14051-33-3

Usage

InChI:InChI=1/C23H26N2O2/c26-21-11-14-23(22(27)24-21,19-9-5-2-6-10-19)20-12-15-25(16-13-20)17-18-7-3-1-4-8-18/h1-10,20H,11-17H2,(H,24,26,27)

Upstream product

• 6767-69-7 [14C]-Benzetimide hydrochloride 
• 83898-32-2 2-(1-benzyl-piperidin-4-yl)-2-phenyl-pentanedinitrile 

Downstream Products

• 19315-71-0 Norbenzylbenzetimide 
• 21888-98-2 [125I]-Dexetimide 
• 21888-99-3 Levetimide 
• 119413-94-4 2-Iodobenzetimide 
• 119391-66-1 2-Bromobenzetimide 
• 119391-65-0 2-Chlorobenzetimide 
• 119391-62-7 2-Fluorobenzetimide 
• 119391-58-1 3-Iodobenzetimide 
• 119391-59-2 3-Bromobenzetimide 
• 119391-57-0 3-Fluorobenzetimide 
• 119391-56-9 4-Iodobenzetimide 
• 119391-63-8 4-Bromobenzetimide 
• 119391-60-5 1'-(3-chloro-benzyl)-3-phenyl-octahydro-[3,4']bipyridinyl-2,6-dione 
• 119391-61-6 1'-(4-chloro-benzyl)-3-phenyl-octahydro-[3,4']bipyridinyl-2,6-dione 

Relevant academic research and scientific papers

Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists

The synthesis and evaluation of benzetimide derivatives showing potent CXCR3 antagonism are described. Optimization of the screening hits led to the identification of more potent CXCR3 antagonists devoid of anti-cholinergic activity and identification of the key pharmacophore moieties of the series.

PIPERIDINE DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS

The present invention relates to a compound of formula (I), aN-oxide thereof, a pharmaceutically acceptable salt thereof, a stereochemically isomeric form thereof or a solvate thereof, wherein X represents N or CH; Y and Z each independently represent C(=O) or CH2 provided that at least one of Y and Z represents C(=O); R1 represents CH(R4)-aryl or CH(R4)-heteroaryl; R2 represents aryl2 or heteroaryl; R3 represents hydrogen; C1-4alkylcarbonyl; C1-6alkyl optionally substituted with C1-6alkyloxy, C1-6alkylthio, C1-6alkyloxycarbonyl or aryl1 ; provided that when Y and Z each represent C(=O), X represents CH, R3 represents hydrogen, R4 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then aryl in the definition of R1 is other than phenyl substituted with one halo or with one or two C1-4alkyl; and provided that when Y and Z each represent C(=O), X represents CH, R3 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then heteroaryl in the definit ion of R1 is other than unsubstituted thienyl or unsubstituted pyridyl. The present invention also relates to the use of a compound of formula (I) for the manufacture of a medicament for preventing or treating a disease mediated through activation of the CXCR3 receptor; to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them.