SAVORY, EDWARD,HIGGINBOTTOM, MICHAEL,OLIVER, KATHRYN,HORGAN, ANNE VIET-ANH
申请号：
NZ59223809
公开号：
NZ592238A
申请日:
2009.09.16
申请国别(地区):
NZ
年份:
2012
代理人:
摘要：
Disclosed are 4-isopropyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine derivatives as represented by the general formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, geometrical isomer, tautomer, optical isomer or N-oxide thereof, wherein: R1 is selected from: hydrogen, alkyl, and NR4AR4B； R2 is selected from: hydrogen, alkyl, haloalkyl, hydroxy-alkyl, alkoxy-alkyl, haloalkoxy-alkyl, NR4AR4B-alkyl, -C(O)NR4AR4B, and -C(O)O-alkyl； R3 is selected from: alkyl, haloalkyl, hydroxy-alkyl, alkoxy-alkyl, haloalkoxy-alkyl, NR4AR4B-alkyl, aryl-alkyl, heteroaryl-alkyl, aryloxy-alkyl, heteroaryloxy-alkyl, cycloalkyl, cycloalkyl-alkyl, heterocyclyl, and heterocyclyl-alkyl, wherein any aryl or heteroaryl residue is optionally substituted with one more substituents independently selected from halogen, hydroxy, cyano, nitro, CF3, alkyl, alkoxy and NR4AR4B, and wherein any cycloalkyl or heterocyclyl residue is optionally substituted with one or more substituents independently selected from halogen, hydroxy, alkyl, alkoxy and NR4AR4B； R4A and R4B are each independently selected from: hydrogen, alkyl, and acyl； provided that when R1 and R2 are hydrogen, then R3 is not benzyl. Representative compounds include 2,2,2-trichloroethyl 4-isopropyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-5-carboxylate, 2-chloro-2,2-difluoroethyl 4-isopropyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]-pyridine-5-carboxylate, pyridin-2-ylmethyl 4-isopropyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-5-carboxylate, benzyl (4S,6S)-6-(aminocarbonyl)-4-isopropyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-5-carboxylate, (5-methylisoxazol-3-yl)methyl 4-isopropyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]-pyridine-5-carboxylate and (3S)-tetrahydrofuran-3-yl (4S)-4-isopropyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]-pyridine-5-carboxylate. Further disclosed is a pharmaceutical formulation which contains a compound as defined above, and or benzyl 4-isopropyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-5-carboxyl
