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PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
专利权人:
发明人:
申请号:
EP10707791.9
公开号:
EP2405913A1
申请日:
2010.03.09
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
MCHR1 antagonists are provided having the following Formula I: wherein A1 and A2 are independently C or N E is C or N D1 is a bond, -CR8R9X-, -XCR8R9-, -CHR8CHR9-, -CR10=CR10-, -C≡C-, or 1,2-cyclopropyl X is O, S or -NR11 R1, R2, and R3 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, lower cycloalkoxy, -CF3, -OCF3, -OR12 and -SR12 G is O or S D2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkycycloalkoxy Z1 and Z2 are independently hydrogen, halogen, lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, halo, -CF3, -OCONR14R14, -CN, -CONR14R14, -SOR12, -SO2R12, -NR14COR14, -NR14CO2R14, -CO2R12, NR14SO2R12 or -COR12 provided that if Z1 is -CH3 and one of R1, R2, or R3 is F, then Z2 cannot be H R5, R6, and R7 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF3, -SR12, lower alkoxy, lower cycloalkoxy, -OCH2OMe, -CN, -CONR14R14, SOR12, SO2R12, NR14COR14, NR14CO2R12, CO2R12, NR14SO2R12 and -COR12 R8, R9, R10, R10, R11 are independently hydrogen or lower alkyl R12 is lower alkyl or lower cycloalkyl and R14 and R14 are independently H, lower alkyl, lower cycloalkyl or R14 and R14 together with the N to which they are attached form a ring having 4 to 7 atoms. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.Linvention concerne des antagonistes de MCHR1 représentés par la formule suivante I, dans laquelle A1 et A2 représentent indépendamment C ou N E représente C ou N D1 représente une liaison, -CR8R9X-, -XCR8R9-, -CHR8CHR9-, -CR10=CR10-, -C≡C- ou 1,2-cyclopropyle X représente O, S ou -NR11 R1, R2 et R3 sont sélectionnés indépendamment dans le groupe constitué par un hydrogène, un halogène, un alkyle inférieur, un cycloalkyle inférieur, un cycloalcoxy inférieur, -CF3, -OCF3, -OR12 et -SR12 G représente O o
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