present invention relates to a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-66alkyl, C3-7cycloalkyl, C1-66alkylo xyC1 -6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents 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 represents hydrogen, cyano, optionally subst ituted C1-66alkyl, C(=O)-O-R5, C(=O)-NR6aR6b, C(=S)-NR6aR6b, S(=O)2-NR6aR6b or C(=O)-R7; R4 represents hydrogen or C1-6alkyl; n is 1, 2, 3, 4 or 5; Z represents a cyclic ring system. The invention also relates to processes for preparing the compounds of formula (I), their use as CCR2 antagonists and pharmaceutical compositions comprising them.

MERCAPTOIMIDAZOLES AS CCR2 RECEPTOR ANTAGONISTS

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.